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Lorbrena lorlatinib 25 mg Tablet, Film Coated, 30-count — NDC 00069-0227-01 package photo
Label image from the product's FDA listing (DailyMed) — may show a different pack size or an older label revision.

Lorbrena lorlatinib 25 mg Tablet, Film Coated, 30-count — NDC 0069-0227-01 (Billing 00069-0227-01)

by Pfizer Laboratories Div Pfizer Inc · 30 TABLET, FILM COATED in 1 BOTTLE

This is a package of 30 tablets of Lorbrena lorlatinib 25 mg Tablet, Film Coated from Pfizer Laboratories Div Pfizer Inc, marketed since Nov 2018 and currently FDA-listed. It is the main listing for this product, which comes in 2 package sizes.

NDC 00069-0227-01
🏷️ FDA NDC (as labeled) 0069-0227-01 billing pads the labeler segment with a zero
This package
Contains30-count Medicaid pays$239.03 / unit · 12 mo Per package$7,170.95 / 30 tablets · Medicaid Pack sizes2 compare ↓
Also priced by: Part D plans $242.90/unit — full pricing hub ↓
Main listing for product 0069-0227 · Also comes in: 120 tablets 0069-0227-03
Rx only Brand On market Non-controlled ⇄ Compare with another NDC
🗂️ FDA directory synced Oct 1, 2026 · this listing last changed Oct 1, 2026 · sources: openFDA · FDA label (DailyMed) · FDA Orange & Purple Book · First Databank · CMS NADAC, ASP, Medicare & Medicaid · RxNorm
📋 All sources & update times →

This page is curated, coded, and maintained by

Compiled from public FDA, CMS, DailyMed, NADAC, and related drug data sources. Editorial policy

NDC database record

One package, one record: these facts belong to NDC 0069-0227-01 alone.

Record
FDA NDC Directory package listing · Human prescription drug
Code segments
0069 labeler · 0227 product · 01 package
Package marketed since
Nov 19, 2018
Sample package
No — commercial package
Listing certified through
Dec 31, 2027
Billing quantity
30 EA per package
Barcode (UPC)
0300690231013, 0300690227016
Medicaid fills, this package
336 prescriptions in the last four reported quarters
FDA record last changed
Oct 1, 2026

Identity & classification

Regulatory identifiers FDA, NLM and CMS codes for this package

FDA NDC (as labeled) 0069-0227-01
Product NDC 0069-0227
11-digit billing NDC 00069022701
NCPDP billing unit EA — each (per item)
RxCUI 2103169, 2103175, 2103177, 2103179
UNII OSP71S83EU
UPC 0300690231013, 0300690227016
Application # NDA210868
SPL Set ID 2b34d62d-e02a-4af3-bc0d-1571dd4ee76d
Established class (EPC) Kinase Inhibitor
Mechanism of action Kinase Inhibitors; Cytochrome P450 3A Inducers; P-Glycoprotein Inducers; Cytochrome P450 2B6 Inducers; Organic Cation Transporter 1 Inhibitors; Organic Anion Transporter 3 Inhibitors; Multidrug and Toxin Extrusion Transporter 1 Inhibitors; Breast Cancer Resistance Protein Inhibitors
DEA schedule Non-controlled
Marketing category NDA
Marketing status On market
FDA listing status Listed (active directory)
Marketing start 2018-11-19
Route ORAL
Dosage form TABLET, FILM COATED
Substance LORLATINIB

Drug-database identifiers Medi-Span GPI and First Databank GCN / HICL / AHFS classification

GPI-14 21530556000320
GCN Seq No 079228
GCN 45687
HICL code 045448
Ingredient (HICL) Lorlatinib
HIC1 code V
Therapeutic class — broad (HIC1) Neoplasms
HIC2 code V1
Therapeutic class — intermediate (HIC2) Antineoplastic Drugs
HIC3 code V1Q
Therapeutic class — specific (HIC3) Antineoplastic Systemic Enzyme Inhibitors
AHFS code 10:00.00.00
AHFS class Antineoplastic Agents
FDB label name LORBRENA 25 MG TABLET
FDB brand name Lorbrena
Legend status F — Federal legend — prescription drug or device
Quick answers
  • GSN (GCN sequence number): 079228
  • GCN: 45687
  • GPI-14 (Medi-Span): 21530556000320
  • HICL (First Databank): 045448
  • AHFS class code: 10:00.00.00
  • RxCUI (RxNorm): 2103169
Why two NDCs? The FDA registers this code as 0069-0227-01 — a 4-4-2 layout, and that's what's printed on the package and shown on DailyMed. For insurance claims, every NDC is standardized to a uniform 11-digit 5-4-2 format by adding a zero to the labeler segment → 00069-0227-01. Same drug, same package — only the format differs.
Where does this data come from?
Identifiers from the FDA openFDA NDC Directory and Structured Product Labeling; RxCUI from RxNorm (NLM); GPI from Medi-Span; GCN / HIC / AHFS / legend from First Databank.

RxNorm drug class

This medicine belongs to the Kinase Inhibitor class.

Pharmacologic class Kinase Inhibitor
Drug family (ATC) Anaplastic lymphoma kinase (ALK) inhibitors
How it works Kinase Inhibitors, Cytochrome P450 2B6 Inducers, Organic Anion Transporter 3 Inhibitors, Breast Cancer Resistance Protein Inhibitors
Where does this data come from?
Therapeutic classes from RxNorm RxClass (U.S. National Library of Medicine) — Established Pharmacologic Class (FDA), ATC drug family (WHO) and mechanism of action, matched by this product’s RxCUI.

Clinical

Label name LORBRENA 25 MG TABLET Ingredient Lorlatinib
📖 What it is MedlinePlus · NLM

Lorlatinib is used to treat a certain type of non-small cell lung cancer (NSCLC). Lorlatinib is in a class of medications called kinase inhibitors. It works by blocking the action of the abnormal protein that signals cancer cells to multiply. This helps to stop or slow the spread of cancer cells.

Read the full MedlinePlus article ↗
📗 Our plain-language guide HelloPharmacist
  • Lorbrena is a targeted therapy designed specifically for non-small cell lung cancer that has a particular gene change called ALK-positive. That gene acts like a stuck accelerator,...
  • What exactly is Lorbrena (lorlatinib) and why was I prescribed it?
  • You can take Lorbrena with or without food — it doesn't make a significant difference in how your body absorbs it. What does matter is consistency: pick a time that works for your...
  • Can I take Lorbrena with food, and does it matter what time of day I take it?
📖 Read our full Lorlatinib guide →
Where does this data come from?
Plain-language summary from MedlinePlus (U.S. National Library of Medicine); supplement & herbal interactions and nutrient depletion data from the Natural Medicines database; our full guide is HelloPharmacist editorial content.

Pricing

A drug doesn't have one price. Each row is a different public payment system, and none is what you'd pay at the counter — that depends on your insurance. The ⓘ on each row explains what it measures.

Price systemPer eachPer package
Retail pharmacies payNADAC · weekly Not in the retail survey — common for institutional, discontinued, or low-volume packs.
Medicaid paysCMS SDUD · 12 mo $239.03 $7,170.95 / 30 tablets
Medicare drug plans payPart D · Q2 2026 $242.90 $7,286.94 / 30 tablets
Where does this data come from?
NADAC (National Average Drug Acquisition Cost) is the CMS weekly pharmacy-acquisition-cost survey — what pharmacies pay. ASP (Average Sales Price) is the CMS Medicare Part B drug-payment file, published quarterly. Medicaid pays is computed by us from CMS State Drug Utilization Data (total reimbursed ÷ units, trailing 12 months) — gross of rebates and inclusive of dispensing fees, so it reflects what Medicaid paid, not an acquisition cost. Medicare drug plans pay is the median negotiated point-of-sale unit cost across plans listing this NDC in the CMS quarterly Prescription Drug Plan pricing files, before rebates. The VA pays is the federal contract price (FSS, and the statutory Big 4 ceiling where listed) from the VA National Acquisition Center pharmaceutical price file. All are free public government data; each measures a different payer, so the figures are not directly comparable.

Packaging — all sizes for this product

Package NDCDescription Marketing startMarketing endStatus
00069-0227-01 You're viewing this Main listing 30 TABLET, FILM COATED in 1 BOTTLE 2018-11-19 — Active
00069-0227-03 0069-0227-03 120 TABLET, FILM COATED in 1 BOTTLE 2025-01-03 Mar 31, 2027 Active

You're viewing the smallest of 2 pack sizes for this product.

In Medicaid, this is the most-dispensed pack of this product — about 97% of fills over the last four reported quarters. See all packs ↓

Pack size FAQ

What quantity is in this package?
This is a 30-count package — 30 tablet, film coated in 1 bottle.
How does this package differ from NDC 00069-0227-03?
Both are Lorbrena lorlatinib 25 mg Tablet, Film Coated — the drug itself is identical. This page's package is the 30-count one, while NDC 00069-0227-03 is the 120 tablets package.
What NDC number is used to bill for this package of Lorbrena lorlatinib 25 mg Tablet, Film Coated?
Use the 11-digit billing form listed in the identifiers section of this page. Pharmacy and medical claims use the 11-digit form; the FDA label may print a shorter form of the same code.

Therapeutic equivalents

ProductLabelerPackNADAC/unitTEStatusPrice vs. this
Lorbrena 25 mgthis 00069-0227-01 Pfizer 30 tablets — — FDA listed —
Lorbrena 25 mg 63539-0927-01 U.S. 30 tablets — — FDA listed —
About this product: this is the brand-name version. We did not find an FDA-approved generic match for this exact strength, form and route.
Where does this data come from?
Equivalents are other NDCs of the same ingredient, form and route from the openFDA NDC Directory, ranked least-expensive-first by NADAC. Therapeutic-equivalence (AB) ratings come from the FDA Orange Book; biologics use the FDA Purple Book for biosimilar & interchangeable status.

Availability & generic status

🏛️
2018
First FDA approval
Nov 2018
📍
2026
Currently FDA-listed
8 years listed
🛡️
2038
Latest patent/protection listed
not a guaranteed launch date
🔒No FDA-approved generic found

We did not find an FDA-approved generic match for this exact strength, form and route. Patent/protection dates below may affect future generic timing.

🛡️ Latest patent/protection date listed: FDA patent/protection data lists protections through Oct 2038. This may affect when a full generic version becomes widely available, but it is not a guaranteed launch date.
📅 FDA approved Nov 2, 2018 RLD RS ⏳ ~12 yr to latest listed protection

Why the date isn’t exact: Generic timing can change because patents may be challenged, settled, licensed, added, removed, or worked around with a narrower label — and FDA approval does not always mean a pharmacy can get the generic today.

Patents & exclusivity — FDA Orange Book
US 10420749 — drug substance (U-2633)
US 10420749 — drug substance (U-2633)
US 10420749 — drug substance (U-3096)
US 10420749 — drug substance (U-3096)
US 11299500 — drug substance
US 11020376 — drug product
US 8680111 — drug substance
US 11020376 — drug product
US 11299500 — drug substance
US 8680111 — drug substance
Exclusivity ODE-349
Exclusivity ODE-349
2018 2020 2022 2024 2026 2028 2030 2032 2034 2036 2038
Today
LOE
Substance patent Formulation patent Method-of-use patent Exclusivity Pediatric +6mo
🏛️FDA exclusivity
FDA-granted marketing protection. It’s separate from patents and may be shorter than patent protection.
🧪Product / substance patents
Patents covering the active ingredient, product, formulation, or related drug features.
🎯Method-of-use patents
Patents covering specific approved uses. These can sometimes be carved out with a “skinny label,” but not always.
🛈 What do these terms mean?
Patent
Legal protection listed in the Orange Book that may delay generic approval or launch. Issued by the U.S. Patent & Trademark Office.
Substance patent
Covers the active drug molecule itself — the hardest to design around. A generic generally can’t launch until it expires.
Formulation (product) patent
Covers a specific formulation or dosage form. A generic can sometimes work around it with a different formulation.
Method-of-use patent
A patent covering one specific approved use of the drug — not necessarily the whole molecule. A generic can sometimes launch with a “skinny label” that carves out the protected use and keeps the others.
Skinny label
A generic label that omits a still-patented use when the FDA allows it — letting a generic reach the market for the unprotected uses.
Exclusivity
FDA-granted marketing protection, separate from patents — e.g. 5-yr new chemical entity, 7-yr orphan drug, or a +6-month pediatric extension.
Paragraph IV
A generic applicant’s formal challenge to a listed patent. It can potentially lead to earlier generic entry, but often involves litigation or a settlement.
RLD / RS
Reference Listed Drug — the brand product the FDA uses as the reference for generic applications. Reference Standard — the product the FDA expects generics to compare against in bioequivalence testing.
TE / AB rating
FDA therapeutic-equivalence rating. An AB rating generally means the FDA considers a generic therapeutically equivalent to — and substitutable for — the brand.
LOE (loss of exclusivity)
The latest patent or exclusivity currently listed — the loss-of-exclusivity / latest-listed-protection date shown on this page. Paragraph-IV challenges and settlements can move the real date earlier; FDA approval and a manufacturer’s decision to market can move it later.

Built from the FDA Orange Book. The bars above are scaled to each protection’s expiry; the red LOE marker is the last one to lapse.

Listed patents (10)
PatentTypeUse codeExpires
US 10420749 ↗ Drug substance U-2633 Jul 27, 2036
US 10420749 ↗ Drug substance U-2633 Jul 27, 2036
US 10420749 ↗ Drug substance U-3096 Jul 27, 2036
US 10420749 ↗ Drug substance U-3096 Jul 27, 2036
US 11299500 ↗ Drug substance — Oct 4, 2038
US 11020376 ↗ Drug product — Jul 27, 2036
US 8680111 ↗ Drug substance — Mar 5, 2033
US 11020376 ↗ Drug product — Jul 27, 2036
US 11299500 ↗ Drug substance — Oct 4, 2038
US 8680111 ↗ Drug substance — Mar 5, 2033
FDA exclusivity
CodeWhat it grantsExpires
ODE-349Orphan Drug Exclusivity (7-year)Mar 3, 2028
ODE-349Orphan Drug Exclusivity (7-year)Mar 3, 2028
Common questions
Is there a generic version of LORBRENA 25 MG TABLET?
No FDA-approved generic equivalent is currently listed in the FDA Orange Book for LORBRENA 25 MG TABLET. Based on the patents and exclusivity currently listed, the Orange Book estimate is that full-label generic entry may be delayed until Oct 2038 — an estimate, not a guaranteed launch date.
The FDA approved a generic — why can’t I get it at my pharmacy yet?
FDA approval and pharmacy availability are two different things. The FDA can approve a generic years before it actually reaches pharmacies, because the brand company may still hold patents or have a settlement that delays the launch. A manufacturer also has to choose to make and sell it, and have supply ready. So a drug can be “FDA-approved generic exists” and still be brand-only at the counter today.
Why do different websites show different generic release dates?
Generic availability is not based on one single date. Some sources use the first exclusivity expiration, some use the last product patent, and others use the latest method-of-use patent. Patent challenges, settlements, licenses, and label carve-outs can also change the real-world launch date. This page shows the underlying Orange Book dates so you can see why estimates may differ.
What does “FDA listed” mean?
It means the product appears in the FDA’s official NDC directory. That’s a good sign a product exists and is intended for the U.S. market, but on its own it does not confirm a pharmacy can fill it today. Where we have recent retail pricing data (NADAC) for a product, we label it “Availability likely” instead.
What does a patent or protection date mean here?
It’s the latest date currently listed in the FDA Orange Book for a patent or exclusivity on the brand product. It can affect when a full generic version becomes widely available — but it is not a guaranteed generic launch date. Generics sometimes arrive earlier (through a settlement or patent challenge) or later (a manufacturer still has to make and sell one).
What does “current Orange Book estimate” mean?
It means we are using the latest patent and exclusivity dates currently listed in the FDA Orange Book. It is not a guaranteed launch date.
Can a generic come out before the last patent expires?
Sometimes. A generic company may challenge a patent, settle with the brand manufacturer, receive a license, or obtain approval with a narrower label that avoids a patented use. In other cases, the last listed protection may delay full-label generic competition.
Can a generic come out after the listed dates?
Yes. Even after patents or exclusivity expire, a generic still needs FDA approval and a manufacturer must choose to market it. Supply, litigation, business decisions, or regulatory issues can delay actual availability.
What is the difference between patents and exclusivity?
Patents are legal protections usually issued by the U.S. Patent and Trademark Office. FDA exclusivity is marketing protection granted by the FDA. They are separate, and either one can affect generic timing.
Why are there multiple patent dates?
One drug can have several patents covering different things: the active ingredient, a formulation, a manufacturing process, or a specific approved use. That is why a page may show several expiration dates instead of one simple generic date.
Built from FDA Orange Book patent and exclusivity data. Dates are refreshed from public FDA data when available; the marker is max(latest patent expiry, latest exclusivity expiry). Paragraph-IV settlements and first-filer 180-day exclusivity can shift the real date; a method-of-use patent may allow an earlier skinny-label generic for non-protected indications. Generic launch timing is an estimate, not a guarantee.
Where does this data come from?
Patents and exclusivity from the FDA Orange Book (small-molecule drugs), refreshed from public FDA data. Generic launch timing is an estimate, not a guarantee.

What it looks like

Color Brown / Purple
ShapeOval
ImprintPfizer;LLN;100
Size17 mm
ScoringNot scored
One label can cover several strengths, so colors may be combined — always confirm a loose pill against the dispensed prescription label or a pharmacist.
Where does this data come from?
Physical description (imprint, shape, color, scoring, coating) from this product’s FDA Structured Product Labeling (SPL), mirrored from DailyMed / openFDA.

Inactive Ingredients / Excipients

Inactive ingredients, also called excipients, are components of the drug product other than the active ingredient. They may include fillers, dyes, coatings, preservatives, flavors, or other formulation ingredients.

💡 Tap an ingredient (hover on desktop) to see what it is and why it’s used.

  • UNII L11K75P92J
    A mineral salt made from calcium and phosphate. It acts as a filler and binder in tablets to add bulk and help hold the medicine together in solid form.
  • UNII 1K09F3G675
    Ferric oxide red is an inorganic iron compound used as a colorant in medicines. It gives tablets, capsules, or other dosage forms a red or reddish tint for identification and appearance.
  • UNII XM0M87F357
    A dark iron oxide compound that gives medicines their black or dark color. It's used as a colorant in tablets and capsules to help identify the product and make it visually distinctive.
  • UNII 3NXW29V3WO
    Hypromellose is a plant-based thickener made from cellulose. It's used in medicines as a binder to hold ingredients together, a coating for tablets, and a thickener for liquids.
  • UNII EWQ57Q8I5X
    Lactose monohydrate is a natural sugar derived from milk. It serves as a filler and binder in tablets and capsules, helping create the proper size, texture, and consistency of the medicine.
  • UNII 70097M6I30
    Magnesium stearate is a salt made from magnesium and stearic acid, a fatty substance. It's used in tablets and capsules as a lubricant and glidant to help ingredients flow smoothly during manufacturing and prevent sticking.
  • UNII OP1R32D61U
    Microcrystalline cellulose is a purified form of cellulose, a natural fiber from plant sources. It acts as a binder and filler in tablets and capsules, helping hold ingredients together and give the medicine its shape and size.
  • UNII 3WJQ0SDW1A
    Polyethylene glycol is a synthetic liquid or solid polymer used in medicines as a solvent, lubricant, and humectant. It helps dissolve active ingredients, reduces friction during manufacturing, and retains moisture in the final product.
  • UNII 5856J3G2A2
    A starch-based powder made from potatoes and processed with sodium. It acts as a disintegrant, helping the tablet or capsule break apart quickly in the stomach so the medicine can be absorbed.
  • UNII 15FIX9V2JP
    Titanium dioxide is a bright white mineral powder commonly used as a colorant and opacifying agent. It makes pills and tablets white or lighter in color and helps make coatings non-transparent.
  • UNII XHX3C3X673
    Triacetin is a clear, oily liquid made from glycerin and acetic acid. It works as a plasticizer and solvent in medicines, helping soften coatings and improve how liquids mix together in formulations.

11 inactive ingredients listed in the exact product block matched to this NDC.

Where does this data come from?
Data sourced from official FDA Structured Product Labeling (SPL) via DailyMed — ingredient classCode="IACT" elements from the exact product block matched by this NDC. Label-section narrative from DailyMed / the openFDA label index is shown separately when available.

Inactive ingredient FAQ

Are inactive ingredients the same for every manufacturer?
No. Inactive ingredients can differ by manufacturer, dosage form, strength, and package / product version.
Why might an inactive ingredient be missing?
Some SPLs do not provide a complete structured inactive-ingredient list, and older or unusual labels may only include the information in narrative text.
Can inactive ingredients matter?
Yes. They can matter for allergies, intolerances, dyes, gluten / lactose concerns, preservatives, and formulation differences — but confirm with a pharmacist or the manufacturer when it’s clinically important.

Manufacturer & labeler

LabelerPfizer Laboratories Div Pfizer Inc
Application holderPFIZER INC
FDA applicationNDA210868 (NDA)
Labeler code00069
First marketedNov 2018
Product typeHuman Prescription Drug
Portfolio242 products on file

More NDCs from Pfizer Laboratories Div Pfizer Inc labeler code 00069

The labeler markets the product; the application holder owns the FDA approval. They’re often the same company but can differ (e.g. a repackager or an authorized generic). A mailing address / phone appears here when the manufacturer includes it in the product’s FDA label (not all do).
Where does this data come from?
Labeler, application holder and registered establishment from the FDA openFDA NDC Directory and Drugs@FDA; address/contact from the product’s FDA label.

Full prescribing information FDA SPL

The complete FDA label for this product — the official prescribing information, verbatim, section by section. Very long sections are excerpted here and marked; the full text is on DailyMed (linked in the sources below). Jump with a chip, search within the label, or expand everything.
🎯 Indications and Usage ⏱️ Dosage and Administration 💊 Dosage Forms and Strengths ⛔ Contraindications ⚠️ Warnings and Cautions 🤒 Adverse Reactions 🔄 Drug Interactions 👥 Use in Specific Populations 🤰 Pregnancy 🧒 Pediatric Use 🧓 Geriatric Use 🧬 Clinical Pharmacology 🧬 Mechanism of Action 📦 How Supplied / Storage and Handling 📦 Storage and Handling 📋 Description 💬 Information for Patients 🧬 Pharmacokinetics 🧬 Pharmacodynamics 🔬 Clinical Studies 🧪 Nonclinical Toxicology 📄 Carcinogenesis, Mutagenesis, Impairment of Fertility 📄 Patient Package Insert 📄 Recent Major Changes 📄 Package Label / Principal Display Panel
🎯 Indications and Usage 71 words ▾

1 INDICATIONS AND USAGE LORBRENA ® is indicated for the treatment of adult patients with metastatic non-small cell lung cancer (NSCLC) whose tumors are anaplastic lymphoma kinase (ALK)-positive as detected by an FDA-approved test. LORBRENA is a kinase inhibitor indicated for the treatment of adult patients with metastatic non-small cell lung cancer (NSCLC) whose tumors are anaplastic lymphoma kinase (ALK)-positive as detected by an FDA-approved test. ( 1 , 2.1 )

⏱️ Dosage and Administration ~3 min read ▾

2 DOSAGE AND ADMINISTRATION Recommended dosage : 100 mg orally once daily. ( 2.2 ) Severe Hepatic Impairment : 50 mg orally once daily. ( 2.5 , 8.6 , 12.3 ) Renal Impairment : 75 mg orally once daily. ( 2.6 , 8.7 , 12.3 )

2.1Patient Selection Select patients for the treatment of metastatic NSCLC with LORBRENA based on the presence of ALK positivity in tumor specimens [see Indications and Usage (1) and Clinical Studies (14) ] . Information on FDA-approved tests for the detection of ALK rearrangements in NSCLC is available at http://www.fda.gov/CompanionDiagnostics .

2.2Recommended Dosage The recommended dosage of LORBRENA is 100 mg orally once daily, with or without food, until disease progression or unacceptable toxicity [see Clinical Pharmacology (12.3) ] . Swallow tablets whole. Do not chew, crush or split tablets.

Do not ingest if tablets are broken, cracked, or otherwise not intact. Take LORBRENA at the same time each day. If a dose is missed, then take the missed dose unless the next dose is due within 4 hours.

Do not take 2 doses at the same time to make up for a missed dose. Do not take an additional dose if vomiting occurs after LORBRENA but continue with the next scheduled dose.

2.3Dosage Modifications for Adverse Reactions The recommended dose reductions are: • First dose reduction: LORBRENA 75 mg orally once daily • Second dose reduction: LORBRENA 50 mg orally once daily Permanently discontinue LORBRENA in patients who are unable to tolerate 50 mg orally once daily. Dosage modifications for adverse reactions of LORBRENA are provided in Table 1. Table 1 Recommended LORBRENA Dosage Modifications for Adverse Reactions Adverse Reaction Grade based on National Cancer Institute (NCI) Common Terminology Criteria for Adverse Events (CTCAE) version 4.03.

Dosage Modifications Abbreviation: AV=atrioventricular; DBP=diastolic blood pressure; SBP=systolic blood pressure. Central Nervous System Effects [see Warnings and Precautions (5.2) ] Grade 1 Continue at the same dose or withhold the dose until recovery to baseline. Resume LORBRENA at the same dose or at a reduced dose.

Grade 2 OR Grade 3 Withhold dose until Grade 0 or 1. Resume LORBRENA at a reduced dose. Grade 4 Permanently discontinue LORBRENA.

Hyperlipidemia [see Warnings and Precautions (5.3) ] Grade 4 hypercholesterolemia OR Grade 4 hypertriglyceridemia Withhold LORBRENA until recovery of hypercholesterolemia and/or hypertriglyceridemia to less than or equal to Grade 2. Resume LORBRENA at the same dose. If severe hypercholesterolemia and/or hypertriglyceridemia recurs, resume LORBRENA at a reduced dose.

Atrioventricular (AV) Block [see Warnings and Precautions (5.4) ] Second-degree AV block Withhold LORBRENA until PR interval is less than 200 ms. Resume LORBRENA at a reduced dose. First occurrence of complete AV block Withhold LORBRENA until • pacemaker placed OR • PR interval less than 200 ms.

If a pacemaker is placed, resume LORBRENA at the same dose. If no pacemaker is placed, resume LORBRENA at a reduced dose. Recurrent complete AV block Place pacemaker or permanently discontinue LORBRENA.

Interstitial Lung Disease (ILD)/Pneumonitis [see Warnings and Precautions (5.5) ] Any Grade treatment–related ILD/Pneumonitis Permanently discontinue LORBRENA. Hypertension [see Warnings and Precautions (5.6) ] Grade 3 (SBP greater than or equal to 160 mmHg or DBP greater than or equal to 100 mmHg; medical intervention indicated; more than one antihypertensive drug, or more intensive therapy than previously used indicated) Withhold LORBRENA until hypertension has recovered to Grade 1 or less (SBP less than 140 mmHg and DBP less than 90 mmHg), then resume LORBRENA at the same dose.

If Grade 3 hypertension recurs, withhold LORBRENA until recovery to Grade 1 or less, and resume at a reduced dose. If adequate hypertension control cannot be achieved with optimal medical management, permanently discontinue LORBRENA. Grade 4 (life-threatening consequences, urgent intervention indicat… [Excerpted — this section continues on DailyMed.]

💊 Dosage Forms and Strengths 65 words ▾

3 DOSAGE FORMS AND STRENGTHS Tablets: • 25 mg: 8 mm round, tan, immediate release, film-coated, debossed with "Pfizer" on one side and "25" and "LLN" on the other side • 100 mg: 8.5 mm × 17 mm oval, lavender, immediate release, film-coated, debossed with "Pfizer" on one side and "LLN 100" on the other side Tablets: 25 mg or 100 mg. ( 3 )

⛔ Contraindications 34 words ▾

4 CONTRAINDICATIONS LORBRENA is contraindicated in patients taking strong CYP3A inducers, due to the potential for serious hepatotoxicity [see Warnings and Precautions (5.1) ] . Concomitant use with strong CYP3A inducers. ( 4 )

⚠️ Warnings and Cautions ~3 min read ▾

5 WARNINGS AND PRECAUTIONS • Risk of Serious Hepatotoxicity with Concomitant Use of Strong CYP3A Inducers : Discontinue strong CYP3A inducers for 3 plasma half-lives of the strong CYP3A inducer prior to initiating LORBRENA. ( 2.4 , 5.1 ) • Central Nervous System (CNS) Effects : CNS effects include seizures, psychotic effects and changes in cognitive function, mood (including suicidal ideation), speech, mental status, and sleep. Withhold and resume LORBRENA at same or reduced dose or permanently discontinue LORBRENA based on severity.

( 2.3 , 5.2 ) • Hyperlipidemia : Initiate or increase the dose of lipid-lowering agents. Withhold and resume LORBRENA at same or reduced dose based on severity. ( 2.3 , 5.3 ) • Atrioventricular Block : Withhold and resume LORBRENA at same or reduced dose based on severity.

( 2.3 , 5.4 ) • Interstitial Lung Disease/Pneumonitis : Immediately withhold LORBRENA in patients with suspected ILD/pneumonitis. Permanently discontinue LORBRENA for treatment-related ILD/pneumonitis of any severity. ( 2.3 , 5.5 ) • Hypertension : Monitor blood pressure after 2 weeks and then at least monthly during treatment.

For severe hypertension, withhold LORBRENA, then dose reduce or permanently discontinue. ( 2.3 , 5.6 ) • Hyperglycemia : Assess fasting serum glucose prior to starting LORBRENA and regularly during treatment. If not adequately controlled with optimal medical management, withhold LORBRENA, then consider dose reduction or permanently discontinue, based on severity.

( 2.3 , 5.7 ) • Embryo-Fetal Toxicity : Can cause fetal harm. Advise females of reproductive potential of the potential risk to a fetus. Advise males and females of reproductive potential to use an effective non-hormonal method of contraception.

( 5.8 , 7.2 , 8.1 , 8.3 )

5.1Risk of Serious Hepatotoxicity with Concomitant Use of Strong CYP3A Inducers Severe hepatotoxicity occurred in 10 of 12 healthy subjects receiving a single dose of LORBRENA with multiple daily doses of rifampin, a strong CYP3A inducer. Grade 4 alanine aminotransferase (ALT) or aspartate aminotransferase (AST) elevations occurred in 50% of subjects, Grade 3 ALT or AST elevations occurred in 33% and Grade 2 ALT or AST elevations occurred in 8%. ALT or AST elevations occurred within 3 days and returned to within normal limits after a median of 15 days (7 to 34 days); the median time to recovery was 18 days in subjects with Grade 3 or 4 ALT or AST elevations and 7 days in subjects with Grade 2 ALT or AST elevations [see Drug Interactions (7.1) ] .

LORBRENA is contraindicated in patients taking strong CYP3A inducers. Discontinue strong CYP3A inducers for 3 plasma half-lives of the strong CYP3A inducer prior to initiating LORBRENA [see Contraindications (4) , Drug Interactions (7.1) ] .

5.2Central Nervous System Effects A broad spectrum of central nervous system (CNS) effects can occur in patients receiving LORBRENA. These include seizures, psychotic effects and changes in cognitive function, mood (including suicidal ideation), speech, mental status, and sleep. Overall, CNS effects occurred in 52% of the 476 patients who received 100 mg LORBRENA once daily in clinical trials [see Adverse Reactions (6.1) ] .

Cognitive effects occurred in 28% of the 476 patients; 2.9% of these events were severe (Grade 3 or 4). Mood effects occurred in 21% of patients; 1.7% of these events were severe. Speech effects occurred in 11% of patients; 0.6% of these events were severe.

Psychotic effects occurred in 7% of patients; 0.6% of these events were severe. Mental status changes occurred in 1.3% of patients; 1.1% of these events were severe. Seizures occurred in 1.9% of patients, sometimes in conjunction with other neurologic findings.

Sleep effects occurred in 12% of patients. The median time to first onset of any CNS effect was 1.4 months (1 day to 3.4 years). Overall, 2.1% of patients required permanent discontinuation of LORBRENA for a CNS effect; 10% required temporary discontinuation and 8% re… [Excerpted — this section continues on DailyMed.]

🤒 Adverse Reactions ~3 min read ▾

6 ADVERSE REACTIONS The following adverse reactions are described elsewhere in the labeling: • Risk of Serious Hepatotoxicity with Concomitant Use of Strong CYP3A Inducers [see Warnings and Precautions (5.1) ] • Central Nervous System Effects [see Warnings and Precautions (5.2) ] • Hyperlipidemia [see Warnings and Precautions (5.3) ] • Atrioventricular Block [see Warnings and Precautions (5.4) ] • Interstitial Lung Disease/Pneumonitis [see Warnings and Precautions (5.5) ] • Hypertension [see Warnings and Precautions (5.6) ] • Hyperglycemia [see Warnings and Precautions (5.7) ] Most common (incidence ≥20%) adverse reactions and Grade 3–4 laboratory abnormalities are edema, peripheral neuropathy, weight gain, cognitive effects, fatigue, dyspnea, arthralgia, diarrhea, mood effects, hypercholesterolemia, hypertriglyceridemia, and cough.

( 6.1 ) To report SUSPECTED ADVERSE REACTIONS, contact Pfizer Inc. at 1-800-438-1985 or www.pfizer.com or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch .

6.1Clinical Trials Experience Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in practice. The pooled safety population described in the Warnings and Precautions section reflects exposure to LORBRENA in 476 patients who received 100 mg LORBRENA once daily in Study B7461001 (N=327) and Study B7461006 (N=149). Among 476 patients who received LORBRENA, 75% were exposed for 6 months or longer and 61% were exposed for greater than 1 year.

In this pooled safety population, the most frequent adverse reactions in ≥ 20% of 476 patients who received LORBRENA were edema (56%), peripheral neuropathy (44%), weight gain (31%), cognitive effects (28%), fatigue (27%), dyspnea (27%), arthralgia (24%), diarrhea (23%), mood effects (21%), and cough (21%). The most frequent Grade 3–4 laboratory abnormalities in ≥ 20% of 476 patients who received LORBRENA were hypercholesterolemia (21%) and hypertriglyceridemia (21%). Previously Untreated ALK-Positive Metastatic NSCLC (CROWN Study) The safety of LORBRENA was evaluated in 149 patients with ALK-positive NSCLC in a randomized, open-label, active-controlled trial for the treatment of patients with ALK-positive, locally advanced or metastatic, NSCLC who had not received previous systemic treatment for advanced disease [see Clinical Studies (14) ].

The median duration of exposure to LORBRENA was 16.7 months (4 days to 34.3 months) and 76% received LORBRENA for at least 12 months. Serious adverse reactions occurred in 34% of patients treated with LORBRENA; the most frequently reported serious adverse reactions were pneumonia (4.7%), dyspnea (2.7%), respiratory failure (2.7%), cognitive effects (2.0%), and pyrexia (2.0%). Fatal adverse reactions occurred in 3.4% of patients treated with LORBRENA and included pneumonia (0.7%), respiratory failure (0.7%), cardiac failure acute (0.7%), pulmonary embolism (0.7%), and sudden death (0.7%).

Permanent discontinuation of LORBRENA due to adverse reactions occurred in 6.7% of patients. The most frequent adverse reaction that led to permanent discontinuation of LORBRENA was cognitive effects (1.3%). Adverse reactions leading to dose interruptions occurred in 49% of patients treated with LORBRENA.

The most frequent adverse reactions that led to dose interruptions of LORBRENA were hypertriglyceridemia (7%), edema (5%), pneumonia (4.7%) cognitive effects (4.0%), mood effects (4.0%), and hypercholesterolemia (3.4%). Adverse reactions leading to dose reductions occurred in 21% of patients treated with LORBRENA. The most frequent adverse reactions that led to dose reductions were edema (5%), hypertriglyceridemia (4.0%), and peripheral neuropathy (3.4%).

Tables 2 and 3 summarize most frequent adverse reactions and laboratory abnormalities, respectively, in patients treated with LORBRENA in Stud… [Excerpted — this section continues on DailyMed.]

🔄 Drug Interactions ~3 min read ▾

7 DRUG INTERACTIONS • Strong CYP3A Inducers : Contraindicated. ( 2.4 , 7.1 ) • Moderate CYP3A Inducers : Avoid concomitant use. If concomitant use cannot be avoided, increase the LORBRENA dose.

( 2.4 , 7.1 ) • Strong CYP3A Inhibitors : Avoid concomitant use; reduce LORBRENA dose if concomitant use cannot be avoided. ( 2.4 , 7.1 ) • Fluconazole : Avoid concomitant use; reduce LORBRENA dose if concomitant use cannot be avoided. ( 2.4 , 7.1 ) • Certain CYP3A Substrates : Avoid concomitant use with CYP3A substrates for which minimal concentration changes may lead to serious therapeutic failures.

( 7.2 ) • Certain P-gp Substrates : Avoid concomitant use with P-gp substrates for which minimal concentration changes may lead to serious therapeutic failures. ( 7.2 )

7.1Effect of Other Drugs on LORBRENA Strong CYP3A Inducers LORBRENA is contraindicated in patients taking strong CYP3A inducers [see Contraindication (4) ] . Discontinue strong CYP3A inducers for 3 plasma half-lives of the strong CYP3A inducer prior to initiating LORBRENA [see Dosage and Administration (2.3) ] . Concomitant use of LORBRENA with a strong CYP3A inducer decreased lorlatinib plasma concentrations [see Clinical Pharmacology (12.3) ] , which may decrease the efficacy of LORBRENA.

Severe hepatotoxicity occurred in healthy subjects receiving LORBRENA with rifampin, a strong CYP3A inducer. In 12 healthy subjects receiving a single 100 mg dose of LORBRENA with multiple daily doses of rifampin, Grade 3 or 4 increases in ALT or AST occurred in 83% of subjects and Grade 2 increases in ALT or AST occurred in 8%. A possible mechanism for hepatotoxicity is through activation of the pregnane X receptor (PXR) by LORBRENA and rifampin, which are both PXR agonists.

Moderate CYP3A Inducers Avoid concomitant use of moderate CYP3A inducers with LORBRENA. If concomitant use is unavoidable, increase the LORBRENA dose [see Dosage and Administration (2.4) ] . Concomitant use of LORBRENA with a moderate CYP3A inducer decreased lorlatinib plasma concentrations, which may decrease the efficacy of LORBRENA [see Clinical Pharmacology (12.3) ] .

Strong CYP3A Inhibitors Avoid concomitant use of LORBRENA with a strong CYP3A inhibitor. If concomitant use cannot be avoided, reduce the LORBRENA dosage [see Dosage and Administration (2.4) ] . Concomitant use with a strong CYP3A inhibitor increased lorlatinib plasma concentrations [see Clinical Pharmacology (12.3) ] , which may increase the incidence and severity of adverse reactions of LORBRENA.

Fluconazole Avoid concomitant use of LORBRENA with fluconazole. If concomitant use cannot be avoided, reduce the LORBRENA dosage [see Dosage and Administration (2.4) ] . Concomitant use of LORBRENA with fluconazole may increase lorlatinib plasma concentrations [see Clinical Pharmacology (12.3) ] , which may increase the incidence and severity of adverse reactions of LORBRENA.

7.2Effect of LORBRENA on Other Drugs Certain CYP3A Substrates Avoid concomitant use of LORBRENA with certain CYP3A substrates, for which minimal concentration changes may lead to serious therapeutic failures. If concomitant use is unavoidable, increase the CYP3A substrate dosage in accordance with approved product labeling. LORBRENA is a moderate CYP3A inducer.

Concomitant use of LORBRENA decreases the concentration of CYP3A substrates [see Clinical Pharmacology (12.3) ] , which may reduce the efficacy of these substrates. Certain P-glycoprotein (P-gp) Substrates Avoid concomitant use of LORBRENA with certain P-gp substrates for which minimal concentration changes may lead to serious therapeutic failures. If concomitant use is unavoidable, increase the P-gp substrate dosage in accordance with approved product labeling.

LORBRENA is a moderate P-gp inducer. Concomitant use of LORBRENA decreases the concentration of P-gp substrates [see Clinical Pharmacology (12.3) ] , which may reduce the efficacy of these substrates.

👥 Use in Specific Populations ~3 min read ▾

8 USE IN SPECIFIC POPULATIONS Lactation : Advise not to breastfeed. ( 8.2 )

8.1Pregnancy Risk Summary Based on findings from animal studies and its mechanism of action [see Clinical Pharmacology (12.1) ] , LORBRENA can cause embryo-fetal harm when administered to a pregnant woman. There are no available data on LORBRENA use in pregnant women. Administration of lorlatinib to pregnant rats and rabbits by oral gavage during the period of organogenesis resulted in malformations, increased post-implantation loss, and abortion at maternal exposures that were equal to or less than the human exposure at the recommended dose of 100 mg once daily based on AUC (see Data ) .

Advise a pregnant woman of the potential risk to a fetus. In the U.S. general population, the estimated background risk of major birth defects and miscarriage in clinically recognized pregnancies are 2 to 4% and 15 to 20%, respectively. Data Animal Data Preliminary embryo-fetal development studies investigating the administration of lorlatinib during the period of organogenesis were conducted in rats and rabbits.

In rabbits, lorlatinib administration resulted in abortion and total loss of pregnancy at doses of 15 mg/kg (approximately 3 times the human exposure at the recommended dose of 100 mg) or greater. At a dose of 4 mg/kg (approximately 0.6 times the human exposure at the recommended dose of 100 mg) toxicities included increased post-implantation loss and malformations including rotated limbs, malformed kidneys, domed head, high arched palate, and dilation of the cerebral ventricles. In rats, administration of lorlatinib resulted in total loss of pregnancy at doses of 4 mg/kg (approximately 5 times the human exposure at the recommended dose of 100 mg) or greater.

At a dose of 1 mg/kg (approximately equal to the human exposure at the recommended dose of 100 mg) there was increased post-implantation loss, decreased fetal body weight, and malformations including gastroschisis, rotated limbs, supernumerary digits, and vessel abnormalities.

8.2Lactation Risk Summary There are no data on the presence of lorlatinib or its metabolites in either human or animal milk or its effects on the breastfed infant or on milk production. Because of the potential for serious adverse reactions in breastfed infants, instruct women not to breastfeed during treatment with LORBRENA and for 7 days after the final dose.

8.3Females and Males of Reproductive Potential Pregnancy Testing Verify pregnancy status in females of reproductive potential prior to initiating LORBRENA [see Use in Specific Populations (8.1) ] . Contraception LORBRENA can cause embryo-fetal harm when administered to a pregnant woman [see Use in Specific Populations (8.1) ] . Females Advise female patients of reproductive potential to use effective non-hormonal contraception during treatment with LORBRENA and for at least 6 months after the final dose.

Advise females of reproductive potential to use a non-hormonal method of contraception, because LORBRENA can render hormonal contraceptives ineffective [see Drug Interactions (7.2) ] . Males Based on genotoxicity findings, advise males with female partners of reproductive potential to use effective contraception during treatment with LORBRENA and for at least 3 months after the final dose [see Nonclinical Toxicology (13.1) ] . Infertility Males Based on findings from animal studies, LORBRENA may transiently impair male fertility [see Nonclinical Toxicology (13.1) ] .

8.4Pediatric Use The safety and effectiveness of LORBRENA in pediatric patients have not been established.

8.5Geriatric Use Of the patients in Study B7461001 (N=295) and Study B7461006 (N=149) who received 100 mg LORBRENA orally once daily, 18% and 40% of patients, respectively, were aged 65 years or older. No clinically important differences in safety or efficacy were observed between patients aged 65 years or older and younger patients.

8.6Hepatic Impairment In patients with severe hepatic impairment (Ch… [Excerpted — this section continues on DailyMed.]

🤰 Pregnancy ~1 min read ▾

8.1Pregnancy Risk Summary Based on findings from animal studies and its mechanism of action [see Clinical Pharmacology (12.1) ] , LORBRENA can cause embryo-fetal harm when administered to a pregnant woman. There are no available data on LORBRENA use in pregnant women. Administration of lorlatinib to pregnant rats and rabbits by oral gavage during the period of organogenesis resulted in malformations, increased post-implantation loss, and abortion at maternal exposures that were equal to or less than the human exposure at the recommended dose of 100 mg once daily based on AUC (see Data ) .

Advise a pregnant woman of the potential risk to a fetus. In the U.S. general population, the estimated background risk of major birth defects and miscarriage in clinically recognized pregnancies are 2 to 4% and 15 to 20%, respectively. Data Animal Data Preliminary embryo-fetal development studies investigating the administration of lorlatinib during the period of organogenesis were conducted in rats and rabbits.

In rabbits, lorlatinib administration resulted in abortion and total loss of pregnancy at doses of 15 mg/kg (approximately 3 times the human exposure at the recommended dose of 100 mg) or greater. At a dose of 4 mg/kg (approximately 0.6 times the human exposure at the recommended dose of 100 mg) toxicities included increased post-implantation loss and malformations including rotated limbs, malformed kidneys, domed head, high arched palate, and dilation of the cerebral ventricles. In rats, administration of lorlatinib resulted in total loss of pregnancy at doses of 4 mg/kg (approximately 5 times the human exposure at the recommended dose of 100 mg) or greater.

At a dose of 1 mg/kg (approximately equal to the human exposure at the recommended dose of 100 mg) there was increased post-implantation loss, decreased fetal body weight, and malformations including gastroschisis, rotated limbs, supernumerary digits, and vessel abnormalities.

🧒 Pediatric Use 16 words ▾

8.4Pediatric Use The safety and effectiveness of LORBRENA in pediatric patients have not been established.

🧓 Geriatric Use 54 words ▾

8.5Geriatric Use Of the patients in Study B7461001 (N=295) and Study B7461006 (N=149) who received 100 mg LORBRENA orally once daily, 18% and 40% of patients, respectively, were aged 65 years or older. No clinically important differences in safety or efficacy were observed between patients aged 65 years or older and younger patients.

🧬 Clinical Pharmacology ~3 min read ▾

12 CLINICAL PHARMACOLOGY

12.1Mechanism of Action Lorlatinib is a kinase inhibitor with in vitro activity against ALK and ROS1 as well as TYK1, FER, FPS, TRKA, TRKB, TRKC, FAK, FAK2, and ACK. Lorlatinib demonstrated in vitro activity against multiple mutant forms of the ALK enzyme, including some mutations detected in tumors at the time of disease progression on crizotinib and other ALK inhibitors. In mice subcutaneously implanted with tumors harboring EML4 fusions with either ALK variant 1 or ALK mutations, including the G1202R and I1171T mutations detected in tumors at the time of disease progression on ALK inhibitors, administration of lorlatinib resulted in antitumor activity.

Lorlatinib also demonstrated anti-tumor activity and prolonged survival in mice implanted intracranially with EML4-ALK-driven tumor cell lines. The overall antitumor activity of lorlatinib in in vivo models was dose-dependent and correlated with inhibition of ALK phosphorylation.

12.2Pharmacodynamics Exposure-response relationships for Grade 3 or 4 hypercholesterolemia and for any Grade 3 or 4 adverse reaction were observed at steady-state exposures achieved at the recommended dosage, with higher probability of the occurrence of adverse reactions with increasing lorlatinib exposure. Cardiac Electrophysiology In 295 patients who received LORBRENA at the recommended dosage of 100 mg once daily and had an ECG measurement in Study B7461001, the maximum mean change from baseline for PR interval was 16.4 ms (2-sided 90% upper confidence interval [CI] 19.4 ms).

Among the 284 patients with PR interval <200 ms at baseline, 14% had PR interval prolongation ≥200 ms after starting LORBRENA. The prolongation of PR interval occurred in a concentration-dependent manner. Atrioventricular block occurred in 1% of patients.

In 275 patients who received LORBRENA at the recommended dosage in the activity-estimating portion of Study B7461001, no large mean increases from baseline in the QTcF interval (i.e., >20 ms) were detected.

12.3Pharmacokinetics At the recommended dosage, the mean (coefficient of variation [CV] %) maximum plasma concentration (C max ) is 577 ng/mL (42%) and the AUC 0-24h is 5,650 ng·h/mL (39%). Steady-state lorlatinib C max increases proportionally and AUC increased slightly less than proportionally over the dose range of 10 mg to 200 mg orally once daily (0.1 to 2 times the recommended dosage). Absorption The median lorlatinib T max is 1.2 hours (0.5 to 4 hours) following a single oral 100 mg dose and 2 hours (0.5 to 23 hours) following 100 mg orally once daily at steady‑state.

The mean absolute bioavailability is 81% (90% CI 76%, 86%). Effect of Food No clinically significant differences in lorlatinib pharmacokinetics were observed following administration of a high fat, high calorie meal (approximately 1000 calories with 150 calories from protein, 250 calories from carbohydrate, and 500 to 600 calories from fat). Distribution Lorlatinib is 66% bound to plasma proteins, in vitro.

The blood-to-plasma ratio is 0.99, in vitro. Elimination The mean plasma half‑life (t ½ ) of lorlatinib was 24 hours (40%) after a single oral 100 mg dose of LORBRENA. The mean oral clearance (CL/F) was 11 L/h (35%) following a single oral 100 mg dose and increased to 18 L/h (39%) at steady‑state, suggesting autoinduction.

Metabolism Lorlatinib is metabolized primarily by CYP3A4 and UGT1A4, with minor contribution from CYP2C8, CYP2C19, CYP3A5, and UGT1A3. In plasma, a benzoic acid metabolite (M8) of lorlatinib resulting from the oxidative cleavage of the amide and aromatic ether bonds of lorlatinib accounted for 21% of the circulating radioactivity. The oxidative cleavage metabolite, M8, is pharmacologically inactive.

Excretion Following a single oral 100 mg dose of radiolabeled lorlatinib, 48% of the radioactivity was recovered in urine (<1% as unchanged) and 41% in feces (about 9% as unchanged). Specific Populations No clinically significant differences in lorlatinib p… [Excerpted — this section continues on DailyMed.]

🧬 Mechanism of Action 139 words ▾

12.1Mechanism of Action Lorlatinib is a kinase inhibitor with in vitro activity against ALK and ROS1 as well as TYK1, FER, FPS, TRKA, TRKB, TRKC, FAK, FAK2, and ACK. Lorlatinib demonstrated in vitro activity against multiple mutant forms of the ALK enzyme, including some mutations detected in tumors at the time of disease progression on crizotinib and other ALK inhibitors. In mice subcutaneously implanted with tumors harboring EML4 fusions with either ALK variant 1 or ALK mutations, including the G1202R and I1171T mutations detected in tumors at the time of disease progression on ALK inhibitors, administration of lorlatinib resulted in antitumor activity.

Lorlatinib also demonstrated anti-tumor activity and prolonged survival in mice implanted intracranially with EML4-ALK-driven tumor cell lines. The overall antitumor activity of lorlatinib in in vivo models was dose-dependent and correlated with inhibition of ALK phosphorylation.

📦 How Supplied / Storage and Handling 143 words ▾

16 HOW SUPPLIED/STORAGE AND HANDLING Table 11 describes the available strengths and package configurations for LORBRENA: Table 11 LORBRENA Tablets Strength (mg) Package Configuration NDC Description 25 30 tablets bottle with a child-resistant closure 0069-0227-01 8 mm round, tan, immediate release film‑coated tablet, debossed with “Pfizer” on one side and “25” and “LLN” on the other side 25 120 tablets bottle with a child-resistant closure 0069-0227-03 8 mm round, tan, immediate release film‑coated tablet, debossed with “Pfizer” on one side and “25” and “LLN” on the other side 100 30 tablets bottle with a child-resistant closure 0069-0231-01 8.5 mm × 17 mm oval, lavender, immediate release, film‑coated tablet, debossed with “Pfizer” on one side and “LLN 100” on the other side Store at 20°C to 25°C (68°F to 77°F); excursions permitted between 15°C to 30°C (59°F to 86°F) [see USP Controlled Room Temperature].

📦 Storage and Handling 22 words ▾

Store at 20°C to 25°C (68°F to 77°F); excursions permitted between 15°C to 30°C (59°F to 86°F) [see USP Controlled Room Temperature].

📋 Description 152 words ▾

11 DESCRIPTION LORBRENA (lorlatinib) is a kinase inhibitor for oral administration. The molecular formula is C 21 H 19 FN 6 O 2 (anhydrous form) and the molecular weight is 406.41 Daltons. The chemical name is (10 R )-7-amino-12-fluoro-2,10,16-trimethyl-15-oxo-10,15,16,17-tetrahydro-2 H -4,8-methenopyrazolo[4,3- h ][2,5,11] benzoxadiazacyclotetradecine-3-carbonitrile.

The chemical structure is shown below: Lorlatinib is a white to off-white powder with a pKa of 4.92. The solubility of lorlatinib in aqueous media decreases over the range pH 2.55 to pH 8.02 from 32.38 mg/mL to 0.17 mg/mL. The log of the distribution coefficient (octanol/water) at pH 9 is 2.45.

LORBRENA is supplied as tablets containing 25 mg or 100 mg of lorlatinib with the following inactive ingredients: microcrystalline cellulose, dibasic calcium phosphate anhydrous, sodium starch glycolate, and magnesium stearate. The film-coating contains hydroxypropyl methylcellulose (HPMC) 2910/hypromellose, lactose monohydrate, macrogol/polyethylene glycol (PEG) 3350, triacetin, titanium dioxide, ferrosoferric oxide/black iron oxide, and iron oxide red. Chemical Structure

💬 Information for Patients ~2 min read ▾

17 PATIENT COUNSELING INFORMATION Advise the patient to read the FDA-approved patient labeling (Patient Information). Risk of Serious Hepatotoxicity with Concomitant Use of Strong CYP3A Inducers Inform patients of the potential risk of hepatotoxicity with the concomitant use of strong CYP3A inducers. Advise patients to inform their healthcare providers of all medications they are taking, including prescription medicines, over-the-counter drugs, vitamins, and herbal products (e.g., St.

John's wort) [see Warnings and Precautions (5.1) ] . Central Nervous System (CNS) Effects Advise patients to notify their healthcare provider if they experience new or worsening CNS symptoms [see Warnings and Precautions (5.2) ] . Hyperlipidemia Inform patients that serum cholesterol and triglycerides will be monitored during treatment.

Advise patients that initiation or an increase in the dose of lipid-lowering agents may be required [see Warnings and Precautions (5.3) ] . Atrioventricular (AV) Block Inform patients of the risks of AV block. Advise patients to contact their healthcare provider immediately to report new or worsening cardiac symptoms [see Warnings and Precautions (5.4) ] .

Interstitial Lung Disease (ILD)/Pneumonitis Inform patients of the risks of severe ILD/pneumonitis. Advise patients to contact their healthcare provider immediately to report new or worsening respiratory symptoms [see Warnings and Precautions (5.5) ] . Hypertension Advise patients of the risks of hypertension and to promptly report signs or symptoms of hypertension to their healthcare provider.

Advise patients with hypertension that antihypertension medications may need to be initiated or adjusted during treatment with LORBRENA [see Warnings and Precautions (5.6) ] . Hyperglycemia Inform patients of the risks of new or worsening hyperglycemia and of the need to periodically monitor glucose levels and to promptly report hyperglycemia to their healthcare provider. Advise patients with newly occurring hyperglycemia during treatment with LORBRENA that antihyperglycemic medications may need to be initiated.

Inform patients with diabetes mellitus or glucose intolerance that antihyperglycemic medications may need to be adjusted during treatment with LORBRENA [see Warnings and Precautions (5.7) ] . Embryo-Fetal Toxicity Advise females of reproductive potential of the potential risk to a fetus. Advise females to inform their healthcare provider of a known or suspected pregnancy [see Warnings and Precautions (5.8) , Use in Specific Populations (8.1) ] .

Advise females of reproductive potential to use effective non-hormonal contraception during treatment with LORBRENA and for at least 6 months after the final dose [see Use in Specific Populations (8.3) ] . Advise male patients with female partners of reproductive potential to use effective contraception during treatment with LORBRENA and for at least 3 months after the final dose [see Use in Specific Populations (8.3) , Nonclinical Toxicology (13.1) ] . Lactation Advise women not to breastfeed during treatment with LORBRENA and for 7 days after the final dose [see Use in Specific Populations (8.2) ] .

Infertility Advise males of reproductive potential that LORBRENA may transiently impair fertility [see Use in Specific Populations (8.3) , Nonclinical Toxicology (13.1) ] .

🧬 Pharmacokinetics ~3 min read ▾

12.3Pharmacokinetics At the recommended dosage, the mean (coefficient of variation [CV] %) maximum plasma concentration (C max ) is 577 ng/mL (42%) and the AUC 0-24h is 5,650 ng·h/mL (39%). Steady-state lorlatinib C max increases proportionally and AUC increased slightly less than proportionally over the dose range of 10 mg to 200 mg orally once daily (0.1 to 2 times the recommended dosage). Absorption The median lorlatinib T max is 1.2 hours (0.5 to 4 hours) following a single oral 100 mg dose and 2 hours (0.5 to 23 hours) following 100 mg orally once daily at steady‑state.

The mean absolute bioavailability is 81% (90% CI 76%, 86%). Effect of Food No clinically significant differences in lorlatinib pharmacokinetics were observed following administration of a high fat, high calorie meal (approximately 1000 calories with 150 calories from protein, 250 calories from carbohydrate, and 500 to 600 calories from fat). Distribution Lorlatinib is 66% bound to plasma proteins, in vitro.

The blood-to-plasma ratio is 0.99, in vitro. Elimination The mean plasma half‑life (t ½ ) of lorlatinib was 24 hours (40%) after a single oral 100 mg dose of LORBRENA. The mean oral clearance (CL/F) was 11 L/h (35%) following a single oral 100 mg dose and increased to 18 L/h (39%) at steady‑state, suggesting autoinduction.

Metabolism Lorlatinib is metabolized primarily by CYP3A4 and UGT1A4, with minor contribution from CYP2C8, CYP2C19, CYP3A5, and UGT1A3. In plasma, a benzoic acid metabolite (M8) of lorlatinib resulting from the oxidative cleavage of the amide and aromatic ether bonds of lorlatinib accounted for 21% of the circulating radioactivity. The oxidative cleavage metabolite, M8, is pharmacologically inactive.

Excretion Following a single oral 100 mg dose of radiolabeled lorlatinib, 48% of the radioactivity was recovered in urine (<1% as unchanged) and 41% in feces (about 9% as unchanged). Specific Populations No clinically significant differences in lorlatinib pharmacokinetics were observed based on age (19 to 85 years), sex, race/ethnicity (52% White, 8% Black, 27% Asian), body weight (32-156 kg), CL cr 30 to 89 mL/min (estimated by Cockcroft Gault), mild (total bilirubin ≤ ULN and AST > ULN or total bilirubin > 1 to 1.5 × ULN and any AST) to moderate (Child-Pugh B) hepatic impairment, or metabolizer phenotypes for CYP3A5 and CYP2C19.

Patients with Moderate or Severe Hepatic Impairment Following administration of a single oral 100 mg dose of LORBRENA, lorlatinib AUC increased 1.1-fold in non-cancer subjects with moderate hepatic impairment (Child-Pugh B) and 1.8-fold in non-cancer subjects with severe hepatic impairment (Child-Pugh C). Patients with Renal Impairment Following administration of a single oral 100 mg dose of LORBRENA, lorlatinib AUC increased 1.4-fold in subjects with CL cr 15 to <30 mL/min (estimated by Cockcroft Gault). The pharmacokinetics of lorlatinib have not been studied in patients with end-stage renal disease requiring hemodialysis.

Drug Interaction Studies Clinical Studies and Model-Informed Approaches Strong CYP3A Inducers : Rifampin (a strong CYP3A inducer that also activates PXR) 600 mg once daily for 8 days (Days 1 to 8) coadministered with a single oral 100 mg dose of LORBRENA on Day 8 reduced the mean lorlatinib AUC by 85% and C max by 76%. Grade 2 to 4 increases in ALT or AST occurred within 3 days. Grade 4 ALT or AST elevations occurred in 50%, Grade 3 ALT or AST elevations in 33%, and Grade 2 ALT or AST elevations occurred in 8% of subjects.

ALT and AST returned to within normal limits within 7 to 34 days (median 15 days). Moderate CYP3A Inducers : Modafinil (a moderate CYP3A inducer) decreased lorlatinib AUC by 23% and C max by 22% of a single oral 100 mg dose of LORBRENA. Strong CYP3A Inhibitors : Itraconazole (a strong CYP3A inhibitor) increased lorlatinib AUC 1.4-fold and C max 1.2-fold of a single oral 100 mg dose of LORBRENA.

Fluconazole : Fluconazole is predicted to increase lorlatinib AUC 1.6-fold and… [Excerpted — this section continues on DailyMed.]

🧬 Pharmacodynamics 157 words ▾

12.2Pharmacodynamics Exposure-response relationships for Grade 3 or 4 hypercholesterolemia and for any Grade 3 or 4 adverse reaction were observed at steady-state exposures achieved at the recommended dosage, with higher probability of the occurrence of adverse reactions with increasing lorlatinib exposure. Cardiac Electrophysiology In 295 patients who received LORBRENA at the recommended dosage of 100 mg once daily and had an ECG measurement in Study B7461001, the maximum mean change from baseline for PR interval was 16.4 ms (2-sided 90% upper confidence interval [CI] 19.4 ms).

Among the 284 patients with PR interval <200 ms at baseline, 14% had PR interval prolongation ≥200 ms after starting LORBRENA. The prolongation of PR interval occurred in a concentration-dependent manner. Atrioventricular block occurred in 1% of patients.

In 275 patients who received LORBRENA at the recommended dosage in the activity-estimating portion of Study B7461001, no large mean increases from baseline in the QTcF interval (i.e., >20 ms) were detected.

🔬 Clinical Studies ~3 min read ▾

14 CLINICAL STUDIES Previously Untreated ALK-Positive Metastatic NSCLC (CROWN Study) The efficacy of LORBRENA for the treatment of patients with ALK-positive NSCLC who had not received prior systemic therapy for metastatic disease was established in an open-label, randomized, active-controlled, multicenter study (Study B7461006; NCT03052608). Patients were required to have an ECOG performance status of 0–2 and ALK-positive NSCLC as identified by the VENTANA ALK (D5F3) CDx assay. Neurologically stable patients with treated or untreated asymptomatic CNS metastases, including leptomeningeal metastases, were eligible.

Patients were required to have finished radiation therapy, at least 2 weeks (for stereotactic or partial radiation) or 4 weeks (for whole brain irradiation) prior to randomization. Patients with severe acute or chronic psychiatric conditions, including recent (within the past year) or active suicidal ideation or behavior, were excluded. Patients were randomized 1:1 to receive LORBRENA 100 mg orally once daily or crizotinib 250 mg orally twice daily.

Randomization was stratified by ethnic origin (Asian vs. non-Asian) and the presence or absence of CNS metastases at baseline. Treatment on both arms was continued until disease progression or unacceptable toxicity. The major efficacy outcome measure was progression-free survival (PFS) as determined by Blinded Independent Central Review (BICR) according to Response Evaluation Criteria in Solid Tumors (RECIST) version 1.1 (v1.1).

Additional efficacy outcome measures were overall survival (OS) and tumor assessment related data by BICR, including overall response rate (ORR), and duration of response (DOR). In patients with measurable CNS metastases at baseline, additional outcome measures were intracranial overall response rate (IC-ORR) and intracranial duration of response (IC-DOR) by BICR. A total of 296 patients were randomized to LORBRENA (n=149) or crizotinib (n=147).

The demographic characteristics of the overall study population were: median age 59 years (range: 26 to 90 years), age ≥65 years (35%), 59% female, 49% White, 44% Asian, and 0.3% Black. The ECOG performance status at baseline was 0 or 1 in 96% of patients. The majority of patients had adenocarcinoma (95%) and never smoked (59%).

CNS metastases were present in 26% (n=78) of patients: of these, 30 patients had measurable CNS lesions. Efficacy results from Study B7461006 as assessed by BICR are summarized in Table 6 and Figure 1. Results demonstrated a significant improvement in PFS for the LORBRENA arm over the crizotinib arm.

At the data cutoff point OS data was not mature. Table 6 Efficacy Results in Study B7461006 (CROWN) Efficacy Parameter LORBRENA N=149 Crizotinib N=147 Abbreviations: CI=confidence interval; N=number of patients; NE=not estimable; PFS=progression‑free survival. Progression-free survival Number of events, n (%) 41 (28%) 86 (59%) Progressive disease, n (%) 32 (22%) 82 (56%) Death, n (%) 9 (6%) 4 (3%) Median, months (95% CI) Based on the Brookmeyer and Crowley method.

NE (NE, NE) 9.3 (7.6, 11.1) Hazard ratio (95% CI) Hazard ratio based on Cox proportional hazards model. 0.28 (0.19, 0.41) p-value p-value based on 1-sided stratified log-rank test. <0.0001 Overall response rate Overall response rate (95% CI) Using exact method based on binomial distribution. 76% (68, 83) 58% (49, 66) Complete response 3% 0% Partial response 73% 58% Duration of response Number of responders, n 113 85 Median, months (Range) NE (0.9, 31.3) 11 (1.1, 27.5) Response duration ≥6 months, n (%) 101 (89%) 53 (62%) Response duration ≥12 months, n (%) 79 (70%) 23 (27%) Response duration ≥18 months, n (%) 34 (30%) 9 (11%) Figure 1: Kaplan-Meier Plot of Progression-Free Survival by BICR in Study B7461006 (CROWN) The results of prespecified exploratory analyses of intracranial response rate in 30 patients with measurable CNS lesions at baseline as assessed by BICR are summarized in Table 7.

Table 7 Intracranial Response Rat… [Excerpted — this section continues on DailyMed.]

🧪 Nonclinical Toxicology 204 words ▾

13 NONCLINICAL TOXICOLOGY

13.1Carcinogenesis, Mutagenesis, Impairment of Fertility Carcinogenicity studies have not been conducted with lorlatinib. Lorlatinib was aneugenic in an in vitro assay in human lymphoblastoid TK6 cells and positive for micronuclei formation in vivo in the bone marrow of rats. Lorlatinib was not mutagenic in an in vitro bacterial reverse mutation (Ames) assay.

Dedicated fertility studies were not conducted with lorlatinib. Findings in male reproductive organs occurred in repeat-dose toxicity studies and included lower testicular, epididymal, and prostate weights; testicular tubular degeneration/atrophy; prostatic atrophy; and/or epididymal inflammation at 15 mg/kg/day and 7 mg/kg/day in rats and dogs, respectively (approximately 8 and 2 times, respectively, the human exposure at the recommended dose of 100 mg based on AUC). The effects on male reproductive organs were reversible.

13.2Animal Toxicology and/or Pharmacology Distended abdomen, skin rash, and increased cholesterol and triglycerides occurred in animals. These findings were accompanied by hyperplasia and dilation of the bile ducts in the liver and acinar atrophy of the pancreas in rats at 15 mg/kg/day and in dogs at 2 mg/kg/day (approximately 8 and 0.5 times, respectively, the human exposure at the recommended dose of 100 mg based on AUC). All effects were reversible within the recovery period.

📄 Carcinogenesis, Mutagenesis, Impairment of Fertility 125 words ▾

13.1Carcinogenesis, Mutagenesis, Impairment of Fertility Carcinogenicity studies have not been conducted with lorlatinib. Lorlatinib was aneugenic in an in vitro assay in human lymphoblastoid TK6 cells and positive for micronuclei formation in vivo in the bone marrow of rats. Lorlatinib was not mutagenic in an in vitro bacterial reverse mutation (Ames) assay.

Dedicated fertility studies were not conducted with lorlatinib. Findings in male reproductive organs occurred in repeat-dose toxicity studies and included lower testicular, epididymal, and prostate weights; testicular tubular degeneration/atrophy; prostatic atrophy; and/or epididymal inflammation at 15 mg/kg/day and 7 mg/kg/day in rats and dogs, respectively (approximately 8 and 2 times, respectively, the human exposure at the recommended dose of 100 mg based on AUC). The effects on male reproductive organs were reversible.

📄 Patient Package Insert ~3 min read ▾

PATIENT INFORMATION LORBRENA (lor-BREN-ah) (lorlatinib) tablets This Patient Information has been approved by the U.S. Food and Drug Administration. Revised: January 2026 What is the most important information I should know about LORBRENA?

LORBRENA can cause serious side effects, including: • Liver problems due to interactions with other medicines. Liver problems can be severe. It is important to know what medicines not to take during treatment with LORBRENA.

See “ Tell your healthcare provider about all the medicines you take, including .” • Central nervous system (CNS) effects. CNS effects can be severe. Tell your healthcare provider if you get any new or worsening symptoms of CNS effects, including: o problems with thinking, such as forgetfulness or confusion o changes in mood, such as depression and thoughts about suicide or dying o psychotic effects, such as seeing or hearing things that are not real (hallucinations) o seizures o changes in speech o changes in sleep • Increases in the cholesterol and triglycerides (lipid) levels in your blood.

Most people will get an increase in the lipid levels in their blood during treatment with LORBRENA. o If you get increases in the lipid levels in your blood, your healthcare provider may start you on a new medicine or increase your dose if you are already taking a medicine to lower the lipid levels in your blood. o Your healthcare provider will do blood tests to check the lipid levels in your blood before starting treatment, 1 and 2 months after starting treatment, and during treatment with LORBRENA. • Heart problems.

LORBRENA can cause very slow or abnormal heartbeats. Your healthcare provider will check your heart rhythm (electrocardiogram or EKG) before starting and during treatment with LORBRENA. In some people, these problems are severe, and you may need to get a pacemaker.

Tell your healthcare provider right away if you feel dizzy or faint or have abnormal heartbeats. • Lung problems. LORBRENA can cause severe or life-threatening swelling (inflammation) of the lungs during treatment that can lead to death. Symptoms may be like those from lung cancer.

Tell your healthcare provider right away if you get any new or worsening symptoms of lung problems, including trouble breathing, shortness of breath, cough, or fever. • High blood pressure (hypertension). Your healthcare provider will check your blood pressure before starting treatment, 2 weeks after starting treatment, and then at least every month during treatment with LORBRENA. Your healthcare provider may start or change your blood pressure medicine if you get high blood pressure.

Tell your healthcare provider right away if you get signs or symptoms of high blood pressure, including: headaches, dizziness, blurred vision, chest pain or shortness of breath. • High blood sugar (hyperglycemia). LORBRENA can cause new or worsening increases in your blood sugar levels. Your healthcare provider will do blood tests to check your blood sugar levels before starting and during treatment with LORBRENA.

Your healthcare provider may start or change your blood sugar medicine if you get high blood sugar. Tell your healthcare provider right away if you get any signs and symptoms of high blood sugar, including: o feeling very thirsty o needing to urinate more than usual o feeling very hungry o feeling sick to your stomach o feeling weak or tired o feeling confused If you get serious side effects during treatment, your healthcare provider may change your dose, temporarily stop, or permanently stop treatment with LORBRENA.

See " What are possible side effects of LORBRENA? " for more information about side effects. What is LORBRENA? LORBRENA is a prescription medicine used to treat adults with non-small cell lung cancer (NSCLC): • that is caused by an abnormal anaplastic lymphoma kinase (ALK) gene, and • that has spread to other parts of your body (metastatic).

Your healthcare provider will perform a test to make sure that LORBRENA is right for yo… [Excerpted — this section continues on DailyMed.]

📄 Recent Major Changes 28 words ▾

Dosage Modifications for Drug Interactions ( 2.4 ) 1/2026 Recommended Dosage for Severe Hepatic Impairment ( 2.5 ) 1/2026 Recommended Dosage for Renal Impairment ( 2.6 ) 1/2026

📄 Package Label / Principal Display Panel 62 words ▾

PRINCIPAL DISPLAY PANEL - 25 mg Tablet Bottle Label Pfizer NDC 0069-0227-01 Lorbrena ® (lorlatinib) tablets 25 mg 30 Tablets Rx only PRINCIPAL DISPLAY PANEL - 25 mg Tablet Bottle Label

PRINCIPAL DISPLAY PANEL - 100 mg Tablet Bottle Label Pfizer NDC 0069-0231-01 Lorbrena ® (lorlatinib) tablets 100 mg 30 Tablets Rx only PRINCIPAL DISPLAY PANEL - 100 mg Tablet Bottle Label

Source: FDA Structured Product Labeling, mirrored from DailyMed / openFDA. Prefer the government’s original formatting? View this label on DailyMed ↗

Medicaid utilization & spend

📍 This exact package only: Medicaid data is reported per full 11-digit NDC — labeler, product and pack size — so every number here is for this package alone, not the drug overall. Other pack sizes report separately.
💊 Pharmacy benefit only: These are Medicaid outpatient pharmacy claims, billed by NDC. They exclude the medical benefit — clinic- or hospital-administered drugs billed under HCPCS J-codes — so drugs used mostly that way (e.g. Avastin, Lucentis, Keytruda) can look low or missing here. That’s expected, not an error.
📅 Q1 2025 – Q1 2026 · 5 quarters of data
ⓘ The newest quarter is usually incomplete when first published; states restate recent quarters in later CMS releases, so the latest figures typically revise upward. State coverage-policy changes can also shift quarter-to-quarter totals.
Prescriptions last 4 qtrs
336
Units reimbursed last 4 qtrs
27.4K
Gross reimbursed last 4 qtrs
$6.56M
Avg / prescription
$19,517.36
Avg / unit
$239.03
Latest quarter Q1 2026
77Rx
Fee-for-service vs managed care ⓘ
87% FFS 13% MCO
Fee-for-service · 292 Rx Managed care · 44 Rx
State Medicaid map
Alaska: no data reported AK Maine: no data reported ME Washington: no data reported WA Idaho: no data reported ID Montana: no data reported MT North Dakota: no data reported ND Minnesota: no data reported MN Wisconsin: 1,980 units · 33.5 per 100k residents WI Michigan: 2,580 units · 25.7 per 100k residents MI New York: 12,834 units · 65.6 per 100k residents NY Vermont: no data reported VT New Hampshire: no data reported NH Oregon: no data reported OR Nevada: no data reported NV Wyoming: no data reported WY South Dakota: no data reported SD Iowa: no data reported IA Illinois: no data reported IL Indiana: no data reported IN Ohio: no data reported OH Pennsylvania: no data reported PA New Jersey: no data reported NJ Massachusetts: no data reported MA California: 6,006 units · 15.4 per 100k residents CA Utah: no data reported UT Colorado: no data reported CO Nebraska: no data reported NE Missouri: no data reported MO Kentucky: no data reported KY West Virginia: no data reported WV Virginia: no data reported VA Maryland: no data reported MD Connecticut: no data reported CT Rhode Island: no data reported RI Arizona: no data reported AZ New Mexico: no data reported NM Kansas: no data reported KS Arkansas: no data reported AR Tennessee: no data reported TN North Carolina: 4,035 units · 37.2 per 100k residents NC South Carolina: no data reported SC Delaware: no data reported DE Oklahoma: no data reported OK Louisiana: no data reported LA Mississippi: no data reported MS Alabama: no data reported AL Georgia: no data reported GA D.C.: no data reported DC Hawaii: no data reported HI Texas: no data reported TX Florida: no data reported FL
Units reimbursed · per 100k residents
15.465.6
gray = no data reported ⓘ
Colors are per 100,000 residents, so big states don’t automatically dominate. Tap or hover a state for its actual totals.
Tap or hover a state
…for its Medicaid breakdown
🏆 Top states by units · per 100k residents
1 New York 65.6 /100k
2 North Carolina 37.2 /100k
3 Wisconsin 33.5 /100k
4 Michigan 25.7 /100k
5 California 15.4 /100k
National units — by quarter
💵 About the dollar figures: “reimbursed” is what Medicaid paid pharmacies before confidential manufacturer rebates, so the program’s real net cost is lower than these numbers. Fee-for-service and managed-care claims are combined unless split above. Source: CMS State Drug Utilization Data; per-100k rates use 2023 Census population estimates.

Medicaid utilization by pack size

Medicaid (SDUD) totals over the four most recent reported quarters for every package size of this drug — handy when a specific package (e.g. a starter/titration pack) carries little or no Medicaid volume on its own.
30 tablets this page00069-0227-01 336 Rx · $6,557,833
120 tablets00069-0227-03 11 Rx · $157,080
Drug total (last 4 qtrs): 347 Rx · 28,275 units · $6,714,913 gross reimbursed
Tap a pack size to open its page. Source: CMS State Drug Utilization Data, last 4 quarters.

Medicare Part D spend CMS · PART D · 2026 (Q1)

Medicare Part D (outpatient prescription) spending for Lorbrena — the program that covers self-administered drugs. 1 manufacturer.
⚠️ Drug-level data: CMS publishes Part D spending by drug, not by NDC — these figures combine every manufacturer, strength and package size sold under the name Lorbrena. That’s a different level of aggregation than the Medicaid card above, which is specific to this exact 11-digit NDC (pack size included), so the two aren’t directly comparable.
Period
Total Part D spend
$62.71M
Claims incl. refills
3.2K
Beneficiaries
1.2K
Spend / beneficiary
$50,528.55
Spend / claim
$19,377.61
Trend by period
💵 About the dollar figures: spending is what Part D plans paid before confidential manufacturer rebates, so the program’s real net cost is lower. A blank patient count means fewer than 11 people — CMS hides counts that small to protect privacy. Source: CMS Medicare Quarterly Part D Spending by Drug (data.cms.gov), updated quarterly.

Reported adverse events (FAERS)

Read carefully: FAERS reports are voluntary and unverified. Counts are not incidence, do not establish causation, are subject to reporting bias, and cannot be used to compare one drug to another. Shown for signal context only. Reports for Lorbrena (this brand).

Top reported reactions

Death1,304
Neoplasm Progression621
Hallucination404
Weight Increased399
Blood Cholesterol Increased348
Dyspnoea270
Oedema269

Age at onset

Infant1
Child24
Adolescent3
Adult575
Elderly271

Reporter sex

6,977 reports
Male · 47%
Female · 53%

Serious outcomes

Death1,867
Hospitalization1,530
Life-threatening158
Disabling90
Reports over time (by year) — tap or hover for the count & year
2019 2021 2023 2026 1,565 0
Most recent year is provisional (FAERS lags ~3 months).
Where does this data come from?
Adverse-event reports from the FDA Adverse Event Reporting System (FAERS) via openFDA. FAERS reports are voluntary and unverified — counts are not incidence and don’t establish causation.

About this NDC listing & data coverage

Finished prescription product
What data is (and isn’t) available for this NDC — tap to expand
NDC identity (package / product / labeler codes) ✓ Available
Labeler ✓ Available
Product & package description ✓ Available
Marketing category & status ✓ Available
Active ingredient / dosage form / route ✓ Available
FDA label (SPL via DailyMed) ✓ Available
Package photos ✓ Available
Inactive ingredients (structured) ✓ Available
NADAC pharmacy acquisition price (CMS) — Not published for this NDC CMS publishes NADAC only for NDCs reported in its retail-pharmacy survey.
Orange Book / therapeutic-equivalence data ✓ Available
HCPCS J-code billing crosswalk — Not published for this NDC Most self-administered / retail products have no J-code — that is normal.
Medicaid utilization (CMS SDUD) ✓ Available
“Not published” reflects what the public FDA / CMS / NLM sources provide for this exact package code — it is a property of the data feeds, not a judgment about the product.

Questions about this listing

Why is there no price listed?
The pricing shown on our NDC pages comes from CMS NADAC, a voluntary survey of retail community pharmacy invoices. CMS does not publish a NADAC for every NDC — packages outside the retail survey (institutional and hospital products, bulk packages, discontinued items, and many OTC items) may never receive one. A missing price reflects the survey's scope, not this product's actual cost, and does not mean the product is free or unavailable.
Is the NDC printed on the package the same as the 11-digit billing NDC?
Yes, they identify this exact package in different formats. The form printed on the packaging and shown on DailyMed is the one the FDA registered. Insurance claims use a fixed 11-digit 5-4-2 format, so the short segment is padded with a leading zero and the dashes are dropped. The Identity section at the top of this page lists each form of this code.
Is this package still being marketed?
Yes, per the latest FDA NDC Directory data on this page: this package is listed as actively marketed, with no marketing end date reported by Pfizer Laboratories Div Pfizer Inc. Listing status can change — the directory data on this page refreshes weekly.
Does this product come in other package sizes?
Yes — the FDA directory lists 1 other package presentation of this same product, including 120 tablets (00069-0227-03). Each has its own NDC and its own page — see the package list near the top of this page.
Who lists this product with the FDA?
Pfizer Laboratories Div Pfizer Inc is the labeler of record for this NDC — the company under whose FDA-assigned code the package is listed. The labeler may be the manufacturer itself or a distributor marketing the product under its own code.
Do I need a prescription for this product?
This NDC is listed with FDA as a prescription product, so it is dispensed under a prescriber's order. Your pharmacist can tell you whether any over-the-counter forms of the same medication exist.
This page identifies an FDA-listed package (the NDC) and reports public regulatory and pricing data about the listing. It is reference information, not a medical recommendation — talk to your pharmacist or prescriber about your own medication.
Where does this data come from?
Listing facts (marketing category, packager status, marketing dates) from the FDA openFDA NDC Directory; label availability from DailyMed; pricing coverage from CMS NADAC; equivalence scope from the FDA Orange Book.
← 00069-0223-02 · Pfizer 00069-0228-02 · Pfizer →
For educational and professional reference only — not medical advice. Pricing reflects published NADAC and CMS ASP (free public data) and may differ from your acquisition cost; always verify before billing or dispensing.