FDA-filed SPL labeling · retrieved through openFDA

Lorlatinib

Lorlatinib is a targeted cancer medicine used to treat metastatic non-small cell lung cancer (NSCLC) in adults whose tumors carry a specific genetic change called ALK-positive.

Brand name Lorbrena
Drug class Kinase Inhibitor
Rx Form 1 Route Oral
Dr. Brian Staiger, PharmD, BCPS
Reviewed by Last reviewed Jul 10, 2026
🧬 Where this information comes from Click to expand

The clinical label records used on this page are FDA-filed Structured Product Labeling (SPL) retrieved through openFDA. We identified 2 clinical label sets within the page’s selected clinical scope after exact ingredient or ingredient-combination matching and applicable route/form matching. Forms, routes, brands, labelers, strengths, and NDC product-record counts are built separately from matching FDA National Drug Code Directory records. The linked DailyMed document is a representative official source for verification, not the page’s only clinical source. View the linked label on DailyMed →

At a glance
Linked label effectiveJun 26, 2026
Clinical labels in scope 2
AvailabilityRx
Earliest approval/marketing year 2018
FDA-listed product records 12
Boxed warningNone found in compared labels
How we combine label and product data →
Lorlatinib at a glance The quick version — the full detail is in the Patient Information Guide below.
💊
HelloPharmacist Editorial Team Bottom Line
Lorlatinib (Lorbrena) is a once-daily oral targeted therapy for adults with ALK-positive metastatic non-small cell lung cancer. It is effective but comes with important risks — particularly serious liver toxicity if combined with certain interacting medicines, and effects on the brain, heart, cholesterol, and blood sugar that require regular monitoring. Work closely with your oncology team, keep all lab and follow-up appointments, and tell every provider you see that you are taking this medicine.

📖 Lorlatinib: Patient Information Guide

A plain-language walkthrough of Lorlatinib — what it treats, how it works, how it’s taken, side effects, warnings and interactions. Tap any section to expand it.

🎯What it's used for

Lorlatinib is a targeted therapy used to treat a specific type of advanced lung cancer in adults. Below is the full set of supported uses based on the available product evidence.

  • Lorbrena (oral tablet) is indicated for adults with metastatic non-small cell lung cancer (NSCLC) whose tumors test positive for an ALK gene rearrangement, confirmed by an FDA-approved diagnostic test.
  • Lorbrena has been studied in patients who have not yet received systemic treatment for advanced NSCLC, as well as in patients whose disease progressed after treatment with other ALK inhibitors (such as crizotinib or others).
⚙️How it works

Lorlatinib works by blocking a protein called ALK (anaplastic lymphoma kinase) — a faulty enzyme that, when abnormally active due to a gene rearrangement, drives cancer cells to grow and multiply out of control. By inhibiting ALK, lorlatinib cuts off these growth signals. It also blocks a related protein called ROS1, along with several other kinases. Lorlatinib is designed to penetrate into the brain, giving it activity against tumors that have spread there.

Importantly, lorlatinib can block multiple mutated forms of the ALK enzyme, including some that develop when tumors become resistant to earlier ALK-blocking medicines. This makes it a useful option even after other treatments have stopped working.

💊How it's taken

Lorbrena is taken as a film-coated tablet by mouth, once daily, with or without food. It should be swallowed whole — never chewed, crushed, or split — and taken at the same time each day. Treatment continues until the disease progresses or side effects become unacceptable.

  • If a dose is missed, take it as soon as you remember — unless the next dose is due within 4 hours.
  • Never take two doses at once to make up for a missed one.
  • If you vomit after a dose, do not take another — just take the next scheduled dose.
  • Your prescriber may reduce your dose if you experience certain side effects or if you have severe liver or significant kidney impairment.
🤒Side effects — in detail

The most common side effects — reported in at least 20% of patients taking Lorbrena — include:

  • Edema (swelling, especially in the legs, feet, face, or around the eyes)
  • Peripheral neuropathy (numbness, tingling, pain, or weakness in the hands or feet)
  • Weight gain
  • Cognitive effects (memory problems, trouble concentrating, confusion)
  • Fatigue
  • Shortness of breath (dyspnea)
  • Joint pain (arthralgia)
  • Diarrhea
  • Mood changes (depression, anxiety, irritability)
  • Cough
  • High cholesterol and high triglycerides (common lab findings)

Serious reactions — including lung inflammation, severe CNS effects, dangerous heart rhythm changes, very high blood pressure, or high blood sugar — require prompt medical attention. Tell your care team about any new or worsening symptoms right away.

⚠️Warnings & precautions
  • Serious liver damage with certain interacting medicines: Taking Lorbrena together with strong CYP3A inducers (like rifampin) caused severe liver enzyme elevations in nearly all study participants tested. This combination is contraindicated — it must be avoided entirely.
  • Central nervous system effects: More than half of patients in clinical trials experienced some type of CNS effect, including cognitive changes, mood disturbances (including suicidal thoughts), seizures, speech problems, psychotic symptoms, or sleep disturbances. Report any of these to your doctor promptly.
  • High cholesterol and triglycerides (hyperlipidemia): Very common — most patients needed cholesterol-lowering medication during treatment. Levels are monitored before starting and regularly during treatment.
  • Heart rhythm changes (AV block): Lorbrena can slow the electrical conduction in the heart. Regular ECG monitoring is recommended.
  • Lung inflammation (ILD/pneumonitis): Although uncommon, this can be severe or life-threatening. Lorbrena must be permanently stopped if this occurs.
  • High blood pressure (hypertension): Blood pressure should be controlled before starting and monitored throughout treatment.
  • High blood sugar (hyperglycemia): Fasting blood sugar is checked before and during treatment.
  • Embryo-fetal toxicity: Lorbrena can cause serious harm to an unborn baby. Effective non-hormonal contraception is required for both men and women during treatment.
🔀What it interacts with

Lorbrena is broken down by liver enzymes, and several medicines can significantly alter its levels in your body — or have their own levels affected by Lorbrena:

  • Strong CYP3A inducers (e.g., rifampin): Completely contraindicated — caused severe liver damage in clinical studies.
  • Moderate CYP3A inducers: Should be avoided; if unavoidable, your Lorbrena dose may need to be increased.
  • Strong CYP3A inhibitors (e.g., certain antifungals, some HIV medicines): Can raise Lorbrena levels and increase side effects — avoid if possible, or reduce the Lorbrena dose.
  • Fluconazole (antifungal): Can raise Lorbrena levels — avoid or reduce dose if unavoidable.
  • Hormonal contraceptives (pill, patch, ring, implant): Lorbrena can make hormonal birth control ineffective — switch to a non-hormonal method.
  • Certain CYP3A substrates and P-gp substrates: Lorbrena can lower the blood levels of some other medicines, potentially making them less effective — always tell your prescriber what else you are taking.

This is not a complete list of interactions. Always talk with your doctor or pharmacist before starting, stopping, or changing any medication.

📋Before taking it
  • Pregnancy: Lorbrena can cause fetal malformations, pregnancy loss, and other serious harm — do not use if pregnant.
  • Contraception (women): Use effective non-hormonal birth control during treatment and for at least 6 months after the last dose; hormonal methods (pill, patch, ring) may not work while taking Lorbrena.
  • Contraception (men): Use effective contraception during treatment and for at least 3 months after the last dose if your partner could become pregnant.
  • Breastfeeding: Do not breastfeed during treatment or for 7 days after the final dose.
  • Severe liver impairment: A lower starting dose is recommended; tell your doctor about any liver disease.
  • Significant kidney impairment: A lower dose is recommended for patients with substantially reduced kidney function.
  • Children: Safety and effectiveness in patients under 18 have not been established.
  • Older adults (65+): Lorbrena was used safely in older patients in clinical trials, but regular monitoring remains important.
  • All other medicines and supplements: Tell your prescriber and pharmacist about everything you take — many common drugs can interact with Lorbrena.
📡Pharmacodynamics — effects in the body

At the doses used in treatment, higher lorlatinib exposure in the blood is linked to a greater chance of developing serious side effects, including very high cholesterol or triglycerides and other severe reactions. Lorbrena also affects the heart's electrical system — specifically, it can lengthen the PR interval (the time it takes for an electrical signal to travel through part of the heart), which can lead to slow or blocked heart conduction (AV block) in some patients.

🔬Pharmacokinetics — how your body processes it

After taking a Lorbrena tablet by mouth, the medicine is absorbed quickly, with peak blood levels reached in about 1 to 2 hours. Food does not meaningfully affect how much lorlatinib is absorbed, so it can be taken with or without a meal. It has a half-life of about 24 hours — meaning it takes roughly a day for the body to clear half of the dose — which supports once-daily dosing. Lorlatinib is mainly broken down in the liver by enzymes called CYP3A4 and UGT1A4, and roughly half is eliminated in the urine and about 41% in the stool.

📦How to store it

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) .

📄 Written from Lorlatinib’s FDA-approved label information, summarized in plain language with AI, and reviewed by our pharmacy team before publication. Every point is grounded in that labeling — nothing is invented. How we use AI →

153

Supplements & herbs that interact with Lorlatinib

153 supplements and herbal products have documented interactions with Lorlatinib in the licensed clinical database we use. Most are manageable — but your pharmacist should know about everything you take, including vitamins and herbals.

Severity mix
  • Major · 3
  • Moderate · 110
  • Minor · 40
Every supplement checked against Lorlatinib — ranked by severity The full interaction hub: 3 major · 110 moderate · 40 minor · every one linked to its full report. Check Lorlatinib against your exact supplements

Educational information from a licensed clinical database (Natural Medicines) — see our data sources & update cadence. Not medical advice: an interaction being documented does not mean it will happen to you; do not start or stop medications or supplements without professional guidance.

🩺 Pharmacist Counseling Corner

Quick, plain-English answers to the questions patients ask most about Lorlatinib — the kind of thing our pharmacy team would talk through with you at the counter.

What exactly is Lorbrena (lorlatinib) and why was I prescribed it?
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, telling cancer cells to keep multiplying. Lorbrena blocks that signal. Your doctor confirmed this gene change with a specific test before prescribing it, so it is matched to what's actually driving your cancer.
Can I take Lorbrena with food, and does it matter what time of day I take 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 daily routine and stick to it every day. Swallow the tablet whole; do not chew, crush, or split it, and don't take a tablet that looks broken or cracked.
What side effects should I expect, and which ones mean I should call my doctor right away?
The most common things people notice are swelling (especially in the legs or face), tingling or numbness in the hands and feet, weight gain, fatigue, and changes in memory or concentration. High cholesterol is also very common, which is why most patients are started on a cholesterol-lowering medicine early in treatment. On the more serious side — call your doctor right away if you notice new or worsening shortness of breath or fever (possible lung inflammation), feel your heart beating very slowly or you faint, experience a seizure, or have thoughts of harming yourself. These need prompt attention.
Are there any medicines I absolutely cannot take while on Lorbrena?
Yes — some medicines can cause a dangerous reaction when combined with Lorbrena. The most critical ones are a group called strong CYP3A inducers, like the antibiotic rifampin. Combining them caused severe liver damage in nearly everyone tested. Lorbrena also interacts with other drugs that affect the same liver enzymes, and it can make hormonal birth control pills, patches, and rings stop working properly. Before starting Lorbrena, give your care team a complete list of every medicine, supplement, and herbal product you take.
Is it safe to get pregnant or father a child while taking Lorbrena?
No — Lorbrena can seriously harm an unborn baby, including causing birth defects and pregnancy loss. If you are a woman who could become pregnant, you need to use effective non-hormonal birth control (since Lorbrena can make hormonal methods ineffective) during treatment and for at least 6 months after your last dose. If you are a man with a partner who could become pregnant, use effective contraception during treatment and for at least 3 months after stopping. Also, do not breastfeed while taking Lorbrena or for 7 days after your last dose.
What happens if I miss a dose or accidentally vomit after taking it?
If you miss a dose, take it as soon as you remember — but if your next scheduled dose is less than 4 hours away, just skip the missed one and carry on as normal. Never take two doses to make up for a missed one. And if you vomit after swallowing Lorbrena, don't take another tablet — your body has already absorbed most of what it needs. Just take your next dose at the regular time.
Is Lorlatinib available over the counter?
Lorlatinib is dispensed by prescription according to its FDA labeling, so it isn't sold over the counter. Your prescriber and pharmacist will determine if it's appropriate for you.
When was Lorlatinib first available?
Lorlatinib has been available in the United States since at least 2018, based on FDA approval history (Drugs@FDA) and product marketing records.
Who makes Lorlatinib?
Lorlatinib is supplied by 3 manufacturers listed in the FDA NDC Directory, including Pfizer Laboratories Div Pfizer Inc, Pfizer Manufacturing Deutschland GmbH (Betriebssttte Freiburg), U.S. Pharmaceuticals.

💬 Answers drafted from Lorlatinib’s FDA-approved label information, summarized in plain language with AI, and reviewed by our pharmacy team before publication. Grounded in that labeling — nothing is made up. How we use AI →

🧰 Keep exploring

💊 How Lorlatinib comes

Lorlatinib is available in 1 form. Different forms and brands can have different approved uses, doses, schedules, and directions. Follow the instructions for your exact product, and do not switch forms without guidance from your prescriber or pharmacist.

Tablet

By mouth
Brands Lorbrena
How this form is used
What it may be used for
  • Lorbrena is used to treat adults with ALK-positive metastatic non-small cell lung cancer (NSCLC) confirmed by an FDA-approved test
  • Lorbrena has been studied in both previously untreated patients and those whose cancer progressed on other ALK inhibitors
Important instructions
  • Lorbrena tablets are taken once daily by mouth, with or without food, at the same time each day
  • Swallow Lorbrena tablets whole — do not chew, crush, split, or take a tablet that is broken or cracked
  • If you miss a Lorbrena dose, take it as soon as you remember unless the next dose is within 4 hours; never double up
  • If you vomit after taking Lorbrena, do not take an extra dose — continue with your next scheduled dose
Available strengths 2 strengths
12 FDA-listed product records

📊 Lorlatinib across the U.S. market

How Lorlatinib appears in the FDA’s National Drug Code Directory — including its dosage forms, strengths, brand names, manufacturers, and FDA-listed product records. These are directory records, not sales or prescription volume.

1
Dose forms
3
Manufacturers
1
Brand names
12
FDA-listed product records
2018
First marketed
Pfizer Laboratories Div Pfizer Inc67%
Pfizer Manufacturing Deutschland GmbH (Betriebssttte Freiburg)17%
U.S. Pharmaceuticals17%

Share of FDA-listed product records by manufacturer — FDA National Drug Code Directory. Record counts are not sales or prescription volume.

📈 How widely Lorlatinib is used

A general measure of how commonly Lorlatinib is prescribed, based on Medicaid — one of the largest public drug programs. The figure below is prescriptions filled in Q1–Q4 2025, summed across every form and brand of the drug.

Think of this as a proxy for how widely Lorlatinib is used, drawn from freely available public data. Medicaid is just one program — these numbers don’t include Medicare, other government coverage, or commercial and cash-pay prescriptions, so real-world use is higher than what’s shown here.

846
Medicaid prescriptions filled (Q1–Q4 2025)
$17.1M gross Medicaid reimbursement (before mandatory rebates — net cost is lower)

How commonly is Lorlatinib prescribed? Of the 1,594 medications we measure, Lorlatinib ranks #1,309 by Medicaid prescriptions — more than 18% of them.

Where Lorlatinib ranks among the drugs we measure · Q1–Q4 2025 · neighbors ±5

Utilization by Lorlatinib product

Pick a product to see its own Medicaid numbers. Each chip is one clinical product — a specific strength & dosage form as defined by RxNorm — with brand-name and generic versions combined.

The 100 mg oral tablet is the most-dispensed Lorlatinib product — about 61% of these Medicaid prescriptions.

lorlatinib 100 MG Oral Tablet Most dispensed

517 Medicaid prescriptions (Q1–Q4 2025) 61% of Lorlatinib prescriptions shown $10.6M gross reimbursement (before rebates) ≈ $20,521 per prescription (gross)

Summed across the 1 of 2 listed NDC products with Medicaid activity — every brand and generic of this exact strength & form. RxNorm 2103177

lorlatinib 25 MG Oral Tablet

329 Medicaid prescriptions (Q1–Q4 2025) 39% of Lorlatinib prescriptions shown $6.5M gross reimbursement (before rebates) ≈ $19,694 per prescription (gross)

Summed across the 1 of 4 listed NDC products with Medicaid activity — every brand and generic of this exact strength & form. RxNorm 2103169

Shares are of the Medicaid prescriptions shown here. Product grouping follows RxNorm (the National Library of Medicine’s drug terminology), so “one product” means one strength & dosage form regardless of manufacturer. Dollar figures are gross Medicaid reimbursement before mandatory rebates — rebates (often large, especially for brand-name drugs) are confidential, so actual net cost to Medicaid is lower than shown.

Source: Medicaid State Drug Utilization Data (CMS), aggregated by generic ingredient — summed across every NDC (all brands, strengths, salt forms and dosage forms) of Lorlatinib, and across all states and both fee-for-service and managed-care claims. A general popularity signal; it excludes Medicare, commercial insurance and cash prescriptions, so it is not total U.S. use. Based on the 2 of 6 listed Lorlatinib NDCs with Medicaid activity.

🔍 Compare Lorlatinib products

A representative set of FDA-listed product records for Lorlatinib — across manufacturers, strengths, and dosage forms, grouped by form with each product’s manufacturer and how the FDA approved it. The same medicine may be made and packaged by different companies, so a single drug can have many directory entries. (It’s also why a refill can look different — a new shape, color, or box — even though it contains the same medication.)

Strength Route Manufacturer / Labeler Category Details
💊Tablet
25 mg Oral Pfizer Laboratories Div Pfizer Inc × 4 listings NDA View NDC →
100 mg Oral Pfizer Laboratories Div Pfizer Inc × 4 listings NDA View NDC →
25 mg Pfizer Manufacturing Deutschland GmbH (Betriebssttte Freiburg) DRUG FOR FURTHER PROCESSING View NDC →
100 mg Pfizer Manufacturing Deutschland GmbH (Betriebssttte Freiburg) DRUG FOR FURTHER PROCESSING View NDC →
25 mg Oral U.S. Pharmaceuticals × 2 listings NDA View NDC →

Showing 12 of 12 products — FDA National Drug Code Directory. See every product, package size and price: browse all 12 Lorlatinib NDCs →

RxNorm Concept Web — From Ingredient to Every Form and Strength

This page starts with one ingredient concept (IN). The branches below show its dose-form concepts (SCDF), then the available clinical drug and strength concepts (SCD). Combination products remain separate concepts with their own pages.

Ingredient (IN) Lorlatinib RxCUI 2103164 1 dose form · 2 strengths
  1. Dose form (SCDF) Oral Tablet RxCUI 2103168 In current FDA listings
    Clinical drug / strength (SCD) 25 MG RxCUI 2103169 100 MG RxCUI 2103177

Look up RxCUI 2103164 in the RxCUI Atlas →

RxNorm is the U.S. National Library of Medicine’s normalized drug vocabulary. Its concept hierarchy can include forms that are not currently marketed; the status on each branch compares that concept with current FDA listings. RxCUIs identify vocabulary concepts, not individual packages or manufacturers.

🏷️ Sold under these brand names

Lorbrena

🏭 Manufacturers & labelers

Pfizer Laboratories Div Pfizer Inc 8 Pfizer Manufacturing Deutschland GmbH (Betriebssttte Freiburg) 2 U.S. Pharmaceuticals 2

RxNorm drug class

Lorlatinib 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

Classified by RxNorm RxClass — the U.S. National Library of Medicine's standardized drug-classification service (Established Pharmacologic Class from the FDA, the ATC drug family from the WHO, and mechanism of action). Reference only, not medical advice.

🔬 Where this comes from

Core label, product, RxNorm, safety, and utilization data on this page come from the sources identified below. AI-written, editorial, and licensed sections are labeled separately.

📄
FDA-filed drug labels (SPL) Uses, dosing, warnings & side effects from SPL records retrieved through openFDA; the linked representative set can be verified on DailyMed. ✓ Linked label effective Jun 26, 2026
🏭
Forms, brands & labelersAggregated from ingredient-matched FDA National Drug Code Directory product records for Lorlatinib.
📈
Real-world reportsThe FDA Adverse Event Reporting System (FAERS), served through openFDA.
🚨
Recalls & shortagesopenFDA drug-enforcement reports and the FDA drug-shortage database.
🧾 Clinical label set — FDA-filed SPL labels retained for Lorlatinib after exact ingredient or ingredient-combination matching and applicable route/form matching
Clinical labels in scope
2
NDC products indexed
12
Distinct labelers/manufacturers represented
3
Linked representative label
Pfizer Laboratories Div Pfizer Inc
Linked label effective
Jun 26, 2026
Composite sections available
21
Linked SPL Set ID
2b34d62d-e02a-4af3-bc0d-1571dd4ee76d
Linked SPL Document ID
46cb56ce-da15-49af-b72b-f9e377cae4a6
Open the linked representative label on DailyMed ↗

How we combine label and product data

HelloPharmacist combines public FDA and NLM records; we don’t author the underlying clinical facts. We identified 2 FDA-filed SPL label sets within the page’s selected clinical scope after exact ingredient or ingredient-combination matching and applicable route/form matching. The representative label is the starting point for the displayed reference monograph; the 12 largest stored in-scope SPL records, which may include that representative, are compared section by section, and the longest available version of each section is retained. Forms, routes, brands, labelers, product-listed strengths, and product-record counts are aggregated separately from ingredient-matched FDA NDC Directory records; package records listed above are associated with the linked SPL; and the normalized concept hierarchy comes from NLM RxNorm.

For canonical ingredient pages, bounded product-attributed indication and administration excerpts may be added to the AI evidence, and the generator is instructed to preserve available product, brand, route, and form qualifiers instead of treating one label as universal. Where a section is identified as AI-written, its plain-language text is generated from bounded label evidence. New draft drug pages remain in the admin review queue before first publication. Pfizer Laboratories Div Pfizer Inc is the representative DailyMed label linked for verification and dates; it is not the sole source used for the page.

This is general education, not medical advice — always consult your doctor or pharmacist about your medications and any medical condition. For the exact wording of the linked representative label, view that label on DailyMed; some displayed composite sections may come from other in-scope SPL labels. Learn how we use AI and our data sources & update cadence.