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Ensacove ensartinib 100 mg Capsule, 60-count — NDC 83076-1100-06 package photo
Label image from the product's FDA listing (DailyMed) — may show a different pack size or an older label revision.

Ensacove ensartinib 100 mg Capsule, 60-count — NDC 83076-1100-6 (Billing 83076-1100-06)

by Xcovery Holdings, Inc. · 60 CAPSULE in 1 BOTTLE

This is a package of 60 capsules of Ensacove ensartinib 100 mg Capsule from Xcovery Holdings, Inc., marketed since Apr 2025 and currently FDA-listed. It is this product's only package size.

NDC 83076-1100-06
🏷️ FDA NDC (as labeled) 83076-1100-6 billing pads the package segment with a zero
Rx only Brand On market Non-controlled ⇄ Compare with another NDC
🗂️ FDA directory synced Oct 1, 2026 · this listing last changed Jul 24, 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 83076-1100-6 alone.

Record
FDA NDC Directory package listing · Human prescription drug
Code segments
83076 labeler · 1100 product · 6 package
Package marketed since
Apr 30, 2025
Sample package
No — commercial package
Listing certified through
Dec 31, 2027
Billing quantity
60 EA per package
Barcode (UPC)
0383076102534
FDA record last changed
Jul 24, 2026

Identity & classification

Regulatory identifiers FDA, NLM and CMS codes for this package

FDA NDC (as labeled) 83076-1100-6
Product NDC 83076-1100
11-digit billing NDC 83076110006
NCPDP billing unit EA — each (per item)
RxCUI 2712634, 2712640, 2712642, 2712644
UNII C2FR6VT1BQ
UPC 0383076102534
Application # NDA218171
SPL Set ID 1e1b2f79-678a-472a-b924-66909c8a4b2e
DEA schedule Non-controlled
Marketing category NDA
Marketing status On market
FDA listing status Listed (active directory)
Marketing start 2025-04-30
Route ORAL
Dosage form CAPSULE
Substance ENSARTINIB HYDROCHLORIDE

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

GPI-14 21533015200140
GCN Seq No 086956
GCN 56761
HICL code 050112
Ingredient (HICL) Ensartinib Hydrochloride
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 ENSACOVE 100 MG CAPSULE
FDB brand name Ensacove
Legend status F — Federal legend — prescription drug or device
Quick answers
  • GSN (GCN sequence number): 086956
  • GCN: 56761
  • GPI-14 (Medi-Span): 21533015200140
  • HICL (First Databank): 050112
  • AHFS class code: 10:00.00.00
  • RxCUI (RxNorm): 2712634
Why two NDCs? The FDA registers this code as 83076-1100-6 — a 5-4-1 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 package segment → 83076-1100-06. 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.

Clinical

Label name ENSACOVE 100 MG CAPSULE Ingredient Ensartinib Hydrochloride
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 No recent Medicaid claims on file for this NDC — rare and low-volume NDCs are suppressed in the public data.
Medicare drug plans payPart D · Q2 2026 $314.90 $18,894.26 / 60 capsules
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
83076-1100-06 You're viewing this Main listing 60 CAPSULE in 1 BOTTLE 2025-04-30 — Active

Therapeutic equivalents

ProductLabelerPackNADAC/unitTEStatusPrice vs. this
Ensacove 100 mgthis 83076-1100-06 Xcovery 60 capsules — — 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

🏛️
2024
First FDA approval
Dec 2024
📍
2026
Currently FDA-listed
2 years listed
🛡️
2037
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 Jun 2037. This may affect when a full generic version becomes widely available, but it is not a guaranteed launch date.
📅 FDA approved Dec 18, 2024 RLD RS ⏳ ~10.7 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 10899744 — drug substance (U-4099)
US 10899744 — drug substance (U-4099)
US 9296724 — drug substance (U-4099)
US 9296724 — drug substance (U-4099)
US 9126947 — drug substance
US 8551995 — drug substance
US 8551995 — drug substance
US 9126947 — drug substance
Exclusivity NCE
Exclusivity NCE
2024 2026 2028 2030 2032 2034 2036
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 (8)
PatentTypeUse codeExpires
US 10899744 ↗ Drug substance U-4099 Jun 1, 2037
US 10899744 ↗ Drug substance U-4099 Jun 1, 2037
US 9296724 ↗ Drug substance U-4099 Jun 18, 2029
US 9296724 ↗ Drug substance U-4099 Jun 18, 2029
US 9126947 ↗ Drug substance — Nov 29, 2031
US 8551995 ↗ Drug substance — Feb 9, 2029
US 8551995 ↗ Drug substance — Feb 9, 2029
US 9126947 ↗ Drug substance — Nov 29, 2031
FDA exclusivity
CodeWhat it grantsExpires
NCENew Chemical Entity (5-year)Dec 18, 2029
NCENew Chemical Entity (5-year)Dec 18, 2029
Common questions
Is there a generic version of ENSACOVE 100 MG CAPSULE?
No FDA-approved generic equivalent is currently listed in the FDA Orange Book for ENSACOVE 100 MG CAPSULE. Based on the patents and exclusivity currently listed, the Orange Book estimate is that full-label generic entry may be delayed until Jun 2037 — 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 white / blue / yellow
ShapeOval
ImprintX396;100;mg
Size22 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 8PJ61P6TS3
    Butyl alcohol is a clear liquid organic solvent derived from petroleum or natural sources. In medicines, it helps dissolve active ingredients and serves as a solvent in liquid formulations and some topical products.
  • UNII 3K9958V90M
    A liquid solvent derived from fermentation or chemical synthesis. In medicines, alcohol dissolves active ingredients, helps preserve the product, and improves how the body absorbs certain drugs.
  • UNII H3R47K3TBD
    FD&C Blue No. 1 is a synthetic blue dye approved for use in foods and medicines. It serves as a colorant to give the medication its distinctive appearance and help with product identification.
  • UNII I753WB2F1M
    FD&C Yellow No. 5 is a synthetic yellow colorant approved by the FDA. It is added to medicines to make pills, tablets, or liquids visually distinct and easier to identify.
  • 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 ND2M416302
    Isopropyl alcohol is a clear liquid solvent derived from petroleum. In medicines, it dissolves active ingredients and other components, helps the product flow smoothly, and aids in sterilization during manufacturing.
  • 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 FZ989GH94E
    Povidone is a synthetic polymer made from a plastic-like material. It acts as a binder to hold tablet ingredients together and as a disintegrant to help the tablet break apart in your stomach so the medicine can be absorbed.
  • UNII 6DC9Q167V3
    Propylene glycol is a clear liquid derived from petroleum or vegetable sources. It acts as a solvent, humectant, and preservative in medicines, helping dissolve active ingredients and maintain product stability.
  • UNII 46N107B71O
    Shellac is a natural resin secreted by the lac beetle. It's used as a coating on tablets and capsules to control how quickly the medicine dissolves and to improve appearance and stability.
  • UNII 55X04QC32I
    A strong alkaline chemical used to adjust and maintain the pH balance of liquid medicines. It helps keep the medicine stable and ensures it stays effective during storage.
  • UNII 4ELV7Z65AP
    Stearic acid is a fatty acid derived from plant or animal sources. It acts as a binder and lubricant in tablets and capsules, helping them hold together and flow smoothly during manufacturing.
  • 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.

15 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

LabelerXcovery Holdings, Inc.
Application holderXCOVERY HOLDINGS INC
FDA applicationNDA218171 (NDA)
Labeler code83076
First marketedApr 2025
Product typeHuman Prescription Drug
Portfolio2 products on file

More NDCs from Xcovery Holdings, Inc. labeler code 83076

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 📋 Description 💬 Information for Patients 🍼 Nursing Mothers 🧬 Pharmacokinetics 🧬 Pharmacodynamics 🔬 Clinical Studies 🧪 Nonclinical Toxicology 📄 Carcinogenesis, Mutagenesis, Impairment of Fertility 📄 Patient Package Insert 📄 Package Label / Principal Display Panel
🎯 Indications and Usage 90 words ▾

1 INDICATIONS AND USAGE ENSACOVE is indicated for the treatment of adult patients with anaplastic lymphoma kinase (ALK)-positive locally advanced or metastatic non-small cell lung cancer (NSCLC)as detected by an FDA-approved test [see Dosage and Administration ( 2.1 )] who have not previously received an ALK-inhibitor. ENSACOVE is a kinase inhibitor indicated for the treatment of adult patients with anaplastic lymphoma kinase (ALK)-positive locally advanced or metastatic non-small cell lung cancer (NSCLC) as detected by an FDA-approved test who have not previously received an ALK-inhibitor.

( 1 , 2.1 )

⏱️ Dosage and Administration ~3 min read ▾

2 DOSAGE AND ADMINISTRATION Select patients with ALK-positive locally advanced or metastatic NSCLC for treatment with ENSACOVE. ( 2.1 ) Prior to initiating ENSACOVE, evaluate liver function tests and fasting blood glucose. ( 2.2 ) Recommended dosage: 225 mg orally once daily with or without food until disease progression or unacceptable toxicity. ( 2.3 )

2.1Patient Selection Select patients for the treatment of locally advanced or metastatic NSCLC with ENSACOVE based on the presence of ALK rearrangement(s) in tumor specimens [see Clinical Studies ( 14.1 )] . Information on FDA-approved tests for the detection of ALK rearrangements in NSCLC is available at http://www.fda.gov/CompanionDiagnostics .

2.2Recommended Testing and Advice Prior to Initiating ENSACOVE Prior to initiating ENSACOVE, evaluate liver function tests [see Warnings and Precautions ( 5.2 )] and fasting blood glucose [see Warnings and Precautions ( 5.5 )].

2.3Recommended Dosage The recommended dosage of ENSACOVE is 225 mg orally once daily, with or without food [see Clinical Pharmacology ( 12.3 )] , until disease progression or unacceptable toxicity. Swallow capsules whole, do not crush or chew. Do not open or dissolve the contents of the capsule.

Take ENSACOVE at the same time each day. Missed dose If a dose is missed, then take the missed dose as soon as possible unless the next dose is due within 12 hours. Do not take 2 doses on the same day.

Vomiting If vomiting occurs after taking a dose, do not take an additional dose and take the next dose at its scheduled time.

2.4Dosage Modification for Adverse Reactions The recommended dose reductions for adverse reactions are provided in Table 1. Table 1: Recommended Dose Reductions for Adverse Reactions Dose Reduction Recommended Dose and Schedule First 200 mg orally once daily Second 150 mg orally once daily Permanently discontinue ENSACOVE if patients are unable to tolerate 150 mg orally once daily. Once the dose has been reduced for adverse reactions, do not subsequently increase the dose of ENSACOVE.

The recommended dosage modifications for the management of adverse reactions are provided in Table 2. Table 2: Recommended ENSACOVE Dosage Modifications for Adverse Reactions Adverse Reaction Severity* ENSACOVE Dose Modification and Management for Adverse Reactions Interstitial Lung Disease (ILD)/Pneumonitis [see Warnings and Precautions ( 5.1 )] Any Grade Permanently discontinue ENSACOVE. Hepatotoxicity [see Warnings and Precautions ( 5.2 )] Grade 3 or 4 elevation (greater than 5 times ULN) of either ALT or AST with concurrent total bilirubin less than or equal to 2 times ULN Withhold ENSACOVE until recovery to Grade ≤1 (≤3 times ULN) or to baseline.

Resume ENSACOVE at reduced dose as per Table 1. Grade 2 to 4 elevation (greater than 3 times ULN) of either ALT or AST with concurrent total bilirubin elevation greater than 2 times ULN in the absence of cholestasis or hemolysis Permanently discontinue ENSACOVE. Dermatologic Adverse Reactions [see Warnings and Precautions ( 5.3 )] Grade 1 Consider topical corticosteroids.

Grade 2 Administer topical corticosteroids. If not improved in ≤7 days after initiation of topical corticosteroids, administer oral corticosteroids. If not improved in ≤7 days after initiation of oral corticosteroids, withhold ENSACOVE until recovery to Grade ≤1.

Resume ENSACOVE at reduced dose as per Table 1. Grade 3 Withhold ENSACOVE. Administer topical corticosteroids.

If not improved after 7 days of initiation of topical corticosteroids, administer oral corticosteroids. Resume ENSACOVE at reduced dose as per Table 1 upon improvement to Grade ≤1. Grade 4 Permanently discontinue ENSACOVE.

Administer systemic corticosteroids and consider antibiotic use. Bradycardia (HR less than 60 bpm) [see Warnings and Precautions ( 5.4 )] Symptomatic bradycardia Withhold ENSACOVE until recovery to asymptomatic bradycardia or to a resting heart rate of 60 bpm or above. If a concomitant medication known to cause b… [Excerpted — this section continues on DailyMed.]

💊 Dosage Forms and Strengths 93 words ▾

3 DOSAGE FORMS AND STRENGTHS ENSACOVE capsules are available as: 25 mg: size 2 capsule, white opaque cap and body, with “X-396” on the cap and “25 mg” on the body printed in blue ink. Each capsule contains the equivalent of 25 mg of ensartinib. 100 mg: size 0 capsule, blue opaque cap and yellow opaque body, with “X-396” on the cap and “100 mg” on the body printed in white ink.

Each capsule contains the equivalent of 100 mg of ensartinib. Capsules: 25 mg and 100 mg of ensartinib ( 3 )

⛔ Contraindications 53 words ▾

4 CONTRAINDICATIONS ENSACOVE is contraindicated in patients who have experienced a severe hypersensitivity reaction to ENSACOVE, FD&C Yellow No. 5 (tartrazine), or to any of its components [see Warnings and Precautions ( 5.10 )] . Hypersensitivity reaction to ENSACOVE, FD&C Yellow No. 5 (tartrazine), or to any of its components. ( 4 )

⚠️ Warnings and Cautions ~3 min read ▾

5 WARNINGS AND PRECAUTIONS Interstitial Lung Disease (ILD)/Pneumonitis : Monitor patients for new or worsening symptoms indicative of ILD/pneumonitis. Permanently discontinue in patients with ILD/pneumonitis. ( 5.1 ) Hepatotoxicity : Monitor liver function tests during treatment with ENSACOVE.

Withhold, reduce the dose, or permanently discontinue ENSACOVE based on severity. (5.2 ) Dermatologic Adverse Reaction : Monitor for dermatologic adverse reactions during treatment with ENSACOVE. Withhold, reduce the dose, or permanently discontinue ENSACOVE based on severity.

( 5.3 ) Bradycardia : Monitor heart rate regularly during treatment with ENSACOVE. Withhold, reduce the dose, or permanently discontinue ENSACOVE based on severity. ( 5.4 ) Hyperglycemia : Monitor serum glucose periodically during treatment with ENSACOVE.

Withhold, reduce the dose, or permanently discontinue ENSACOVE based on severity. ( 5.5 ) Visual Disturbances : Advise patients to report visual symptoms during treatment with ENSACOVE. Withhold ENSACOVE and obtain ophthalmologic evaluation, then reduce the dose or permanently discontinue ENSACOVE.

(5.6) Increased Creatine Phosphokinase (CPK) : Monitor CPK periodically during treatment with ENSACOVE. Withhold, reduce the dose, or permanently discontinue ENSACOVE based on severity. ( 5.7 ) Hyperuricemia : Monitor uric acid periodically during treatment with ENSACOVE.

Withhold, reduce the dose, or permanently discontinue ENSACOVE based on severity. ( 5.8 ) Embryo-Fetal Toxicity : Can cause fetal harm. Advise patients of the potential risk to a fetus and to use effective contraception.

( 5.9 )

5.1Interstitial Lung Disease/Pneumonitis ENSACOVE can cause severe interstitial lung disease (ILD)/pneumonitis. In the pooled safety population [see Adverse Reactions ( 6.1 )], ILD/pneumonitis occurred in 5% of patients treated with ENSACOVE, including Grade 3 in 1.3% and Grade 4 in 0.4%. ILD/pneumonitis leading to dose interruption occurred in 0.4% and permanent discontinuation of ENSACOVE in 1.5% of patients.

Monitor patients for new or worsening symptoms indicative of ILD/pneumonitis (e.g., dyspnea, cough, and fever) during treatment with ENSACOVE. Immediately withhold ENSACOVE in patients with suspected ILD/pneumonitis. Permanently discontinue ENSACOVE if ILD/pneumonitis is confirmed [see Dosage and Administration ( 2.4 )].

5.2Hepatotoxicity ENSACOVE can cause hepatotoxicity including drug-induced liver injury. In the pooled safety population [see Adverse Reactions ( 6.1 )], 59% of patients treated with ENSACOVE had increased alanine aminotransferase (ALT), including 5% Grade 3. Increased aspartate aminotransferase (AST) occurred in 58% of patients treated with ENSACOVE, including 1.8% Grade 3.

Increased bilirubin occurred in 12% of patients treated with ENSACOVE, including 2.3% Grade 3 and 0.2% Grade 4. There was one case of drug-induced liver injury in ENSACOVE-treated patients. The median time to first onset of increased ALT or AST was 5.3 weeks (range: 0.4 to 152 weeks).

The dose of ENSACOVE was interrupted in 4.6% of patients for increased ALT or AST. Increased ALT or AST leading to dose reduction occurred in 2.6% and permanent discontinuation of ENSACOVE in 1.1% of patients. The dose of ENSACOVE was interrupted in 1.3% of patients for increased bilirubin.

Increased bilirubin leading to dose reduction occurred in 0.7% and permanent discontinuation of ENSACOVE in 1.3% of patients. Monitor liver function tests including ALT, AST, and total bilirubin at baseline and every 2 weeks during the first cycle of treatment with ENSACOVE, and then monthly and as clinically indicated. Withhold, reduce the dose, or permanently discontinue ENSACOVE based on the severity of the adverse reaction [see Dosage and Administration ( 2.4 )] .

5.3Dermatologic Adverse Reactions ENSACOVE can cause dermatologic adverse reactions, including drug reaction with eosinophilia and systemic symptoms (DRESS), rash, pruritus, and photosensitivity. In… [Excerpted — this section continues on DailyMed.]

🤒 Adverse Reactions ~3 min read ▾

6 ADVERSE REACTIONS The following clinically significant adverse reactions are described elsewhere in the labeling: Interstitial Lung Disease/Pneumonitis [see Warnings and Precautions ( 5.1 )] Hepatoxicity [see Warnings and Precautions ( 5.2 )] Dermatologic Adverse Reactions [see Warnings and Precautions ( 5.3 )] Bradycardia [see Warnings and Precautions ( 5.4 )] Hyperglycemia [see Warnings and Precautions ( 5.5 )] Visual Disturbances [see Warnings and Precautions ( 5.6 )] Increased Creatine Phosphokinase [see Warnings and Precautions ( 5.7 )] Hyperuricemia [see Warnings and Precautions ( 5.8 )] FD&C Yellow No.

5 (Tartrazine) [see Warnings and Precautions ( 5.10 ) ] Most common adverse reactions (incidence ≥20%) were rash, musculoskeletal pain, constipation, pruritus, cough, nausea, edema, vomiting, fatigue, and pyrexia. ( 6.1 ) Most common Grade 3-4 laboratory abnormality (incidence ≥2%) were increased uric acid, decreased lymphocytes, increased alanine aminotransferase, decreased phosphate, increased gamma glutamyl transferase, increased magnesium, increased amylase, decreased sodium, increased glucose, decreased hemoglobin, increased bilirubin, decreased potassium, and increased creatine phosphokinase.

( 6.1 ) To report SUSPECTED ADVERSE REACTIONS, contact Xcovery Holdings, Inc. at (866) 367-2268 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 reflects exposure to ENSACOVE as a single agent in 458 patients with locally advanced or metastatic ALK-positive NSCLC in the following trials: eXALT3 Study (N=143) [see Clinical Studies ( 14.1 ) ], Study 101 (NCT01625234, N=98), Study BTP-28311 (NCT02959619, N=35), and Study BTP-42322 (NCT03215693, N=182).

Patients received ENSACOVE 225 mg orally once daily, with or without food, until disease progression or unacceptable toxicity. Among 458 patients who received ENSACOVE, 63% were exposed for 6 months or longer and 47% were exposed for greater than one year. In this pooled safety population, the most common adverse reactions (≥20%) were rash, musculoskeletal pain, constipation, pruritus, cough, nausea, edema, vomiting, fatigue, and pyrexia.

The most frequent Grade 3 or 4 laboratory abnormalities (≥2%) were increased uric acid, decreased lymphocytes, increased alanine aminotransferase, decreased phosphate, increased gamma glutamyl transferase, increased magnesium, increased amylase, decreased sodium, increased glucose, decreased hemoglobin, increased bilirubin, decreased potassium, and increased creatine phosphokinase. TKI-naive ALK-Positive Locally Advanced or Metastatic NSCLC The safety of ENSACOVE was evaluated in the eXALT3 study [see Clinical Studies ( 14.1 ) ].

Patients received ENSACOVE 225 mg orally once daily, with or without food, until disease progression or unacceptable toxicity . Among patients who received ENSACOVE, 78% were exposed for 6 months or longer and 66% were exposed for greater than one year. The median age of patients who received ENSACOVE was 54 years (range: 25-86); 50% male; 54% Asian, 43% White; 0.7% Black or African American; and 11% Hispanic or Latino.

Serious adverse reactions occurred in 23% of patients treated with ENSACOVE. Serious adverse reactions that occurred in ≥1% were pneumonia (4.9%), hemorrhage (2.1%), rash (2.1%) and cellulitis (1.4%). One fatal adverse reaction (0.7%) occurred due to bronchopneumonia.

Permanent discontinuation of ENSACOVE due to an adverse reaction occurred in 12% of patients. Adverse reactions which resulted in permanent discontinuation of ENSACOVE (≥1%) included increased blood bilirubin (1.4%), increased conjugated bilirubin (1.4%), increased ALT (2.1%), inc… [Excerpted — this section continues on DailyMed.]

🔄 Drug Interactions ~1 min read ▾

7 DRUG INTERACTIONS Moderate or Strong CYP3A Inhibitors : Avoid concomitant use with ENSACOVE. ( 7.1 ) Moderate or Strong CYP3A Inducers : Avoid concomitant use with ENSACOVE. ( 7.1 ) P-gp Inhibitor : Avoid concomitant use with ENSACOVE. ( 7.1 )

7.1Effect of Other Drugs on ENSACOVE Table 5 describes drug interactions where concomitant use of another drug affects ENSACOVE. Table 5: Effect of Other Drugs on ENSACOVE Strong or Moderate CYP3A Inhibitors Prevention or Management Avoid concomitant use of strong or moderate CYP3A inhibitors with ENSACOVE. Mechanism and Clinical Effect(s) This recommendation is based upon a mechanistic understanding of ensartinib pharmacokinetics and it being a CYP3A4 substrate in vitro [see Clinical Pharmacology ( 12.3 )] .

Concomitant use with strong or moderate CYP3A inhibitors may increase ensartinib exposure; however, this has not been studied clinically. Strong or Moderate CYP3A Inducers Prevention or Management Avoid concomitant use of strong or moderate CYP3A inducers with ENSACOVE. Mechanism and Clinical Effect(s) This recommendation is based upon a mechanistic understanding of ensartinib pharmacokinetics and it being a CYP3A4 substrate in vitro [see Clinical Pharmacology ( 12.3 )] .

Concomitant use with strong or moderate CYP3A inducers may decrease ensartinib exposure; however, this has not been studied clinically. P-gp Inhibitors Prevention or Management Avoid concomitant use of P-gp inhibitors with ENSACOVE. Mechanism and Clinical Effect(s) This recommendation is based upon a mechanistic understanding of ensartinib pharmacokinetics and it being a P-gp substrate in vitro [see Clinical Pharmacology ( 12.3 )] .

Concomitant use with P-gp inhibitors may increase ensartinib exposure; however, this has not been studied clinically.

👥 Use in Specific Populations ~3 min read ▾

8 USE IN SPECIFIC POPULATIONS Lactation : Advise not to breastfeed. ( 8.2 ) Severe Hepatic Impairment: Avoid use of ENSACOVE in patients with severe hepatic impairment. (8.6 )

8.1Pregnancy Risk Summary Based on findings from animal studies and its mechanism of action [see Clinical Pharmacology ( 12.1 )] , ENSACOVE can cause fetal harm when administered to a pregnant woman. There are no available data on the use of ENSACOVE in pregnant women to inform a drug-associated risk. Oral administration of ensartinib to pregnant rats during the period of organogenesis caused adverse developmental outcomes, including embryo-fetal mortality, alterations to growth, and structural abnormalities.

Adverse embryo-fetal findings were seen at maternal exposures approximately equivalent to the human exposure at the recommended dose of 225 mg/day based on AUC ( see Data ). Advise pregnant women 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 is 2% to 4% and 15% to 20%, respectively.

Data Animal Data In an embryo-fetal development study, pregnant rats received 20, 40, or 80 mg/kg/day of ensartinib during the period of organogenesis (gestation day 6 to 17). Ensartinib doses ≥40 mg/kg/day (approximately equivalent to the human exposure at the recommended dose of 225 mg/day based on AUC) resulted in an increase in the incidence of fetal malformations (aortic dislocation, ventricular septal defect, separated vertebrae) and dose-dependent delayed skeletal development, including decreased or delayed ossification of the vertebrae.

Ensartinib at 80 mg/kg (approximately 6.4 times the human exposure at the recommended dose of 225 mg/day based on AUC) resulted in maternal toxicity (reduced body weight and food consumption), decreased fetal body weight, increased pre- and post-implantation loss, decreases in the number of live fetuses, and visceral variations (missing renal papillae, pyelectasis).

8.2Lactation Risk Summary There are no data on the presence of ensartinib or its metabolites in human milk, the effects on the breastfed child, or the effects on milk production. Because of the potential for serious adverse reactions in breastfed children, advise women not to breastfeed during treatment with ENSACOVE and for 1 week after the last dose.

8.3Females and Males of Reproductive Potential ENSACOVE can cause fetal harm when administered to a pregnant woman [see Use in Specific Populations ( 8.1 ) ]. Pregnancy Testing Verify the pregnancy status of females of reproductive potential prior to initiating ENSACOVE. Contraception Females Advise females of reproductive potential to use effective contraception during treatment with ENSACOVE and for at 1 week after the last dose.

Males Advise male patients with female partners of reproductive potential to use effective contraception during treatment with ENSACOVE and for 1 week after the last dose.

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

8.5Geriatric Use Of the 458 patients enrolled in clinical studies and received ENSACOVE 225 mg once daily, 16% of the participants were aged 65 years or older. Clinical studies of ENSACOVE did not include sufficient numbers of patients ages 65 and over to determine whether they respond differently from younger patients. Exploratory analysis suggests a higher incidence of serious adverse events (43% vs 27%), more frequent adverse events leading to treatment discontinuations (18% vs 10%) and dose modifications (34% vs 16%) in patients 65 years or older as compared to those younger than 65 years.

8.6Hepatic Impairment Ensartinib is primarily metabolized by the liver and patients with hepatic impairment may have increased exposures [see Clinical Pharmacology ( 12.3 )]. Avoid use of ENSACOVE for patients with severe hepatic impairment (total bilirubin >3 times ULN and any AST) since it has not b… [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 )] , ENSACOVE can cause fetal harm when administered to a pregnant woman. There are no available data on the use of ENSACOVE in pregnant women to inform a drug-associated risk. Oral administration of ensartinib to pregnant rats during the period of organogenesis caused adverse developmental outcomes, including embryo-fetal mortality, alterations to growth, and structural abnormalities.

Adverse embryo-fetal findings were seen at maternal exposures approximately equivalent to the human exposure at the recommended dose of 225 mg/day based on AUC ( see Data ). Advise pregnant women 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 is 2% to 4% and 15% to 20%, respectively.

Data Animal Data In an embryo-fetal development study, pregnant rats received 20, 40, or 80 mg/kg/day of ensartinib during the period of organogenesis (gestation day 6 to 17). Ensartinib doses ≥40 mg/kg/day (approximately equivalent to the human exposure at the recommended dose of 225 mg/day based on AUC) resulted in an increase in the incidence of fetal malformations (aortic dislocation, ventricular septal defect, separated vertebrae) and dose-dependent delayed skeletal development, including decreased or delayed ossification of the vertebrae.

Ensartinib at 80 mg/kg (approximately 6.4 times the human exposure at the recommended dose of 225 mg/day based on AUC) resulted in maternal toxicity (reduced body weight and food consumption), decreased fetal body weight, increased pre- and post-implantation loss, decreases in the number of live fetuses, and visceral variations (missing renal papillae, pyelectasis).

🧒 Pediatric Use 16 words ▾

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

🧓 Geriatric Use 96 words ▾

8.5Geriatric Use Of the 458 patients enrolled in clinical studies and received ENSACOVE 225 mg once daily, 16% of the participants were aged 65 years or older. Clinical studies of ENSACOVE did not include sufficient numbers of patients ages 65 and over to determine whether they respond differently from younger patients. Exploratory analysis suggests a higher incidence of serious adverse events (43% vs 27%), more frequent adverse events leading to treatment discontinuations (18% vs 10%) and dose modifications (34% vs 16%) in patients 65 years or older as compared to those younger than 65 years.

🧬 Clinical Pharmacology ~2 min read ▾

12 CLINICAL PHARMACOLOGY

12.1Mechanism of Action Ensartinib is a kinase inhibitor of anaplastic lymphoma kinase (ALK) and inhibits other kinases including MET and ROS1. In vitro, ensartinib inhibited phosphorylation of ALK and its downstream signaling proteins AKT, ERK, and S6, thereby blocking ALK-mediated signaling pathways and inhibiting proliferation in cell lines harboring ALK fusions and mutations. In vivo, ensartinib showed anti-tumor activity in a mouse xenograft model of human NSCLC harboring an ALK fusion.

12.2Pharmacodynamics Exposure-response relationship Ensartinib exposure-response relationships and the time course of the pharmacodynamic response have not been fully characterized. Cardiac Electrophysiology At the approved recommended dosage, a mean increase in the QTc interval > 20 ms was not observed.

12.3Pharmacokinetics Ensartinib mean (coefficient of variation [CV%]) maximum concentration (Cmax) is 292 ng/mL (60%), and the area under the concentration-time curve (AUC0–24h) is 4,920 ng·h /ml (62%) at the approved recommended dosage. Ensartinib steady state is reached within 15 days with a mean accumulation ratio of 2.7. Absorption Ensartinib median (minimum, maximum) time to reach Cmax (Tmax) at steady state is 3 hours (2, 8 hours).

Effect of Food No clinically significant differences in ensartinib pharmacokinetics were observed following administration of ENSACOVE with a high-fat meal (total 800-1000 calories, > 50% fat) compared to fasted conditions. Distribution Ensartinib mean (CV%) apparent volume of distribution is 1,720 L (42%). Ensartinib is 91.6% bound to human plasma protein.

Elimination Ensartinib mean (standard deviation [SD]) steady-state half-life (t1/2) is 30 (20) hours. Metabolism Ensartinib is predominantly metabolized by CYP3A. Excretion Following a single oral 200 mg dose of radiolabeled ensartinib, 91% of the radioactivity was recovered in feces (38% as unchanged) and 10% in urine (4.4% as unchanged).

Specific Populations No clinically significant differences in the pharmacokinetics of ensartinib were observed based on age (20 to 86 years), sex, race (Asian vs White), body weight (38 to 148 kg), mild to moderate renal impairment (eGFR 30 to 89 mL/min) and mild hepatic impairment (total bilirubin ≤ upper limit of normal (ULN) and AST > ULN or total bilirubin 1 to 1.5 x ULN and any AST). The effect of severe renal impairment (eGFR 15 to 29 mL/min), end-stage renal disease (eGFR <15 mL/min) with or without hemodialysis, and moderate (total bilirubin >1.5 to ≤ 3 ULN and any AST) or severe (total bilirubin >3 times ULN and any AST) hepatic impairment on ensartinib pharmacokinetics is unknown.

Drug Interaction Studies In Vitro Studies Cytochrome P450 (CYP) Enzymes: Ensartinib does not inhibit CYP1A2, CYP2B6, CYP2C8, CYP2C9, CYP2C19, CYP2D6 and does not induce CYP1A2, CYP2B6, or CYP3A. Transporter Systems: Ensartinib is a P-gp substrate but is not a substrate of BCRP, OATP1B1, OATP1B3, OAT1, OAT3, OCT1 or OCT2. Ensartinib does not inhibit BCRP, P-gp, OATP1B1, OATP1B3, OAT1, OAT3, OCT1, OCT2 or OCT3.

🧬 Mechanism of Action 72 words ▾

12.1Mechanism of Action Ensartinib is a kinase inhibitor of anaplastic lymphoma kinase (ALK) and inhibits other kinases including MET and ROS1. In vitro, ensartinib inhibited phosphorylation of ALK and its downstream signaling proteins AKT, ERK, and S6, thereby blocking ALK-mediated signaling pathways and inhibiting proliferation in cell lines harboring ALK fusions and mutations. In vivo, ensartinib showed anti-tumor activity in a mouse xenograft model of human NSCLC harboring an ALK fusion.

📦 How Supplied / Storage and Handling 129 words ▾

16 HOW SUPPLIED ENSACOVE (ensartinib) capsules are supplied as follows: Capsule Strength Description Package Configuration NDC Code 25 mg Size 2 capsule, white opaque cap and body, with “X-396” on the cap and “25 mg” on the body printed in blue ink. Bottles of 30 83076-1025-3 100 mg Size 0 capsule, blue opaque cap and yellow opaque body, with “X- 396” on the cap and “100 mg” on the body printed in white ink. Bottles of 60 83076-1100-6 Store at controlled room temperature 20ºC to 25ºC (68ºF to 77ºF); excursions permitted to 15ºC to 30ºC (59ºF to 86ºF) [see USP Controlled Room Temperature] .

Store and dispense in the original bottle with desiccant to protect from moisture. Do not remove desiccant from bottle. Keep out of reach of children

📋 Description 183 words ▾

11 DESCRIPTION ENSACOVE capsules contain ensartinib, a kinase inhibitor, present as ensartinib hydrochloride with the chemical name 6-amino-5-[(1 R )-1-(2,6-dichloro-3-fluorophenyl)ethoxy]-N-{4-[(3 R ,5 S )- 3,5-dimethylpiperazine-1-carbonyl]phenyl}pyridazine-3-carboxamide, dihydrochloride. The molecular formula is C26H27Cl2FN6O3·2HCl and its molecular weight is 634.4 g/mol with the following structure: ENSACOVE capsules are intended for oral administration and are available in two dosage strengths: 25 mg ensartinib (equivalent to 28.25 mg ensartinib hydrochloride) and 100 mg ensartinib (equivalent to 113.02 mg ensartinib hydrochloride).

The inactive ingredients of ENSACOVE capsules are microcrystalline cellulose and stearic acid. The inactive ingredients of the 25 mg empty capsule shells are hypromellose and titanium dioxide. The inactive ingredients of the 100 mg empty capsules shells are black iron oxide, FD&C Blue No.

1, FD&C Yellow No. 5, hypromellose, red iron oxide, and titanium dioxide. The imprinting ink for the 25 mg capsules contains butyl alcohol, dehydrated alcohol, FD&C Blue No.

2, isopropyl alcohol, propylene glycol, shellac, and strong ammonia solution. The imprinting ink for the 100 mg capsules contains butyl alcohol, dehydrated alcohol, isopropyl alcohol, povidone, propylene glycol, shellac, sodium hydroxide, and titanium dioxide. Chemical Structure

💬 Information for Patients ~3 min read ▾

17 PATIENT COUNSELING INFORMATION Advise the patient to read the FDA-approved patient labeling (Patient Information). Interstitial Lung Disease (ILD)/Pneumonitis Inform patients of the risk of severe ILD/pneumonitis during treatment with ENSACOVE. Advise patients to contact their healthcare provider immediately to report new or worsening respiratory symptoms [see Warnings and Precautions ( 5.1 )].

Hepatoxicity Inform patients of the potential risk of hepatoxicity during treatment with ENSACOVE and of the need to monitor for aspartate aminotransferase (AST), alanine aminotransferase (ALT) and total bilirubin elevations during treatment with ENSACOVE. Advise patients to inform their healthcare provider of any new or worsening symptoms [see Warnings and Precautions ( 5.2 )]. Dermatologic Adverse Reactions Inform patients of the potential risk of dermatologic adverse reactions, including rash, pruritus, and photosensitivity during treatment with ENSACOVE.

If dermatologic reactions occur, advise patients to limit sun exposure while taking ENSACOVE and for at least 1 week after the final dose [see Warnings and Precautions ( 5.3 )]. Bradycardia Advise patients of the risk of bradycardia during treatment with ENSACOVE and to report any symptoms of bradycardia. Advise patients to inform their healthcare provider about the use of any heart or blood pressure medications during treatment with ENSACOVE [see Warnings and Precautions ( 5.4 )].

Hyperglycemia Inform patients of the risks of new or worsening hyperglycemia during treatment with ENSACOVE and the need to periodically monitor glucose levels. Advise patients with diabetes mellitus or glucose intolerance that antihyperglycemic medications may need to be adjusted during treatment with ENSACOVE [see Warnings and Precautions ( 5.5 )]. Visual Disturbances Advise patients to inform their healthcare provider of any new or worsening vision symptoms during treatment with ENSACOVE [see Warnings and Precautions ( 5.6 )].

Creatine Phosphokinase (CPK) Elevation Inform patients of the signs and symptoms of creatine phosphokinase (CPK) elevation and the need for monitoring during treatment with ENSACOVE. Advise patients to inform their healthcare provider of any new or worsening symptoms [see Warnings and Precautions ( 5.7 )]. Hyperuricemia Inform patients of the signs and symptoms of hyperuricemia.

Advise patients to inform their healthcare provider if they experience signs or symptoms associated with hyperuricemia during treatment with ENSACOVE [see Warnings and Precautions ( 5.8 )]. 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.

Advise females of reproductive potential to use effective contraception during treatment with ENSACOVE and for 1 week after the last dose [see Warnings and Precautions ( 5.9 ) and Use in Specific Populations ( 8.1, 8.3 )] . Advise males with female partners of reproductive potential to use effective contraception during treatment with ENSACOVE and for 1 week after the last dose [see Warnings and Precautions ( 5.9 ) and Use in Specific Populations ( 8.3 )] . FD&C Yellow No.

5 (tartrazine) Advise patients that this product contains FD&C Yellow No. 5 (tartrazine) which may cause allergic-type or asthma-type reactions in certain susceptible persons (e.g., patients who also have aspirin hypersensitivity) [see Warnings and Precautions ( 5.10 )] . Advise patients to contact their healthcare provider and seek medical help right away if they develop symptoms of an allergic reaction to FD&C Yellow No.

5 (tartrazine). Lactation Advise women not to breastfeed during treatment with ENSACOVE and for 1 week after the last dose [see Use in Specific Populations ( 8.2 )] . Administration Instruct patients to take ENSACOVE once a day with or without food and to swallow ENSACOVE capsules whole [see Dosage and Administration ( 2.2 )] .

Missed Dose Advise pa… [Excerpted — this section continues on DailyMed.]

🍼 Nursing Mothers 92 words ▾

8.3Females and Males of Reproductive Potential ENSACOVE can cause fetal harm when administered to a pregnant woman [see Use in Specific Populations ( 8.1 ) ]. Pregnancy Testing Verify the pregnancy status of females of reproductive potential prior to initiating ENSACOVE. Contraception Females Advise females of reproductive potential to use effective contraception during treatment with ENSACOVE and for at 1 week after the last dose.

Males Advise male patients with female partners of reproductive potential to use effective contraception during treatment with ENSACOVE and for 1 week after the last dose.

🧬 Pharmacokinetics ~2 min read ▾

12.3Pharmacokinetics Ensartinib mean (coefficient of variation [CV%]) maximum concentration (Cmax) is 292 ng/mL (60%), and the area under the concentration-time curve (AUC0–24h) is 4,920 ng·h /ml (62%) at the approved recommended dosage. Ensartinib steady state is reached within 15 days with a mean accumulation ratio of 2.7. Absorption Ensartinib median (minimum, maximum) time to reach Cmax (Tmax) at steady state is 3 hours (2, 8 hours).

Effect of Food No clinically significant differences in ensartinib pharmacokinetics were observed following administration of ENSACOVE with a high-fat meal (total 800-1000 calories, > 50% fat) compared to fasted conditions. Distribution Ensartinib mean (CV%) apparent volume of distribution is 1,720 L (42%). Ensartinib is 91.6% bound to human plasma protein.

Elimination Ensartinib mean (standard deviation [SD]) steady-state half-life (t1/2) is 30 (20) hours. Metabolism Ensartinib is predominantly metabolized by CYP3A. Excretion Following a single oral 200 mg dose of radiolabeled ensartinib, 91% of the radioactivity was recovered in feces (38% as unchanged) and 10% in urine (4.4% as unchanged).

Specific Populations No clinically significant differences in the pharmacokinetics of ensartinib were observed based on age (20 to 86 years), sex, race (Asian vs White), body weight (38 to 148 kg), mild to moderate renal impairment (eGFR 30 to 89 mL/min) and mild hepatic impairment (total bilirubin ≤ upper limit of normal (ULN) and AST > ULN or total bilirubin 1 to 1.5 x ULN and any AST). The effect of severe renal impairment (eGFR 15 to 29 mL/min), end-stage renal disease (eGFR <15 mL/min) with or without hemodialysis, and moderate (total bilirubin >1.5 to ≤ 3 ULN and any AST) or severe (total bilirubin >3 times ULN and any AST) hepatic impairment on ensartinib pharmacokinetics is unknown.

Drug Interaction Studies In Vitro Studies Cytochrome P450 (CYP) Enzymes: Ensartinib does not inhibit CYP1A2, CYP2B6, CYP2C8, CYP2C9, CYP2C19, CYP2D6 and does not induce CYP1A2, CYP2B6, or CYP3A. Transporter Systems: Ensartinib is a P-gp substrate but is not a substrate of BCRP, OATP1B1, OATP1B3, OAT1, OAT3, OCT1 or OCT2. Ensartinib does not inhibit BCRP, P-gp, OATP1B1, OATP1B3, OAT1, OAT3, OCT1, OCT2 or OCT3.

🧬 Pharmacodynamics 40 words ▾

12.2Pharmacodynamics Exposure-response relationship Ensartinib exposure-response relationships and the time course of the pharmacodynamic response have not been fully characterized. Cardiac Electrophysiology At the approved recommended dosage, a mean increase in the QTc interval > 20 ms was not observed.

🔬 Clinical Studies ~3 min read ▾

14 CLINICAL STUDIES

14.1TKI-naive ALK-Positive Locally Advanced or Metastatic NSCLC (eXALT3 Study) The efficacy of ENSACOVE was evaluated in eXALT3 (NCT02767804), an open-label, randomized, active-controlled, multicenter study in adult patients with locally advanced (stage IIIB following prior chemotherapy or chemoradiation or not amenable to curative intent therapy) or metastatic ALK-positive NSCLC. Patients were required to have ALK-positive NSCLC in tumor specimens as determined in local laboratories using immunohistochemistry (IHC), next-generation sequencing (NGS), polymerase chain reaction (PCR) or fluorescence in situ hybridization (FISH) tests.

Of these patients, 85% (247/290) had centrally confirmed ALK rearrangements with the Vysis Break Apart FISH Probe Kit. Patients could have received one prior regimen of chemotherapy but could not have previously received an ALK-targeted therapy; patients with an ECOG performance status of 0, 1, or 2 were eligible. Patients with asymptomatic, untreated brain metastases who were not on corticosteroids and patients with asymptomatic, treated brain metastases who were on stable or decreasing dose of corticosteroids were eligible.

Patients were required to have completed radiation therapy at least 2 weeks, or chemotherapy at least 4 weeks, prior to enrollment. Patients with leptomeningeal disease were ineligible. Patients were randomized 1:1 to receive ENSACOVE 225 mg orally once daily or crizotinib 250 mg orally twice daily in 28-day cycles until disease progression or unacceptable toxicity.

Randomization was stratified by prior chemotherapy (0 vs. 1), ECOG performance status (0 or 1 vs. 2), presence of central nervous system (CNS) metastases (yes or no), and geographic region (Asia vs. the rest of the world).

Tumor assessments were performed every 8 weeks. The main efficacy outcome measure was progression-free survival (PFS) as evaluated by Blinded Independent Central Review (BICR) according to RECIST version 1.1. The key secondary efficacy outcome measure was overall survival (OS); other secondary outcome measures included CNS response rate, time to CNS progression, and overall response rate (ORR).

A total of 290 patients were randomized to ENSACOVE (n=143) or crizotinib (n=147). The baseline demographic characteristics of the overall study population were median age 54 years (range: 25-90); 16% age > 65 years; 51% male; 56% Asian; 41% White and 1% Black; 7% Hispanic or Latino; ECOG PS 0 or 1 (95%); and 62% never smokers. Patients had Stage IIIB (8%) or Stage IV NSCLC (92%); 32% had received prior chemotherapy and 17% had received prior radiation.

Baseline CNS metastases were present in 36% of the patients. The eXALT3 study demonstrated a statistically significant improvement in PFS for patients randomized to ENSACOVE compared to patients randomized to crizotinib. The efficacy results as assessed by BICR are summarized in Table 6 and Figure 1.

Table 6: Efficacy Results for eXALT3 Study According to BICR Assessment Efficacy Parameter ENSACOVE N=143 Crizotinib N=147 Progression-free survival Number of events, n (%) 59 (41%) 80 (54%) Progressive disease, n (%) 51 (36%) 77 (52%) Death, n (%) 8 (6%) 3 (2%) Median, months (95% CI) 25.8 (21.8, NE) 12.7 (9.2, 16.6) Hazard ratio (95% CI) 0.56 (0.40, 0.79) p-value a 0.0008 Overall response rate Overall response rate % (95% CI) 74% (66, 81) 67% (58, 74) Complete response % 12% 5% Partial response % 62% 61% Duration of response Number of responders, n 106 98 Median, months (95% CI) NE (22.0, NE) 27.3 (12.9, NE) CI = Confidence Interval, NE=not estimable, BICR = Blinded Independent Central Review a p-value based on unstratified log-rank test Figure 1 Kaplan-Meier Plot of Progression-Free Survival by IRR from Study 301 (eXALT3) At the time of the primary PFS analysis, OS results were immature.

At the time of final analysis of OS, there was no statistically significant difference (p-value = 0.4570) between ENSACOVE and crizotinib. Median OS was… [Excerpted — this section continues on DailyMed.]

🧪 Nonclinical Toxicology 81 words ▾

13 NONCLINICAL TOXICOLOGY

13.1Carcinogenesis, Mutagenesis, Impairment of Fertility Carcinogenicity studies have not been conducted with ensartinib. Ensartinib was not mutagenic in a bacterial reverse mutation (Ames) assay and was not clastogenic in an in vitro human lymphocyte chromosome aberration assay or an in vivo rat bone marrow micronucleus assay. Dedicated fertility studies were not conducted with ensartinib.

No adverse effects on male or female reproductive organs were observed in up to 3-month repeat-dose toxicology studies conducted in rats and dogs.

📄 Carcinogenesis, Mutagenesis, Impairment of Fertility 78 words ▾

13.1Carcinogenesis, Mutagenesis, Impairment of Fertility Carcinogenicity studies have not been conducted with ensartinib. Ensartinib was not mutagenic in a bacterial reverse mutation (Ames) assay and was not clastogenic in an in vitro human lymphocyte chromosome aberration assay or an in vivo rat bone marrow micronucleus assay. Dedicated fertility studies were not conducted with ensartinib.

No adverse effects on male or female reproductive organs were observed in up to 3-month repeat-dose toxicology studies conducted in rats and dogs.

📄 Patient Package Insert ~3 min read ▾

PATIENT INFORMATION ENSACOVE TM (En-sa-kowv) (ensartinib) capsules, for oral use What is ENSACOVE? ENSACOVE 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, that has spread to other parts of your body, and who have not received medicines called ALK-inhibitors. Your healthcare provider will perform a test to make sure that ENSACOVE is right for you.

It is not known if ENSACOVE is safe and effective in children. Do not use ENSACOVE if you are allergic to ENSACOVE, FD&C No. 5 (tartrazine), or to any of the ingredients in ENSACOVE.

See the end of this leaflet for a complete list of ingredients in ENSACOVE. Before using ENSACOVE, tell your healthcare provider about all of your medical conditions, including if you: have lung or breathing problems have liver problems have problems with your heartbeat have diabetes mellitus or glucose intolerance have problems with your vision are pregnant or plan to become pregnant. ENSACOVE can harm your unborn baby.

Your healthcare provider will do a pregnancy test before you start treatment with ENSACOVE. Tell your healthcare provider right away if you become pregnant or think you may be pregnant during treatment with ENSACOVE. Females who are able to become pregnant should use effective birth control (contraception) during treatment with ENSACOVE and for 1 week after the last dose of ENSACOVE.

Talk to your healthcare provider about birth control choices that are right for you during treatment with ENSACOVE. Males who who have female partners who are able to become pregnant should use effective birth control (contraception) during treatment with ENSACOVE and for 1 week after the last dose of ENSACOVE. are breastfeeding or plan to breastfeed. It is not known if ENSACOVE passes into your breast milk.

Do not breastfeed during treatment with ENSACOVE and for 1 week after the last dose. Talk to your healthcare provider about the best way to feed your baby during this time. Tell your healthcare provider about all the other medicines you take, including prescription and over-the-counter medicines, vitamins and herbal supplements.

Certain other medicines may affect the way that ENSACOVE works and may increase your risk of certain side effects. Know the medicines you take. Keep a list of them to show to your healthcare provider and pharmacist when you get a new medicine.

How should I take ENSACOVE? Take ENSACOVE exactly as your healthcare provider tells you to take it. Do not change your dose or stop taking ENSACOVE unless your healthcare provider tells you to.

Swallow ENSACOVE capsules whole. Do not crush or chew capsules. Do not open or dissolve the contents of the capsule.

Take ENSACOVE 1 time a day, at the same time each day. You may take ENSACOVE with or without food. If you miss a dose, take it as soon as you remember.

If your next dose is due within 12 hours, skip the missed dose and take your next dose at your regular time. Do not take 2 doses of ENSACOVE on the same day to make up for the missed dose. If you vomit after taking a dose of ENSACOVE, do not take an extra dose.

Take your next dose at your regular time. What should I avoid while taking ENSACOVE? Limit your time in the sun during treatment with ENSACOVE and for at least 1 week after your last dose.

ENSACOVE may make your skin sensitive to sunlight. You may burn more easily and get severe sunburns. When you are in the sun, wear a hat and protective clothing, and use a broad-spectrum sunscreen and lip balm with a Sun Protection Factor (SPF) of 30 or greater to protect against sunburn.

What are the possible side effects of ENSACOVE? ENSACOVE can cause serious side effects, including: Lung problems . ENSACOVE can cause severe or life-threatening swelling (inflammation) of the lungs.

Symptoms may be similar to those from lung cancer. Tell your healthcare provider right away if you get any new or worsening symptoms of lung problems duri… [Excerpted — this section continues on DailyMed.]

📄 Package Label / Principal Display Panel 52 words ▾

PRINCIPAL DISPLAY PANEL - 25 mg ENSACOVE ™ (ensartinib) capsules - 25 mg Bottle of 30 Capsules NDC 83076-1025-3 25 mg Bottle label 25mg Carton Label

PRINCIPAL DISPLAY PANEL - 100 mg ENSACOVE ™ (ensartinib) capsules - 100 mg Bottle of 60 Capsules NDC 83076-1100-6 100 mg bottle label 100mg Carton Label

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

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

Medicare Part D (outpatient prescription) spending for Ensacove — 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 Ensacove. 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.
Total Part D spend
$410.6K
Claims incl. refills
38
Beneficiaries
14
Spend / beneficiary
$29,325.44
Spend / claim
$10,804.11
💵 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 ENSACOVE (this brand).

Top reported reactions

Rash6
Disease Progression4
Pruritus4
Constipation3
Fatigue3
Oedema3
Alanine Aminotransferase Increased2

Age at onset

Adult12
Elderly7

Reporter sex

32 reports
Male · 52%
Female · 48%

Serious outcomes

Hospitalization7
Disabling2
Death2
Reports over time (by year) — tap or hover for the count & year
2021 2022 2024 2026 15 2
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) — Not published for this NDC CMS reports utilization only for NDCs with Medicaid claims above its privacy threshold.
“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 Xcovery Holdings, Inc.. Listing status can change — the directory data on this page refreshes weekly.
Who lists this product with the FDA?
Xcovery Holdings, 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.
← 83076-1025-03 · Xcovery 83077-0100-02 · Merus →
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.