Entrectinib
Entrectinib is a targeted cancer medicine (a kinase inhibitor) used for ROS1-positive metastatic non-small cell lung cancer in adults and for NTRK gene fusion-positive solid tumors in adults and children older than 1 month.
🧬 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 1 clinical label set 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 →
Entrectinib (Rozlytrek) is a once-daily targeted cancer medicine, on the U.S. market since about 2019, that blocks the abnormal ROS1, TRK and ALK fusion proteins keeping some tumors growing; specialists use it when an FDA-approved test finds ROS1-positive metastatic non-small cell lung cancer or an NTRK gene fusion in a solid tumor. It is usually manageable, though tiredness, constipation, taste changes, dizziness and weight gain are common. It carries no boxed warning, but shortness of breath or worsening swelling can signal heart failure and needs prompt attention. Expect regular checks of your heart, liver tests and uric acid, and report confusion, vision changes or new bone pain promptly.
Clinical pearls
- Avoid grapefruit and grapefruit juice throughout treatment, because they raise entrectinib levels and side effects.
- Have every new medicine, even a short course, screened first, since many drugs shift entrectinib levels or add heart rhythm risk.
- Oral pellets go on soft food, never down a feeding tube; capsules can be made into a liquid suspension instead.
- It can harm an unborn baby, so use contraception during treatment and for 5 weeks after (women) or 3 months (men).
Patient information guide A plain-language walkthrough of Entrectinib, written from its FDA label.
What Entrectinib is used for
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Entrectinib is a kinase inhibitor used for cancers with specific gene changes.
- Rozlytrek is used for adults with ROS1-positive metastatic non-small cell lung cancer, as detected by an FDA-approved test.
- Rozlytrek is used for adults and children older than 1 month with NTRK gene fusion-positive solid tumors that are metastatic or hard to remove safely, and that have progressed or have no satisfactory alternative.
- The solid tumor use is under accelerated approval based on response rate and durability of response.
How Entrectinib works
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Entrectinib blocks the TRK, ROS1 and ALK proteins. When these are fused abnormally, they can drive cancer cells to grow without limits. By blocking them, entrectinib interrupts that growth signal.
Its main active breakdown product, M5, works in a similar way. Entrectinib also reached the brain in animal studies.
Entrectinib dosage
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Rozlytrek is taken once daily by mouth, with or without food, until the cancer progresses or side effects become unacceptable. Your prescriber picks the form and dose.
- Capsules are swallowed whole, or prepared as a suspension if you can’t swallow them or use a feeding tube.
- Pellets are sprinkled on soft food. They are not for feeding tubes.
- If you vomit right after a dose, repeat it.
- If you miss a dose, make it up unless the next dose is due within 12 hours.
Dosing details from the FDA-approved label
From the Entrectinib prescribing information (“Dosage and Administration”). Doses are set by your prescriber for your product, condition, kidney function and age — never change a dose on your own.
- Adult ROS1-Positive Non-Small Cell Lung Cancer
- 600 mg orally once daily with or without food until disease progression or unacceptable toxicity
- Adult NTRK Gene Fusion-Positive Solid Tumors
- 600 mg orally once daily until disease progression or unacceptable toxicity
- Capsules or oral pellets, with or without food
- Pediatric patients with NTRK Gene Fusion-Positive Solid Tumors, BSA ≥1.51 m2
- 600 mg orally once daily until disease progression or unacceptable toxicity
- Based on age and body surface area
- Pediatric patients >6 months with NTRK Gene Fusion-Positive Solid Tumors, BSA ≤0.50 m2
- 300 mg/m2 orally once daily
- To enable dosing increments of 10 mg, capsules prepared as an oral suspension must be used
- Pediatric patients >6 months with NTRK Gene Fusion-Positive Solid Tumors, BSA 0.51 to 0.80 m2
- 200 mg orally once daily
- Pediatric patients >6 months with NTRK Gene Fusion-Positive Solid Tumors, BSA 0.81 to 1.10 m2
- 300 mg orally once daily
- Pediatric patients >6 months with NTRK Gene Fusion-Positive Solid Tumors, BSA 1.11 to 1.50 m2
- 400 mg orally once daily
- Pediatric patients >1 month to ≤6 months with NTRK Gene Fusion-Positive Solid Tumors
- 250 mg/m2 orally once daily
- To enable dosing increments of 10 mg, capsules prepared as an oral suspension must be used
Read the label’s full dosing text
2 DOSAGE AND ADMINISTRATION Select patients for treatment based on the presence of ROS1 rearrangement(s) or NTRK gene fusion. ( 2.1 ) Evaluate left ventricular ejection fraction, serum uric acid levels and QT interval and electrolytes prior to ROZLYTREK initiation. ( 2.2 ) Select appropriate dosage form: oral capsules, capsules prepared as an oral suspension or oral pellets. ( 2.3 ) Use capsules prepared as suspension for enteral tube administration. Do not use pellets for enteral tube administration. ( 2.3 ) Administer ROZLYTREK capsules, capsules prepared as a suspension, or pellets once daily, with or without food. ( 2.4 ) Adult Dosage for ROS1- Positive Non-Small Cell Lung Cancer: 600 mg orally once daily. ( 2.5 ) Adult and Pediatric Dosage for NTRK Gene Fusion-Positive Solid Tumors: Adults: 600 mg orally once daily. ( 2.6 ) Pediatric Patients: Recommended dosage is based on age and body surface area (BSA) as shown below. ( 2.6 ) Age Recommended Daily Dosage >6 months ≤0.50 m 2 : 300 mg/m 2 0.51 to 0.80 m 2 : 200 mg 0.81 to 1.10 m 2 : 300 mg 1.11 to 1.50 m 2 : 400 mg BSA ≥1.51 m 2 : 600 mg once daily >1 month to ≤6 months 250 mg/m 2 once daily Modify dosage of ROZLYTREK if coadministration with moderate or strong CYP3A inhibitors cannot be avoided. ( 2.8 ) See preparation and administration instructions. ( 2.9 ) 2.1 Patient Selection Select patients for the treatment of metastatic NSCLC with ROZLYTREK based on the presence of ROS1 rearrangement(s) in tumor or plasma specimens [see Clinical Studies (14.1) ] . Testing using plasma specimens is only appropriate for patients for whom tumor tissue is not available for testing. Information on FDA-approved tests for the detection of ROS1 rearrangement(s) in NSCLC is available at http://www.fda.gov/CompanionDiagnostics. Select patients for treatment of locally advanced or metastatic solid tumors with ROZLYTREK based on the presence of a NTRK gene fusion in tumor or plasma specimens [see Clinical Studies (14.2) ] . Testing using plasma specimens is only appropriate for patients for whom tumor tissue is not available for testing. Information on FDA-approved tests for the detection of NTRK gene fusion(s) in solid tumors is available at http://www.fda.gov/CompanionDiagnostics.
Excerpted — the section continues on the label. Read the full Dosage and Administration section on DailyMed →
Entrectinib side effects
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The most common side effects reported were:
Common side effects
- Tiredness
- Constipation
- Changes in taste
- Swelling (edema)
- Dizziness
- Diarrhea
- Nausea and vomiting
- Weight gain
- Numbness or tingling
- Muscle and joint pain
- Memory or thinking problems
- Cough
- Fever
When to get medical help
- Call your doctor if you have shortness of breath or swelling, which can be signs of heart failure.
- Tell your doctor about confusion, memory problems, hallucinations, mood changes, or sleep trouble.
- Get help promptly for new pain, trouble moving, or deformity, which can signal a bone fracture.
- Report fainting, a racing or irregular heartbeat, or dizziness that could signal a heart rhythm problem (QT prolongation).
- Tell your doctor right away about new vision changes such as blurred vision, double vision, or sensitivity to light.
- Report symptoms of high uric acid (hyperuricemia) or liver problems.
- Seek help right away for thoughts of self-harm or severe depression.
Entrectinib warnings and precautions
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- Heart failure: heart function is checked before starting. Report shortness of breath or swelling.
- Nervous system effects: confusion, memory trouble, mood changes, dizziness and sleep problems can occur. Avoid driving if affected.
- Fractures: risk is higher in children, and some fractures happened without trauma.
- Liver injury: liver tests are checked every 2 weeks in the first month, then monthly.
- High uric acid: levels are checked before and during treatment.
- QT prolongation: an ECG and electrolytes are checked.
- Vision problems: report new changes promptly.
- Fetal harm: it can harm an unborn baby.
Entrectinib interactions
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Some drugs and foods change entrectinib levels or add risk.
- Strong or moderate CYP3A inhibitors raise levels and side effects. Avoid them, or your dose may be reduced.
- Grapefruit products act as CYP3A inhibitors, so avoid them.
- Strong or moderate CYP3A inducers lower levels and may reduce effectiveness. Avoid them.
- Other QT-prolonging drugs add to heart rhythm risk. Avoid them.
Interactions listed in the FDA-approved label
From the Entrectinib prescribing information (“Drug Interactions”): what the manufacturer studied or reported to the FDA.
- Moderate and strong CYP3A inhibitors (adults and pediatric patients 2 years and older): Increases entrectinib plasma concentrations, which could increase the frequency or severity of adverse reactions. Avoid coadministration; if unavoidable, reduce the ROZLYTREK dose.
- Moderate and strong CYP3A inhibitors (pediatric patients less than 2 years): Increases entrectinib plasma concentrations. Avoid coadministration of ROZLYTREK with moderate or strong CYP3A inhibitors.
- Grapefruit products: They contain inhibitors of CYP3A. Avoid grapefruit products during treatment with ROZLYTREK.
- Moderate and strong CYP3A inducers: Decreases entrectinib plasma concentrations, which may reduce ROZLYTREK efficacy. Avoid coadministration of strong and moderate CYP3A inducers with ROZLYTREK.
- Drugs that prolong QTc interval: QTc interval prolongation can occur with ROZLYTREK. Avoid coadministration with other products with a known potential to prolong QT/QTc interval.
Read the label’s full interactions text
7 DRUG INTERACTIONS Moderate and Strong CYP3A Inhibitors : For adult and pediatric patients 2 years and older, reduce the dose of ROZLYTREK if coadministration of moderate or strong CYP3A inhibitors cannot be avoided. ( 2.8 , 7.1 ) For pediatric patients less than 2 years, avoid coadministration with ROZLYTREK. ( 7.1 ) Moderate and Strong CYP3A Inducers : Avoid coadministration with ROZLYTREK. ( 7.1 ) Drugs That Prolong QTc Interval : Avoid concomitant use with ROZLYTREK. ( 7.2 ) 7.1 Effect of Other Drugs on ROZLYTREK Moderate and Strong CYP3A Inhibitors Adults and Pediatric Patients 2 Years and Older Coadministration of ROZLYTREK with a strong or moderate CYP3A inhibitor increases entrectinib plasma concentrations [see Clinical Pharmacology (12.3) ], which could increase the frequency or severity of adverse reactions. Avoid coadministration of strong or moderate CYP3A inhibitors with ROZLYTREK. If coadministration is unavoidable, reduce the ROZLYTREK dose [see Dosage and Administration (2.8) , Clinical Pharmacology (12.3) ]. Pediatric Patients less than 2 Years Avoid coadministration of ROZLYTREK with moderate or strong CYP3A inhibitors [see Clinical Pharmacology (12.3) ] . Avoid grapefruit products during treatment with ROZLYTREK, as they contain inhibitors of CYP3A. Moderate and Strong CYP3A Inducers Coadministration of ROZLYTREK with a strong or moderate CYP3A inducer decreases entrectinib plasma concentrations [see Clinical Pharmacology (12.3) ], which may reduce ROZLYTREK efficacy. Avoid coadministration of strong and moderate CYP3A inducers with ROZLYTREK . 7.2 Drugs That Prolong QTc Interval QTc interval prolongation can occur with ROZLYTREK. Avoid coadministration of ROZLYTREK with other products with a known potential to prolong QT/QTc interval [see Warnings and Precautions (5.6) , Clinical Pharmacology (12.2) ] .
Not a complete list. The label covers the interactions the manufacturer studied or reported, and our own interaction database does not cover every medicine either. Bring your full medication list, including vitamins and herbal products, to your pharmacist.
Before taking Entrectinib
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- Tell your doctor about heart problems, long QT, or electrolyte problems.
- Pregnancy should be ruled out before starting. Use effective contraception during treatment and for 5 weeks after (females) or 3 months after (males with female partners).
- Do not breastfeed during treatment and for 7 days after the last dose.
- Moderate or severe liver impairment: safety is unknown, so closer monitoring is needed.
- Severe kidney impairment has not been studied.
- Children older than 1 month may be treated for NTRK solid tumors. Fractures were more common in children.
- Older adults: there is not enough data to know if they respond differently.
What Entrectinib does in the body
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How exposure relates to effect over time is unknown. In clinical trials, about 3% of patients had a meaningful lengthening of the QT interval, a heart rhythm measure. About 0.6% had a QTc over 500 ms.
How your body processes Entrectinib
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Entrectinib reaches its highest blood level about 4 to 6 hours after a dose. Food, even a high-fat meal, did not significantly change exposure to the capsules. It is broken down mainly by the liver enzyme CYP3A4 into an active metabolite, M5.
Half-lives are about 20 hours for entrectinib and 40 hours for M5. Steady state is reached within about 1 to 2 weeks of daily use. Most of the drug leaves in the stool, with very little in urine.
How to store Entrectinib
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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) . Store ROZLYTREK capsules in the original container and keep the bottle tightly closed in order to protect from moisture.
Written from the FDA-approved label with AI and reviewed by our pharmacy team. How we use AI →
Supplements & herbs that interact with Entrectinib
175 supplements and herbal products have documented interactions with Entrectinib in the licensed clinical database we use. Most are manageable — but your pharmacist should know about everything you take, including vitamins and herbals.
- Major · 11
- Moderate · 127
- Minor · 37
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.
Entrectinib: pharmacist answers to common questions
Quick, plain-English answers to the questions patients ask most about Entrectinib — the kind of thing our pharmacy team would talk through with you at the counter.
What is entrectinib for?
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How do I take it?
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What side effects should I expect?
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Are there foods or medicines I should avoid?
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What monitoring will I need?
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Is it safe in pregnancy?
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Is Entrectinib available over the counter?
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When was Entrectinib first available?
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Answers drafted from the FDA-approved label with AI and reviewed by our pharmacy team. How we use AI →
More about Entrectinib on HelloPharmacist
Entrectinib forms and strengths (how it comes)
Entrectinib is available in 2 forms. 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.
Capsule
How this form is used
- Rozlytrek is used for ROS1-positive metastatic NSCLC in adults.
- Rozlytrek is used for NTRK gene fusion-positive solid tumors in adults and children older than 1 month.
- Rozlytrek capsules are swallowed whole once daily, with or without food, by patients who can swallow capsules.
- Rozlytrek capsules can be prepared as an oral suspension for people who have trouble swallowing capsules or who use a feeding tube.
Other oral form
How this form is used
- Rozlytrek oral pellets are for patients who can’t swallow capsules but can swallow soft food.
- Rozlytrek pellets are sprinkled on one or more spoonfuls of soft food and taken once daily, with or without food.
- Do not use Rozlytrek pellets in a feeding tube, because they may clog it.
- Do not use Rozlytrek pellets to make a suspension, and do not use partial amounts from a 50 mg packet.
Entrectinib on the U.S. market: products, makers and brands
How Entrectinib 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 company lists 3 Entrectinib product records with the FDA, mostly as capsule, other oral form; the earliest marketing or approval year on record is 2019. Brand names on the directory include Rozlytrek; the rest are generics.
FDA-listed product records by dose form (tablet variants merged) — FDA National Drug Code Directory. Record counts are not sales or prescription volume.
Also listed with the FDA, not a patient dose form: Powder (1) — bulk drug substance sold to compounders/manufacturers and multi-item kits. These aren’t counted in the dose-form total above.
How widely Entrectinib is used (Medicaid data)
A general measure of how commonly Entrectinib 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 Entrectinib 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.
How commonly is Entrectinib prescribed? Of the 1,601 medications we measure, Entrectinib ranks #1,544 by Medicaid prescriptions — more than 4% of them.
Utilization by Entrectinib 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.
entrectinib 200 MG Oral Capsule
Summed across the 1 of 5 listed NDC products with Medicaid activity — every brand and generic of this exact strength & form. RxNorm 2197875
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 Entrectinib, 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 1 of 5 listed Entrectinib NDCs with Medicaid activity.
Compare Entrectinib products
A representative set of FDA-listed product records for Entrectinib — 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 |
|---|---|---|---|---|
| 💊Capsule | ||||
| 100 mg | Oral | Genentech, Inc. | NDA | View NDC → |
| 200 mg | Oral | Genentech, Inc. | NDA | View NDC → |
| 💊Other oral form | ||||
| 50 mg/201 | Oral | Genentech, Inc. | NDA | View NDC → |
Showing 3 of 3 products — FDA National Drug Code Directory. See every product, package size and price: browse all 3 Entrectinib NDCs →
Entrectinib side effects reported to the FDA (FAERS)
After a medicine reaches the market, patients, doctors and drugmakers can send the FDA reports of problems they think may be linked to it. Here’s what’s been reported for Entrectinib — a signal of what to watch for, not proof the drug caused it.
Source: openFDA, from the FDA Adverse Event Reporting System (FAERS). These are voluntary reports — they don’t prove the drug caused the effect, and counts reflect how often something was reported, not how often it actually happens. Reports also often name the very problem the medicine is taken for — a common reason to file one is that the drug didn’t help — so for a pain reliever you may see “pain” high on the list; that points to why the report was filed, not to the drug causing the symptom. This counts every report that lists Entrectinib in any role, so the total runs higher than the FDA’s official dashboard, which counts only cases where the drug is the suspect. For the authoritative figures, see the FDA FAERS Public Dashboard. Always talk to your pharmacist or doctor.
Entrectinib FDA approval history
How Entrectinib went from FDA review to the pharmacy shelf — the key milestones in its regulatory journey.
Source: Drugs@FDA.
Entrectinib recall history
A recall is when a specific batch of a medicine is pulled from the market — usually a manufacturing issue, not a problem with the drug itself. Class I is most serious, Class III least.
The FDA’s enforcement reports list no Entrectinib recalls since July 2021.
✅No Entrectinib recalls on record since July 2021Source: FDA enforcement (recall) reports, via openFDA; our copy was last updated Sep 24, 2026.
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.
RxCUI 2197862 2 dose forms · 3 strengths
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Dose form (SCDF) Oral Capsule RxCUI 2197866In current FDA listings -
Dose form (SCDF) Oral Pellet RxCUI 2668594In current FDA listingsClinical drug / strength (SCD) 50 MGRxCUI 2668595
Look up RxCUI 2197862 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.
Entrectinib supply and shortage status
Whether Entrectinib is in short supply in the U.S. right now, plus any shortage history the FDA has on record. A shortage usually reflects a manufacturing or demand issue — not a safety problem with the drug.
Source: openFDA, from the FDA Drug Shortages database.
Entrectinib brand names
Entrectinib is sold under one brand name in the FDA directory — Rozlytrek. A brand and its generic contain the same active ingredient; the brand name belongs to one company's product.
Who makes Entrectinib: manufacturers and labelers
One company lists Entrectinib products with the FDA. By number of product records, the largest are Genentech, Inc.. Labelers include manufacturers and repackagers; the product in your bottle depends on which one your pharmacy stocks.
Entrectinib drug class (RxNorm)
Entrectinib belongs to the Other protein kinase inhibitors class.
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.
Sources for this Entrectinib page
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.
How this page is built
HelloPharmacist combines public FDA and NLM records and does not author the underlying clinical facts. The plain-language sections are written with AI from the FDA-approved label text and reviewed by our pharmacy team before publication. Genentech, Inc. is the representative DailyMed label linked for verification and dates. This is general education, not medical advice: always talk to your doctor or pharmacist about your own medicines. How we build and review drug pages →