Rozlytrek (entrectinib)
An approved treatment for NTRK Fusion Cancer.
The same compound appears under different names depending on the context. Here is how to identify Entrectinib wherever you encounter it, plus the key facts at a glance.
- Generic name
- Entrectinib
- Brand name
- Rozlytrek
- Development codes
- RXDX-101, NMS-E628
- Drug class
- TRK and ROS1 inhibitor (first generation)
- Manufacturer
- Genentech (Roche)
- How it's taken
- Adults take 600 mg once a day by mouth, with or without food.
An oral TRK and ROS1 inhibitor approved under accelerated approval for adults and children older than 1 month with NTRK fusion solid tumors, and separately for ROS1-positive lung cancer. Its distinguishing feature is that it reaches tumors in the brain.
Where Entrectinib fits
One of 3 FDA-approved TRK inhibitors. Compared with Vitrakvi (larotrectinib), it is approved from 1 month of age rather than birth, reports stronger brain penetration, and carries extra warnings for heart failure and QT prolongation because it also hits ROS1 and ALK. Augtyro (repotrectinib) is the option after resistance to either first-generation drug.
How Entrectinib works
Entrectinib blocks the TRK proteins that an NTRK gene fusion keeps switched on, so the growth signal stops. It also blocks ROS1 and ALK, 2 other proteins that drive some lung cancers. It was engineered to pass through the blood-brain barrier, the filter that keeps most drugs out of the brain, which matters because NTRK fusion cancers can spread there and some start there.
Mechanism: Inhibitor of the TRKA, TRKB and TRKC proteins plus ROS1 and ALK, designed to cross the blood-brain barrier
Side effects and safety
- Heart failure. Congestive heart failure occurred in trials; heart function (LVEF) is measured before starting in people with symptoms or risk factors.
- Nervous system effects. Cognitive changes, mood changes, dizziness and sleep disturbance; avoid driving if affected.
- Bone fractures. Fractures occurred in adults and children; report new bone pain.
- Liver injury and high uric acid. Liver enzymes and uric acid are monitored; dosing is adjusted for high readings.
- QT prolongation and vision changes. ECG and electrolytes are checked in people at risk; blurred vision and other eye symptoms should be reported.
- Harm to a fetus. Use contraception during treatment and for 5 weeks after the last dose.
- Heart function (LVEF) before starting if at risk
- Liver tests every 2 weeks for the first month, then monthly
- Uric acid, ECG and electrolytes as needed
The most common side effects in the label's pooled safety set of 355 patients were fatigue (48%), constipation (46%), altered taste (44%), swelling (40%), dizziness (38%), diarrhea, nausea, nerve pain or numbness, weight gain, cough and raised creatinine. The label warns about congestive heart failure (heart pumping is checked before starting), nervous system effects such as confusion and mood changes, bone fractures, liver injury, high uric acid, QT interval prolongation on the ECG, vision changes and harm to a fetus. There is no boxed warning.
This is not a complete list of side effects. Talk to your doctor or pharmacist about what to expect and when to seek medical attention.
Taking Entrectinib
Adults take 600 mg once a day by mouth, with or without food. Children older than 1 month are dosed by age and body surface area, from 250 mg per square meter in infants to 600 mg in larger children. It comes as 100 mg and 200 mg capsules and, since October 2023, as 50 mg oral pellets that can be sprinkled on soft food, which is how young children take it. Strong CYP3A inhibitors and inducers should be avoided or the dose adjusted.
Availability and cost
Only available as the brand-name product.
A specialty oral cancer drug sold by Genentech. The Genentech Oncology Co-pay Assistance Program covers commercially insured patients and the Genentech Patient Foundation covers free drug for eligible uninsured or underinsured patients.
Help paying for Rozlytrek
Pick your insurance to see which help fits. Drugmaker copay cards can't be used with Medicare, Medicaid or TRICARE; charity funds are the usual route there.
- Copay help
Genentech Oncology Co-pay Assistance Program for commercially insured patients taking Rozlytrek for an FDA-approved indication; eligibility criteria and benefit limits apply. Call 855-692-6729 or visit CopayAssistanceNow.com. Not valid under federal or state programs.
For: private insurance · source - Free medicine program
Genentech Patient Foundation gives free Genentech medicine to people without insurance coverage or with financial concerns who meet income requirements; insured patients with coverage must first pursue other assistance. Call 888-941-3331.
For: no insurance, underinsured, private insurance, Medicare, Medicaid · source - Insurance and case manager help
Rozlytrek Access Solutions handles benefits investigation, prior authorization, appeals and specialty pharmacy coordination, and refers patients with commercial or public insurance to independent co-pay foundations.
For: private insurance, Medicare, Medicaid · source
Good to know: The co-pay program's dollar cap is not stated on Genentech's readable pages. Foundation income thresholds are shown on the Genentech site.
Access and eligibility
Approved for solid tumors with an NTRK gene fusion found by an FDA-approved test, without a known acquired resistance mutation, that are metastatic or where surgery would cause severe harm, and that have progressed after treatment or have no satisfactory alternative. Patients must be older than 1 month. The separate ROS1 lung cancer indication is for adults only.
Source: Rozlytrek patient support, Genentech
Access program details are provided for informational purposes and may vary based on insurance coverage, geographic location, and individual circumstances. Confirm current eligibility directly with the manufacturer or your specialty pharmacy.
Clinical trial results
In the label, adults with NTRK fusion solid tumors from the ALKA, STARTRK-1 and STARTRK-2 studies (54 patients) had a 59% response rate with 13% complete responses, and 56% of responses lasted 12 months or longer[1]. In children from STARTRK-NG and TAPISTRY (33 patients), the response rate was 70% with 42% complete responses and a median response duration of 25.4 months; infantile fibrosarcoma responded in 7 of 8 children and primary brain tumors in 53%. Intracranial responses were seen in 3 of 4 adults with measurable brain metastases. GLOBOTRK (NCT06528691), led by St. Jude and started in May 2026, is testing entrectinib as the first treatment for children under 3 with NTRK or ROS1 fused brain tumors.
Development history
Entrectinib was discovered by Nerviano Medical Sciences and developed by Ignyta, which Roche bought in 2018. The FDA granted accelerated approval on August 15, 2019 for NTRK fusion solid tumors in adults and children 12 and older, and for ROS1-positive non-small cell lung cancer[2]. On October 20, 2023 the NTRK indication was extended to children older than 1 month and the oral pellet formulation was approved[3]. The NTRK indication remains under accelerated approval as of the December 2025 label, with continued approval contingent on confirmatory data.
Explore NTRK Fusion Cancer trials
Other NTRK Fusion Cancer treatments
Common questions about Entrectinib
▸What is Entrectinib (Rozlytrek)?
An oral TRK and ROS1 inhibitor approved under accelerated approval for adults and children older than 1 month with NTRK fusion solid tumors, and separately for ROS1-positive lung cancer. Its distinguishing feature is that it reaches tumors in the brain.
▸How does Entrectinib work?
Entrectinib blocks the TRK proteins that an NTRK gene fusion keeps switched on, so the growth signal stops. It also blocks ROS1 and ALK, 2 other proteins that drive some lung cancers. It was engineered to pass through the blood-brain barrier, the filter that keeps most drugs out of the brain, which matters because NTRK fusion cancers can spread there and some start there.
▸What are the side effects of Entrectinib?
The most common side effects in the label's pooled safety set of 355 patients were fatigue (48%), constipation (46%), altered taste (44%), swelling (40%), dizziness (38%), diarrhea, nausea, nerve pain or numbness, weight gain, cough and raised creatinine. The label warns about congestive heart failure (heart pumping is checked before starting), nervous system effects such as confusion and mood changes, bone fractures, liver injury, high uric acid, QT interval prolongation on the ECG, vision changes and harm to a fetus. There is no boxed warning.
▸How is Entrectinib taken?
Adults take 600 mg once a day by mouth, with or without food. Children older than 1 month are dosed by age and body surface area, from 250 mg per square meter in infants to 600 mg in larger children. It comes as 100 mg and 200 mg capsules and, since October 2023, as 50 mg oral pellets that can be sprinkled on soft food, which is how young children take it. Strong CYP3A inhibitors and inducers should be avoided or the dose adjusted.
▸Is Entrectinib FDA approved?
Yes, Entrectinib (Rozlytrek) is FDA approved (2019) for the treatment of NTRK Fusion Cancer.
▸What is the difference between Rozlytrek and Vitrakvi?
Both block TRK proteins and both are approved for NTRK fusion solid tumors regardless of tumor type. Rozlytrek also blocks ROS1 and ALK and was designed to cross into the brain, which is why it is also approved for ROS1-positive lung cancer and is often chosen when brain metastases are present. Vitrakvi hits only TRK, has an oral solution for infants, no lower age limit and full rather than accelerated approval. No trial has compared them head to head.
▸What is the response rate for Rozlytrek in NTRK fusion cancer?
In the label, 59% of 54 adults responded, 13% completely, and 56% of those responses lasted a year or more. In 33 children, 70% responded and 42% had complete responses, with a median response duration of 25.4 months.
▸Can babies take Rozlytrek?
Yes, from 1 month of age. Since October 2023 it comes as 50 mg oral pellets that can be sprinkled on soft food, dosed by body surface area. Children aged 1 to 6 months take 250 mg per square meter once a day.
▸Is Rozlytrek fully approved?
Not for NTRK fusion cancer. That indication has been under accelerated approval since August 15, 2019, based on response rate and duration, and the FDA lists it as ongoing pending confirmatory data. The ROS1 lung cancer indication is a separate approval.
▸Does Rozlytrek treat brain metastases?
It was designed to cross the blood-brain barrier. In the label, 3 of 4 adults with measurable brain metastases had their brain tumors shrink, and 53% of children with primary brain tumors responded. A St. Jude trial (GLOBOTRK, NCT06528691) is now testing it as first treatment for infants with NTRK-fused brain tumors.
Sources and references
Every factual claim on this page is drawn from the public sources listed below. Click any reference to open the original document.
- U.S. National Library of Medicine, DailyMed · 2025-12-04. Rozlytrek (entrectinib) capsules and oral pellets: prescribing information. https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=c7c71b0c-2549-4495-86b6-c2807fa54908
- National Cancer Institute, Cancer Currents · 2019-08-30. FDA approves entrectinib based on tumor genetics rather than cancer type. https://www.cancer.gov/news-events/cancer-currents-blog/2019/fda-entrectinib-ntrk-fusion
- U.S. Food and Drug Administration · 2023-10-20. FDA expands pediatric indication for entrectinib and approves new pellet formulation. https://www.fda.gov/drugs/resources-information-approved-drugs/fda-expands-pediatric-indication-entrectinib-and-approves-new-pellet-formulation
- ClinicalTrials.gov. STARTRK-2: basket study of entrectinib in solid tumors with NTRK1/2/3, ROS1 or ALK gene rearrangements. https://clinicaltrials.gov/study/NCT02568267
- ClinicalTrials.gov. GLOBOTRK: entrectinib in young children with NTRK or ROS1 fusion CNS tumors. https://clinicaltrials.gov/study/NCT06528691