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Entrectinib (Rozlytrek) is a pill for NTRK-fusion cancers and ROS1 lung cancer that reaches brain metastases.
Entrectinib is a multikinase inhibitor of TRKA, TRKB, TRKC, ROS1 and ALK that was designed to cross the blood-brain barrier. It is a tumour-agnostic drug for solid tumours with NTRK gene fusions, which occur across salivary gland tumours, sarcomas, colorectal cancer and many other types, and for ROS1-positive metastatic NSCLC. An integrated analysis of STARTRK-2, STARTRK-1 and ALKA showed a 57% response rate in NTRK-fusion tumours and 77% in ROS1-positive NSCLC, with activity against brain metastases. Japan approved it in June 2019 for NTRK-fusion tumours, the US in August 2019 for both indications and the EU in 2020; the paediatric label was extended in 2023 to infants from one month of age. Weight gain, dizziness, cognitive effects and cardiac failure are class-related TRK toxicities. Entrectinib treats cancers by their fusion gene rather than their organ of origin.
Multikinase inhibitor of TRKA/B/C, ROS1 and ALK designed to cross the blood-brain barrier. Connects to NTRK, ROS1 and ALK.
1.Entrectinib slips into a pocket on NTRK.
Oral, self-administered, so it is a Part D drug: covered through a stand-alone Part D plan or Medicare Advantage drug benefit, usually on the specialty tier with 25 to 33% coinsurance until the annual cap ($2,000 in 2025, $2,100 in 2026).
Covered for FDA-labelled and NCCN-listed uses, but almost always behind prior authorisation confirming diagnosis, biomarker and line of therapy; dispensed through a specialty pharmacy. NTRK fusion or ROS1 rearrangement by an approved test.
Part D out-of-pocket capped at $2,000 (2025) / $2,100 (2026). Medicare patients cannot use manufacturer co-pay cards; charity funds (PAN, HealthWell, CancerCare) and the Extra Help subsidy are the routes.
Sources: Medicare.gov: Drug coverage (Part D) · Medicare.gov: Costs for Medicare drug coverage (annual out-of-pocket cap). Not medical or financial advice; verify with your plan.
Sources: NICE TA643 · NHS England Cancer Drugs Fund list · SMC advice: entrectinib. Funding decisions are indication-specific and change monthly; verify with NICE and your treating team.
Treatment of adult and pediatric patients 12 years of age and older with solid tumors that have a neurotrophic tyrosine receptor kinase (NTRK) gene fusion without a known acquired resistance mutation, are metastatic or where surgical resection is likely to result in severe morbidity, and have progressed following treatment or have no satisfactory alternative therapy . *
Accelerated approval on a surrogate endpoint; the confirmatory requirement was still open 7.1 years later, when the FDA's table was read. source
Formulation: Adult and pediatric patients older than 1 month of age with solid tumors that have a neurotrophic tyrosine receptor kinase (NTRK) gene fusion without a known acquired resistance mutation as detected by an FDA-approved test, are metastatic or where surgical resection is likely to result in severe morbidity and have progressed following treatment or have no satisfactory alternative therapy .
Accelerated approval on a surrogate endpoint; the confirmatory requirement was still open 2.9 years later, when the FDA's table was read. source
| Region | Year | Indication |
|---|---|---|
| JP | 2019 | NTRK fusion solid tumours |
| US | 2019 | ROS1-positive metastatic NSCLC; NTRK fusion solid tumours (≥12 years, extended to ≥1 month 2023) |
| EU | 2020 | Same |
| UK | 2020 | NTRK fusion-positive solid tumours: NICE TA644 (12 August 2020) recommended entrectinib within the Cancer Drugs Fund; it was replaced by TA1118 (terminated appraisal, 7 January 2026) because the company did not make a submission, and only people already on treatment continue · https://www.nice.org.uk/guidance/terminated/ta1118 |
| England (NICE) | 2020 | NTRK fusion-positive solid tumours, including colorectal cancer · TA644, published 12 August 2020, withdrawn: replaced by TA1118, which NICE terminated on 7 January 2026 with no complete evidence submission. People already treated through the Cancer Drugs Fund may continue. |
| England (NICE) | 2020 | ROS1-positive advanced non-small-cell lung cancer in patients who have not had a ROS1 inhibitor · TA643, published 12 August 2020, subject to the commercial arrangement. This is a separate appraisal from the tumour-agnostic NTRK guidance. |
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Entrectinib is an approved tumour-agnostic TRK inhibitor with an advantage in patients with brain metastases, and it is also approved for ROS1-positive lung cancer.
Entrectinib is a first-line ROS1 inhibitor with brain activity, preferred over crizotinib when brain metastases are present, though repotrectinib and taletrectinib now offer longer control.
The document that made biomarker testing part of routine pancreatic cancer care in the United States; the 2018 version it built on fixed the second-line chemotherapy sequence still used in most guidelines.
Query for this drug: (TITLE:"Entrectinib" OR ABSTRACT:"Entrectinib" OR TITLE:"Rozlytrek" OR ABSTRACT:"Rozlytrek") AND (cancer OR tumor OR tumour OR oncology OR carcinoma OR lymphoma OR leukemia OR leukaemia OR myeloma OR sarcoma OR melanoma OR glioma). Results are unfiltered search hits about Entrectinib, not a curated reading list.
Shares Secretory carcinoma of the breast, Colorectal cancer drugs in England: what NICE has recommended, University of Colorado Cancer Center, Metastatic Pancreatic Cancer: ASCO Guideline Update.
Shares PROFILE 1001 ROS1 expansion cohort, ROS1 fusion (ROS1-positive), Thyroid cancer (KEGG map), NTRK1/2/3 gene fusion.
Shares A Study Evaluating the Efficacy and Safety of Multiple Therapies in Cohorts of Participants With Locally Advanced, Unresectable, Stage III Non-Small C, A Study of Multiple Therapies in Biomarker-selected Participants With Resectable Stages IB-III Non-small Cell Lung Cancer (NSCLC), Tumor-agnostic Precision Immuno-oncology and Somatic Targeting Rational for You (TAPISTRY) Platform Study, DETERMINE.
Shares A Study to Compare the Efficacy and Safety of Entrectinib and Crizotinib in Participants With Advanced or Metastatic ROS1 Non-small Cell Lung Cancer (NSCLC) With and Without Central Nervous System (CNS) Metastases, PROFILE 1001 ROS1 expansion cohort, ROS1 fusion (ROS1-positive), University of Colorado Cancer Center.
Shares PROFILE 1001 ROS1 expansion cohort, Basket Study of Entrectinib (RXDX-101) for the Treatment of Patients With Solid Tumors Harboring NTRK 1/2/3 (Trk A/B/C), ROS1, or ALK Gene Rearrangeme, NTRK fusion-positive non-small-cell lung cancer, ROS1-positive non-small-cell lung cancer.
Shares ROS1 fusion (ROS1-positive), NTRK1/2/3 gene fusion, Papillary thyroid cancer, Tumour-agnostic (tissue-agnostic) approval.
Shares ROS1 fusion (ROS1-positive), ROS1, Gene fusion, ALK.
Shares ROS1 fusion (ROS1-positive), NTRK1/2/3 gene fusion, Tumour-agnostic (tissue-agnostic) approval, Gene fusion.