# Entrectinib

Source: https://onco.cc/drugs/entrectinib/  
OnCo record `entrectinib` (Treatment). Data CC BY-NC 4.0, attribute "Data from OnCo (onco.cc)"; commercial use needs a licence.

## TL;DR

Entrectinib (Rozlytrek) is a pill for NTRK-fusion cancers and ROS1 lung cancer that reaches brain metastases.

## Summary

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.

## Fields

- Kind: Treatment
- Status: approved
- Last checked: 2026-09-08
- Tags: gap-fill
- Brand: Rozlytrek
- Modality: Small-molecule TRK/ROS1/ALK TKI (CNS-penetrant)
- Mechanism: Multikinase inhibitor of TRKA/B/C, ROS1 and ALK designed to cross the blood-brain barrier.
- Approvals: 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; England (NICE) 2020: NTRK fusion-positive solid tumours, including colorectal cancer; England (NICE) 2020: ROS1-positive advanced non-small-cell lung cancer in patients who have not had a ROS1 inhibitor

## Notes

- Pancreatic cancer: entrectinib's tumour-agnostic NTRK indication (FDA accelerated approval; EU marketing authorisation 31 July 2020) applies to the rare NTRK fusion-positive pancreatic tumours, but in England the Cancer Drugs Fund route closed with the terminated TA1118 in January 2026, leaving larotrectinib (TA630) as the funded option.

## Sources

- Wikipedia: https://en.wikipedia.org/wiki/Entrectinib
- Label (DailyMed): https://dailymed.nlm.nih.gov/dailymed/search.cfm?labeltype=all&query=entrectinib
- NICE TA1118: entrectinib for NTRK fusion-positive solid tumours, terminated appraisal (7 January 2026): https://www.nice.org.uk/guidance/ta1118
- NICE TA644 (12 August 2020), replaced: https://www.nice.org.uk/guidance/ta644
- EMA Rozlytrek product page: https://www.ema.europa.eu/en/medicines/human/EPAR/rozlytrek
- NICE TA643: entrectinib for treating ROS1-positive advanced non-small-cell lung cancer: https://www.nice.org.uk/guidance/ta643

## Connected records

- biomarkers: [NTRK1/2/3 gene fusion](https://onco.cc/biomarkers/ntrk-fusion/), [ROS1 fusion (ROS1-positive)](https://onco.cc/biomarkers/ros1-fusion/)
- cancers: [Colorectal cancer](https://onco.cc/cancers/colorectal/), [Gallbladder cancer](https://onco.cc/cancers/gallbladder/), [Inflammatory myofibroblastic tumour (IMT)](https://onco.cc/cancers/inflammatory-myofibroblastic-tumour/), [KRAS wild-type pancreatic ductal adenocarcinoma](https://onco.cc/cancers/kras-wild-type-pdac/), [Lung cancer (all types)](https://onco.cc/cancers/lung-cancer/), [Metastatic cancer (cancer that has spread)](https://onco.cc/cancers/metastatic-cancer/), [Non-small-cell lung cancer](https://onco.cc/cancers/nsclc/), [NTRK fusion-positive non-small-cell lung cancer](https://onco.cc/cancers/ntrk-fusion-nsclc/), [Paediatric high-grade glioma (excluding diffuse midline glioma)](https://onco.cc/cancers/paediatric-high-grade-glioma/), [Pancreatic ductal adenocarcinoma](https://onco.cc/cancers/pancreatic/), [Papillary thyroid cancer](https://onco.cc/cancers/papillary-thyroid-cancer/), [ROS1-positive non-small-cell lung cancer](https://onco.cc/cancers/ros1-positive-nsclc/), [Salivary gland cancers](https://onco.cc/cancers/salivary-gland/), [Sarcomas (soft tissue, bone, GIST)](https://onco.cc/cancers/sarcoma/), [Secretory carcinoma of the breast](https://onco.cc/cancers/secretory-carcinoma-breast/), [Uterine sarcoma](https://onco.cc/cancers/uterine-sarcoma/)
- technologies: [Small-molecule kinase inhibitors](https://onco.cc/technologies/kinase-inhibitors/)
- targets: [ALK](https://onco.cc/targets/alk/), [NTRK](https://onco.cc/targets/ntrk/), [ROS1](https://onco.cc/targets/ros1/)
- companies: [Roche / Genentech](https://onco.cc/companies/roche-genentech/)
- terms: [Blood-brain barrier (BBB)](https://onco.cc/terms/blood-brain-barrier/), [Colorectal cancer drugs in England: what NICE has recommended](https://onco.cc/terms/colorectal-uk-drug-access/), [Gene fusion](https://onco.cc/terms/gene-fusion/), [Lung cancer drugs in England: what NICE has recommended](https://onco.cc/terms/lung-uk-drug-access/), [Pancreatic cancer drugs in England: NICE appraisals and the Cancer Drugs Fund (September 2026)](https://onco.cc/terms/pancreatic-cancer-uk-drug-access/), [Tumour-agnostic (tissue-agnostic) approval](https://onco.cc/terms/tumour-agnostic/)
- trials: [A Study Evaluating the Efficacy and Safety of Multiple Therapies in Cohorts of Participants With Locally Advanced, Unresectable, Stage III Non-Small C](https://onco.cc/trials/nct05170204/), [A Study of Multiple Therapies in Biomarker-selected Participants With Resectable Stages IB-III Non-small Cell Lung Cancer (NSCLC)](https://onco.cc/trials/nct04302025/), [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](https://onco.cc/trials/nct04603807/), [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](https://onco.cc/trials/nct02568267/), [CUPISCO](https://onco.cc/trials/cupisco/), [DETERMINE](https://onco.cc/trials/determine-trial/), [PROFILE 1001 ROS1 expansion cohort](https://onco.cc/trials/profile-1001-ros1/), [Study Of Entrectinib (Rxdx-101) in Children and Adolescents With Locally Advanced Or Metastatic Solid Or Primary CNS Tumors And/Or Who Have No Satisfactory Treatment Options](https://onco.cc/trials/nct02650401/), [Tumor-agnostic Precision Immuno-oncology and Somatic Targeting Rational for You (TAPISTRY) Platform Study](https://onco.cc/trials/nct04589845/)
- key papers: [Entrectinib in NTRK fusion-positive solid tumours: integrated analysis of three trials](https://onco.cc/key-papers/paper-doebele-entrectinib-ntrk-lancet-oncol-2020/), [Entrectinib in ROS1 fusion-positive non-small-cell lung cancer: integrated analysis of three trials](https://onco.cc/key-papers/paper-drilon-entrectinib-ros1-lancet-oncol-2020/), [Metastatic Pancreatic Cancer: ASCO Guideline Update](https://onco.cc/key-papers/paper-asco-metastatic-pancreatic-cancer-guideline-update-jco-2020/)
- institutions: [University of Colorado Cancer Center](https://onco.cc/institutions/colorado-cancer-center/)
- pathways: [Pancreatic cancer (KEGG map)](https://onco.cc/pathways/pancreatic-cancer-signalling/), [Receptor tyrosine kinase activation](https://onco.cc/pathways/rtk-activation/), [Thyroid cancer (KEGG map)](https://onco.cc/pathways/thyroid-cancer-signalling/)
- roadmaps: [Targeted therapy roadmap: imatinib → designed for resistance → the undruggable drivers fall](https://onco.cc/roadmaps/targeted-therapy-roadmap/)

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JSON: https://onco.cc/api/v1/entities/entrectinib.json