Drugs / Entrectinib
last change Jun 2026 re-read 2 minutes ago

Entrectinib

also known as NMS-E628 · Rozlytrek · RXDX-101

Small molecule targets ALK, NTRK1, NTRK2, NTRK3, ROS1 via inhibition

Developed for
cancer · non-small cell lung carcinoma · hematopoietic and lymphoid cell neoplasm · acute myeloid leukemia · breast cancer · cancer of unknown primary site · female breast carcinoma · glioma
+32 more · melanoma · metastatic malignant neoplasm · NTRK fusion positive cancer · soft tissue sarcoma · anaplastic large cell lymphoma · brain neoplasm · central nervous system neoplasm · cholangiocarcinoma · colorectal cancer · cutaneous melanoma · digestive system cancer · estrogen-receptor positive breast cancer · Her2-receptor negative breast cancer · invasive lobular breast carcinoma · lymphoproliferative syndrome · malignant pancreatic neoplasm · metastatic malignant neoplasm in the brain · metastatic neoplasm · neuroendocrine neoplasm · ovarian cancer · ovarian carcinoma · pancreatic ductal adenocarcinoma · pancreatic large cell neuroendocrine carcinoma · primary brain neoplasm · prostate carcinoma · renal cell carcinoma · salivary gland cancer · salivary gland carcinoma · sarcoma · thyroid gland carcinoma · thyroid gland papillary carcinoma · uveal melanoma
Investigated by
Hoffmann-La Roche · Genentech, Inc. · Oregon Health and Science University · OHSU Knight Cancer Institute · Cancer Research UK · Eli Lilly and Company
+87 more · Royal Marsden NHS Foundation Trust · University of Birmingham · University of Manchester · Alliance for Clinical Trials in Oncology · Amgen · Arkadiusz Z. Dudek, MD · AstraZeneca · Bayer · Boehringer Ingelheim · Bristol-Myers Squibb · Changhai Hospital · Clovis Oncology - Pharma and · Dalian Friendship Hospital Affiliated to Dalian Medical University · Dutch Cancer Society · Eisai Inc. · Fondazione per la Medicina Personalizzata · Foundation Medicine · Fred Hutchinson Cancer Center · Fudan University · Fujian Cancer Hospital · GlaxoSmithKline · Haukeland University Hospital · HealthPartners Institute Regions Cancer Care Center · Helse Fonna · Helse Forde · Helse Møre og Romsdal HF · Helse Nord-Trøndelag HF · Helse Stavanger HF · Helsinki University Central Hospital · Henan Cancer Hospital · Hospital of Southern Norway Trust · Hunan Provincial People's Hospital · Incyte Corporation · Innlandet Hospital Trust · Ipsen · Janssen, LP · Jiangsu Cancer Institute & Hospital · Jules Bordet Institute · Kazia Therapeutics Limited · Liaoning Cancer Hospital & Institute · Lovisenberg Diakonale Hospital · Merck Sharp & Dohme LLC · Midwest Melanoma Partnership · Mirati Therapeutics Inc. · National Cancer Institute (NCI) · Nordland Hospital · Northwell Health · Novartis · Novartis Pharmaceuticals · Oslo University Hospital · Ostfold Hospital Trust · Peking Union Medical College · Peking Union Medical College Hospital · Peking University Hospital of Stomatology · Peking University Shenzhen Hospital · Pfizer · Presage Biosciences · Roche Pharma AG · Ruijin Hospital · Shanghai 10th People's Hospital · Shanghai 6th People's Hospital · Shanghai General Hospital, Shanghai Jiao Tong University School of Medicine · Shanghai Ninth People's Hospital Affiliated to Shanghai Jiao Tong University · Shanxi Province Cancer Hospital · Sir Run Run Shaw Hospital · St. Jude Children's Research Hospital · St. Olavs Hospital · Stelvio for Life · Sun Yat-Sen Memorial Hospital of Sun Yat-Sen University · Sun Yat-sen University · Sykehuset Telemark · Taiho Oncology, Inc. · The Affiliated Hospital of Inner Mongolia Medical University · The First Affiliated Hospital of Anhui University of Chinese Medicine · all 93 on the full record

Regulatory milestones approvals, filings & regulatory actions · 3 recorded

MilestoneJurisdictionBrandIndicationDateSentence it was read from
Label expansion US (FDA) ROZLYTREK 2023-10-20 fda.gov
Approved · conditional EU (EMA) Rozlytrek 2020-07-31 europa.eu
Approved US (FDA) ROZLYTREK 2019-08-15 fda.gov

Trials 34 · a red edge is where a trial was stopped

PhaseRegistry idDatesIndicationSponsorStatusOutcome
Phase 01 trial
Phase 0 NCT05238831 Jan 2023 → May 2026 female breast carcinoma, ovarian carcinoma, pancreatic ductal adenocarcinoma, pancreatic large cell neuroendocrine carcinoma +2 OHSU Knight Cancer Institute Withdrawn No outcome recorded
Phase 18 trials
Phase 1 NCT05396859 Oct 2022 → Jun 2024 overdue acute myeloid leukemia OHSU Knight Cancer Institute Active not recruiting No outcome recorded
Phase 1 NCT03878524 Apr → Dec 2020 acute myeloid leukemia, atypical chronic myeloid leukemia, BCR-ABL1 negative, blast phase chronic myelogenous leukemia, BCR-ABL1 positive, castration-resistant prostate carcinoma +14 OHSU Knight Cancer Institute Terminated No outcome recorded
Phase 1 NCT04226833 Feb 2020 → Sep 2021 liver disorder Hoffmann-La Roche Completed No outcome recorded
Phase 1 NCT03961100 Jun → Aug 2019 cancer Genentech, Inc. Completed No outcome recorded
Phase 1 NCT03796260 Jan → Feb 2019 Genentech, Inc. Completed No outcome recorded
Phase 1 NCT03330990 Nov 2017 → Jul 2018 neoplasm Hoffmann-La Roche Completed No outcome recorded
Phase 1 NCT03056599 Dec 2016 → Jul 2021 soft tissue sarcoma Presage Biosciences Completed No outcome recorded
Phase 1 NCT02097810 Jul 2014 → Jun 2020 metastatic neoplasm Hoffmann-La Roche Completed No outcome recorded
Phase 1/21 trial
Phase 1/2 NCT04589832 Jan 2021 → Mar 2022 uveal melanoma Arkadiusz Z. Dudek, MD Terminated No outcome recorded
Phase 216 trials
Phase 2 NCT06528691 May 2026 → Nov 2027 expected central nervous system neoplasm, glioma St. Jude Children's Research Hospital Recruiting No outcome recorded
Phase 2 NCT06692491 Jan 2025 → Dec 2027 expected Peking University Shenzhen Hospital Not yet recruiting No outcome recorded
Phase 2 NCT06145308 Aug 2023 → Jul 2028 expected salivary gland carcinoma Peking Union Medical College Recruiting No outcome recorded
Phase 2 NCT05159245 Dec 2021 → Nov 2026 expected cancer, hematopoietic and lymphoid cell neoplasm Helsinki University Central Hospital Recruiting No outcome recorded
Phase 2 NCT06482086 Jun 2021 → Dec 2024 overdue thyroid gland carcinoma West China Hospital Recruiting No outcome recorded
Phase 2 NCT04817956 Apr 2021 → Mar 2040 expected metastatic malignant neoplasm Oslo University Hospital Recruiting No outcome recorded
Phase 2 NCT04589845 Jan 2021 → Sep 2032 expected cancer Hoffmann-La Roche Active not recruiting No outcome recorded
Phase 2 NCT04551495 Jan 2021 → Jan 2025 Her2-receptor negative breast cancer, estrogen-receptor positive breast cancer, invasive lobular breast carcinoma Jules Bordet Institute Unknown No outcome recorded
Phase 2 NCT04632992 Jan 2021 → Dec 2023 cancer of unknown primary site Genentech, Inc. Completed No outcome recorded
Phase 2 NCT04302025 Nov 2020 → Nov 2026 expected non-small cell lung carcinoma Genentech, Inc. Recruiting No outcome recorded
Phase 2/33 trials
Phase 2/3 NCT05770544 Nov 2025 → Oct 2029 expected brain neoplasm, cancer, glioma, hematopoietic and lymphoid cell neoplasm +2 Cancer Research UK Recruiting No outcome recorded
Phase 2/3 NCT05722886 Mar 2023 → Oct 2029 expected cancer, hematopoietic and lymphoid cell neoplasm Cancer Research UK Recruiting No outcome recorded
Phase 2/3 NCT03178552 Sep 2017 → Oct 2026 expected non-small cell lung carcinoma Hoffmann-La Roche Active not recruiting No outcome recorded
Phase 33 trials
Phase 3 NCT05862285 Jun 2023 → Mar 2033 expected cancer Hoffmann-La Roche Recruiting No outcome recorded
Phase 3 NCT05170204 Nov 2022 → Jun 2030 expected non-small cell lung carcinoma Hoffmann-La Roche Active not recruiting No outcome recorded
Phase 3 NCT04603807 Sep 2021 → Jun 2028 expected non-small cell lung carcinoma Hoffmann-La Roche Active not recruiting No outcome recorded
Phase 41 trial
Phase 4 NCT06195228 Jan 2020 → Dec 2026 expected Fudan University Recruiting No outcome recorded
Phase not stated1 trial
NCT03066661 Hoffmann-La Roche No longer available No outcome recorded
Also used as a comparator or background therapy in 1 trial
PhaseRegistry idDatesIndicationSponsorStatusOutcome
Phase 1/2 NCT02650401 Comparator May 2016 → Jun 2026 overdue cancer, central nervous system neoplasm Hoffmann-La Roche Active not recruiting No outcome recorded

Press releases naming this drug 9 releases

DateIssuerRelease
2022-06-09 Roche Global Development U.S. FDA approves Foundation Medicine’s FoundationOne®CDx as a companion diagnostic for Roche’s Rozlytrek® (entrectinib) roche.com
2020-08-03 Roche Global Development Rozlytrek, Roche’s first tumour-agnostic therapy, approved in Europe for people with NTRK fusion-positive solid tumours and for people with ROS1-positive advanced non-small cell lung cancer roche.com
2020-05-29 Roche Global Development CHMP recommends EU approval of Roche’s Rozlytrek for people with NTRK fusion-positive solid tumours and for people with ROS1-positive, advanced non-small cell lung cancer roche.com
2019-08-16 Roche Global Development FDA approves Roche’s RozlytrekTM (entrectinib) for people with ROS1-positive, metastatic non-small cell lung cancer and NTRK gene fusion-positive solid tumours roche.com
2019-06-18 Roche Global Development Japan becomes the first country to approve Roche’s personalised medicine Rozlytrek roche.com
2019-05-16 Roche Global Development Roche's personalised medicine entrectinib shrank tumours harbouring NTRK, ROS1 or ALK gene fusions in children and adolescents roche.com
2019-02-19 Roche Global Development FDA grants Priority Review to Roche's personalised medicine entrectinib roche.com
2018-10-21 Roche Global Development Roche's investigational personalised medicine entrectinib shrank tumours in people with NTRK fusion-positive solid tumours roche.com
2018-09-24 Roche Global Development Roche's investigational medicine entrectinib showed a durable response of more than two years in people with a specific type of lung cancer roche.com

Evidence & citations 12 cited values

Every value below carries the sentence it was read from. 38 sources stand behind the page.

FieldValueCited text
Known as entrectinib entrectinib used outside of indication, based on biomarker” NCT04817956
34

entrectinib 600 mg orally once daily” NCT06145308

NCT06692491

NCT05722886

NCT03961100

NCT04603807

NCT04589832

NCT06528691

NCT04302025

NCT06482086

NCT03878524

NCT05159245

NCT04551495

NCT03330990

NCT05862285

NCT02097810

NCT03066661

NCT04589845

NCT03994796

NCT03498521

NCT02568267

NCT02650401

NCT02925234

NCT04226833

NCT05170204

NCT06195228

NCT05396859

NCT05770544

NCT03178552

NCT04632992

NCT02587650

NCT03056599

NCT03796260

NCT04591431

NCT05238831

Known as NMS-E628 ChEMBL registry synonym — accepted as the source's own label CHEMBL1983268
Known as Rozlytrek ChEMBL registry synonym — accepted as the source's own label CHEMBL1983268
Known as RXDX-101 “Entrectinib (RXDX-101) is an orally available inhibitor of the tyrosine kinases TrkA (coded by the gene NTRK1), TrkB (coded by the gene NTRK2), TrkC (coded by the gene NTRK3),...” NCT02097810
Action Inhibit “Entrectinib (RXDX-101) is an orally available inhibitor” NCT02097810
Modality Small molecule “Entrectinib (RXDX-101) is an orally available tyrosine kinase inhibitor, including TrkA.” PMID 26565381 Dec 2015
Route Oral “received entrectinib orally at a dose of at least 600 mg once per day” PMID 31838007 Dec 2019
Target ALK “Entrectinib (RXDX-101) is an orally available inhibitor of the tyrosine kinases TrkA (coded by the gene NTRK1), TrkB (coded by the gene NTRK2), TrkC (coded by the gene NTRK3),...” NCT02097810
Target NTRK1 “Entrectinib (RXDX-101) is an orally available inhibitor of the tyrosine kinases TrkA (coded by the gene NTRK1), TrkB (coded by the gene NTRK2), TrkC (coded by the gene NTRK3),...” NCT02097810
Target NTRK2 “Entrectinib (RXDX-101) is an orally available inhibitor of the tyrosine kinases TrkA (coded by the gene NTRK1), TrkB (coded by the gene NTRK2), TrkC (coded by the gene NTRK3),...” NCT02097810
Target NTRK3 “Entrectinib (RXDX-101) is an orally available inhibitor of the tyrosine kinases TrkA (coded by the gene NTRK1), TrkB (coded by the gene NTRK2), TrkC (coded by the gene NTRK3),...” NCT02097810
Target ROS1 “Entrectinib (RXDX-101) is an orally available inhibitor of the tyrosine kinases TrkA (coded by the gene NTRK1), TrkB (coded by the gene NTRK2), TrkC (coded by the gene NTRK3),...” NCT02097810