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entrectinib

Trade name: Rozlytrek

Small moleculeapprovedOrphan Drug FDABreakthrough Therapy FDA

Approved

Aug 15, 2019

Entrectinib (previously known as RXDX-101, NMS-E628) is an investigational drug, potent inhibitor of ALK, ROS1, and, importantly, of TRK family kinases, which shows promise for therapy of tumors bearing oncogenic forms of these proteins. Entrectinib (RXDX-101) is a selective inhibitor for all three Trk receptor tyrosine kinases encoded by the three NTRK genes, as well as the ROS1 and ALKreceptor tyrosine kinases.This investigational drug is active at low nanomolar concentrations, allowing for once-daily oral administration to patients whose tumors have been shown to have gene rearrangements in NTRK, ROS1, or ALK. Nerviano Medical Sciences, the original sponsor for entrectinib (formerly referred to as NMS-1191372), initiated the first-in-human Phase 1 study ALKA-372-001 in Italy in October 2012. The study is currently ongoing in Italy. Entrectinib is currently being tested in a global phase 2 basket clinical trial called STARTRK-2. In the U.S., entrectinib has orphan drug designation and rare pediatric disease designation for the treatment of neuroblastoma and orphan drug designation for treatment of TrkA-, TrkB-, TrkC-, ROS1- and ALK-positive non-small cell lung cancer (NSCLC) and metastatic colorectal cancer (mCRC). — NCATS

Clinical trial activity

42 trials · 53 clinical orgs · 2 marketing orgs

Phase 1
16
Phase 2
24
Phase 3
5
Phase 4
1

Earliest trial started Jun 1, 2014 (NCT02097810)

Timeline

2010s

  1. Jan 1, 2014

    Earliest Phase 1 Sponsor(trial)

  2. Jan 1, 2015

    Earliest Phase 2 Sponsor(trial)

  3. Feb 3, 2015

    Orphan Drug Designation

  4. Aug 15, 2019

    Roche — Earliest FDA Approval

  5. Aug 15, 2019

    Genentech — Marketing Organization

  6. Aug 15, 2019

    Roche — NDA Organization

2020s

  1. Jan 1, 2021

    Roche — Earliest Phase 3 Sponsor(trial)

Indications

Approved for

Studied for

Mechanism of action

Approval history

  • approvedPriority reviewAcceleratedBreakthroughAug 15, 2019

Chemistry & pharmacology

Loading structure…

SMILES

CN1CCN(CC1)C2=CC=C(C(=O)NC3=NNC4=CC=C(CC5=CC(F)=CC(F)=C5)C=C34)C(NC6CCOCC6)=C2
Mol. weight
560.6375 g/mol
Lipinski Ro5
2 violation(s)
Rule of 3
No
Chirality
Achiral Molecule
Inorganic
No
Polymer
No
Delivery
Oral
Availability
Prescription Only

Oral

Yes

Parenteral

No

Topical

No

Sources

Also known as

  • entrectinib
  • entrectinib
  • entrectinib
  • entrectinib
  • entrectinib
  • nms-e628
  • nms-e628
  • nms-e628
  • rxdx-101
  • rxdx-101
  • rxdx-101

Clinical trials

NCT IDPhaseStart dateSponsor(s)
NCT07223671Phase 1Nov 12, 2025Bristol-Myers Squibb
NCT06692491Phase 2Jan 1, 2025Peking University
NCT06528691Phase 2Dec 31, 2024Roche, St. Jude Children's Hospital
NCT06315010Phase 2Nov 30, 2024Medical University of Vienna, MedSIR
NCT06552234Phase 2Oct 31, 2024Centre Hospitalier Intercommunal de Toulon La Seyne sur Mer, Groupe Francais De Pneumo-Cancerologie, Groupe Français de Pneumo-Cancérologie, University of Lyon
NCT06493409Phase 1Aug 26, 2024Bristol-Myers Squibb
NCT06408168Phase 2Aug 8, 2024University of Texas at Houston
NCT06352528Phase 1Apr 29, 2024Bristol-Myers Squibb
NCT06140836Phase 3Jan 15, 2024Bristol-Myers Squibb, Zai Lab Pty. Ltd.
NCT05770544Phase 2/Phase 3 (Phase 3)Dec 31, 2023Cancer Research UK, Roche, Royal Marsden Hospital NHS Trust, The Christie NHS Foundation Trust, University of Birmingham, University of Manchester
NCT06145308Phase 2Dec 1, 2023Peking University
NCT05722886Phase 2/Phase 3 (Phase 3)Mar 1, 2023Cancer Research UK, Roche, Royal Marsden Hospital NHS Trust, The Christie NHS Foundation Trust, University of Birmingham, University of Manchester
NCT05238831Phase 2Dec 1, 2022Genentech, OHSU Knight Cancer Institute, Oregon Health and Science University
NCT05170204Phase 3Nov 1, 2022Roche
NCT05396859Phase 1Oct 28, 2022Genentech, OHSU Knight Cancer Institute, Oregon Health and Science University, Otsuka
NCT05828277Phase 1Jul 28, 2022Bristol-Myers Squibb, Turning Point Therapeutics
NCT05159245Phase 2Dec 10, 2021University of Helsinki
NCT05004116Phase 1/Phase 2 (Phase 2)Aug 9, 2021Memorial Sloan-Kettering Cancer Center
NCT06482086Phase 2Jun 1, 2021Sichuan University
NCT04772235Phase 1Apr 30, 2021Institute of Oncology Dr. Rosell (IOR), Turning Point Therapeutics
Showing 20 of 42 trials
Page 1 / 3

Organizations

Research & Development (53)

OrganizationOrg typeTrialsAs lead sponsorPhasesEarliest year
RocheFor profit14632017
GenentechFor profit9522019
Bristol-Myers SquibbFor profit6532022
Ignyta, Inc.For profit4432014
Turning Point TherapeuticsFor profit3222019
Cancer Research UKAcademic/Hospital2212023
OHSU Knight Cancer InstituteAcademic/Hospital2222022
Oregon Health and Science UniversityAcademic/Hospital2022022
Peking UniversityAcademic/Hospital2112023
Royal Marsden Hospital NHS TrustAcademic/Hospital2012023
The Christie NHS Foundation TrustAcademic/Hospital2012023
University of BirminghamAcademic/Hospital2012023
University of ManchesterAcademic/Hospital2012023
Anhui College of Traditional Chinese MedicineAcademic/Hospital1012020
Central South UniversityAcademic/Hospital1012020
Centre Hospitalier Intercommunal de Toulon La Seyne sur MerAcademic/Hospital1112024
Changhai HospitalAcademic/Hospital1012020
Chinese Academy of Medical SciencesAcademic/Hospital1012020
Dalian Medical UniversityAcademic/Hospital1012020
Foundation MedicineFor profit1012018
53 organizations
Page 1 / 3

Marketing (2)

OrganizationOrg typeRelationshipDate
GenentechFor profitMKTGAug 15, 2019
RocheFor profitNDAAug 15, 2019