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Drug

Entrectinib

Approved medicine
ClassALK tyrosine kinase receptor inhibitorResearchOngoing clinical research

Also known as Rozlytrek.

RxNorm2197862ChEMBLCHEMBL1983268ATCL01EX14UNIIL5ORF0AN1I
17
Active clinical trials
5
Protein targets
12
Regulatory events
Latest activity
beta

Recent clinical, regulatory, research and industry developments relating to this drug.

Label change: ENTRECTINIB (NDA212725)

Regulatory2026-10-01FDA

Label change: ENTRECTINIB (NDA218550)

Regulatory2026-10-01FDA

Randomized, Open Label, Multicenter, Phase III Study of Entrectinib Versus Crizotinib in Patients With Locally-Advanced or Metastatic Non-Small Cell Lung Cancer Harboring ROS1 Gene Rearrangements With and Without Central Nervous System Metastases

Clinical trial2026-09-30Primary completion · ClinicalTrials.gov

A Phase 1/2, Open-Label, Dose-Escalation And Expansion Study Of Entrectinib (Rxdx-101) In Pediatrics With Locally Advanced Or Metastatic Solid Or Primary CNS Tumors And/Or Who Have No Satisfactory Treatment Options

Clinical trial2026-09-23Results expected Q2 2027 · ClinicalTrials.gov

A Phase II/III Multicenter Study Evaluating the Efficacy and Safety of Multiple Targeted Therapies as Treatments for Patients With Advanced or Metastatic Non-Small Cell Lung Cancer (NSCLC) Harboring Actionable Somatic Mutations Detected in Blood (B-FAST: Blood-First Assay Screening Trial)

Clinical trial2026-09-03Results expected Q2 2027 · ClinicalTrials.gov

An Open-Label, Multicenter Extension Study in Patients Previously Enrolled in a Genentech and/or F. Hoffmann-La Roche Ltd Sponsored Study

Clinical trial2026-09-02Results expected Q1 2033 · ClinicalTrials.gov

An Open-Label, Multicenter, Global Phase 2 Basket Study of Entrectinib for the Treatment of Patients With Locally Advanced or Metastatic Solid Tumors That Harbor NTRK1/2/3, ROS1, or ALK Gene Rearrangements

Clinical trial2026-08-25Results expected Q2 2027 · ClinicalTrials.gov

NAUTIKA1: A Multicenter, Phase II, Neoadjuvant and Adjuvant Study of Multiple Therapies in Biomarker-selected Patients With Resectable Stages IB-III Non-small Cell Lung Cancer

Clinical trial2026-08-11Results expected Q4 2026 · ClinicalTrials.gov

A Phase I-III, Multicenter Study Evaluating the Efficacy and Safety of Multiple Therapies in Cohorts of Patients Selected According to Biomarker Status, With Locally Advanced, Unresectable, Stage III Non-Small Cell Lung Cancer

Clinical trial2026-08-05Results expected Q2 2030 · ClinicalTrials.gov

Tumor-agnostic Precision Immuno-oncology and Somatic Targeting Rational for You (TAPISTRY) Phase II Platform Trial

Clinical trial2026-08-05Results expected Q3 2032 · ClinicalTrials.gov

Label change: ENTRECTINIB (NDA212725)

Regulatory2024-01-26FDA

Indication expansion: ENTRECTINIB (NDA212725)

Regulatory2023-10-20FDA

Profile

Identifiers & mechanism

Canonical identifiers, marketed brand names and mechanism, resolved across RxNorm, ChEMBL and ATC.

Canonical name
Entrectinib
Aliases & brands
Rozlytrek
RxNorm CUI
2197862
ChEMBL ID
CHEMBL1983268
ATC codes
L01EX14
UNII
L5ORF0AN1I
Primary mechanism
ALK tyrosine kinase receptor inhibitor
Regulatory jurisdictions
fdaema

Pharmacology & targets

5 targets

Known molecular targets and mechanisms supported by curated pharmacology databases.

ALK tyrosine kinase receptor
ALK · Q9UM73
INHIBITORALK tyrosine kinase receptor inhibitor
Proto-oncogene tyrosine-protein kinase ROS
ROS1 · P08922
INHIBITORProto-oncogene tyrosine-protein kinase ROS inhibitor
High affinity nerve growth factor receptor
NTRK1 · P04629
INHIBITORNeurotrophic tyrosine kinase receptor inhibitor
BDNF/NT-3 growth factors receptor
NTRK2 · Q16620
INHIBITORNeurotrophic tyrosine kinase receptor inhibitor
NT-3 growth factor receptor
NTRK3 · Q16288
INHIBITORNeurotrophic tyrosine kinase receptor inhibitor

Regulatory timeline

12 events

The complete regulatory record, grouped by authority — approvals, safety advisories and label changes. Each authority shows its most recent events; expand one to read its full history.

Approval / market entry confirmed across FDA and EMA (2019-08-15 → 2020-07-31)
Earliest approval
2019-08-15
Latest approval
2023-10-20
Authorities
FDA · EMA
Total events
12
fdaU.S. Food and Drug Administration· 11 events
2026-10-01Label change
Label change: ENTRECTINIB (NDA218550)
Evidence ↗
2026-10-01Label change
Label change: ENTRECTINIB (NDA212725)
Evidence ↗
2024-01-26Label change
Label change: ENTRECTINIB (NDA212725)
Evidence ↗
emaEuropean Medicines Agency· 1 event
2020-07-31Conditional marketing authorisationMulti-authority
Conditional marketing authorisation: Rozlytrek (EMA)
Indication: Rozlytrek as monotherapy is indicated for the treatment of adult and paediatric patients 12 years of age and older with solid tumours expressing a neurotrophic tyrosine receptor… Show full indication

Rozlytrek as monotherapy is indicated for the treatment of adult and paediatric patients 12 years of age and older with solid tumours expressing a neurotrophic tyrosine receptor kinase (NTRK) gene fusion, who have a disease that is locally advanced, metastatic or where surgical resection is likely to result in severe morbidity, and who have not received a prior NTRK inhibitor who have no satisfactory treatment options. Rozlytrek as monotherapy is indicated for the treatment of adult patients with ROS1 positive, advanced non small cell lung cancer (NSCLC) not previously treated with ROS1 inhibitors.

Evidence ↗

Data from the U.S. Food and Drug Administration (U.S. Food and Drug Administration), public domain (CC0).

Contains information from the European Medicines Agency (European Medicines Agency), © EMA, reused under CC BY 4.0.

Clinical trials

29 trials

The current development programme across all trial phases — status mix, phase distribution and the late-stage studies shaping the evidence base.

Development programme
CLINICALTRIALS.GOV · LIVE REGISTRY
29
registered trials across all phases
LATEST COMPLETION 2024
17
Active studies
9
Recruiting
6
Late-stage (III+)
6
Completed
6
Discontinued
PHASE DISTRIBUTIONn = 29
Early Phase 11Phase 16Phase 1 / 22Phase 214Phase 2 / 33Phase 33

Late-stage studies

Phase III+ trials still open or recently active — where late-stage evidence is being generated.

An Open-Label, Multicenter Extension Study in Patients Previously Enrolled in a Genentech and/or F. Hoffmann-La Roche Ltd Sponsored Study

RecruitingPH IIIHoffmann-La Rochen=1002033

A Phase I-III, Multicenter Study Evaluating the Efficacy and Safety of Multiple Therapies in Cohorts of Patients Selected According to Biomarker Status, With Locally Advanced, Unresectable, Stage III Non-Small Cell Lung Cancer

Active, not recruitingPH IIIHoffmann-La Rochen=682030

DETERMINE (Determining Extended Therapeutic Indications for Existing Drugs in Rare Molecularly Defined Indications Using a National Evaluation Platform Trial): An Umbrella-Basket Platform Trial to Evaluate the Efficacy of Targeted Therapies in Rare Adult, Paediatric and Teenage/Young Adult (TYA) Cancers With Actionable Genomic Alterations, Including Common Cancers With Rare Actionable Alterations. Treatment Arm 03: Entrectinib in Adult, Paediatric and Teenage/Young Adult Patients With ROS1 Gene Fusion-Positive Cancers.

RecruitingPH II/IIICancer Research UKn=302029

DETERMINE (Determining Extended Therapeutic Indications for Existing Drugs in Rare Molecularly Defined Indications Using a National Evaluation Platform Trial): An Umbrella-Basket Platform Trial to Evaluate the Efficacy of Targeted Therapies in Rare Adult, Paediatric and Teenage/Young Adult (TYA) Cancers With Actionable Genomic Alterations, Including Common Cancers With Rare Actionable Alterations

RecruitingPH II/IIICancer Research UKn=8252029

Randomized, Open Label, Multicenter, Phase III Study of Entrectinib Versus Crizotinib in Patients With Locally-Advanced or Metastatic Non-Small Cell Lung Cancer Harboring ROS1 Gene Rearrangements With and Without Central Nervous System Metastases

Active, not recruitingPH IIIHoffmann-La Rochen=2172028

Recent completions

Trials that read out recently, adding to the completed evidence base.

A Phase II, Randomized, Active-Controlled, Multi-Center Study Comparing the Efficacy and Safety of Targeted Therapy or Cancer Immunotherapy Guided by Genomic Profiling Versus Platinum-Based Chemotherapy in Patients With Cancer of Unknown Primary Site Who Have Received Three Cycles of Platinum Doublet Chemotherapy

CompletedPH IIHoffmann-La Rochen=5292024

MyTACTIC: An Open-Label Phase II Study Evaluating Targeted Therapies in Patients Who Have Advanced Solid Tumors With Genomic Alterations or Protein Expression Patterns Predictive of Response

CompletedPH IIGenentech, Inc.n=2522024

An Open-Label, One Treatment, Four Group, Parallel Group Study to Investigate the Effect of Impaired Hepatic Function on the Pharmacokinetics of Entrectinib in Volunteers With Different Levels of Hepatic Function

CompletedPH IHoffmann-La Rochen=382021

A Phase 1, Multicenter, Open-Label Study of Oral Entrectinib (RXDX-101) in Adult Patients With Locally Advanced or Metastatic Cancer Confirmed to be Positive for NTRK1, NTRK2, NTRK3, ROS1, or ALK Molecular Alterations

CompletedPH IHoffmann-La Rochen=842020

A Randomized, Open-Label, Two Part Study to Explore the Performance of Entrectinib Prototype Mini-Tablet Formulations and the Effect of Drug Substance Particle Size On Entrectinib Bioavailability in Healthy Volunteers

CompletedPH IGenentech, Inc.n=312019

A Phase 1 Study to Evaluate the Potential Pharmacokinetic Interaction Between Entrectinib and Midazolam in Cancer Patients

CompletedPH IHoffmann-La Rochen=152018
References & data sources
  • RxNorm (U.S. National Library of Medicine) — drug identity
  • ChEMBL (EMBL-EBI) & UniProt — pharmacology and targets
  • ClinicalTrials.gov — clinical trials
  • Regulatory event sources are credited in the Regulatory Timeline above.