Drug · Small Molecule

Entrectinib

CI-DRUG-00000215Explore in graph →NCIt C114984 CHEMBL1983268 CIViC Approved

Regulatory

Approvals (8)

Each record names the authority, jurisdiction, indication text and status. A drug approved in one jurisdiction for one indication is not 'approved' in general.

openfdaRegulatory5 approval records · authority, jurisdiction and indication text as published.

Jurisdiction · authority	Cancer	Indication	Status	Approval date	Source
US FDA	Lung Non-Small Cell Carcinoma	Adult patients with ROS1- positive metastatic non-small cell lung cancer (NSCLC) as detected by an FDA-approved test.	approved	Oct 20, 2023	openfda
US FDA	Tumor-agnostic	Adult and pediatric patients older than 1 month of age with solid tumors that: have a neurotrophic tyrosine receptor kinase ( NTRK) gene fusion, as detected by an FDA-approved test 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. This indication is approved under accelerated approval based on tumor response rate and durability of response. Continued approval for this indication may be contingent upon verification and description of clinical benefit in the confirmatory trials.accelerated	approved	Oct 20, 2023	openfda
US FDA	—	Efficacy supplement 2023-10-20 (see label)	approved	Oct 20, 2023	openfda

Health Canada records are DIN-level: one row per marketed product (brand, strength, form). The Drug Product Database does not publish indications, so no cancer is stated for these rows, and a cancelled or dormant DIN is the status of that one product — not a withdrawal of the molecule.

Data updated 2 days agoSource updated unknown

Derived

Development pipeline

Most advanced stage across all cancers, then per top-level cancer reached through trial conditions or approval indications. Approval in any ingested jurisdiction outranks trial phase; counts are interventional studies.

Scope	Stage	Max phase	Active	Recruiting	Phase 3	Trials	Approvals	Jurisdictions	First approval	First trial
All cancers	Approved	Phase 3	17	8	6	28	8	CA, EU, US	Aug 15, 2019	Jul 28, 2014
Malignant Lung Neoplasm	Approved	Phase 3	5	1	3	6	3	EU, US	Aug 15, 2019	Nov 19, 2015
Malignant Thyroid Gland Neoplasm	Phase2	Phase 2	2	1	0	2	0	—	—	Nov 19, 2015
Malignant Breast Neoplasm	Phase2	Phase 2	1	0	0	5

Curated evidence

Clinical evidence (73)

CIViC items in which this therapy appears, grouped by cancer context, then molecular profile. 50 items per page.

civicCuratedShowing 1–50 of 73 evidence items · levels, directions and significance as curated at the source; each row links to its CIViC record.

Therapy	Cancer	Type	Level	Direction · significance	Rating (1–5)	Status	Evidence	Source
NTRK3 Fusion6
Entrectinib	Acute Myeloid Leukemia

Clinical trials

Trials with this intervention (33)

Most recently updated first, 50 per page.

clinicaltrialsPublishedShowing 1–33 of 33 studies · status and phase as posted by the registrant; each row links to the study record.

NCT	Title	Status	Phase	Enrollment (n)	Sponsor	Countries	Last update	Source
NCT03994796	Genetic Testing in Guiding Treatment for Patients With Brain Metastases	active not recruiting	Phase 2	50	Alliance for Clinical Trials in OncologyOTHER	1	Sep 28, 2026	clinicaltrials
NCT02650401	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(STARTRK-NG)

Molecule

Record

Kind: Small Molecule
Mechanism: Neurotrophic tyrosine kinase receptor inhibitor; Proto-oncogene tyrosine-protein kinase ROS inhibitor; ALK tyrosine kinase receptor inhibitor
Targets: 5 genes
UNII: L5ORF0AN1I
Aliases: Entrectinib, N-(5-(3,5-Difluorobenzyl)-1H-indazol-3-yl)-4-(4-methylpiperazin-1yl)-2-(tetrahydro-2H-pyran-4-ylamino)benzamide, NMS-E628, Rozlytrek, ROZLYTREK, RXDX 101, RXDX-101, RXDX101

Data updated 22 hours agoSource updated unknown

Identifiers

Codes (6)

Upstream identifiers kept as first-class codes; each links to its registry where a stable public URL exists.

System	Code	Label
ATC (WHO)	L01EX14	ENTRECTINIB
DIN (Health Canada)	02495007	ROZLYTREK

NTRK2 Fusion2
Entrectinib	Brain GlioblastomaALIAS	Predictive	C	Supports Sensitivity Response	1	accepted	EID12035 A 67-year-old male with a diagnosis of Glioblastoma multiforme (GBM), IDH-wildtype, WHO grade 4 underwent a craniotomy with gross total resection. A BCR::NTRK2 fusion (ex1::ex17) was detected by compr… (full text at CIViC) PMID 35673607 · Grogan et al., 2022 · Open in CIViC	civic
〃	Ganglioglioma	Predictive	C	Does Not Support Sensitivity Response	2	accepted	EID12053 In the STARTRK-NG (NCT02650401) phase 1/2 trial, a 10 year old patient with prior chemotherapy treatment who had Ganglioglioma in the Spine, with a tumor category of low grade glioma, and WHO histolog… (full text at CIViC) PMID 35395680 · Desai et al., 2022 · Open in CIViC	civic

NTRK1 Fusion4
Entrectinib	Colorectal Adenocarcinoma	Predictive	C	Supports Sensitivity Response	3	accepted	EID2960 A gene fusion between exon 11 of LMNA and exon 10 of NTRK1 was observed in a patient with metastatic colorectal cancer after therapy with first-line FOLFOX, second-line FOLFIRI/cetuximab, and third-li… (full text at CIViC) PMID 26546295 · Russo et al., 2016 · Open in CIViC	civic
〃	Malignant Colorectal NeoplasmCURATED_BROADER	Predictive	C	Supports Sensitivity Response	4	accepted	EID8900 After disease progression with no objective response to therapy, a 75-year-old with metastatic colorectal cancer that spread to the liver displayed elevated NTRK1 expression in both primary tumor and … (full text at CIViC) PMID 26563355 · Sartore-Bianchi et al., 2016 · Open in CIViC	civic
〃	Malignant NeoplasmALIAS	Predictive	D	Supports Sensitivity Response	3	accepted	EID10095 BaF3 cells were transduced with a number of NTRK fusions. IC50 values were measured following treatment with entrectinib: TPM3-NTRK1 (2.5nM), LMNA-NTRK1 (1.4nM), ETV6-NTRK1 (2.5nM), VCL-NTRK2 (4.3nM),… (full text at CIViC) PMID 26884591 · Drilon et al., 2016 · Open in CIViC	civic
〃	Malignant NeoplasmALIAS	Predictive	D	Supports Sensitivity Response	3	accepted	EID11354 In a head-to-head comparison of 4 NTRK inhibitors (larotrectinib, entrectinib, repotrectinib, and selitrectinib) with Ba/F3 cells harboring LMNA::NTRK1 with or without kinase domain mutations, the ent… (full text at CIViC) PMID 34625502 · Murray et al., 2021 · Open in CIViC	civic

ROS1 Fusion2
Entrectinib	Diffuse Midline Glioma, H3 K27-Altered	Predictive	C	Supports Sensitivity Response	3	accepted	EID11849 In a phase 1/2 trial of entrectinib in pediatric patients, tumors with fusions in NTRK, ROS1, or ALK had an overall response (ORR) of 57.7% (95% CI; 36.9-76.7). This included one patient (4 yo) with … (full text at CIViC) PMID 35395680 · Desai et al., 2022 · Open in CIViC	civic
〃	Low Grade Glioma	Predictive	C	Supports Sensitivity Response	1	accepted	EID11855 In a phase 1/2 trial of entrectinib in pediatric patients, tumors with fusions in NTRK, ROS1, or ALK had an overall response (ORR) of 57.7% (95% CI; 36.9-76.7). This included one patient (8 yo) with … (full text at CIViC) PMID 35395680 · Desai et al., 2022 · Open in CIViC	civic

NTRK3 Fusion3
Entrectinib	Infantile FibrosarcomaALIAS	Predictive	C	Supports Sensitivity Response	2	accepted	EID11859 In a phase 1/2 trial of entrectinib in pediatric patients, tumors with fusions in NTRK, ROS1, or ALK had an overall response (ORR) of 57.7% (95% CI; 36.9-76.7). This included a patient with infantile… (full text at CIViC) PMID 35395680 · Desai et al., 2022 · Open in CIViC	civic
〃	Lung Adenocarcinoma	Predictive	C	Supports Sensitivity Response	4	accepted	EID11099 A 45-year-old non-smoking female patient was diagnosed with a stage IV lung adenocarcinoma and magnetic resonance imaging showed multiple brain metastases. Targeted NGS analysis on the pleural biopsy … (full text at CIViC) PMID 36419889 · Lazzari et al., 2022 · Open in CIViC	civic
〃	Lung Non-Small Cell CarcinomaCURATED_BROADER	Predictive	C	Supports Sensitivity Response	2	accepted	EID10636 The paper mentions a 43-year-old-male with an EML4::NTRK3 rearrangement in metastatic non-small cell lung cancer initially treated with carboplatin/paclitaxel chemotherapy. Upon identification of an … (full text at CIViC) PMID 34625502 · Murray et al., 2021 · Open in CIViC	civic

ROS1 Fusion2
Entrectinib	Inflammatory Myofibroblastic Tumor	Predictive	C	Supports Sensitivity Response	2	accepted	EID11860 In a phase 1/2 trial of entrectinib in pediatric patients, tumors with fusions in NTRK, ROS1, or ALK had an overall response (ORR) of 57.7% (95% CI; 36.9-76.7). This included a patient with inflammat… (full text at CIViC) PMID 35395680 · Desai et al., 2022 · Open in CIViC	civic
〃	Inflammatory Myofibroblastic Tumor	Predictive	C	Supports Sensitivity Response	1	accepted	EID11862 In a phase 1/2 trial of entrectinib in pediatric patients, tumors with fusions in NTRK, ROS1, or ALK had an overall response (ORR) of 57.7% (95% CI; 36.9-76.7). This included a patient with myofibrob… (full text at CIViC) PMID 35395680 · Desai et al., 2022 · Open in CIViC	civic