Skip to content

Entrectinib

FDA-approved product (capsule, oral), marketed as Rozlytrek.

Registered studies
46
Lab records
0
Pathogens at ≥40%
3 of 4

Chemical structure

Chemical structure of Entrectinib
A drawing shows what the molecule is, not what it does.

Existing / approved use

Documented · FDA, WHO, ChEMBL

Approved for

  • Cancer
  • Neoplasm
  • Non-small cell lung carcinoma

Indications ChEMBL records as approved, from FDA and DailyMed labels. Label ↗

WHO therapeutic group
Other protein kinase inhibitors
Anti-infective classification
Not classified as an anti-infective.

Repurposing investigation

This medicine is being investigated here for AI-predicted antimicrobial activity against MRSA, E. coli and M. tuberculosis. It was surfaced computationally for further investigation; it is not an established treatment for these infections.

AI-predicted activity

AI prediction · nothing measured
  • MRSA54.8% AI-predicted activityAt or above the ≥40% mark this site uses to surface candidates.
  • E. coli50.9% AI-predicted activityAt or above the ≥40% mark this site uses to surface candidates.
  • K. pneumoniae39.6% AI-predicted activityBelow the ≥40% mark this site uses to surface candidates.
  • M. tuberculosis54.1% AI-predicted activityAt or above the ≥40% mark this site uses to surface candidates.

A model’s estimate of laboratory activity against each pathogen species. It is not clinical effectiveness.

Evidence

Clinical and experimental

Documented evidence

Clinical

46registered studies name this medicine, for any condition. See them below.

Experimental

No evidence found

No laboratory measurement against the four pathogens in the ChEMBL records loaded here.

Docking

Computational · nothing measured

Dihydrofolate reductase ↗ (E. coli)

-10.0 kcal/mol

0better fit →-12

KPC-2 carbapenemase ↗ (K. pneumoniae)

-8.0 kcal/mol

0better fit →-12

Enoyl-ACP reductase (InhA) ↗ (M. tuberculosis)

-11.6 kcal/mol

0better fit →-12

Dihydrofolate reductase ↗ (MRSA)

-10.6 kcal/mol

0better fit →-12

AutoDock Vina, one experimentally solved protein per pathogen. This project’s screening target is -7.0 kcal/mol, its own mark rather than a universal cutoff. A docking score is a structural hypothesis, not proof of binding, and requires experimental validation.

Other medicines to investigate

AI prediction · nothing measured

Other repurposing candidates: approved medicines besides Entrectinib with AI-predicted activity ≥40% against the chosen pathogen, leaving out existing antimicrobials. They are computational candidates for further investigation, not alternatives and not recommendations.

Sorted by AI-predicted activity, high to low. The order is not a ranking of which medicine is better.

Registered studies

A registration describes a study; it does not establish a positive result.

  • A Retrospective and Prospective Real-world Study of Molecular Typing in the Treatment of Advanced Thyroid Cancer

    NCT06195228 · start 2020-01-01

    Registered record
    Registry ID
    NCT06195228
    Conditions
    Advanced Thyroid Cancer Patients Who Received Target Therapy
    Interventions
    dabrafenib plus trametinib with or without PD-1 antibody; entrectinib or larotrectinib with or without anti-PD-1 antibdoy; pralsetinib or selpercatinib with or without anti-PD-1 antibdoy; anlotinib or anlotinib plus anti-PD-1 antibody; lenvatinib plus anti-PD-1 antibody; Other Targets: precise treatment based on the target
    Study type
    INTERVENTIONAL
    Phase
    Phase 4
    Registry status
    Recruiting
    Start
    2020-01-01
    Completion
    2028-12-31
    Enrolment
    800

    As stored from ClinicalTrials.gov. Registration describes a study; it does not mean the study worked.

    ConditionAdvanced Thyroid Cancer Patients Who Received Target Therapy
    Interventiondabrafenib plus trametinib with or without PD-1 antibody; entrectinib or larotrectinib with or without anti-PD-1 antibdoy; pralsetinib or selpercatinib with or without anti-PD-1 antibdoy; anlotinib or anlotinib plus anti-PD-1 antibody +2 more
    PhasePhase 4
    Registry statusRecruiting
  • Genetic Testing in Guiding Treatment for Patients With Brain Metastases

    NCT03994796 · start 2019-10-17

    Registered record
    Registry ID
    NCT03994796
    Conditions
    CDK Gene Mutation; Metastatic Malignant Neoplasm in the Brain; Metastatic Malignant Solid Neoplasm; NTRK Family Gene Mutation; PI3K Gene Mutation; ROS1 Gene Mutation; KRAS G12C Mutation
    Interventions
    Abemaciclib; PI3K Inhibitor paxalisib; Entrectinib; Adagrasib
    Study type
    INTERVENTIONAL
    Phase
    Phase 2
    Registry status
    Active not recruiting
    Start
    2019-10-17
    Completion
    2028-06
    Enrolment
    50

    As stored from ClinicalTrials.gov. Registration describes a study; it does not mean the study worked.

    ConditionCDK Gene Mutation; Metastatic Malignant Neoplasm in the Brain; Metastatic Malignant Solid Neoplasm; NTRK Family Gene Mutation +3 more
    InterventionAbemaciclib; PI3K Inhibitor paxalisib; Entrectinib; Adagrasib
    PhasePhase 2
    Registry statusActive not recruiting
  • A Performance and Bioavailability Study of Entrectinib in Healthy Volunteers.

    NCT03961100 · start 2019-06-06

    Registered record
    Registry ID
    NCT03961100
    Conditions
    Solid Tumor
    Interventions
    Entrectinib 600 mg (T1); Entrectinib 600 mg (T2); Entrectinib 200 mg (R); Entrectinib 200 mg (T)
    Study type
    INTERVENTIONAL
    Phase
    Phase 1
    Registry status
    Completed
    Start
    2019-06-06
    Completion
    2019-08-09
    Enrolment
    31

    As stored from ClinicalTrials.gov. Registration describes a study; it does not mean the study worked.

    ConditionSolid Tumor
    InterventionEntrectinib 600 mg (T1); Entrectinib 600 mg (T2); Entrectinib 200 mg (R); Entrectinib 200 mg (T)
    PhasePhase 1
    Registry statusCompleted
  • A Study to Investigate the Bioequivalence of Two Different Forms of Entrectinib (Forms A and C) Under Fasted Conditions in Healthy Subjects

    NCT03796013 · start 2019-01-10

    Registered record
    Registry ID
    NCT03796013
    Conditions
    Healthy Volunteers
    Interventions
    Entrectinib Form A; Entrectinib Form C
    Study type
    INTERVENTIONAL
    Phase
    Phase 1
    Registry status
    Completed
    Start
    2019-01-10
    Completion
    2019-02-06
    Enrolment
    28

    As stored from ClinicalTrials.gov. Registration describes a study; it does not mean the study worked.

    ConditionHealthy Volunteers
    InterventionEntrectinib Form A; Entrectinib Form C
    PhasePhase 1
    Registry statusCompleted
  • A Study to Investigate the Relative Bioavailability of Entrectinib Capsule Formulations F1 and F06 Under Fed Conditions in Healthy Participants

    NCT03796260 · start 2019-01-09

    Registered record
    Registry ID
    NCT03796260
    Conditions
    Healthy Volunteers
    Interventions
    Entrectinib Test Formulation (F1); Entrectinib Reference Formulation (F06)
    Study type
    INTERVENTIONAL
    Phase
    Phase 1
    Registry status
    Completed
    Start
    2019-01-09
    Completion
    2019-02-04
    Enrolment
    14

    As stored from ClinicalTrials.gov. Registration describes a study; it does not mean the study worked.

    ConditionHealthy Volunteers
    InterventionEntrectinib Test Formulation (F1); Entrectinib Reference Formulation (F06)
    PhasePhase 1
    Registry statusCompleted
  • A Phase II Randomized Study Comparing the Efficacy and Safety of Targeted Therapy or Cancer Immunotherapy Versus Platinum-Based Chemotherapy in Patients With Cancer of Unknown Primary Site

    NCT03498521 · start 2018-07-10

    Registered record
    Registry ID
    NCT03498521
    Conditions
    Cancer of Unknown Primary Site
    Interventions
    Alectinib; Vismodegib; Ipatasertib; Olaparib; Erlotinib; Bevacizumab; Vemurafenib; Cobimetinib; Trastuzumab Subcutaneous (SC); Pertuzumab; Atezolizumab; Carboplatin; Paclitaxel; Cisplatin; Gemcitabine; Entrectinib; Ivosidenib; Pemigatinib
    Study type
    INTERVENTIONAL
    Phase
    Phase 2
    Registry status
    Completed
    Start
    2018-07-10
    Completion
    2024-11-07
    Enrolment
    529

    As stored from ClinicalTrials.gov. Registration describes a study; it does not mean the study worked.

    ConditionCancer of Unknown Primary Site
    InterventionAlectinib; Vismodegib; Ipatasertib; Olaparib +14 more
    PhasePhase 2
    Registry statusCompleted
  • RNASARC - Molecular Screening Program of Soft Tissue Sarcomas With Complex Genomic Profile to Detect NTRK1/2/3, ROS1 or ALK Gene Fusions.

    NCT03375437 · start 2018-02-15

    Registered record
    Registry ID
    NCT03375437
    Conditions
    Soft Tissue Sarcoma; Advanced Cancer; Metastatic Cancer
    Interventions
    Blood and tumor samples
    Study type
    INTERVENTIONAL
    Phase
    Not applicable
    Registry status
    Unknown
    Start
    2018-02-15
    Completion
    2025-12-15
    Enrolment
    376

    As stored from ClinicalTrials.gov. Registration describes a study; it does not mean the study worked.

    ConditionSoft Tissue Sarcoma; Advanced Cancer; Metastatic Cancer
    InterventionBlood and tumor samples
    PhaseNot applicable
    Registry statusUnknown
  • Evaluate the Effect of Entrectinib on the Pharmacokinetics of Midazolam in Cancer Patients

    NCT03330990 · start 2017-11-14

    Registered record
    Registry ID
    NCT03330990
    Conditions
    Advanced Solid Tumor
    Interventions
    Entrectinib; Midazolam Hydrochloride
    Study type
    INTERVENTIONAL
    Phase
    Phase 1
    Registry status
    Completed
    Start
    2017-11-14
    Completion
    2018-07-11
    Enrolment
    15

    As stored from ClinicalTrials.gov. Registration describes a study; it does not mean the study worked.

    ConditionAdvanced Solid Tumor
    InterventionEntrectinib; Midazolam Hydrochloride
    PhasePhase 1
    Registry statusCompleted
  • A Study to Evaluate the Efficacy and Safety of Multiple Targeted Therapies as Treatments for Participants With Non-Small Cell Lung Cancer (NSCLC)

    NCT03178552 · start 2017-09-22

    Registered record
    Registry ID
    NCT03178552
    Conditions
    Non-Small Cell Lung Cancer
    Interventions
    Alectinib; Atezolizumab; Pemetrexed; Cisplatin; Carboplatin; Gemcitabine; Entrectinib; Cobimetinib; Vemurafenib; Bevacizumab; Divarasib; Docetaxel
    Study type
    INTERVENTIONAL
    Phase
    Phase 2 / Phase 3
    Registry status
    Active not recruiting
    Start
    2017-09-22
    Completion
    2027-06-30
    Enrolment
    1,000

    As stored from ClinicalTrials.gov. Registration describes a study; it does not mean the study worked.

    ConditionNon-Small Cell Lung Cancer
    InterventionAlectinib; Atezolizumab; Pemetrexed; Cisplatin +8 more
    PhasePhase 2 / Phase 3
    Registry statusActive not recruiting
  • Precise Local Injection of Anti-cancer Drugs Using Presage's CIVO Device in Soft Tissue Sarcoma

    NCT03056599 · start 2016-12-15

    Registered record
    Registry ID
    NCT03056599
    Conditions
    Soft Tissue Sarcoma Adult
    Interventions
    Multiple drug microinjection; CIVO device
    Study type
    INTERVENTIONAL
    Phase
    Phase 1
    Registry status
    Completed
    Start
    2016-12-15
    Completion
    2021-09-22
    Enrolment
    23

    As stored from ClinicalTrials.gov. Registration describes a study; it does not mean the study worked.

    ConditionSoft Tissue Sarcoma Adult
    InterventionMultiple drug microinjection; CIVO device
    PhasePhase 1
    Registry statusCompleted
  • The Drug Rediscovery Protocol (DRUP Trial)

    NCT02925234 · start 2016-08

    Registered record
    Registry ID
    NCT02925234
    Conditions
    Cancer; Tumors; Neoplasm; Neoplasia
    Interventions
    Panitumumab; Olaparib; Dabrafenib; Nilotinib; Trametinib; Erlotinib; Trastuzumab and Pertuzumab (combination treatment); Vemurafenib and Cobimetinib (combination treatment); Vismodegib; Regorafenib; Nivolumab; Afatinib; Dabrafenib and trametinib; Ribociclib; Lenvatinib; Pembrolizumab; Durvalumab; Rucaparib; Axitinib; Palbociclib; Crizotinib; Sunitinib; Cabozantinib; Abemaciclib; Alectinib; Atezolizumab and Bevacizumab; Ipilimumab and nivolumab; Entrectinib; Talazoparib; Dacomitinib; Lorlatinib; Erdafitinib; Alpelisib; Niraparib; Pemigatinib; Selpercatinib; Tepotinib
    Study type
    INTERVENTIONAL
    Phase
    Phase 2
    Registry status
    Recruiting
    Start
    2016-08
    Completion
    2027-12
    Enrolment
    1,550

    As stored from ClinicalTrials.gov. Registration describes a study; it does not mean the study worked.

    ConditionCancer; Tumors; Neoplasm; Neoplasia
    InterventionPanitumumab; Olaparib; Dabrafenib; Nilotinib +33 more
    PhasePhase 2
    Registry statusRecruiting
  • 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

    NCT02650401 · start 2016-05-03

    Registered record
    Registry ID
    NCT02650401
    Conditions
    Solid Tumors; CNS Tumors
    Interventions
    Entrectinib
    Study type
    INTERVENTIONAL
    Phase
    Phase 1 / Phase 2
    Registry status
    Active not recruiting
    Start
    2016-05-03
    Completion
    2026-06-30
    Enrolment
    69

    As stored from ClinicalTrials.gov. Registration describes a study; it does not mean the study worked.

    ConditionSolid Tumors; CNS Tumors
    InterventionEntrectinib
    PhasePhase 1 / Phase 2
    Registry statusActive not recruiting
  • 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 Rearrangements (Fusions)

    NCT02568267 · start 2015-11-19

    Registered record
    Registry ID
    NCT02568267
    Conditions
    Breast Cancer; Cholangiocarcinoma; Colorectal Cancer; Head and Neck Neoplasms; Lymphoma, Large-Cell, Anaplastic; Melanoma; Neuroendocrine Tumors; Non-Small Cell Lung Cancer; Ovarian Cancer; Pancreatic Cancer; Papillary Thyroid Cancer; Primary Brain Tumors; Renal Cell Carcinoma; Sarcomas; Salivary Gland Cancers; Adult Solid Tumor
    Interventions
    Entrectinib
    Study type
    INTERVENTIONAL
    Phase
    Phase 2
    Registry status
    Active not recruiting
    Start
    2015-11-19
    Completion
    2027-06-30
    Enrolment
    534

    As stored from ClinicalTrials.gov. Registration describes a study; it does not mean the study worked.

    ConditionBreast Cancer; Cholangiocarcinoma; Colorectal Cancer; Head and Neck Neoplasms +12 more
    InterventionEntrectinib
    PhasePhase 2
    Registry statusActive not recruiting
  • Capmatinib, Ceritinib, Regorafenib, or Entrectinib in Treating Patients With BRAF/NRAS Wild-Type Stage III-IV Melanoma

    NCT02587650 · start 2015-03-26

    Registered record
    Registry ID
    NCT02587650
    Conditions
    ALK Fusion Protein Expression; BRAF wt Allele; Invasive Skin Melanoma; MET Fusion Gene Positive; NRAS wt Allele; NTRK1 Fusion Positive; NTRK2 Fusion Positive; NTRK3 Fusion Positive; RET Fusion Positive; ROS1 Fusion Positive; Stage III Cutaneous Melanoma; Stage IIIA Cutaneous Melanoma; Stage IIIB Cutaneous Melanoma; Stage IIIC Cutaneous Melanoma; Stage IV Cutaneous Melanoma
    Interventions
    Capmatinib; Ceritinib; Entrectinib; Laboratory Biomarker Analysis; Regorafenib
    Study type
    INTERVENTIONAL
    Phase
    Phase 2
    Registry status
    Terminated
    Start
    2015-03-26
    Completion
    2018-07-12
    Enrolment
    1

    As stored from ClinicalTrials.gov. Registration describes a study; it does not mean the study worked.

    ConditionALK Fusion Protein Expression; BRAF wt Allele; Invasive Skin Melanoma; MET Fusion Gene Positive +11 more
    InterventionCapmatinib; Ceritinib; Entrectinib; Laboratory Biomarker Analysis +1 more
    PhasePhase 2
    Registry statusTerminated
  • Study of Oral RXDX-101 in Adult Patients With Locally Advanced or Metastatic Cancer Targeting NTRK1, NTRK2, NTRK3, ROS1, or ALK Molecular Alterations.

    NCT02097810 · start 2014-07-28

    Registered record
    Registry ID
    NCT02097810
    Conditions
    Locally Advanced Solid Tumors; Metastatic Solid Tumors
    Interventions
    Entrectinib
    Study type
    INTERVENTIONAL
    Phase
    Phase 1
    Registry status
    Completed
    Start
    2014-07-28
    Completion
    2020-06-02
    Enrolment
    84

    As stored from ClinicalTrials.gov. Registration describes a study; it does not mean the study worked.

    ConditionLocally Advanced Solid Tumors; Metastatic Solid Tumors
    InterventionEntrectinib
    PhasePhase 1
    Registry statusCompleted