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AMR Drug RepurposingSmart Screeningresearch prototype

Tucatinib

FDA-approved product (tablet, oral), marketed as Tukysa.

Registered studies
50+
Lab records
0
Pathogens at ≥40%
3 of 4

Chemical structure

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

Existing / approved use

Documented · FDA, WHO, ChEMBL

Approved for

  • Breast cancer
  • Breast carcinoma
  • Breast neoplasm
  • Cancer
  • Colorectal carcinoma
  • Colorectal neoplasm
  • HER2 Positive Breast Carcinoma
  • Metastasis
  • Neoplasm

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

WHO therapeutic group
Human epidermal growth factor receptor 2 (her2) tyrosine kinase inhibitors
FDA pharmacologic class
Kinase Inhibitor FDA label ↗
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
  • MRSA51.9% AI-predicted activityAt or above the ≥40% mark this site uses to surface candidates.
  • E. coli51.6% AI-predicted activityAt or above the ≥40% mark this site uses to surface candidates.
  • K. pneumoniae28.5% AI-predicted activityBelow the ≥40% mark this site uses to surface candidates.
  • M. tuberculosis54.0% 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

50+registered studies name this medicine, for any condition. The registry search keeps the first 50, so there may be more. See them below.

Experimental

No evidence found

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

Open Tucatinib in ChEMBL Registered studies below

Docking

Computational · nothing measured

Dihydrofolate reductase ↗ (E. coli)

-9.4 kcal/mol

0better fit →-12

KPC-2 carbapenemase ↗ (K. pneumoniae)

-8.5 kcal/mol

0better fit →-12

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

-9.6 kcal/mol

0better fit →-12

Dihydrofolate reductase ↗ (MRSA)

-10.2 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 Tucatinib 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 Study of Tucatinib vs. Placebo in Combination With Capecitabine & Trastuzumab in Patients With Advanced HER2+ Breast Cancer

    NCT02614794 · start 2016-01-28

    Registered record
    Registry ID
    NCT02614794
    Conditions
    HER2 Positive Breast Cancer
    Interventions
    tucatinib; capecitabine; trastuzumab; placebo
    Study type
    INTERVENTIONAL
    Phase
    Phase 2
    Registry status
    Completed
    Start
    2016-01-28
    Completion
    2022-08-11
    Enrolment
    612

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

    ConditionHER2 Positive Breast Cancer
    Interventiontucatinib; capecitabine; trastuzumab; placebo
    PhasePhase 2
    Registry statusCompleted

  • A Study of Tucatinib (ONT-380) Combined With Ado-trastuzumab Emtansine (T-DM1) in Patients With HER2+ Breast Cancer

    NCT01983501 · start 2014-02-28

    Registered record
    Registry ID
    NCT01983501
    Conditions
    HER2 Positive Breast Cancers
    Interventions
    Tucatinib (ONT-380); T-DM1
    Study type
    INTERVENTIONAL
    Phase
    Phase 1
    Registry status
    Completed
    Start
    2014-02-28
    Completion
    2020-09-03
    Enrolment
    57

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

    ConditionHER2 Positive Breast Cancers
    InterventionTucatinib (ONT-380); T-DM1
    PhasePhase 1
    Registry statusCompleted

  • A Study of Tucatinib (ONT-380) Combined With Capecitabine and/or Trastuzumab in Patients With HER2+ Metastatic Breast Cancer

    NCT02025192 · start 2013-12-31

    Registered record
    Registry ID
    NCT02025192
    Conditions
    HER2 Positive Metastatic Breast Cancers
    Interventions
    Tucatinib; Capecitabine; Trastuzumab
    Study type
    INTERVENTIONAL
    Phase
    Phase 1
    Registry status
    Completed
    Start
    2013-12-31
    Completion
    2020-03-16
    Enrolment
    60

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

    ConditionHER2 Positive Metastatic Breast Cancers
    InterventionTucatinib; Capecitabine; Trastuzumab
    PhasePhase 1
    Registry statusCompleted

  • I-SPY TRIAL: Neoadjuvant and Personalized Adaptive Novel Agents to Treat Breast Cancer

    NCT01042379 · start 2010-03-01

    Registered record
    Registry ID
    NCT01042379
    Conditions
    Breast Neoplasms; Breast Cancer; Breast Tumors; Angiosarcoma; TNBC - Triple-Negative Breast Cancer; HER2-positive Breast Cancer; HER2-negative Breast Cancer; Hormone Receptor Positive Tumor; Hormone Receptor Negative Tumor; Early-stage Breast Cancer; Locally Advanced Breast Cancer
    Interventions
    Standard Therapy; AMG 386 with or without Trastuzumab; AMG 479 (Ganitumab) plus Metformin; MK-2206 with or without Trastuzumab; AMG 386 and Trastuzumab; T-DM1 and Pertuzumab; Pertuzumab and Trastuzumab; Ganetespib; ABT-888; Neratinib; PLX3397; Pembrolizumab - 4 cycle; Talazoparib plus Irinotecan; Patritumab and Trastuzumab; Pembrolizumab - 8 cycle; SGN-LIV1A; Durvalumab plus Olaparib; SD-101 + Pembrolizumab; Tucatinib plus trastuzumab and pertuzumab; Cemiplimab; Cemiplimab plus REGN3767; Trilaciclib with or without trastuzumab + pertuzumab; SYD985 ([vic-]trastuzumab duocarmazine); Oral Paclitaxel + Encequidar + Dostarlimab (TSR-042) + Carboplatin with or without trastuzumab; Oral Paclitaxel + Encequidar + Dostarlimab (TSR-042) with or without trastuzumab; Amcenestrant; Amcenestrant + Abemaciclib; Amcenestrant + Letrozole; ARX788; ARX788 + Cemiplimab; VV1 + Cemiplimab; Datopotamab deruxtecan; Datopotamab deruxtecan + Durvalumab; Zanidatamab; Lasofoxifene; Z-endoxifen; ARV-471; ARV-471 +
    Study type
    INTERVENTIONAL
    Phase
    Phase 2
    Registry status
    Recruiting
    Start
    2010-03-01
    Completion
    2031-12
    Enrolment
    5,000

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

    ConditionBreast Neoplasms; Breast Cancer; Breast Tumors; Angiosarcoma +7 more
    InterventionStandard Therapy; AMG 386 with or without Trastuzumab; AMG 479 (Ganitumab) plus Metformin; MK-2206 with or without Trastuzumab +34 more
    PhasePhase 2
    Registry statusRecruiting

  • Expanded Access Use of Tucatinib for HER2+ Metastatic Breast Cancer

    NCT03424473

    Registered record
    Registry ID
    NCT03424473
    Conditions
    Not recorded
    Interventions
    Tucatinib
    Study type
    EXPANDED_ACCESS
    Phase
    Not recorded
    Registry status
    No longer available
    Start
    Not recorded
    Completion
    Not recorded
    Enrolment
    Not recorded

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

    ConditionNot recorded
    InterventionTucatinib
    PhaseNot recorded
    Registry statusNo longer available