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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 M. tuberculosis, MRSA and E. coli. 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.

  • Treatment With Tucatinib in Patients With an Isolated Brain Progression of a Metastatic Breast Cancer

    NCT05041842 · start 2021-12-17

    Registered record
    Registry ID
    NCT05041842
    Conditions
    Metastatic Breast Cancer With a Isolated Brain Progression
    Interventions
    Tucatinib; Pertuzumab; Trastuzumab; Hormone therapy; Pertuzumab/ Trastuzumab
    Study type
    INTERVENTIONAL
    Phase
    Phase 2
    Registry status
    Active not recruiting
    Start
    2021-12-17
    Completion
    2026-04-30
    Enrolment
    53

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

    ConditionMetastatic Breast Cancer With a Isolated Brain Progression
    InterventionTucatinib; Pertuzumab; Trastuzumab; Hormone therapy +1 more
    PhasePhase 2
    Registry statusActive not recruiting

  • A Study of Tucatinib (MK-7119) in Combination With Trastuzumab and Capecitabine in Participants With Previously Treated Locally Advanced Unresectable or Metastatic Human Epidermal Growth Factor Receptor 2 Positive (HER2+) Breast Carcinoma (MK-7119-001)

    NCT04721977 · start 2021-04-08

    Registered record
    Registry ID
    NCT04721977
    Conditions
    Breast Cancer
    Interventions
    Tucatinib; Trastuzumab; Capecitabine
    Study type
    INTERVENTIONAL
    Phase
    Phase 2
    Registry status
    Active not recruiting
    Start
    2021-04-08
    Completion
    2026-12-31
    Enrolment
    66

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

    ConditionBreast Cancer
    InterventionTucatinib; Trastuzumab; Capecitabine
    PhasePhase 2
    Registry statusActive not recruiting

  • Tucatinib, Trastuzumab, Ramucirumab, and Paclitaxel Versus Paclitaxel and Ramucirumab in Previously Treated HER2+ Gastroesophageal Cancer

    NCT04499924 · start 2021-03-22

    Registered record
    Registry ID
    NCT04499924
    Conditions
    Gastric Adenocarcinoma; Gastroesophageal Junction Adenocarcinoma; Esophageal Adenocarcinoma
    Interventions
    tucatinib; trastuzumab; ramucirumab; paclitaxel; tucatinib placebo; trastuzumab placebo
    Study type
    INTERVENTIONAL
    Phase
    Phase 2 / Phase 3
    Registry status
    Completed
    Start
    2021-03-22
    Completion
    2024-04-17
    Enrolment
    17

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

    ConditionGastric Adenocarcinoma; Gastroesophageal Junction Adenocarcinoma; Esophageal Adenocarcinoma
    Interventiontucatinib; trastuzumab; ramucirumab; paclitaxel +2 more
    PhasePhase 2 / Phase 3
    Registry statusCompleted

  • T-DM1 and Tucatinib Compared With T-DM1 Alone in Preventing Relapses in People With High Risk HER2-Positive Breast Cancer, the CompassHER2 RD Trial

    NCT04457596 · start 2021-03-02

    Registered record
    Registry ID
    NCT04457596
    Conditions
    Anatomic Stage II Breast Cancer AJCC v8; Anatomic Stage III Breast Cancer AJCC v8; HER2 Positive Breast Carcinoma; Invasive Breast Carcinoma; Multifocal Breast Carcinoma; Synchronous Bilateral Breast Carcinoma; Anatomic Stage I Breast Cancer AJCC v8
    Interventions
    Trastuzumab Emtansine; Placebo Administration; Tucatinib; Questionnaire Administration; Quality-of-Life Assessment
    Study type
    INTERVENTIONAL
    Phase
    Phase 3
    Registry status
    Active not recruiting
    Start
    2021-03-02
    Completion
    2035-05-31
    Enrolment
    1,056

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

    ConditionAnatomic Stage II Breast Cancer AJCC v8; Anatomic Stage III Breast Cancer AJCC v8; HER2 Positive Breast Carcinoma; Invasive Breast Carcinoma +3 more
    InterventionTrastuzumab Emtansine; Placebo Administration; Tucatinib; Questionnaire Administration +1 more
    PhasePhase 3
    Registry statusActive not recruiting

  • A Study Evaluating Targeted Therapies in Participants Who Have Advanced Solid Tumors With Genomic Alterations or Protein Expression Patterns Predictive of Response

    NCT04632992 · start 2021-01-13

    Registered record
    Registry ID
    NCT04632992
    Conditions
    Advanced Unresectable or Metastatic Solid Malignancy
    Interventions
    Entrectinib; Inavolisib; Alectinib; Ipatasertib; Atezolizumab; Trastuzumab Emtansine; Pertuzumab, Trastuzumab, and Hyaluronidase-zzxf; Tucatinib; Investigator's Choice of Chemotherapy; Paclitaxel; Tiragolumab; Pralsetinib
    Study type
    INTERVENTIONAL
    Phase
    Phase 2
    Registry status
    Completed
    Start
    2021-01-13
    Completion
    2024-02-27
    Enrolment
    252

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

    ConditionAdvanced Unresectable or Metastatic Solid Malignancy
    InterventionEntrectinib; Inavolisib; Alectinib; Ipatasertib +8 more
    PhasePhase 2
    Registry statusCompleted

  • A Phase 1b/2 Study of T-DXd Combinations in HER2-positive Metastatic Breast Cancer

    NCT04538742 · start 2020-12-28

    Registered record
    Registry ID
    NCT04538742
    Conditions
    Metastatic Breast Cancer
    Interventions
    Trastuzumab deruxtecan; Durvalumab; Paclitaxel; Pertuzumab; Tucatinib
    Study type
    INTERVENTIONAL
    Phase
    Phase 1 / Phase 2
    Registry status
    Active not recruiting
    Start
    2020-12-28
    Completion
    2030-01-31
    Enrolment
    245

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

    ConditionMetastatic Breast Cancer
    InterventionTrastuzumab deruxtecan; Durvalumab; Paclitaxel; Pertuzumab +1 more
    PhasePhase 1 / Phase 2
    Registry statusActive not recruiting

  • A Study of Tucatinib Plus Trastuzumab Deruxtecan in HER2+ Breast Cancer

    NCT04539938 · start 2020-12-01

    Registered record
    Registry ID
    NCT04539938
    Conditions
    HER2 Positive Breast Cancer
    Interventions
    tucatinib; trastuzumab deruxtecan
    Study type
    INTERVENTIONAL
    Phase
    Phase 2
    Registry status
    Completed
    Start
    2020-12-01
    Completion
    2025-03-07
    Enrolment
    70

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

    ConditionHER2 Positive Breast Cancer
    Interventiontucatinib; trastuzumab deruxtecan
    PhasePhase 2
    Registry statusCompleted

  • Tucatinib Plus Trastuzumab and Oxaliplatin-based Chemotherapy or Pembrolizumab-containing Combinations for HER2+ Gastrointestinal Cancers

    NCT04430738 · start 2020-09-15

    Registered record
    Registry ID
    NCT04430738
    Conditions
    Colorectal Carcinoma; Gastric Adenocarcinoma; GEJ Adenocarcinoma; Esophageal Adenocarcinoma; Cholangiocarcinoma; Gallbladder Carcinoma
    Interventions
    tucatinib; trastuzumab; oxaliplatin; leucovorin; fluorouracil; capecitabine; pembrolizumab
    Study type
    INTERVENTIONAL
    Phase
    Phase 2
    Registry status
    Active not recruiting
    Start
    2020-09-15
    Completion
    2026-12-31
    Enrolment
    40

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

    ConditionColorectal Carcinoma; Gastric Adenocarcinoma; GEJ Adenocarcinoma; Esophageal Adenocarcinoma +2 more
    Interventiontucatinib; trastuzumab; oxaliplatin; leucovorin +3 more
    PhasePhase 2
    Registry statusActive not recruiting

  • A Study of Tucatinib vs. Placebo in Combination With Ado-trastuzumab Emtansine (T-DM1) for Patients With Advanced or Metastatic HER2+ Breast Cancer

    NCT03975647 · start 2019-10-02

    Registered record
    Registry ID
    NCT03975647
    Conditions
    HER2-positive Breast Cancer
    Interventions
    tucatinib; placebo; T-DM1
    Study type
    INTERVENTIONAL
    Phase
    Phase 3
    Registry status
    Active not recruiting
    Start
    2019-10-02
    Completion
    2029-03-10
    Enrolment
    466

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

    ConditionHER2-positive Breast Cancer
    Interventiontucatinib; placebo; T-DM1
    PhasePhase 3
    Registry statusActive not recruiting

  • A Safety, Tolerability, and Pharmacokinetic Study of Tucatinib in Healthy Japanese and Caucasian Subjects

    NCT03914755 · start 2019-05-08

    Registered record
    Registry ID
    NCT03914755
    Conditions
    Healthy
    Interventions
    Tucatinib
    Study type
    INTERVENTIONAL
    Phase
    Phase 1
    Registry status
    Completed
    Start
    2019-05-08
    Completion
    2019-08-04
    Enrolment
    36

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

    ConditionHealthy
    InterventionTucatinib
    PhasePhase 1
    Registry statusCompleted

  • A Drug-Drug Interaction Study in Healthy Volunteers of the Effects of Tucatinib on Metformin

    NCT03826602 · start 2019-02-12

    Registered record
    Registry ID
    NCT03826602
    Conditions
    Drug-drug Interaction
    Interventions
    Tucatinib; Metformin; Iohexol
    Study type
    INTERVENTIONAL
    Phase
    Phase 1
    Registry status
    Completed
    Start
    2019-02-12
    Completion
    2019-03-15
    Enrolment
    18

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

    ConditionDrug-drug Interaction
    InterventionTucatinib; Metformin; Iohexol
    PhasePhase 1
    Registry statusCompleted

  • Effects of Tucatinib on Cardiac Repolarization in Healthy Participants

    NCT03777761 · start 2018-12-06

    Registered record
    Registry ID
    NCT03777761
    Conditions
    Healthy
    Interventions
    tucatinib; placebo; moxifloxacin
    Study type
    INTERVENTIONAL
    Phase
    Phase 1
    Registry status
    Completed
    Start
    2018-12-06
    Completion
    2019-03-11
    Enrolment
    55

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

    ConditionHealthy
    Interventiontucatinib; placebo; moxifloxacin
    PhasePhase 1
    Registry statusCompleted

  • Canadian Profiling and Targeted Agent Utilization Trial (CAPTUR)

    NCT03297606 · start 2018-03-23

    Registered record
    Registry ID
    NCT03297606
    Conditions
    Lymphoma, Non-Hodgkin; Multiple Myeloma; Advanced Solid Tumors
    Interventions
    Olaparib; Dasatinib; Nivolumab plus Ipilimumab; Axitinib; Bosutinib; Crizotinib; Palbociclib; Sunitinib; Temsirolimus; Erlotinib; Trastuzumab plus Pertuzumab; Vemurafenib plus Cobimetinib; Vismodegib; Tucatinib
    Study type
    INTERVENTIONAL
    Phase
    Phase 2
    Registry status
    Recruiting
    Start
    2018-03-23
    Completion
    2027-01-31
    Enrolment
    720

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

    ConditionLymphoma, Non-Hodgkin; Multiple Myeloma; Advanced Solid Tumors
    InterventionOlaparib; Dasatinib; Nivolumab plus Ipilimumab; Axitinib +10 more
    PhasePhase 2
    Registry statusRecruiting

  • A Study of the Absorption, Metabolism, and Excretion of Tucatinib in Healthy Participants

    NCT03758339 · start 2017-12-30

    Registered record
    Registry ID
    NCT03758339
    Conditions
    Healthy
    Interventions
    tucatinib
    Study type
    INTERVENTIONAL
    Phase
    Phase 1
    Registry status
    Completed
    Start
    2017-12-30
    Completion
    2018-01-30
    Enrolment
    8

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

    ConditionHealthy
    Interventiontucatinib
    PhasePhase 1
    Registry statusCompleted

  • Trial of ZW25 (Zanidatamab) in Patients With Advanced HER2-expressing Cancers

    NCT02892123 · start 2016-09-30

    Registered record
    Registry ID
    NCT02892123
    Conditions
    HER2-expressing Cancers
    Interventions
    ZW25 (Zanidatamab); Paclitaxel; Capecitabine; Vinorelbine; Tucatinib; Tucatinib
    Study type
    INTERVENTIONAL
    Phase
    Phase 1
    Registry status
    Completed
    Start
    2016-09-30
    Completion
    2024-10-31
    Enrolment
    279

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

    ConditionHER2-expressing Cancers
    InterventionZW25 (Zanidatamab); Paclitaxel; Capecitabine; Vinorelbine +2 more
    PhasePhase 1
    Registry statusCompleted