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Pfizer Oncology
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The safety and efficacy of this agent(s), or use in this setting, has not been established or is subject to confirmation. For an agent(s) whose safety and efficacy has not been established or confirmed, future regulatory approval or commercial availability is not guaranteed.

Tucatinib

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Tucatinib

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Overview + Rationale

  • Tucatinib is an orally bioavailable, reversible, highly selective small molecule tyrosine kinase inhibitor being investigated in multiple human epidermal growth factor receptor 2 (HER2) overexpressed/amplified and HER2 mutated cancers.1,2
    • In cell signaling assays, tucatinib exhibits thousandfold greater selectivity for the HER2 receptor relative to epidermal growth factor receptor (EGFR).1
    • HER2 selectivity may decrease the potential for EGFR-related toxicities (eg, diarrhea, skin rash).1
    • Preclinical data suggest that tucatinib increases surface HER2 expression.2
  • HER2 is overexpressed in multiple cancers, including breast, colorectal, ovarian, lung, gastroesophageal, and bladder.

Mechanism of Action

Stage of Development

Tucatinib has received regulatory approval for specific indications and is being investigated in the tumor types shown below

Small icon representing Breast Cancer in pink
HER2+ Breast Cancer
Phase 2 Combination*

Phase 3 Combination†

Phase 3 Combination*

Phase 3 Combination*
Small icon representing GI Cancer in light blue
HER2+ Colorectal Cancer
Phase 3 Combination
Small icon for other cancer
Solid Tumors with HER2 alterations
Phase 1 Combination*

Phase 2 Combination*
This information is current as of February 4th 2025.

*Closed to Enrollment †Sponsored by Alliance for Clinical Trials in Oncology

REFERENCES:  1. Kulukian A. Mol Cancer Ther. 2020: 976-87; 2. Olson D. Cancer Res Commun. 2023: 1927-39;   3. NCT04539938. https://clinicaltrials.gov/study/NCT04539938; Accessed January 16, 2025; 4. NCT04457596. https://clinicaltrials.gov/study/NCT04457596; Accessed January 16, 2025; 5. NCT05132582. https://clinicaltrials.gov/study/NCT05132582; Accessed January 16, 2025; 6. NCT03975647. https://clinicaltrials.gov/study/NCT03975647; Accessed January 16, 2025; 7. NCT05253651. https://clinicaltrials.gov/study/NCT05253651  Accessed January 16, 2025; 8. NCT05382364. https://clinicaltrials.gov/study/NCT05382364  Accessed January 16, 2025; 9. NCT04579380. https://clinicaltrials.gov/study/NCT04579380  Accessed January 16, 2025.