BackTucatinib
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
Phase 3 Combination†
Phase 3 Combination*
Phase 3 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.