Tucatinib
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
![](/sites/default/files/2024-05/Tucatinib%20Mechanism.jpg)
Stage of Development
Tucatinib is being investigated in the tumor types shown below. Safety and efficacy for the uses listed below have not been established.
HER2+ Breast Cancer
Phase 2 Combination*
Phase 3 Combination†
Phase 3 Combination*
Phase 3 Combination
Phase 3 Combination†
Phase 3 Combination*
Phase 3 Combination
HER2+ Colorectal Cancer
Phase 3 Combination
HER2+ Gastrointestinal Cancers
Phase 1b/2 Combination
Solid Tumors with HER2 alterations
Phase 2 Combination*
HER2+ Metastatic UC
Phase 2 Combination*
Gynecological Cancer
Phase 2 Combination*