Setidegrasib — Investigational Agent
KRAS Inhibitor · Phase 3 · Astellas Pharma
Mechanism of Action
First-in-class KRAS G12D-selective targeted protein degrader (chimeric/PROTAC-type molecule) that recruits an E3 ubiquitin ligase to the mutant KRAS G12D protein, driving its ubiquitination and proteasomal degradation and thereby ablating downstream MAPK/PI3K oncogenic signaling.
Investigational Indications
- KRAS G12D-mutant NSCLC
- KRAS G12D-mutant pancreatic ductal adenocarcinoma
- KRAS G12D-mutant colorectal cancer
- Other KRAS G12D solid tumors