Tersolisib — Investigational Agent
PI3K Inhibitor · Phase 1/2 · Scorpion Therapeutics
Mechanism of Action
Orally bioavailable, mutant-selective allosteric inhibitor of PI3Kα (PIK3CA). Binds a WT-sparing allosteric pocket to selectively inhibit both helical- and kinase-domain hotspot mutants (e.g., E542K, E545K, H1047R) while largely sparing wild-type PI3Kα, aiming to preserve glucose homeostasis and reduce the hyperglycemia and rash that limit orthosteric pan-PI3Kα inhibitors.
Investigational Indications
- PIK3CA-mutant HR+/HER2- advanced breast cancer
- PIK3CA-mutant advanced solid tumors
- Post-CDK4/6 inhibitor HR+ breast cancer (combination endocrine therapy)