Inavolisib (GDC-0077)

Inavolisib (GDC-0077; RG6114) is a potential best-in-class, orally selective PI3Kα inhibitor (IC50=0.038 nM). GDC-0077 (RG6114) exerts its activity by binding to the ATP binding site of PI3K, thereby inhibiting the phosphorylation of PIP2 to PIP3. GDC-0077 (RG6114) is more selective for mutants compared to wild-type PI3Kα. It can trigger the degradation of mutation-producing PIK3α.