Inavolisib (Itovebi)

Mechanism of action

From NCI Drug Dictionary: An orally available inhibitor of phosphatidylinositol 3-kinase (PI3K), with potential antineoplastic activity. Inavolisib binds to and inhibits various members of the PI3K family, including activating mutations in the catalytic alpha isoform PIK3CA. PI3K inhibition prevents the activation of the PI3K-mediated signaling pathway and results in the inhibition of growth and survival of PI3K-overexpressing tumor cells.

Diseases for which it is used

• PIK3CA-mutated breast cancer

History of changes in FDA indication

• 2024-10-10: Approved with palbociclib and fulvestrant for adults with endocrine-resistant, PIK3CA-mutated, hormone receptor (HR)-positive, human epidermal growth-factor receptor 2 (HER2)-negative, locally advanced or metastatic breast cancer, as detected by an FDA-approved test, following recurrence on or after completing adjuvant endocrine therapy. (Based on INAVO120)

Also known as

• Code names: GDC-0077, RG-6114, RO-7113755
• Brand name: Itovebi