Pictilisib Bismesylate

**Semantic type:** Pharmacologic Substance

**Definition:** The orally bioavailable bismesylate salt of pictilisib, a small molecule inhibitor of class I phosphatidylinositol 3 kinase (PI3K), with potential antineoplastic activity. Upon administration, pictilisib selectively binds to PI3K in an ATP-competitive manner, inhibiting the production of the secondary messenger phosphatidylinositol-3,4,5-trisphosphate (PIP3) and activation of the PI3K/Akt signaling pathway. This may result in inhibition of tumor cell growth, motility and survival in susceptible tumor cell populations. Activation of the PI3K/Akt signaling pathway is frequently associated with tumorigenesis; dysregulated PI3K/Akt signaling may contribute to tumor resistance to a variety of antineoplastic agents.

**Synonyms:** - 2-(1H-indazol-4-yl)-6-(4-methanesulfonyl-piperazin-1- ylmethyl)-4-morpholin-4-yl-thieno[3,2-d]pyrimidine, bimesylate salt - GDC-0941 Bismesylate - GDC-0941 Dimesylate - PICTILISIB BISMESYLATE - Pictilisib Dimesylate - Thieno(3,2-d)pyrimidine, 2-(1H-indazol-4-yl)-6-((4-(methylsulfonyl)-1-piperazinyl)methyl)-4-(4-morpholinyl)-, Methanesulfonate (1:2)