Apitolisib, a dual inhibitor of mTOR and phosphatidylinositol 3-kinase (PI3K), was being developed by Roche and Genentech as an orally administered therapy of cancer. Apitolisib is a selective, potent, orally bioavailable inhibitor of Class I PI3 kinase (PI3K) and mTOR kinase (TORC1/2) with excellent pharmacokinetic and pharmaceutical properties. Apitolisib displayed excellent potency against class I PI3K isoforms (IC50 PI3K-α, β, δ and γ = 4.8, 27, 6.7 and 14 nM) and mTOR kinase (IC50 = 17 nM) and selectivity against a large panel of other kinases. Apitolisib is in phase II trials by Genentech for the treatment of breast cancer, prostate cancer, endometrium cancer, kidney cancer. However, no recent development has been reported. It is also in phase I trials by Genentech for the treatment of non-Hodgkin's lymphoma.

Pictilisib is an oral potent inhibitor of class I PI3K with nanomolar activities against p110alpha, p110beta, p110delta, and p110gamma. The drug was developed for the treatment of solid tumors and reached phase II in patients with breast cancer and lung carcinoma, however its development was terminated.

Pictilisib is an oral potent inhibitor of class I PI3K with nanomolar activities against p110alpha, p110beta, p110delta, and p110gamma. The drug was developed for the treatment of solid tumors and reached phase II in patients with breast cancer and lung carcinoma, however its development was terminated.