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apitolisib
- Development stage
- Phase 2
- Lead developer
- Genentech
- Modality
- Small Molecules
- Administration
- Oral
01
Overview
Apitolisib is an orally available, small molecule dual inhibitor of phosphatidylinositol 3 kinase (PI3K) and mammalian target of rapamycin (mTOR), targeting the PI3K/mTOR signaling pathway. It was developed as a potential antineoplastic agent for various cancers, including solid tumors, breast cancer, prostate cancer, renal cell carcinoma, endometrial carcinoma, and non-Hodgkin's lymphoma. By inhibiting both PI3K and mTOR kinases—key regulators in cell growth, survival, and resistance to therapy—apitolisib can induce tumor cell apoptosis and inhibit proliferation in cancer cells with dysregulated PI3K/mTOR pathways. The drug demonstrated broad activity in preclinical tumor models but development has been discontinued for all indications[1][5][7][8].
- Other names
- apitolisib
02
Targets
PIK3CA (Phosphoinositide 3-kinase alpha)PIK3CB (Phosphatidylinositol 3-kinase beta subunit)PIK3CG (Phosphatidylinositol 4,5-bisphosphate 3-kinase gamma)mTOR (Mammalian target of rapamycin kinase)PIK3CD (Phosphatidylinositol 3-kinase delta)
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