Drug intelligence / Profile preview

omipalisib

Development stage
Phase 1
Lead developer
GSK
Modality
Small Molecules
Administration
Oral
01

Overview

Omipalisib is a potent, orally active small molecule inhibitor of phosphoinositide 3-kinase (PI3K) and mammalian target of rapamycin (mTOR), developed primarily by GlaxoSmithKline for the potential treatment of cancer and idiopathic pulmonary fibrosis. It acts as a highly selective inhibitor targeting all class I PI3K isoforms (p110α/β/δ/γ) and both mTOR complexes (mTORC1/2), with low nanomolar potency. By inhibiting the PI3K/mTOR signaling pathway, which is often dysregulated in cancer, omipalisib can induce apoptotic cell death in tumor cells through increased mitochondrial membrane permeability. In preclinical studies, it also attenuates fibroblast proliferation and collagen synthesis relevant to fibrotic diseases. Omipalisib has been evaluated in clinical trials for solid tumors, lymphoma, and idiopathic pulmonary fibrosis[1][2][3][4][5][6].

Other names
omipalisib
02

Targets

DNA-PK (DNA-dependent protein kinase)mTOR (Mammalian target of rapamycin kinase)PIK3CA (Phosphoinositide 3-kinase alpha)PIK3CB (Phosphatidylinositol 3-kinase beta subunit)PIK3CD (Phosphatidylinositol 3-kinase delta)PIK3CG (Phosphatidylinositol 4,5-bisphosphate 3-kinase gamma)

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