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VS‑5584
- Development stage
- Discontinued
- Lead developer
- Verastem Oncology
- Modality
- Metabolically Activated Prodrugs → Prodrugs/Conditional Activator Small Molecules → Small Molecules, DNA Intercalators/Alkylators → Nucleic Acid-Directed Small Molecules → Small Molecules
- Administration
- Oral
01
Overview
VS‑5584 is an orally active, small molecule inhibitor that selectively targets both phosphatidylinositol 3 kinase (PI3K) and mammalian target of rapamycin (mTOR), including all class I PI3K isoforms and both mTORC1 and mTORC2 complexes. By inhibiting these kinases, VS‑5584 disrupts phosphorylation of downstream substrates in the PI3K/mTOR signaling pathway, leading to apoptosis and growth inhibition in susceptible tumor cells. The drug has demonstrated broad antiproliferative activity across a range of cancer cell lines, with particular sensitivity observed in cells harboring mutations in PIK3CA. It was developed for the treatment of various cancers including lymphoma, mesothelioma, metastatic cancer, and solid tumors[1][2][6][8].
- Other names
- 5-(9-isopropyl-8-methyl-2-morpholino-9H-purin-6-yl)pyrimidin-2-amine5-(9-isopropyl-8-methyl-2-morpholinyl)-9H-purinyl-pyrimidinamine
02
Targets
PIK3CB (Phosphatidylinositol 3-kinase beta subunit)PIK3CG (Phosphatidylinositol 4,5-bisphosphate 3-kinase gamma)PIK3CA (Phosphoinositide 3-kinase alpha)PIK3CD (Phosphatidylinositol 3-kinase delta)PIK3C3 (PI3K class III)mTOR (Mammalian target of rapamycin kinase)
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