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bimiralisib
- Development stage
- Phase 2
- Lead developer
- TORQUR
- Modality
- Small Molecules
- Administration
- Oral
01
Overview
Bimiralisib (PQR309) is an orally bioavailable, small molecule dual inhibitor of the phosphatidylinositol 3-kinase (PI3K) and mammalian target of rapamycin (mTOR) pathways. It is designed to target all four isoforms of class I PI3K (alpha, beta, gamma, and delta) as well as mTORC1 and mTORC2. The drug is being investigated for its efficacy in treating various cancers, particularly those with mutations in the PI3K pathway or NOTCH1. In a Phase 2 study led by M.D. Anderson Cancer Center, bimiralisib was evaluated in patients with recurrent or metastatic head and neck squamous cell carcinoma (HNSCC) harboring NOTCH1 loss-of-function mutations, a population that often shows resistance to standard chemotherapy and immunotherapy.
- Other names
- bimiralisib1225037-39-7
02
Targets
PIK3CG (Phosphatidylinositol 4,5-bisphosphate 3-kinase gamma)PIK3CD (Phosphatidylinositol 3-kinase delta)DNA-PK (DNA-dependent protein kinase)PIK3CA (Phosphoinositide 3-kinase alpha)PIK3C3 (PI3K class III)mTOR (Mammalian target of rapamycin kinase)PIK3CB (Phosphatidylinositol 3-kinase beta subunit)
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