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paxalisib
- Development stage
- Phase 3
- Lead developer
- Kazia Therapeutics
- Modality
- Small Molecules
- Administration
- Oral
01
Overview
Paxalisib is an oral, brain-penetrant small molecule inhibitor of phosphatidylinositol 3‑kinase (PI3K), designed to cross the blood-brain barrier and target tumors of the central nervous system. It specifically inhibits PI3K in the PI3K/AKT/mTOR signaling pathway, thereby blocking downstream activation and resulting in inhibition of tumor cell growth and survival. Paxalisib also inhibits mTORC1 and mTORC2 complexes. The drug is under development primarily for glioblastoma, with additional clinical investigation in diffuse intrinsic pontine glioma (DIPG), atypical teratoid/rhabdoid tumors (AT/RT), brain metastases with PI3K pathway mutations, lymphoma, triple negative breast cancer, malignant melanoma, meningeal carcinomatosis, and other cancers. Originally developed by Genentech as GDC‑0084, it is now being advanced by Kazia Therapeutics[1][2][7][8].
- Brand names
- Paxalisib
- Other names
- paxalisib
02
Targets
PI3K (Phosphoinositide-3-kinase regulatory subunit 6)mTOR (Mammalian target of rapamycin kinase)AKT (RAC-alpha serine/threonine-protein kinase)
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