Alpelisib is a phosphatidylinositol 3-kinase (PI3K) inhibitor with potent antitumor activity. It works by selectively inhibiting class I PI3K p110α , which is the catalytic subunit of PI3K, a lipid... Alpelisib was designed to target this enzyme that appears to be mutated at a rate of nearly 30% in human cancers, leading to hyperactivation.
- Mechanism
- Curator reviewed · 3 references
Phosphatidylinositol-3-kinase-α (PI3Kα) is responsible for cell proliferation in response to growth factor-tyrosine kinase pathway activation. In some cancers PI3Kα's p110α catalytic subunit is mutated making it hyperactive. Alpelisib inhibits (PI3K), with the highest specificity for PI3Kα.
- Primary indication
- Alpelisib is indicated in combination with fulvestrant to treat postmenopausal women, and men, with advanced or metastatic breast cancer.Curator reviewed · 3 structured indications
- Formula / weight
- C19H22F3N5O2S · 441.47 g/mol (avg)
- First approval
- Canada, 2020 · United States, 2019 · European Union, 2020
- Code names
- BYL-719 · NVP-BYL719
- Brand names
Resolves to
STUWGJZDJHPWGZ-LBPRGKRZSA-NSMILESCC1=C(SC(NC(=O)N2CCC[C@H]2C(N)=O)=N1)C1=CC(=NC=C1)C(C)(C)C(F)(F)FWhat you can answer from here — as of September 23, 2026
Which drugs share a target with Alpelisib, and which of those have an active Phase 3 trial?
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