Gedatolisib is a pan-PI3K and mTORC1/2 inhibitor used as part of a second-line chemotherapy regimen for HR-positive, HER2-negative advanced breast cancer without a PIK3CA mutation following endocrine therapy. Gedatolisib is a kinase inhibitor that blocks all four class I PI3K isoforms together with both mTOR complexes, mTORC1 and mTORC2, producing downstream inhibition of multiple effectors including AKT.
- Mechanism
- Curator reviewed
Pharmacologically active on Serine/threonine-protein kinase mTOR
- Primary indication
- Gedatolisib is a kinase inhibitor indicated in combination with fulvestrant, with or without palbociclib, for the treatment of adult patients with hormone receptor (HR)-positive, human epidermal growth factor receptor 2 (HER2)-negative locally advanced or metastatic...Curator reviewed · 2 structured indications
- Formula / weight
- C32H41N9O4 · 615.739 g/mol (avg)
- First approval
- United States, 2026
- Code names
- PF-05212384 · PKI-587
- Brand names
Resolves to
Clinical / RWD
Structure
InChIKey
DWZAEMINVBZMHQ-UHFFFAOYSA-NSMILESCN(C)C1CCN(CC1)C(=O)C1=CC=C(NC(=O)NC2=CC=C(C=C2)C2=NC(=NC(=N2)N2CCOCC2)N2CCOCC2)C=C1Targets
What you can answer from here — as of September 19, 2026
2Protein targetsEach mapped to UniProt, with action and pharmacological actionListed above
Which drugs share a target with Gedatolisib, and which of those have an active Phase 3 trial?
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