Gedatolisib · Revtorpyk, PKI-587

What is Gedatolisib?

Gedatolisib is a kinase inhibitor targeting PI3K class I isoforms and mTOR complexes (mTORC1 and mTORC2), resulting in downstream AKT inhibition. It induces apoptosis and reduces tumor cell growth in ER-positive breast cancer models.

Summary written with AI from the sources listed at the end of this page.

At a glance

Also known as

Revtorpyk, PKI-587, PF-05212384

Drug type

Small molecule

Targets

PI3K class I (α, β, δ, γ isoforms) (PIK3CA), mTORC1 (MTOR), AKT (AKT1) (secondary target)

Mechanism

Inhibitor of PI3K class I (α, β, δ, γ isoforms) (PIK3CA) and mTORC1 (MTOR)

Pathways

PI3K/mTOR signaling, apoptosis, cell growth inhibition

Therapy area

Oncology

Developer

Celcuity (CELC)

FDA status

Approved as Revtorpyk (July 14, 2026), NDA219908 · FDA label

UNII

96265TNH2R

✅ FDA-approved uses

• HR-positive, HER2-negative locally advanced or metastatic breast cancer without PIK3CA mutation

From the indications section of the FDA label (version of Jul 14, 2026). Read the full label for the exact wording, limitations and safety information.

🧪 Clinical trials

Trials of the companies BioRadar tracks, from ClinicalTrials.gov, most advanced phase first.

Conditions studied

Breast Cancer

Other drugs acting on PIK3CA / MTOR

Sources

• FDA label (DailyMed)
• FDA label Revtorpyk (2026-07-14), indications
• NCI Thesaurus
• ClinicalTrials.gov NCT05501886

Updated Oct 3, 2026. Something wrong or missing? Report it on the CELC page.