Drug intelligence / Profile preview

gedatolisib + talazoparib

Development stage
Phase 2
Lead developer
Celcuity
Modality
Small Molecules
Administration
Intravenous, Oral
01

Overview

Gedatolisib + talazoparib is an investigational combination therapy consisting of gedatolisib, a dual PI3K/mTOR inhibitor, and talazoparib, a PARP inhibitor. Gedatolisib inhibits all class I isoforms of PI3K and mTOR kinases, which are involved in cell growth, survival, and resistance to therapies. Talazoparib blocks the enzyme poly (ADP-ribose) polymerase (PARP), which is involved in DNA repair. The combination is hypothesized to have synergistic effects, as PI3K pathway inhibition might increase homologous recombination deficiency in cancer cells, potentially sensitizing tumors to PARP inhibitors. This combination is being studied primarily for triple-negative breast cancer (TNBC) and BRCA1/2-positive, HER2-negative breast cancers.

02

Targets

PARP1 (Poly (adp-ribose) polymerase 1)PARP2 (Poly (adp-ribose) polymerase 2)PARP3 (Poly(adp-ribose) polymerase 3)PIK3CA (Phosphoinositide 3-kinase alpha)PIK3CB (Phosphatidylinositol 3-kinase beta subunit)PIK3CG (Phosphatidylinositol 4,5-bisphosphate 3-kinase gamma)PIK3CD (Phosphatidylinositol 3-kinase delta)TNKS (Poly(ADP-ribose) Polymerase 5a)TNKS2 (Tankyrase 2)mTOR (Mammalian target of rapamycin kinase)

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