Drug intelligence / Profile preview

palbociclib + gedatolisib

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

Overview

Palbociclib + gedatolisib is a combination therapy investigated primarily for the treatment of hormone receptor-positive (HR+), human epidermal growth factor receptor 2-negative (HER2-) advanced breast cancer. Palbociclib is a selective small molecule inhibitor of cyclin-dependent kinases 4 and 6 (CDK4/6), which blocks cell cycle progression in tumor cells. Gedatolisib is a dual inhibitor targeting both the phosphatidylinositol 3-kinase (PI3K) and mammalian target of rapamycin (mTOR) pathways, both of which are central to cell proliferation and survival. The combination aims to simultaneously inhibit cell cycle progression and critical oncogenic signaling, particularly useful in overcoming or delaying acquired resistance to CDK4/6 inhibitors. Clinical trials have shown promising response rates and manageable toxicity, with the most common adverse events being neutropenia, stomatitis, rash, and hyperglycemia. This combination is under active investigation in Phase 3 studies for HR+/HER2- advanced breast cancer, both in treatment-naive patients and those previously treated with CDK4/6 inhibitors[1][2][3][9][4][5][7].

Other names
PF-05212384PF05212384PF 05212384
02

Targets

PIK3CG (Phosphatidylinositol 4,5-bisphosphate 3-kinase gamma)CDK6 (Cyclin-dependent kinase 6)CDK4 (Cyclin-dependent kinase 4)PIK3CB (Phosphatidylinositol 3-kinase beta subunit)mTOR (Mammalian target of rapamycin kinase)PIK3CD (Phosphatidylinositol 3-kinase delta)PIK3CA (Phosphoinositide 3-kinase alpha)

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