gedatolisib + letrozole + palbociclib

Gedatolisib + letrozole + palbociclib is an investigational combination therapy for hormone receptor-positive, HER2-negative advanced or metastatic breast cancer. Gedatolisib is a potent, reversible dual inhibitor that selectively targets all class I PI3K isoforms and both mTORC1 and mTORC2 complexes, thereby blocking the PI3K/AKT/mTOR signaling pathway. Letrozole is a nonsteroidal aromatase inhibitor that suppresses estrogen synthesis by inhibiting the aromatase enzyme. Palbociclib is a selective cyclin-dependent kinase 4/6 (CDK4/6) inhibitor that blocks cell cycle progression from G1 to S phase. The rationale for this triplet regimen is to simultaneously inhibit three key pathways involved in tumor growth and resistance—estrogen receptor signaling, CDK4/6-mediated cell cycle progression, and PI3K/mTOR-driven survival/proliferation—potentially providing more effective tumor control than standard-of-care therapies. This combination has shown promising objective response rates and manageable safety in phase 1b clinical trials for patients with HR+/HER2- advanced breast cancer[1][5][6].

Brand names

IbranceFemara

Other names

PF-05212384PF05212384PF 05212384PD-0332991PD0332991PD 0332991CGS 20267CGS20267CGS-20267