palbociclib + pictilisib

Palbociclib + pictilisib is an investigational combination therapy consisting of two small molecule inhibitors: palbociclib, a selective cyclin-dependent kinase 4/6 (CDK4/6) inhibitor, and pictilisib, a pan-class I phosphatidylinositol 3‑kinase (PI3K) inhibitor. Palbociclib blocks cell cycle progression by inhibiting CDK4/6-mediated phosphorylation of the retinoblastoma protein, leading to G1 phase arrest. Pictilisib inhibits PI3K signaling, which is frequently activated in cancer due to mutations such as PIK3CA; this pathway promotes cell growth and survival. The combination aims to overcome resistance mechanisms in cancers—particularly hormone receptor-positive breast cancer—by simultaneously targeting cell cycle progression and PI3K-driven survival pathways. This regimen has been studied in early-phase clinical trials for advanced solid tumors including ER-positive/HER2-negative breast cancer with PIK3CA mutations[2][4][6].

Other names

palbociclib and pictilisibPD-0332991 and GDC-0941PD0332991 and GDC-0941PD 0332991 and GDC-0941