birinapant + gemcitabine

**Birinapant + gemcitabine** is a **combination regimen** composed of birinapant, a bivalent small molecule mimetic of second mitochondria-derived activator of caspase (SMAC) that antagonizes Inhibitor of Apoptosis Proteins (IAPs), and gemcitabine, a pyrimidine analog which inhibits DNA synthesis. Birinapant enhances sensitivity to gemcitabine through degradation of cIAP1, cIAP2, and XIAP, activating the intrinsic apoptotic pathway via caspases, while gemcitabine incorporates into DNA and blocks its elongation, inducing apoptosis. This combination has shown synergistic antitumor efficacy in preclinical models of triple-negative breast cancer (TNBC) and pancreatic cancer, improving apoptosis and cell cycle arrest beyond either agent alone[1][2][3]. Birinapant is still investigational; gemcitabine is approved for various cancers.

Brand names

gemcitabine (Gemzar)birinapant (no approved brand name, still investigational)

Other names

birinapant + gemcitabine