gemcitabine + carboplatin + iniparib

Gemcitabine + carboplatin + iniparib is a combination chemotherapy regimen investigated primarily for the treatment of triple-negative breast cancer, BRCA1/2 mutation-associated breast cancer, and platinum-sensitive ovarian cancer. Gemcitabine is a nucleoside analog that inhibits DNA synthesis, while carboplatin is a platinum-based agent that causes DNA crosslinking and damage. Iniparib (BSI-201) was initially thought to be a poly(ADP-ribose) polymerase (PARP) inhibitor but later studies showed it does not possess typical PARP inhibitory activity. Instead, its mechanism appears to involve induction of DNA damage markers such as gamma-H2AX and cell cycle arrest at the G2/M phase, potentiating the effects of DNA-damaging agents like gemcitabine and carboplatin. The exact molecular targets of iniparib remain unclear; preclinical data suggest its metabolites may uncouple electron transport from oxidative phosphorylation, generating cytotoxic reactive oxygen species[1][3][6]. The combination has been studied by BiPar Sciences/Sanofi for metastatic triple-negative breast cancer and other solid tumors[3][8].

Brand names

Gemzar (for gemcitabine)Paraplatin (for carboplatin)

Other names

GCI regimen