biricodar

Biricodar is a synthetic small molecule, specifically a pipecolinate derivative, developed as a chemosensitizing agent to overcome multidrug resistance in cancer therapy. Its primary mechanism of action is the inhibition of two major drug efflux transporters: P-glycoprotein (also known as MDR1 or ABCB1) and multidrug resistance-associated protein 1 (MRP1 or ABCC1). By binding directly to these transporters and inhibiting their ATP-dependent efflux activity, biricodar increases the intracellular accumulation and retention of cytotoxic chemotherapeutic agents in resistant tumor cells. This restores drug sensitivity in cancers that have become refractory due to overexpression of these efflux pumps. Biricodar was intended for use intravenously alongside standard chemotherapy regimens for various cancers, including breast cancer, ovarian cancer, soft-tissue sarcomas, small cell lung cancer, and prostate cancer. Despite reaching phase II clinical trials, its development was discontinued due to lack of significant efficacy improvement and adverse effects[1][2][3][4][5].

Brand names

Incel

Other names

biricodar dicitrate159997-94-1