encequidar

Encequidar is a highly selective and potent small molecule inhibitor of the ATP-binding cassette (ABC) transporter P-glycoprotein (P-gp; also known as MDR1 or ABCB1), an intestinal efflux pump responsible for eliminating endogenous and xenobiotic substrates, including many chemotherapy drugs. Encequidar acts primarily in the intestine due to its minimal systemic absorption, selectively inhibiting P-gp-mediated drug efflux at this site. This inhibition increases the oral bioavailability and therapeutic efficacy of co-administered chemotherapeutic agents that are otherwise poorly absorbed because of P-gp activity. It has been developed as an adjuvant to enable oral administration of drugs like paclitaxel and irinotecan, which are typically given intravenously due to poor oral absorption[2][3][5]. Encequidar itself does not have significant antitumor activity but serves as a pharmacokinetic enhancer.

Brand names

OraxolOratecan

Other names

Pgp inhibitor hm30181ak