Encequidar (formerly HM-30181; HM30181; HM30181A) is a novel, potent, selective, and orally bioavailable inhibitor of the adenosine triphosphate (ATP)-binding cassette (ABC) transporter P-gp (P-glycoprotein). It was designed to improve the oral bioavailability of drugs that are P-gp substrates which may otherwise be pumped out of cells by P-gp, leading to drug resistance. Encequidar was supported by FDA in March 2021 for the new drug application for combination with oral paclitaxel in the treatment of patients with metastatic breast cancer. Oral paclitaxel and encequidar is the first world taxane to demonstrate superiority in radiologically confirmed tumor response rate, with reduced neuropathy and alopecia compared to IV paclitaxel in women with metastatic breast cancer. Encequidar showed the highest potency (IC(50)=0.63nM) among several MDR1 inhibitors, including cycloporin A, XR9576, and GF120918, and effectively blocked transepithelial transport of paclitaxel in MDCK monolayers (IC(50)=35.4nM). Encequidar is currently under clinical trials.

纯度：≥98%

CAS：849675-66-7