laniquidar

Laniquidar is a third-generation small molecule inhibitor of P-glycoprotein (P-gp; also known as ABCB1), an ATP-binding cassette transporter involved in multidrug resistance. By inhibiting P-glycoprotein-mediated drug efflux, laniquidar increases the intracellular concentration of chemotherapeutic agents in tumor cells that overexpress this transporter. It was developed as an adjuvant to chemotherapy for overcoming multidrug resistance in cancers such as breast cancer and hematologic malignancies. Laniquidar reached phase II clinical trials but development was discontinued due to low oral bioavailability and high inter-patient variability in response[1][3][5].

Other names

laniquidar [INN]methyl 11-[1-[2-[4-(quinolin-2-ylmethoxy)phenyl]ethyl]piperidin-4-ylidene]-5,6-dihydroimidazo[2,1-b][3]benzazepine-3-carboxylatemethyl 6,11-dihydro-11-(1-(2-(4-(2-quinolylmethoxy)phenyl)ethyl)-4-piperidinylidene)-5H-imidazo(2,1-b)(3)benzazepine-3-carboxylate