paclitaxel + encequidar

Paclitaxel + encequidar is an oral combination antineoplastic therapy where **paclitaxel**, a microtubule-stabilizing taxane, is administered orally together with **encequidar**, a minimally absorbed, gut-specific oral P-glycoprotein (P-gp) inhibitor. Encequidar inhibits P-gp-mediated efflux of paclitaxel in the gut, enabling sufficient oral absorption of paclitaxel, which otherwise has low bioavailability due to P-gp-mediated extrusion. Paclitaxel acts by stabilizing microtubules, inhibiting their disassembly, and thus blocking mitosis in cancer cells. Encequidar has no known antineoplastic activity of its own but facilitates delivery of paclitaxel. The combination is developed primarily for the treatment of metastatic breast cancer and has also been investigated in various advanced solid tumors. Clinical studies have shown higher overall response rates, less peripheral neuropathy, and comparable survival to intravenous paclitaxel, but with more gastrointestinal side effects and neutropenia. Regulatory approval has faced delays due to concerns over safety (notably febrile neutropenia) and efficacy endpoints[1][2][3][4][6][7].

Brand names

Oraxol

Other names

oral paclitaxel + encequidar