The novel P-gp inhibitor encequidar (formerly known as HM30181A) forms the cornerstone of our Orascovery platform. Encequidar enables the oral absorption of a wide range of effective anticancer drugs, which can currently only be given intravenously, due to poor oral absorption.
P-glycoprotein (P-gp) is an active transport protein on the surface of the gastrointestinal (GI) tract. Many anticancer drugs are substrates of P-gp, and when orally administered, they will be pumped back into the GI tract, thereby limiting the drugs to intravenous administration. Encequidar, as a selective and potent P-gp inhibitor, has the potential to allow oral delivery of these chemotherapy agents. Current clinical trials are underway globally with encequidar combined with paclitaxel, docetaxel, irinotecan, eribulin, and topotecan.
Encequidar is a novel compound with inhibitory activity specific to P-gp. Encequidar’s distinguishing feature is its minimal oral absorption. This feature localizes P-gp inhibitory activity in the GI tract, improving the absorption of chemotherapy agents, but limiting the potential for unnecessary P-gp inhibition at other places in the body.
We believe the Orascovery approach will establish a new paradigm in the use of oral anticancer drugs.
