Drug intelligence / Profile preview

docetaxel + HM30181A

Development stage
Unknown
Lead developer
Athenex
Modality
Small Molecules
Administration
Oral, Intravenous
01

Overview

**docetaxel + HM30181A** is a combination therapy consisting of docetaxel, a taxane antineoplastic agent, and HM30181A, a potent and selective inhibitor of P-glycoprotein (P-gp). Docetaxel disrupts microtubule function in cancer cells leading to cell death, but its effectiveness can be limited by P-gp-mediated drug efflux, reducing intracellular concentrations particularly in tissues with high P-gp expression such as the gastrointestinal tract and blood-brain barrier. HM30181A acts by selectively inhibiting P-gp, thereby increasing the bioavailability and tissue penetration of docetaxel. Co-administration is being investigated to improve docetaxel exposure and therapeutic potential, particularly in cancers with high P-gp expression or with barriers to drug delivery (e.g., brain tumors)[1][2][3][6][7].

02

Targets

ABCB1 (P-glycoprotein)TUBB (Tubulin (alpha and beta subunits))

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