Drug intelligence / Profile preview

eribulin mesylate + HM30181A

Development stage
Preclinical
Lead developer
Hanmi Pharmaceutical
Modality
Small Molecules
Administration
Intravenous
01

Overview

Eribulin mesylate + HM30181A is a combination of the microtubule inhibitor eribulin mesylate—a synthetic analogue of halichondrin B used in metastatic breast cancer and liposarcoma—and HM30181A, a potent and selective inhibitor of P-glycoprotein (P-gp/ABCB1). Eribulin mesylate disrupts microtubule dynamics, blocking cell division and inducing apoptosis in cancer cells. HM30181A is designed to inhibit the efflux transporter P-glycoprotein, which can limit the absorption, tissue distribution, and effectiveness of many chemotherapeutics by pumping them out of cells, especially at the gastrointestinal tract and blood-brain barrier. The combination aims to improve eribulin’s efficacy in settings where P-gp limits drug effectiveness, such as multidrug-resistant cancers or targeting tumor sites protected by P-gp, including the brain[1][3][4][6].

02

Targets

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

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