Preferred Label : Oraxol;
NCIt synonyms : Paclitaxel-HM30181 Methanesulfonate Monohydrate; Paclitaxel/HM30181A;
NCIt definition : A combination formulation composed of a capsule containing the taxane compound paclitaxel
and a tablet containing the multidrug resistance (MDR) efflux pump P-glycoprotein
(P-gp) inhibitor HM30181A, with potential antineoplastic activity. Upon oral administration
of oraxol, the HM30181A moiety binds to and inhibits P-gp, which prevents P-gp-mediated
efflux of paclitaxel, therefore enhancing its oral bioavailability. In turn, paclitaxel
binds to and stabilizes microtubules, preventing their depolymerization, which results
in the inhibition of cellular motility, mitosis, and replication. Altogether, this
may result in greater intracellular concentration of paclitaxel, and enhanced cytotoxicity
against tumor cells, when compared to the administration of paclitaxel alone. P-gp,
encoded by the MDR-1 gene, is a member of the ATP-binding cassette (ABC) superfamily
of transmembrane transporters; it prevents the intestinal uptake and intracellular
accumulation of various cytotoxic agents.;
NCI Metathesaurus CUI : CL454289;
Origin ID : C112000;
UMLS CUI : C3828699;
Semantic type(s)
- chemical_or_drug_has_mechanism_of_action
- concept_is_in_subset
- has_target
