Preferred Label : Oral Docetaxel;
NCIt synonyms : Docetaxel-P-glycoprotein Inhibitor; Docetaxel-P-gp Inhibitor;
NCIt definition : An oral proprietary P-glycoprotein (P-gp) pump inhibitor-based formulation containing
the taxane docetaxel, a semisynthetic analogue of paclitaxel, and a P-gp pump inhibitor,
with potential antineoplastic activity. Upon administration of oral docetaxel, the
P-gp pump inhibitor moiety, which is not absorbed, binds to the P-gp pump in the gastrointestinal
(GI) tract and prevents the P-gp pump-mediated efflux of docetaxel from cells the
docetaxel has been internalized by back into the GI tract. This decreases P-gp-mediated
excretion and enhances absorption of docetaxel. Upon absorption, docetaxel binds specifically
to the beta-tubulin subunit of the microtubule, stabilizes tubulin and inhibits microtubule
disassembly, which results in cell-cycle arrest at the G2/M phase and cell death.
The P-gp pump inhibitor enhances the bioavailability of certain poorly bioavailable
agents and thereby allows oral administration of those agents. P-gp, an efflux membrane
transporter, plays a key role in active drug export, and prevents cellular uptake
and accumulation of certain substances.;
Drug name : Oradoxel;
NCI Metathesaurus CUI : CL521226;
Origin ID : C131903;
UMLS CUI : C4330857;
Semantic type(s)
- chemical_or_drug_has_mechanism_of_action
- concept_is_in_subset
