Oral docetaxel
Term · Oncology and biomedicine · MLC-T-ONC-015693
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.
| Identifier | MLC-T-ONC-015693 |
|---|---|
| Field | Oncology and biomedicine |
| Synonyms | docetaxel-P-glycoprotein inhibitor; docetaxel-P-gp inhibitor |
| References | National Cancer Institute Thesaurus (CC BY 4.0) |
Record as JSON
{
"id": "MLC-T-ONC-015693",
"term": "Oral docetaxel",
"field": "Oncology and biomedicine",
"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.",
"synonyms": [
"docetaxel-P-glycoprotein inhibitor",
"docetaxel-P-gp inhibitor"
],
"references": [
"National Cancer Institute Thesaurus"
],
"url": "https://mlchart.com/terminology/oncology/oral-docetaxel/"
}
Record 12,312 of 17,717 in Oncology and biomedicine terminology (MLC-0111). Request the full dataset.