Drug intelligence / Profile preview

docetaxel + tariquidar

Development stage
Phase 2
Lead developer
QLT
Modality
Classical Binding Small Molecules → Small Molecules, Covalent Small Molecules → Small Molecules, Nucleic Acid-Directed Small Molecules → Small Molecules
Administration
Intravenous
01

Overview

Docetaxel + tariquidar is an investigational combination therapy consisting of the chemotherapeutic agent docetaxel and the third-generation P-glycoprotein (Pgp) inhibitor tariquidar. Docetaxel is a taxane-class antineoplastic that stabilizes microtubules, thereby inhibiting cell division and inducing apoptosis in cancer cells. Tariquidar is a potent, noncompetitive inhibitor of P-glycoprotein, a drug efflux transporter associated with multidrug resistance in cancer. By inhibiting Pgp, tariquidar increases intracellular concentrations of chemotherapeutic agents like docetaxel in resistant tumor cells. This combination has been studied primarily for its potential to overcome multidrug resistance in solid tumors such as non-small cell lung cancer and ovarian cancer[1][2][4]. Clinical studies have shown that this regimen can be administered safely with manageable toxicity profiles; pharmacodynamic data confirm effective inhibition of Pgp-mediated drug efflux by tariquidar[1][2].

Other names
docetaxel and tariquidarDTX + TRQ
02

Targets

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

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