Drug intelligence / Profile preview

docetaxel + pralatrexate

Development stage
Unknown
Lead developer
Assertio
Modality
Small Molecules
Administration
Intravenous
01

Overview

A combination of docetaxel and pralatrexate, two anticancer agents with different mechanisms of action. Docetaxel is a well-established taxane chemotherapy drug that works by binding to microtubulins, preventing cell division and promoting cell death. Pralatrexate is a novel antifolate designed to have high affinity for the reduced folate carrier type 1, inhibiting dihydrofolate reductase and competitively inhibiting polyglutamylation by the enzyme folylpolyglutamyl synthetase. The rationale for combining these agents is that they may work synergistically to kill more tumor cells than either agent alone. The combination showed significant antitumor activity in patients with non-small cell lung cancer in early clinical testing.

02

Targets

FPGS (Folylpolyglutamate synthase, mitochondrial)DHFR (Dihydrofolate reductase)TUBB (Tubulin (alpha and beta subunits))

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