Drug intelligence / Profile preview

paclitaxel docosahexaenoic acid

Development stage
Phase 3
Lead developer
American Regent
Modality
Metabolically Activated Prodrugs → Prodrugs/Conditional Activator Small Molecules → Small Molecules
Administration
Intravenous
01

Overview

DHA-paclitaxel (Taxoprexin) is an investigational prodrug formed by covalently linking the anti-microtubule agent paclitaxel to the omega-3 fatty acid docosahexaenoic acid (DHA). This conjugation exploits tumor cells’ propensity to take up DHA, thereby delivering higher concentrations of paclitaxel directly into tumor tissue. Once inside the cell, the bond is cleaved and active paclitaxel is released. The mechanism of action involves binding to tubulin and inhibiting microtubule disassembly—arresting cell division—and inducing apoptosis by blocking Bcl-2 function. Compared with conventional paclitaxel formulations, DHA-paclitaxel demonstrates improved pharmacokinetics and toxicity profiles in preclinical models. It has been studied primarily for cancer indications such as metastatic melanoma and oesophago-gastric cancer[1][2][3][4][5].

Brand names
Taxoprexin
Other names
paclitaxel 2'-(all-cis-4,7,10,13,16,19-docosahexaenoate)paclitaxel docosahexaenoic acid ester
02

Targets

BCL-2 (BCL-2 family)TUBB (Tubulin (alpha and beta subunits))

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