Drug intelligence / Profile preview

tretazicar + caricotamide

Development stage
Preclinical
Lead developer
BTG International
Modality
DNA Intercalators/Alkylators → Nucleic Acid-Directed Small Molecules → Small Molecules, Classical Binding Small Molecules → Small Molecules, Covalent Small Molecules → Small Molecules
Administration
Intravenous, Topical
01

Overview

Tretazicar + caricotamide is an investigational combination therapy composed of the prodrug tretazicar (also known as CB1954) and the cosubstrate caricotamide (EP-0152R). Tretazicar is a dinitrobenzamide derivative that acts as a prodrug; it requires enzymatic activation by quinone oxidoreductase 2 (NQO2), which uses caricotamide as an electron donor. Upon activation, tretazicar forms a bifunctional alkylating agent that induces DNA cross-linking and subsequent apoptosis in target cells. This mechanism has been explored primarily for antineoplastic activity in liver cancer and for anti-parasitic effects in cutaneous leishmaniasis models. The combination demonstrates synergistic efficacy compared to monotherapy with either agent alone[1][5][6][9].

Brand names
Prolarix
Other names
tretazicar + caricotamideCB 1954 + EP-0152R
02

Targets

NQO2 (Ribosyldihydronicotinamide dehydrogenase [quinone])DNA

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