Drug intelligence / Profile preview

Tretazicar

Development stage
Preclinical
Lead developer
BTG International
Modality
Metabolically Activated Prodrugs → Prodrugs/Conditional Activator Small Molecules → Small Molecules
Administration
Intraperitoneal, Oral
01

Overview

Tretazicar (CB1954) is an antitumor prodrug that is enzymatically activated to generate a bifunctional agent. This activated form creates DNA-DNA interstrand cross-links, which inhibits DNA replication and induces apoptosis in cancer cells. Its activation involves the reduction of its 4-nitro group to a 4-hydroxylamine by enzymes such as NAD(P)H:quinone oxidoreductase 1 (NQO1) or NAD(P)H quinone oxidoreductase 2 (NQO2). Tretazicar has been investigated for its potential in Gene-Directed Enzyme Prodrug Therapy (GDEPT) and has shown selectivity against certain tumor lines.

Other names
5-(aziridin-1-yl)-2,4-dinitrobenzamide
02

Targets

NQO2 (Ribosyldihydronicotinamide dehydrogenase [quinone])NQO1DNA

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