Drug intelligence / Profile preview

apaziquone

Development stage
Phase 3
Lead developer
Assertio
Modality
Metabolically Activated Prodrugs → Prodrugs/Conditional Activator Small Molecules → Small Molecules
Administration
Intravesical
01

Overview

Apaziquone is a fully synthetic indolequinone bioreductive prodrug and analog of mitomycin C with potential antineoplastic and radiosensitizing activities. It is designed to be activated in hypoxic tumor cells by intracellular reductases, particularly NAD(P)H:quinone oxidoreductase 1 (NQO1), which are present at higher levels in these cells. Upon activation, apaziquone forms cytotoxic species that can alkylate and crosslink DNA, leading to apoptosis. This mechanism is especially effective under hypoxic conditions commonly found in tumors. Apaziquone has been primarily developed for intravesical treatment of non-muscle invasive bladder cancer (NMIBC) following transurethral resection of bladder tumors (TURBT). The drug shows minimal systemic absorption when administered intravesically, resulting in few systemic side effects[1][2][5][6][7].

Brand names
EoquinNeoquinQapzola
Other names
apaziquone
02

Targets

DNANQO1

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