Drug intelligence / Profile preview

azonafide

Development stage
Preclinical
Lead developer
Oncolinx
Modality
Small Molecules
Administration
Intravenous
01

Overview

Azonafide is a synthetic anthracene-based antitumor small molecule that serves as the parent compound of a series of benzisoquinolinedione “azonafide” derivatives and as a highly potent payload for antibody-drug conjugates. It is structurally related to the naphthalimide amonafide but lacks the primary amine and incorporates an anthracene chromophore, and, like amonafide, functions as a DNA-intercalating topoisomerase II inhibitor that induces DNA damage and tumor cell death while retaining activity in multidrug-resistant models.[4][2][5][10] Azonafide and its derivatives have shown broad preclinical anticancer activity across multiple tumor types, including leukemias, breast cancer, melanoma, lung cancer, renal cell carcinoma, ovarian cancer, and others, and more recently have been developed as ADC payloads designed to trigger immunogenic cell death and stimulate antitumor immunity when selectively delivered to malignant cells.[2][4][5][8][9][10]

02

Targets

DNATOP2A (DNA topoisomerase II)TOP2B (DNA topoisomerase II beta)

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