Drug intelligence / Profile preview

acriflavine

Development stage
Unknown
Modality
Small Molecules
Administration
Topical
01

Overview

Acriflavine is a synthetic acridine dye and small molecule that functions as a topical antiseptic and antibacterial agent. First synthesized in 1912 by Paul Ehrlich, it was historically used for wound disinfection and treatment of sleeping sickness. Acriflavine acts primarily by intercalating into DNA, thereby interfering with cellular processes such as replication and transcription. It also inhibits protein kinases and topoisomerases I/II. More recently, it has been identified as a potent inhibitor of hypoxia-inducible factor-1 (HIF-1) dimerization by binding directly to the PAS-B domain of HIF-1α and HIF-2α subunits, suppressing tumor growth and angiogenesis[2][5][6]. Acriflavine additionally exhibits antiviral activity through inhibition of viral proteases such as the papain-like protease (PLpro) in SARS-CoV-2[8]. Commercial preparations are often mixtures containing trypaflavine (3,6-diamino-10-methylacridinium chloride) and proflavine (3,6-diaminoacridine)[2][8].

Other names
acriflavinium chloridetrypaflavineproflavine
02

Targets

DNATOP1 (DNA Topoisomerase I)TOP2A (DNA topoisomerase II)HIF1A (Hypoxia-inducible factor 1-alpha)EPAS1 (Hypoxia-inducible factor 2-alpha)PLpro (Papain-like protease)

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