Drug intelligence / Profile preview

quinacrine

Development stage
Phase 2
Lead developer
Bayer
Modality
Small Molecules
Administration
Oral, Intracavitary, Intrapleural, Intrauterine
01

Overview

Quinacrine is a synthetic acridine derivative and a structural analog of quinine, originally developed as an antimalarial agent. It was widely used for malaria prevention during World War II but has since been largely replaced by chloroquine and hydroxychloroquine due to better efficacy and safety profiles[5][3]. Quinacrine has also been used as an anthelmintic, in the treatment of giardiasis (a protozoal intestinal infection), certain types of lupus erythematosus (notably cutaneous lupus erythematosus), rheumatoid arthritis, and malignant effusions[2][5]. Its mechanism of action is multifaceted: it intercalates into DNA, inhibiting transcription and translation; inhibits succinate oxidation; interferes with electron transport; suppresses the lupus erythematous cell factor by binding nucleoproteins; acts as a strong inhibitor of cholinesterase; inhibits adenosine uptake into host cells infected with parasites; and blocks incorporation of ATP into RNA/DNA in malarial parasites[2][6][8]. Quinacrine may be preferred in patients at risk for ocular toxicity from other antimalarials or those intolerant to chloroquine derivatives[3].

Brand names
AtabrineQuinacrine
Other names
quinacrine hydrochloridemepacrine hydrochloride
02

Targets

DNAENT (Equilibrative nucleoside transporter family)SDH (Mitochondrial electron transport chain complex II)HSP90 (Heat shock protein 90 chaperone complex)TOP2A (DNA topoisomerase II)AcetylcholinesteraseNucleosome (DNA–histone complex)ND1 (Mitochondrial electron transport chain complex I)PrPSc (Major prion protein)

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