Chloroquine is an antimalarial drug used to treat susceptible infections with P. vivax, P. malariae, P. ovale, and P. falciparum. It is also used for second line treatment for rheumatoid arthritis. Chloroquine is an aminoquinolone derivative first developed in the 1940s for the treatment of malaria.
- Mechanism
- Curator reviewed · 10 references
Chloroquine inhibits the action of heme polymerase in malarial trophozoites, preventing the conversion of heme to hemazoin. Plasmodium species continue to accumulate toxic heme, killing the parasite.
Chloroquine passively diffuses through cell membranes and into endosomes, lysosomes, and Golgi vesicles; where it becomes protonated, trapping the chloroquine in the organelle and raising the surrounding pH. The raised pH in endosomes, prevent virus particles from utilizing their activity for fusion and entry into the cell.
Chloroquine does not affect the level of ACE2 expression on cell surfaces, but inhibits terminal glycosylation of ACE2, the receptor that SARS-CoV and SARS-CoV-2 target for cell entry. ACE2 that is not in the glycosylated state may less efficiently interact with the SARS-CoV-2 spike protein, further inhibiting viral entry.
- Primary indication
- Chloroquine is indicated to treat infections of P. vivax, P. malariae, P. ovale, and susceptible strains of P. falciparum.Curator reviewed · 9 structured indications
- Formula / weight
- C18H26ClN3 · 319.872 g/mol (avg)
- First approval
- Canada, 2001 · United States, 1972
- Also known as
- Chloraquine · Chloroquina · Chloroquinium
Resolves to
WHTVZRBIWZFKQO-UHFFFAOYSA-NSMILESCCN(CC)CCCC(C)NC1=CC=NC2=CC(Cl)=CC=C12What you can answer from here — as of September 30, 2026
Which drugs share a target with Chloroquine, and which of those have an active Phase 3 trial?
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