Desethylchloroquine

Desethylchloroquine is an active metabolite of chloroquine (Item Nos. 14194 | 30708) and hydroxychloroquine (Item Nos. 17911 | 30709).^1,2 It is formed from chloroquine and hydroxychloroquine by the cytochrome P450 (CYP) isoforms CYP2C8, CYP3A4, and CYP2D6. Desethylchloroquine (20 µM) inhibits Zika virus-induced plaque formation in Vero cells when used during viral entry or post-entry.³ It protects against the cytopathic effect (CPE) of Zika virus strains PLCal_ZV, MR 766, and PRVABC59 in Vero cells (EC₅₀s = 7.01, 10.15, and 10.72 µM, respectively). Desethylchloroquine also inhibits the growth of the chloroquine-sensitive P. falciparum strain LA 136 with a reduction in activity against the multidrug-resistant P. falciparum Smith strain in vitro (IC₅₀s = 7.8 and 210 ng/ml, respectively).⁴

WARNING This product is not for human or veterinary use.

1. Projean, D., Baune, B., Farinotti, R., et al. In vitro metabolism of chloroquine: Identification of CYP2C8, CYP3A4, and CYP2D6 as the main isoforms catalyzing N-desethylchloroquine formation. Drug Metab. Dispos. 31(6), 748-754 (2003).

2. Paludetto, M.N., Kurkela, M., Kahma, H., et al. Hydroxychloroquine is metabolized by cytochrome P450 2D6, 3A4, and 2C8, and inhibits cytochrome P450 2D6, while its metabolites also inhibit cytochrome P450 3A in vitro. Drug Metab. Dispos. 51(3), 293-305 (2023).

3. Han, Y., Pham, H.T., Xu, H., et al. Antimalarial drugs and their metabolites are potent Zika virus inhibitors. J. Med. Virol. 91(7), 1182-1190 (2019).

4. Aderounmu, F.A. In vitro assessment of the antimalarial activity of chloroquine and its major metabolites. Ann. Trop. Med. Parasitol. 78(6), 581-585 (1984).