Hydroxychloroquine (sulfate)

Hydroxychloroquine is an aminoquinoline with antimalarial, anti-inflammatory, and antiviral activities.{61135,48566,61136,61137} It is active against the chloroquine-sensitive NF54 and D6 strains of P. falciparum (IC50s = 16.3 and 15 nM, respectively) but has decreased activity against chloroquine-resistant P. falciparum strains (IC50s = 422.7-1,735.3 nM).{61135} Hydroxychloroquine inhibits production of IL-22, IL-17A, and IL-6 induced by phorbol 12-myristate 13-acetate (TPA; Item No. 10008014) and ionomycin (Item No. 10004974) in peripheral blood mononuclear cells (PBMCs) isolated from healthy individuals or patients with systemic lupus erythematosus (SLE) or rheumatoid arthritis (RA).{61136} It inhibits accumulation of sequestosome-1 (SQSTM1) puncta, a marker of autophagy, in mouse embryonic fibroblasts (MEFs) in a concentration-dependent manner.{48566} Hydroxychloroquine reduces viral titers of severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) in the culture supernatant of infected Vero E6 cells but does not reduce SARS-CoV-2 viral titers in an in vitro human airway epithelium model or the respiratory tract of infected cynomolgus macaques.{61137} Formulations containing hydroxychloroquine have been used in the prevention or treatment of malaria, as well as in the treatment of RA and SLE.