Formulation: A solid
Formal Name: 6-[(2S,3R,4R,6E)-3-hydroxy-4-methyl-2-(methylamino)-6,8-nonadienoic acid]-cyclosporin A
Purity: ≥98%
Formula Markup: C63H111N11O12
Formula Weight: 1214,6
Shelf life (days): 1460
CAS Number: 515814-01-4
Notes: Voclosporin is an immunosuppressant and a derivative of cyclosporin A (Item No. 12088).{69624,69625} It binds to cyclophilin A (Kd = 15 nM) and inhibits calcineurin activity in isolated human whole blood (IC50 = 120 ng/ml). Voclosporin reduces the proliferation of, and production of IL-2, IFN-γ, and TNF-α in, isolated cynomolgus monkey lymphocytes (EC50s = 202.79, 135.32, 177.11, and 138.56 ng/ml, respectively).{69626} It decreases disease severity in a rat model of experimental autoimmune uveoretinitis induced by interphotoreceptor retinoid-binding protein (IRBP), also known as retinoid binding protein 3 (RBP3), when administered at doses ranging from 2.5 to 40 mg/kg.{69627} Voclosporin (1.75 mg/kg) increases graft survival in a rat model of heterotopic heart transplantation.{69625} Unlike cyclosporin A, voclosporin does not increase serum creatinine levels in rabbits. Voclosporin also inhibits the replication of severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) in infected Calu-3 cells in a concentration-dependent manner.{69628} Formulations containing voclosporin have been used in the treatment of lupus nephritis.
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