Global Chemical Database

Voclosporin

CAS 515814-01-4

Voclosporin
Voclosporin shows how a one-carbon medicinal-chemistry change can reshape the performance of a celebrated natural-product-derived scaffold.
Voclosporin (CAS 515814-01-4) has a chemical story that connects molecular identity with practical chemistry. Voclosporin is a cyclic-peptide calcineurin inhibitor developed from the cyclosporine scaffold. FDA records list development names including ISA247 and describe a one-carbon modification at amino-acid residue 1 relative to cyclosporine A. The marketed drug substance is enriched to about 90-95% in the trans geometric isomer. The modification changed pharmacodynamic and metabolic behavior while retaining calcineurin inhibition. By suppressing calcineurin-dependent NFAT signaling, voclosporin reduces lymphocyte proliferation and T-cell cytokine production. FDA approved LUPKYNIS in 2021, with background immunosuppressive therapy, for adults with active lupus nephritis.

The exact CAS identity matters because related salts, stereoisomers, intermediates and finished medicines can play very different roles even when their names look closely related.

Its story also shows why synthesis and analytical control belong together: chemists must create the intended structure, distinguish it from process-related species and verify the form actually being handled.
Published: 2026-09-21
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