Mechanism of Action

Voclosporin is a structural analog of cyclosporine A, with an additional single carbon extension that has a double-bond on one side chain.

The binding affinities of voclosporin and cyclosporine A for cyclophilin are comparable; however, upon binding, the ethynyl side chain of voclosporin induces structural changes in calcineurin that may result in increased immunosuppressive activity relative to cyclosporine A.

Binding to Calcineurin Occurs Through the Latch Region of Voclosporin

Voclosporin Forms a Heterodimeric Complex With Cyclophilin A that Binds to and Inhibits Calcineurin