Description
Voclosporin, a structurally similar analogue of cyclosporin A, is a new type of calcineurin inhibitor. It has been modified to increase its activity by 3-4 times and exhibits a dual and synergistic mechanism. This drug works by blocking the expression of IL-2 and T cell-mediated immune response, stabilizing renal podocytes. Compared to cyclosporin, voclosporin has the advantage of having less impact on cholesterol and triglycerides and a lower risk of diabetes. In February 2021, vorcyclosporine was approved by the FDA for use in combination immunosuppressive regimens in adult patients with active, lupus nephritis.
Uses
A new agent for the treatment of noninfectious uveitis. Uveitis is an inflammatory, putative Th1-mediated autoimmune disease that affects various parts of the eye and is a leading cause of visual loss. Voclosporin, a rationally designed novel calcineurin inhibitor, exhibits a favorable safety profile, a strong correlation between pharmacokinetic and pharmacodynamic response, and a wide therapeutic window. Immunosuppressant.
Definition
ChEBI: Voclosporin is a homodetic cyclic peptide. It is a semi-synthetic calcineurin (CN) inhibitor that exhibits potent immunosuppressive activity.
Clinical Use
Voclosporin (Lupkynis(TM)) is an oral calcineurin inhibitor immunosuppressant that is being developed by Aurinia Pharmaceuticals. In January 2021, based on positive results from the pivotal phases II and III trials, oral voclosporin received its first approval in the USA for use in combination with a background immunosuppressive therapy regimen for adults with active lupus nephritis.
