Voclosporin is a calcineurin inhibitor for the treatment of lupus nephritis (LN) in patients diagnosed with systemic lupus erythematosus (SLE). LN is a significant cause of renal failure, morbidity, and death in patients with SLE.
- Mechanism
- Curator reviewed · 3 references
Through the inhibition of calcineurin, voclosporin blocks IL-2 expression and T-cell mediated immune responses, stabilizing podocytes in the kidneys.
Voclospoprin is a cyclosporine A analog. It is structurally similar to cyclosporine A (CsA) with the exception of an amino acid modification in one region. This modification changes the binding of voclosporin to calcineurin. Cyclosporine inhibitors reversibly inhibit T-lymphocytes. They also inhibit lymphokine production and release. Cyclosporine A exerts its inhibitory effects on T-lymphocytes by binding to cyclophilin. A cyclophilin-cyclosporine complex is formed, leading to the inhibition of calcium- and calmodulin-dependent serine-threonine phosphatase activity of calcineurin. Along with calcineurin inhibition, the inhibition of many transcription factors necessary for the induction of various cytokine genes such as IL-2, IFN-γ, IL-4 and GM-CSF occurs. This, in turn, reduces inflammation, treating renal glomerulonephritis associated with systemic lupus erythematosus.
- Primary indication
- Voclosporin is used in combination with a background immunosuppressive regimen for the treatment of lupus nephritis.Curator reviewed · 1 structured indication
- Formula / weight
- C63H111N11O12 · 1214.646 g/mol (avg)
- First approval
- United States, 2021 · European Union, 2022
- Also known as
- Lupkynis
- Code names
- ISA-247 · ISATX-247 · LX-211 · R 1524
- Brand names
Resolves to
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Which drugs share a target with Voclosporin, and which of those have an active Phase 3 trial?
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