Calcineurin Inhibitor (CNI)
CNIA class of immunosuppressant drugs that inhibit calcineurin, a calcium-dependent phosphatase required for T-cell activation via the NFAT transcription factor pathway. By blocking IL-2 production, calcineurin inhibitors prevent T-cell proliferation and are the cornerstone of transplant rejection prophylaxis. Major toxicities include nephrotoxicity, neurotoxicity, and diabetogenicity.
Examples
- Cyclosporine — binds cyclophilin to inhibit calcineurin (transplant, psoriasis)
- Tacrolimus — binds FKBP12 to inhibit calcineurin (10-100x more potent than cyclosporine)
- Tacrolimus ointment (Protopic) — topical calcineurin inhibitor (atopic dermatitis)
Did You Know?
A class of immunosuppressant drugs that inhibit calcineurin, a calcium-dependent phosphatase required for T-cell activation via the NFAT transcription factor pathway. By blocking IL-2 production, calcineurin inhibitors prevent T-cell proliferation …