Calcineurin Inhibitors

Calcineurin inhibitors (CNIs) are a class of immunosuppressants utilized to effectively manage various autoimmune disorders, including, but not limited to, lupus nephritis, idiopathic inflammatory myositis, interstitial lung disease, and atopic dermatitis. In addition, they serve as essential components for immunosuppression in solid organ transplantation. CNIs generally bind with high affinity to specific cytoplasmic receptors known as immunophilins, which include cyclophilin and FK-binding proteins. Through targeted inhibition of calcineurin, these medications disrupt the transcription of interleukin-2 and other cytokines within T lymphocytes, thus disrupting the activation, proliferation, and differentiation of T cells. Although their primary effect is on T-helper cells, these inhibitors also concurrently inhibit T suppressor and T cytotoxic cells. This activity illustrates the indications, mechanism of action, and contraindications of CNIs, emphasizing their value in various conditions. This activity also highlights the essential elements such as off-label uses, dosing, pharmacokinetics, monitoring, and relevant interactions of CNIs that are relevant to healthcare professionals across various specialties in their daily clinical practice.