Immunosuppressants Matcher

Reference Table

Drug	Mechanism	Indications	Toxicity	Notes
Cyclosporine	Calcineurin inhibitor; binds cyclophilin. Blocks T-cell activation by preventing IL-2 transcription.	Psoriasis, rheumatoid arthritis.	Nephrotoxicity, hypertension, hyperlipidemia, neurotoxicity, gingival hyperplasia, hirsutism.	Both calcineurin inhibitors are highly nephrotoxic.
Tacrolimus (FK506)	Calcineurin inhibitor; binds FK506 binding protein (FKBP). Blocks T-cell activation by preventing IL-2 transcription.	Immunosuppression after solid organ transplant.	Similar to cyclosporine, risk of diabetes and neurotoxicity; no gingival hyperplasia or hirsutism.	Highly nephrotoxic, especially in high doses or patients with ↓ renal function.
Sirolimus (Rapamycin)	mTOR inhibitor; binds FKBP. Blocks T-cell activation and B-cell differentiation by preventing response to IL-2.	Kidney transplant rejection prophylaxis.	"Pansirtopenia" (pancytopenia), insulin resistance, hyperlipidemia; not nephrotoxic.	Kidney "sir-vives." Synergistic with cyclosporine. Also used in drug-eluting stents.
Basiliximab	Monoclonal antibody; blocks IL-2R.	(See Sirolimus note regarding Sir Basil's Kidney Transplant)	Edema, hypertension, tremor.	(N/A in this table)
Azathioprine	Antimetabolite precursor of 6-mercaptopurine. Inhibits lymphocyte proliferation by blocking nucleotide synthesis.	Rheumatoid arthritis, Crohn disease, glomerulonephritis, other autoimmune conditions.	Pancytopenia.	6-MP degraded by xanthine oxidase; toxicity ↑ by allopurinol.
Mycophenolate mofetil	Reversibly inhibits IMP dehydrogenase, preventing purine synthesis of B and T cells.	Glucocorticoid-sparing agent in rheumatic disease.	GI upset, pancytopenia, hypertension. Less nephrotoxic and neurotoxic.	Associated with invasive CMV infection.
Glucocorticoids	Inhibit NF-κB. Suppress both B- and T-cell function by ↓ transcription of many cytokines. Induce T cell apoptosis.	Many autoimmune and inflammatory disorders, adrenal insufficiency, asthma, CLL, non-Hodgkin lymphoma.	Cushing syndrome, osteoporosis, hyperglycemia, diabetes, amenorrhea, peptic ulcers, psychosis, cataracts, avascular necrosis.	Demargination of WBCs causes artificial leukocytosis. Adrenal insufficiency if stopped abruptly.