↓ Size/lymphoid content of lymph nodes & spleen; Interferes w. cell cycle of activated lymphoid cells;

↓ primary antibody response

Iatrogenic Cushing’s syndrome

Cataracts, fat redistribution, glaucoma, muscle wasting, peptic ulcers

Rheumatoid arthritis, modulate allergic reactions, asthma, organ/ stem cell transplants

Blocks antigen receptor-induced differentiation of T cells. Binds to cyclophilin and forms a complex that inhibits calcineurin which is necessary for the activation of NF-AT, a T-cell transcription factor involved in synthesis of IL-2

Nephrotoxicity, hypertension,

hyperglycemia, liver dysfunction,

hyperkalemia, altered mental status, seizures

gingival hyperplasia, hirsutism

Organ transplantation, graft-versus-host disease after hematopoietic stem cell transplant, select autoimmune diseases

Immunosuprressant macrolide antibiotic. Binds to immunophilin FK-binding protein (FKBP) and forms a complex that inhibits calcineurin (like cyclosporine)

Nephrotoxicity, neurotoxicity,

hyperglycemia, hypertension,

hyperkalemia

Organ & stem cell

transplants, graft vs. host,

atopic dermatitis, psoriasis

Binds to FK506-binding protein 12, forming a complex that blocks the molecular target of rapamycin (mTOR), a key part of a signaling pathway for cell growth, angiogenesis, and metabolism. Leads to inhibition of T-cell, and possibly B cell, proliferation.

Myelosuppression (esp.

thrombocytopenia), hepatotoxicity, diarrhea,

hypertriglyceridemia,

pneumonitis

Solid organ allografts, graft vs. host in hematopoietic stem cell transplant, dermatologic disorders, uveoretinitis, estenosis

Inhibits T- and B-lymphocyte responses by

inhibiting purine synthesis

Hypertension, reversible

Myelosuppression (neutropenia)

organ transplants, IBS, chronic allograft vasculopathy (cardiac transplant), graft vs. host, lupus nephritis, rheumatoid arthritis,

Inhibits angiogenesis, anti-inflammatory, immunomodulatory effects.

Inhibits TNF-α, ↓phagocytosis by neutrophils, ↑production of IL-10, alters adhesion molecules expression, enhances cell-mediated immunity via interactions with T-cells

Very teratogenic!

Fetal abnormalities

Peripheral neuropathy,

constipation, hypothyroidism,

increased risk of DVT

Rx: multiple myeloma, leprosy, erythema

nodosum leprosum, lupus

CI: pregnancy

Antimetabolite; interferes with purine metabolism at steps required for the wave of lymphoid cell proliferation following antigenic stimulation. Block cellular immunity and primary and secondary antibody responses.

Bone marrow suppression

(leukopenia, anemia,

thrombocytopenia)

Maintain renal allografts, acute glomerulonephritis, lupus erythematosus, rheumatoid arthritis, Crohn’s disease, multiple sclerosis

Alkylating agent

Destroys proliferating lymphoid cells and

alkylates some resting cells.

Pancytopenia, hemorrhagic

cystitis, cardiac toxicity

Autoimmune disorders (lupus), bleeding syndromes (acquired factor XIII antibodies), autoimmune hemolytic anemia, Ab-induced pure red cell aplasia,

Wegener's granulomatosis

Inhibits pyrimidine synthesis

Elevation of liver enzymes

(potential liver damage), renal

impairment, teratogenic effects

rheumatoid arthritis

(CH 36) Folate analog

Inhibits dihydrofolate reductase

Hepatotoxicity, mucositis, bone marrow depression w/ leukopenia & thrombocytopenia

rheumatoid arthritis, graft vs. host

Monoclonal antibody against T-cell surface protein CD3.  Blocks killing by cytotoxic T cells and other T cell functions.

Renal transplant rejection

Bind TNF-α, a proinflammatory cytokine.

Suppresses downstream inflammatory cytokines (IL-1, IL-6)

Completely human IgG₁

Increased risk of lymphoma

 Rheumatoid arthritis

Bind TNF-α, a proinflammatory cytokine.

Suppresses downstream inflammatory cytokines (IL-1, IL-6) & adhesion molecules for leukocyte activation & migration.

Dimeric fusion IgG₁

Increased risk of lymphoma

Adult rheumatoid arthritis, juvenile

rheumatoid arthritis, psoriatic arthritis

Bind TNF-α, a proinflammatory cytokine.

Suppresses downstream inflammatory cytokines (IL-1, IL-6) & adhesion molecules for leukocyte activation & migration.

Human-mouse chimeric IgG₁

Increased risk of lymphoma

Crohn's disease, ulcerative colitis,

rheumatoid arthritis, ankylosing spondylitis, psoriatic arthritis

Inhibits T-cell activation by binding to cell surface CD2, thus inhibiting normal  CD2/LFA-3 interaction

Reduced # of circulating T cells

Monitor CD4 count and T cell levels

Plaque psoriasis

Chimeric mouse-human IgG₁

Binds to CD25, the IL-2 receptor α chain on

activated lymphocytes. It therefore acts as an IL-2 antagonist, blocking it from binding to activated lymphocytes

prophylaxis of acute organ rejection in renal transplant, immunosuppressive regimen with glucocorticoids & cyclosporine

Humanized IgG1

Binds to the α subunit of the IL-2 receptor, blocking it from binding to activated lymphocytes

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Same as basiliximab