What is the MOA of MMF? MMF is an inactive prodrug that is hydrolyzed to active MPA. MPA is a reversible inhibitor of inosine-5’-monophosphate dehydrogenase (IMPDH), which is an enzyme necessary for the de novo synthesis of the purine, guanosine. Lymphocytes (T and B cells) depend on IMPDH to generate sufficient guanosine levels to initiate …
What is mycophenolic acid? MPA (Myfortic) is enteric-coated, delayed-release mycophenolate sodium. It comes in 180-mg and 360-mg delayed-release tablets. Dose conversion is 360 mg of Myfortic is equivalent to 500 mg of MMF. Some patients will tolerate Myfortic when they have experienced severe GI side effects with MMF. Cost of 720 mg BID is $280/month …
Mechanism of action and metabolism of AZA AZA is a prodrug converted to 6-MP, which is then converted to thiopurine nucleotides (6-TGN), which decrease de novo synthesis of purine nucleotides with resultant inhibition of DNA, RNA, and protein synthesis. This results in both cytotoxicity and decreased cellular proliferation. 6-TGN metabolite levels can be measured within …
How is MMF supplied and used? • Available formulations: 250-mg, 500-mg capsules; oral suspension (200 mg/mL) and intravenous (IV) form (500 mg/20 mL) available. • Side effects: GI (especially diarrhea 25%), leukopenia, anemia, hepatotoxicity, infections (Pneumocystis jirovecii, progressive multifocal leukoencephalopathy, herpes zoster, and CMV); lymphoproliferative malignancies (Epstein–Barr virus [EBV]-associated). • Dosage: 500 to 1500 mg two times a …
What rheumatic diseases are commonly treated with AZA? • Rheumatoid arthritis (RA; less effective than methotrexate [MTX] and slower onset). • Systemic lupus erythematosus (SLE). • Idiopathic inflammatory myopathies (polymyositis, dermatomyositis, necrotizing myopathies). • Behçet’s syndrome. • Antineutrophil cytoplasmic antibody (ANCA)-associated vasculitis (remission maintenance). • Many other rheumatic diseases (in an attempt to decrease glucocorticoid dosage). Pearl: AZA is more effective as …
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How is AZA used? • Available formulations: 50-mg tablets (Imuran), 75-mg tablets (Azasan), 100-mg/20-mL vial. • Side effects: bone marrow depression, nausea, vomiting, skin rash, malignancy (some studies show lymphoma increased two times), hepatotoxicity (liver enzymes mildly increased in 33%, isolated hyperbilirubinemia , severe toxicity is rare), infections (herpes zoster, cytomegalovirus [CMV]), pancreatitis, hypersensitivity syndrome (rash, fever, …
time, cost, and success rate of developing a new drug for treating a rheumatic disease It takes 10 years and $1 to $2 billion from the time a new drug is tested in mice until it makes it to the market. • Preclinical phase (efficacy, toxicity, and pharmacokinetics in animals): only 2% of new drugs tested …
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