Mizoribine
Mizoribine is an immunosuppressive agent and antimetabolite that is used in organ transplantation and autoimmune diseases. It was first isolated from the culture broth of the bacterium Streptomyces hygroscopicus var. aspergillus in 1974 by the Japanese company Sankyo Co. Ltd..
Mechanism of Action
Mizoribine inhibits the synthesis of DNA and RNA by interfering with the inosine monophosphate dehydrogenase (IMPDH) and guanosine monophosphate synthetase (GMPS) enzymes. This results in the depletion of guanosine triphosphate (GTP) and deoxyguanosine triphosphate (dGTP), which are essential for DNA and RNA synthesis.
Medical Uses
Mizoribine is used in the treatment of nephrotic syndrome, rheumatoid arthritis, and lupus nephritis. It is also used in organ transplantation to prevent graft rejection.
Side Effects
Common side effects of Mizoribine include nausea, vomiting, diarrhea, and leukopenia. In rare cases, it can cause serious side effects such as pancytopenia, hepatotoxicity, and interstitial lung disease.
Pharmacokinetics
Mizoribine is well absorbed after oral administration and has a bioavailability of approximately 90%. It is primarily excreted unchanged in the urine.
See Also
References
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Contributors: Prab R. Tumpati, MD
