Mizoribine

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

• Immunosuppressive drugs
• Antimetabolites
• Organ transplantation
• Autoimmune diseases