mitoguazone

Mitoguazone is a synthetic guanylhydrazone derivative and small molecule antineoplastic agent. It acts primarily as a competitive inhibitor of S-adenosyl-L-methionine decarboxylase (SAMD or AdoMetDC), an enzyme essential for the biosynthesis of polyamines such as spermidine and spermine, which are required for DNA synthesis, cell proliferation, and thymidine kinase production. By inhibiting this enzyme, mitoguazone disrupts polyamine metabolism in tumor cells, leading to decreased cell proliferation, antimitochondrial effects, and induction of p53-independent apoptosis. Mitoguazone has also been shown to inhibit diamine oxidase and induce spermidine/spermine N-acetyltransferase activity. It was investigated in clinical trials from the 1960s onward for various cancers including lymphoma (especially AIDS-related non-Hodgkin's lymphoma), leukemia, multiple myeloma, head and neck cancer, esophageal cancer, prostate cancer, as well as HIV infections. However, its development was discontinued due to significant toxicities such as myelosuppression and mucositis[1][2][3][4][5][6][7].

Brand names

Zyrkamine

Other names

methylglyoxal bisguanylhydrazonemethyl-GAGmethyl Gmitoguazonamitoguazonummitoguazone dihydrochloride