Alkylating agents sarcomas

A variety of other therapeutic compounds have mechanisms that probably involve alkylation. Procarbazine and dacarbazine are the two most successful agents in this group. Dacarbazine is a synthetic compound that functions as an alkylating agent, following metabolic activation by liver microsomal enzymes, to yield diazomethane. It has been used successfully in the treatment of sarcomas. 

Dacarbazine is converted to an active metabolite that is thought to be an alkylating agent. It has been used to treat metastatic melanoma and, in combination regimens, soft-tissue sarcomas and Hodgkin s disease. 

Ifosfamide is an alkylating agent belonging to the group of oxazaphosphorines. It is used to treat a variety of solid tumors in children, including rhabdomyosarcoma, soft tissue sarcomas, Wilms tumor, bone sarcomas, and neuroblastoma, and leukemias and lymphomas in adults. It is also sometimes used in combination with other drugs, such as doxorubicin or cisplatin and etoposide. 

Trade names Carboplat Carbosin Ercar Oncocarbin Paraplatin (Bristol-Myers Squibb) Paraplatine Indications Various carcinomas and sarcomas Category Alkylating agent Antineoplastic Half-life terminal 22—40 hours... 

Indications Cancers, sarcomas, leukemias, lymphomas Category Alkylating agent Half-life 4-15 hours... 

Polymer (VI) has been shown to have antitumor activity against adenocarcinoma 755, Dunning ascites leukemia. Friend leukemia virus, and Lewis lung carcinoma. In the latter case, polymer (VI) showed activity about equal to that of cyclophosphamide (an alkylating agent) and was more effective than 6-mercaptopurine (an antimetabolite) ( ). The DIVEMA polymer (V) Is also active against some cancer causing viruses such as Friend leukemia, Moloney sarcoma and Rauscher leukemia ( ). 

In summary, ifosfamide, an alkylating agent with anti-neoplastic properties (1.2 g/mVday fV for 5 days), is indicated in the treatment of testicular cancer. In addition, ifosfamide has been used in lung cancer, Hodgkin s and non-Hodgkin s lymphoma, breast cancer, acute and chronic lymphocytic leukemia, ovarian cancer, and sarcomas. 

Uracil mustard, an alkylating agent with antineoplastic activity (1 to 2 mg p.o. daily for three months), is indicated in treatment of chronic lymphocytic and myelocytic leukemia Hodgkin s disease, non-Hodgkin s lymphomas of the histiocytic and lymphocytic types reticulum cell sarcoma lymphomas mycosis fungoides polycythemia vera and ovarian, cervical, and lung cancer. 

ShimoyamaM (1975) The cytocidal action of alkylating agents and anticancer antibodies against in-vitro cultured Yoshida ascites sarcoma cells. J Jpn Soc Cancer Ther 10 63-72... 

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