Cytoxan alkylating agent

Cyclophosphamide (Cytoxan) is the most versatile and useful of the nitrogen mustards. Preclinical testing showed it to have a favorable therapeutic index and to possess the broadest spectrum of antitumor activity of all alkylating agents. As with the other nitrogen mustards, cyclophosphamide administration results in the formation of cross-links within DNA due to a reaction of the two chloroethyl moieties of cyclophosphamide with adjacent nucleotide bases. Cyclophosphamide must be activated metabofically by microsomal enzymes of the cytochrome P450 system before ionization of the chloride atoms and formation of the cyclic ethylenimmonium ion can occur. The metabolites phosphoramide mustard and acrolein are thought to be the ultimate active cytotoxic moiety derived from cyclophosphamide. 

Clinical Use. Cyclophosphamide (Cytoxan, Neosar) is an anticancer alkylating agent that is commonly used in a variety of neoplastic disorders (see Chapter 36). This drug may also be helpful in suppressing the immune response in certain autoimmune diseases, such as multiple sclerosis, systemic lupus erythematosus, and rheumatoid arthritis.12 43 High doses of cyclophosphamide are also used to prevent tissue rejection in patients receiving bone marrow transplants and other organ transplants. 

As an alkylating agent, cyclophosphamide (Cytoxan) and its active metabolites destroy the rapidly proliferating lymphocytes and, hence, are potent immunosuppressive agents. Those metabolites that are devoid of alkylating properties also lack an immunosuppressive capability. Because the... 

Alkylating agents interfere with DNA replication and transcription, resulting in depression of T- and/or B-cell populations. The most commonly used alkylating agents in uveitis management include cyclophosphamide (Cytoxan ) and chlorambucil (Leukeran ). 

Mustard is an alkylating agent similar to drugs that have been used in cancer chemotherapy, such as nitrogen mustards, Cytoxan, and cis-platin. Since DNA is one of mustard s most sensitive targets, it is not surprising that carcinogenesis and radiomimetic effects are seen. ... 

ALKYLATING AGENTS Cyclophosphamide (cytoxan, neosar) is an effective cytotoxic and immunosuppressive agent. 

Cyclophosphamide Cytoxan Neosar Cytophosphan Endoxan Clafen Oxazaphosphorine alkylating agent ( Nitrogen mustard ) mp 143 °C Treatment of lymphomas leukemias, multiple myeloma, and other cancers n O. NH C1 C1... 

Cyclophos- phamide (Cytoxan) Not phase-specific Metabolized to phosphoramide mustard, which is a DNA alkylating agent. ... 

Cyclo- phosphamide (e.g., Cytoxan) PRODRUG is converted by liver to an alkylating agent which crosslinks DNA. Proliferation of B-cells is inhibited more than T-cells. May also attack immunocompetent lymphocytes to inhibit established immune respones. Drug of choice for Wegener s granulomatosis. Also used for severe rheumatoid arthritis autoimmune blood disorders. Alopecia, Gl distress, hemorrhagic cystitis of the bladder, bone marrow depression. 

Cyclophosphamide (Cytoxan), an alkylating agent widely used for the treatment of various malignancies, offers an... 

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