Cyclophosphamide Powder Cas No.50-18-0

Cyclophosphamide is a synthetic nitrogen mustard alkylating agent with broad-spectrum antitumor activity and potent immunosuppressive effects. As a prodrug, it requires hepatic activation in vivo to become active. It inhibits the growth of rapidly proliferating cells (e.g., tumor cells, lymphocytes) by interfering with DNA replication and transcription.

1. Antitumor Function: As a non-specific cell cycle agent, it directly disrupts tumor cell DNA structure, preventing division and proliferation.

2. Immunosuppressive Function: Suppresses the proliferation and function of T lymphocytes and B lymphocytes, thereby regulating abnormal immune responses.

1. Oncology: Widely used to treat various malignancies, including non-Hodgkin lymphoma, Hodgkin lymphoma, multiple myeloma, leukemia, breast cancer, ovarian cancer, and neuroblastoma.

2. Rheumatology and Immunology: Used to treat severe autoimmune diseases unresponsive to other medications, such as systemic lupus erythematosus (particularly lupus nephritis), rheumatoid arthritis, granulomatous polyangiitis, microscopic polyangiitis, and scleroderma.

Cyclophosphamide undergoes oxidative metabolism in the liver via the cytochrome P450 enzyme system, generating the pharmacologically active metabolite 4-hydroxycyclophosphamide. This active metabolite is further transported to target tissues, where it breaks down into phosphoramidite nitrogen mustard with potent alkylating activity. Phosphoramidite nitrogen mustard cross-links with guanine bases on DNA strands, disrupting the double helix structure. This impedes DNA replication, transcription, and RNA synthesis, ultimately causing cell death through disruption of genetic information.

1. Therapeutic Effects:

  • Antitumor Effects: Directly damages tumor cell DNA, inducing tumor shrinkage or regression.

  • Immunosuppressive Effects: Significantly reduces circulating lymphocyte counts and suppresses antibody production, thereby controlling the progression of autoimmune diseases.

2. Adverse Reactions:

  • Myelosuppression: Causes leukopenia and thrombocytopenia, increasing infection and bleeding risks.

  • Urinary Toxicity: The metabolite acrolein may cause hemorrhagic cystitis; long-term use increases bladder cancer risk.

  • Gastrointestinal Reactions: Common nausea, vomiting, and loss of appetite.

  • Reproductive Effects: May cause infertility and amenorrhea.

  • Other: Includes alopecia, oral mucositis, and increased risk of secondary malignancies (e.g., leukemia).