An Overview of Cyclophosphamide


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An Overview of Cyclophosphamide 

Cyclophosphamide is a nitrogen mustard derivative that enters the human body and is hydrolyzed by excess phosphoramidase or phosphatase present in the liver or tumor to become an activated phosphoramidite mustard. The broad anti-tumor spectrum is the first so-called "latent" broad-spectrum anti-tumor drug that is effective against both leukemia and solid tumors.

This product has no activity in vitro, mainly through the hydrolysis of liver P450 enzyme to aldehyde phosphoramide and then into the tissue to form phosphoramide nitrogen mustard and play a role. Cyclophosphamide can be deactivated by dehydrogenase to carboxyphosphoramide, or excreted in the form of acrolein, leading to urinary tract toxicity. It belongs to the cycle non-specific medicine, and its mechanism of action is the same as that of nitrogen mustard.

On October 27, 2017, the World Health Organization’s International Agency for Research on Cancer published a preliminary list of carcinogens, and cyclophosphamide was included in the list of carcinogens.


  1. As an antitumor drug, used in malignant lymphoma, multiple myeloma, breast cancer, small cell lung cancer, ovarian cancer, neuroblastoma, retinoblastoma, Ewing's sarcoma, soft tissue sarcoma, acute leukemia and chronic lymphoma Cellular leukemia, etc. It also has a certain effect on testicular tumors, squamous cell carcinoma of the head and neck, nasopharyngeal carcinoma, rhabdomyosarcoma, and osteosarcoma. At present, it is often combined with other anti-cancer drugs to form a combined chemotherapy regimen.
  2. As an immunosuppressant, used in various autoimmune diseases, such as severe rheumatoid arthritis, systemic lupus erythematosus, childhood nephrotic syndrome, multiple granuloma, pemphigus, ulcerative colitis, idiopathic Thrombocytopenic purpura, etc. It is also used for anti-rejection during organ transplantation, usually in combination with prednisone and anti-lymphocyte globulin.
  3. This medicine eye drops can be used for erosive corneal ulcers after pterygium and corneal transplantation.

Clinical application

Oral: 50~100mg/time, 2~3 times/day, the total amount of one course of treatment is 10~15g. Intravenous injection: 0.2 g/time, once a day or every other day; or 0.6 to 0.8 g/time, once a week, for a total treatment course of 8 to 10 g.

Adverse reactions

Bone marrow suppression (minimum 1 to 2 weeks, generally maintained for 7 to 10 days, 3 to 5 weeks to recover), hair loss, gastrointestinal reactions, stomatitis, cystitis, pneumonia, excessive antidiuretic hormone (ADH) secretion have been reported Wait. The general dose has little effect on platelets and rarely causes anemia. In addition, cyclophosphamide can kill sperm, but it is reversible. Ultra high dose (>120mg/kg) can cause myocardial damage and nephrotoxicity.


This product can cause hemorrhagic cystitis, drink plenty of water, and use mesna to antagonize if necessary.

Attention should be paid to cystitis when CTX is administered in large quantities. It should be used with caution in patients with history of gout, history of urinary stones, or renal impairment.

Drug contraindications

Those who are allergic to this product, pregnant and lactating women are prohibited. Infection, liver and kidney function damage are prohibited or used with caution.

medicine interactions

  1. CTXcan increase the serum uric acid level. It is equivalent to anti-gout drugs such as allopurinol. The dosage of anti-gout drugs should be adjusted. Allopurinol can increase the bone marrow toxicity of CTX, as if it should be closely observed for its toxic effects.
  2. With high-dose barbiturate or corticosteroids can increase acute toxicity.
  3. The same with doxorubicin can increase cardiotoxicity; the total dose of doxorubicin should not exceed 400mg/m.

Note: The above content is for introduction only. Drug use must be carried out under the guidance of a doctor in a regular hospital.

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