Alkylating cytostatic agents—nitrosoureas and N -lost derivatives


See also Cytotoxic and immunosuppressant drugs

General information

Alkylating cytostatic drugs include:

  • Nitrosoureas: carmustine, lomustine, nimustine, streptozocin.

  • N -lost derivatives: bendamustine, chlormethine, cyclophosphamide, estramustine.

  • Others: busulfan, chlorambucil, dacarbazine, ifosfamide, melphalan, mitobronitol, mitomycin, procarbazine, thiotepa, temozolomide, treosulfan.

The first two groups (apart from cyclophosphamide) are covered in this monograph.

Nitrosoureas

Carmustine (BCNU) is used to treat myeloma, lymphomas, breast cancer, and brain tumors, topical carmustine has been used to treat mycosis fungoides [ ].

Lomustine (CCNU) is used to treat lymphomas and some solid tumors, particularly brain tumors, often in combination with procarbazine and vincristine [ ].

Nimustine (ACNU) is used to treat malignant glioma [ ].

Streptozocin (streptozotocin) is produced by Streptomyces achromogenes . It is used to treat metastatic islet cell carcinoma of the pancreas, but because of its high nephrotoxic and emetogenic potential should be reserved for patients with symptomatic or progressive disease.

N -lost derivatives

Bendamustine is used to treat non-Hodgkin's lymphoma, multiple myeloma, and chronic myelocytic leukemia in patients for whom fludarabine combination chemotherapy is not suitable.

Chlormethine (mechlorethamine, mustine, nitrogen mustard) is mainly used topically in the early stages of mycosis fungoides [ ].

Cyclophosphamide (see separate monograph) is used in the treatment of various solid tumors, and as an immunosuppressant in conditions such as Wegener’s granulomatosis and in conditioning regimens for bone marrow transplantation.

Estramustine is a conjugated derivative of estradiol and chlormethine, mainly used to treat prostate cancer [ , ].

Organs and systems

Respiratory

Carmustine pulmonary toxicity is well documented. Eight patients developed interstitial pulmonary fibrosis 12–17 years after exposure to carmustine in a total dose of carmustine of 770–1410 mg/m 2 [ ].

Lung fibrosis has been described in a long-term follow up 13–17 years after treatment of 31 children given carmustine for brain tumors; six died, and of eight still available for study, six had upper zone fibrotic changes of their lungs on X-ray [ ].

You're Reading a Preview

Become a Clinical Tree membership for Full access and enjoy Unlimited articles

Become membership

If you are a member. Log in here