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Description: An alkylating agent of value against both hematologic malignancies and solid tumors. [PubChem]
Drug Type: Small Molecule; Approved
Pharmacology: Lomustine is an alkylating agent of the nitrosourea type. Lomustine and its metabolites interferes with the function of DNA and RNA. It is cell cycle–phase nonspecific. Cancers form when some cells within the body multiply uncontrollably and abnormally. These cells then spread and destroy nearby tissues. Lomustine acts by slowing this process down. It kills cancer cells by damaging the DNA (the genetic material inside the cells) and stops them from dividing.
Mechanism of Action: Lomustine is a highly lipophilic nitrosourea compound which undergoes hydrolysis in vivo to form reactive metabolites. These metabolites cause alkylation and cross-linking of DNA. Other biologic effects include inhibition of DNA synthesis and some cell cycle phase specificity. Nitrosureas generally lack cross-resistance with other alkylating agents.
Indication: Indicated primarily for the treatment of brain tumours. Also for the treatment of breast cancer, Hodgkin's disease, lung cancer, malignant melanoma, multiple myeloma, Non-Hodgkin's lymphomas, ovarian cancer, pancreatic cancer, and renal cell cancer.
Half Life: Approximately 94 minutes, however the metabolites have a serum half-life of 16 to 48 hours.
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Individual Studies
  • Liver Pharmacology and Xenobiotic Response Repertoire

    Rattus norvegicus Rattus norvegicus | RNA Expression   RNA Expression

    A definition of RNA expression changes that correlate with liver response programs and an understanding of the similarities and differences in responses to different classes of chemicals would aid in new chemical or drug characterization and add to our understanding of liver biology.

    Authors: Natsoulis G, Pearson CI, Gollub J et al.

    Organization: Iconix Biosciences 325 E. Middlefield Rd…

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Thought leaders and organizations working on research involving 1-(2-chloroethyl)-3-cyclohexyl-1-nitrosourea.

  • V Gadjeva
  • D J Reed
  • C Pueyo
  • H E May
  • M Weller
  • Children's Oncology Group
  • M.D. Anderson Cancer Center
  • Memorial Sloan-Kettering Cancer Center
  • Radiation Therapy Oncology Group
  • AstraZeneca
  • University of Washington
  • Universidad de Córdoba
  • University of Manchester
  • Trakia University
  • University of Tuebingen

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