• Corpus ID: 23736856

Preclinical pharmacology of CB30900, a novel dipeptide inhibitor of thymidylate synthase, in mice.

  title={Preclinical pharmacology of CB30900, a novel dipeptide inhibitor of thymidylate synthase, in mice.},
  author={Michael I. Walton and William Gibson and G. Wynne Aherne and N. Lawrence and Trevor C. Stephens and M N Smith and Ann L. Jackman},
  journal={The Journal of pharmacology and experimental therapeutics},
  volume={277 2},
CB30900 is a novel, potent thymidylate synthase inhibitor which can not be polyglutamated and may be active in cancers expressing low or defective folylpolyglutamate synthetase. Pharmacokinetics were studied in mouse tumors and tissues after bolus or infusion protocols. Elimination was triphasic after 100 mg kg-1 i.v. (T 1/2 alpha, 2.8 min; T 1/2 beta, 19.1 min and T 1/2 gamma, 4.1 hr). Peak concentrations were 716 microM; clearance, 1.19 ml g-1 hr-1; and area under the curve (AUC 0-2 hr), 131… 
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