Dianhydrogalactitol (NSC-132313): Pharmacokinetics in Normal and Tumor-Bearing Rat Brain and Antitumor Activity Against Three Intracerebral Rodent Tumors 2
- 1 March 1976
- journal article
- research article
- Published by Oxford University Press (OUP) in JNCI Journal of the National Cancer Institute
- Vol. 56 (3) , 535-539
- https://doi.org/10.1093/jnci/56.3.535
Abstract
Dianhydrogalactitol (DAG; NSC-132313), a hexitol epoxide, was used to treat intracerebral rodent tumors. DAG was most active against the murine ependymoblastoma [treated/controls (TIC)>440%], less active against murine glioma 26 (T/C≈112–150%), and least active against rat 9L gliosarcoma (T/C=100%). Application of a two-compartment open model for plasma disappearance of HC-DAG in rats gave a volume of distribution at steady state of approximately 872 ml, a clearance of approximately 9.4 ml/minute, and an elimination constant of 0.025/minute. Entry of 14C-DAG was more rapid into the 9L tumor than into the normal brain. When a two-compartment series model for brain and tumor entry was applied, the t1/2 (half-time) for compartmental equilibrium was approximately 22 and 105 minutes in the brain, and 4 and 56 minutes in the 9L tumor. The drug rapidly entered the brain and tumor intracellular compartments. Binding to RNA was linear with time, and the absolute amount of binding...Keywords
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