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systemic radioprotection

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ProCertus has patented a new family of low molecular weight aminothiols that have properties superior to the existing aminothiols and aminothiol phosphoesters that have been in use for decades.

Significant systemic toxicity occurs frequently in patients treated with the marketed aminothiol phosphoester, amifostine. The organ toxicity seen with systemically-administered amifostine may involve the irreversible, G2 cell cycle block that has been reported in human cells exposed to pharmacologic concentrations of an aminothiol phosphoester (Grdina et al., Radiation Research 138:44-52, 1994).

ProCertus has created a new generation of bifunctional aminothiol radioprotectors that scavenge oxygen free radicals, and reversibly bind to DNA to create a reversible, G1/S phase cell cycle block. Our proprietary compound, PrC-210, is the prototype of this family of low molecular weight aminothiols. Its excellent efficacy as a systemic radioprotector is seen in the panel below. Systemic PrC-210 administered just prior to whole-body radiation confers complete protection against the otherwise 100% lethal dose of gamma radiation to the mice. Mice not only survived whole-body radiation but maintained nearly normal weight gain in the post-irradiation period.

This combination of highly efficient oxygen free radical scavenging and reversible cell cycle block provides what ProCertus believes is an effective, next generation, systemic radioprotector suitable for military, civil defense and related applications.