Compound Technology

TECHNOLOGY:
Retinyl Ethers, Derivatives and Analogues for Inhibition of Breast Carcinogenesis

DESCRIPTION:
Numerous studies in experimental cancer models have demonstrated that certain retinoids suppress or delay the development of carcinogen-induced malignances.  Their usefulness, however, is limited due to toxicity in pharmacological doses, storage of retinyl esters in the liver and the resulting hepatotoxicity, inadequate target-organ specificity and insufficient accumulation in target organs.  These problems have led to the study of retinoid derivatives for use as chemopreventative agents.

This series of retinyl ethers and their derivatives show potential for inhibiting breast carcinogenesis with reduced toxicity.  Our lead compound in this series is Retinyl 3,4,5-Trimethoxybenzyl Ether (RTMBE).  These compounds are suitable for parenteral administration alone or in combination with other anti-neoplastic agents for prophylactic or therapeutic use.  Evaluations of RTMBE in rats against MNU-induced mammary cancer showed a reduction in the number of tumors by about 45%.

DEVELOPMENT STATUS: Pre-clinical

PATENT PROTECTION: US Patent 6,281,250

REFERENCE NUMBER: S0221

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