Compound Technology

TECHNOLOGY:
Opioid Analgesic Compounds Devoid of Side Effects

DESCRIPTION:
This series of naltrexone-derived compounds has several indications including (i) use as analgesics for treating patients suffering from pain, (ii) treatment of drug abuse including cocaine, methamphetamine and opioids such as morphine and heroin, and (iii) use as immunomodulatory agents.

These compounds exhibit high d-antagonist potency and selectively target the d-opioid receptor on the superfamily of G-protein coupled receptors that mediate the analgesic and other pharmacological actions of morphine and related opioids. This selectivity potentially enables the compounds to have analgesic activity devoid of side effects such as respiratory depression, depression of GI motility, and physical dependence associated with potent analgesics such as morphine. In vivo evaluations show the compounds having a high binding potency at the d-receptor without overt signs of toxicity.

The compounds may be given by oral or parenteral routes alone or in combination with other therapeutic agents. Suitable oral dosage forms include liquids, tablets, and hard or soft gelatin capsules.

DEVELOPMENT STATUS: Pre-clinical

PATENT PROTECTION: US Patent Nos. 6,465,479; 7,015,326 and US Patent Application No. 60/497,901

REFERENCE NUMBER: S0237, S0239

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