Development of Non-Narcotic Intravenous Analgesics

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DESCRIPTION (provided by applicant): Intravenous drug administration is often clinically desired over oral administration, particularly for patients who have difficulty taking an oral drug due to their disease or condition (eg, unconsciousness, anesthetized). IV administration also produces a faster therapeutic onset and permits more accurate dose administration and titration. Although variables related to drug absorption are circumvented by IV administration, IV drugs must have good water solubility to avoid issues related to blood clotting and formation of embolisms. Therefore, the solubility characteristics of new drug candidates have a significant effect on their chance for therapeutic (and commercial) success. We have been exploring a series of new and proprietary analogs of acetaminophen that show good oral efficacy but are devoid of hepatotoxic effects. Under this Phase I project we will prepare water-soluble analogs of these compounds, and determine the feasibility for further development of each of these target-candidate compounds as IV analgesics. This technology will fulfill one of our target profiles, defined as a drug that is clinically useful as an IV treatment for postoperative pain and other types of pain, including patients that may have compromised liver function (eg. elderly, cancer patients, and patients with alcoholic liver injury or hepatitis).