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Ajulemic acid (IP-751): Synthesis, proof of principle, toxicity studies, and clinical trials

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Abstract

Ajulemic acid (CT-3, IP-751,1’,1’-dimethylheptyl-Δ8 acid) (AJA) has a cannabinoid-derived structure; however, there is no evidence that it produces psychotropic actions when given at therapeutic doses. In a variety of animal assays, AJA shows efficacy in models for pain and inflammation. Furthermore, in the rat adjuvant arthritis model, it displayed a remarkable action in preventing the destruction of inflamed joints. A phase-2 human trial with chronic, neuropathic pain patients suggested that AJA could become a useful drug for treating this condition. Its low toxicity, particularly its lack of ulcerogenicity, further suggests that it will have a highly favorable therapeutic index and may replace some of the current anti-inflammatory/analgesic medications. Studies to date indicate a unique mechanism of action for AJA that may explain its lack of adverse side effects.

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Authors and Affiliations

  1. Department of Biochemistry and Molecular Pharmacology, University of Massachusetts Medical School, 364 Plantation Street, 01605, Worcester, MA

    Summer Burstein

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  1. Summer Burstein
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Correspondence to Summer Burstein.

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Published: June 29, 2005

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Burstein, S. Ajulemic acid (IP-751): Synthesis, proof of principle, toxicity studies, and clinical trials. AAPS J 7, 15 (2005). https://doi.org/10.1208/aapsj070115

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  • DOI: https://doi.org/10.1208/aapsj070115

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