Ajulemic acid (IP-751): Synthesis, proof of principle, toxicity studies, and clinical trials
Journal Title: The AAPS Journal - Year 2005, Vol 7, Issue 1
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.
Authors and Affiliations
Summer Burstein
Summary Workshop Report: Facilitating Oral Product Development and Reducing Regulatory Burden Through Novel Approaches to Assess Bioavailability/Bioequivalence
This summary workshop report highlights presentations and over-arching themes from an October 2011 workshop. Discussions focused on best practices in the application of biopharmaceutics in oral drug product development a...
Mathematical Models to Explore Potential Effects of Supersaturation and Precipitation on Oral Bioavailability of Poorly Soluble Drugs
The online version of this article (doi:10.1208/s12248-015-9748-2) contains supplementary material, which is available to authorized users.
A Mechanistic Pharmacokinetic Model Elucidating the Disposition of Trastuzumab Emtansine (T-DM1), an Antibody–Drug Conjugate (ADC) for Treatment of Metastatic Breast Cancer
Trastuzumab emtansine (T-DM1) is an antibody–drug conjugate (ADC) therapeutic for treatment of human epidermal growth factor receptor 2 (HER2)-positive cancers. The T-DM1 dose product contains a mixture of drug-t...
Therapeutic MicroRNA Strategies in Human Cancer
MicroRNAs (miRNAs) are ~22 nucleotide long, noncoding, endogenous RNA molecules which exert their functions by base pairing with messenger RNAs (mRNAs), thereby regulate protein-coding gene expression. In eukaryotic cell...
AAPS–FIP Summary Workshop Report: Pharmacogenetics in Individualized Medicine: Methods, Regulatory, and Clinical Applications
The workshop “Pharmacogenetics in Individualized Medicine: Methods, Regulatory, and Clinical Applications” was held November 15–16, 2008 in Atlanta, Georgia, USA. This workshop provided an opportu...