8808 Characterization and pre-clinical study on a novel hormonal compound with potent analgesic and anti-inflammatory properties

Abstract Disclosure: T. Antakly: Other; Self; Theriac Biomedical. A. Brox: Owner/Co-Owner; Self; Theriac Biomedical. J. Menezes: Advisory Board Member; Self; Theriac Biomedical. H.H. Zingg: None. Hormones and naturally occurring compounds with therapeutic benefits have provided the basis of some of the most celebrated drugs e.g. Taxol (extracted from the Pacific Hew tree) and Premarin, a hormone replacement therapy (extracted from horse urine). Our team has discovered and chemically identified a bioactive compound (called “HIP-2”) found in folk medicinal admixtures. It has unique analgesic and anti-inflammatory properties. The chemical structure of HIP-2 consists of small fatty acid molecules which bind and activate the PPAR-gamma transcription factor, and furthermore they have HDAC inhibitory properties. A synthetic replica of the bioactive compounds was obtained and administered orally or by injection in a single dosage form. Using animal models for pain and inflammation, HIP-2 has demonstrated an outstanding efficacy and safety profile in animals (rats, mice) rendered experimentally inflamed (e.g. carrageenan injection) or osteoarthritic (surgery or iodoacetate injection). Pain and inflammation have decreased (by up to 50%) after HIP-2 administration. Inflammatory cytokines biomarkers were also reduced by about 50% as compared to baseline or to the positive controls (classical NSAID’s). HIP-2, with an outstanding safety and efficacy profile, offers an advantage over currently available analgesic and anti-inflammatory drugs, which have significant draw-backs due to limited efficacy and significant side effects such as gastrointestinal bleeding/ulcers/perforation and cardiac toxicity (Advil, Celebrex), osteoporosis and immunosuppression (corticosteroids), or addiction (opioids). As a potential solution to these problems, HIP-2 is likely to be superior both at the safety and efficacy levels. The HIP-2 IMP was cleared by FDA and is entering Phase 2 clinical trials. Presentation: 6/3/2024