NEO6860

NEO6860 is an orally available, modality-selective small molecule antagonist of the transient receptor potential vanilloid 1 (TRPV1) receptor, developed primarily for the treatment of pain associated with osteoarthritis and other pain conditions. Unlike earlier TRPV1 antagonists, which block all modes of TRPV1 activation and are associated with adverse effects such as hyperthermia and impaired heat sensation, NEO6860 selectively blocks capsaicin-induced activation of TRPV1 but has little or no effect on pH or heat activation. This selectivity aims to provide analgesic efficacy without the typical side effects seen in non-selective TRPV1 antagonists. Clinical studies have shown that while it demonstrates a trend toward analgesic activity in osteoarthritis knee pain, it did not statistically significantly outperform placebo in phase II trials. The safety profile was less favorable than naproxen or placebo, with adverse events including feeling hot, headache, nausea, dizziness, fatigue, hypoaesthesia (reduced sense of touch), and increased blood pressure; however, importantly no hyperthermia or change in heat pain perception was observed[2][3][4][6][8].

Other names

NEO6860NEO-6860NEO 6860