pipadaxetan

Pipadaxetan (GIBH-130) is a small molecule 5-HT6 receptor antagonist developed by the Guangzhou Institute of Biomedicine and Health (GIBH), Chinese Academy of Sciences, for the treatment of Alzheimer's disease. The 5-HT6 receptor is a G protein-coupled receptor primarily expressed in the central nervous system, particularly in brain regions associated with learning and memory, such as the hippocampus and cortex. By antagonizing this receptor, pipadaxetan aims to modulate the release of various neurotransmitters, including acetylcholine and glutamate, which are often depleted or dysregulated in neurodegenerative conditions. This modulation is intended to improve cognitive function and memory in patients with Alzheimer's. Pipadaxetan has been evaluated in Phase 1 clinical trials in China (e.g., CTR20182230) to assess its safety, tolerability, and pharmacokinetics in healthy adult volunteers.