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tegiletidine
- Development stage
- Unknown
- Lead developer
- Hengrui Pharmaceutical
- Modality
- Small Molecules
- Administration
- Intravenous
01
Overview
Tegiletidine (SHR8554) is a novel small-molecule μ-opioid receptor (MOR) biased agonist developed by Jiangsu Hengrui Pharmaceuticals for the management of acute postoperative pain. It is designed to selectively activate the G-protein signaling pathway while minimizing the recruitment of β-arrestin 2, a mechanism intended to provide potent analgesia with a reduced risk of opioid-related adverse events (ORAEs) such as respiratory depression, nausea, and vomiting. Tegiletidine was approved by the National Medical Products Administration (NMPA) of China in May 2024 for the treatment of moderate to severe acute pain following surgery. It is typically administered via intravenous injection, including patient-controlled intravenous analgesia (PCIA) regimens.
- Brand names
- Ruishuding
- Other names
- tegiletidine fumarate
02
Targets
DOR (Opioid Receptor Delta 1)KOR (Kappa opioid receptor)MOR (Mu opioid receptor)
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