Chemistry:Susineridine
Susineridine (INN; developmental code name YZJ-4729) is an atypical μ-opioid receptor (MOR) agonist and opioid analgesic which is under development for the treatment of postoperative pain.[1][2][3][4] It is given intravenously.[1]
The drug acts as a selective biased partial agonist of the MOR, with functional selectivity for activation of G protein signaling over β-arrestin2 recruitment.[3][4] Its mechanism of action and pharmacological activity are said to be similar to those of oliceridine.[3][4] However, in-vitro findings suggest that susineridine may have a greater degree of G protein bias than oliceridine.[3] The drug produces analgesic effects in multiple animal models of pain and produces less respiratory depression than morphine or oliceridine.[3][4] The pharmacokinetics of susineridine in humans have been studied.[3][4]
Susineridine was patented[5] and first described in the scientific literature in 2023.[3][4] It is under development by Shanghai Haiyan Pharmaceutical Technology in China.[1][2] As of May 2025, the drug is in phase 3 clinical trials for postoperative pain.[1][2]
See also
- μ-Opioid receptor § Biased agonists
References
- ↑ 1.0 1.1 1.2 1.3 "YZJ 4729". AdisInsight. Springer Nature Switzerland AG. 2 April 2025. https://adisinsight.springer.com/drugs/800080418.
- ↑ 2.0 2.1 2.2 "Delving into the Latest Updates on YZJ-4729 with Synapse". 30 August 2025. https://synapse.patsnap.com/drug/5b6a5852e7d04a8f97171ed44e3e881c.
- ↑ 3.0 3.1 3.2 3.3 3.4 3.5 3.6 "Pharmacokinetics, metabolite profiling, safety and tolerability of YZJ-4729 tartrate, a novel G protein-biased μ-opioid receptor agonist, in healthy Chinese subjects". Frontiers in Pharmacology 14. 2023. doi:10.3389/fphar.2023.1295319. PMID 38264529.
- ↑ 4.0 4.1 4.2 4.3 4.4 4.5 "Development and validation of an LC-MS/MS method for quantifying a new G protein selective μ-opioid receptor agonist YZJ-4729 and its major metabolite M10 in human plasma to support a phase I study in healthy subjects". Journal of Chromatography. B, Analytical Technologies in the Biomedical and Life Sciences 1263. September 2025. doi:10.1016/j.jchromb.2025.124714. PMID 40577954.
- ↑ Hu B, Xie J, Zhang K, Yang W, Shi X, Guan H, "Azabicyclic substituted oxaspiro derivative, preparation method therefor and medical use thereof", US patent 2023/0128062A1, published 27 April 2023, assigned to Yangtze River Pharmaceutical Group Co Ltdand Shanghai Haiyan Pharmaceutical Technology Co Ltd
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