Chemistry:Usmarapride

From HandWiki

Usmarapride (INN; developmental code name SUVN-D4010) is a serotonin 5-HT4 receptor agonist which is or was under development for the treatment of cognitive deficits in Alzheimer's disease and schizophrenia.[1][2][3] It is taken orally.[1]

Pharmacology

The drug is a potent and selective partial agonist of the serotonin 5-HT4 receptor.[2][3] It is highly selective against the serotonin 5-HT3 receptor and other closely related receptors.[2] The drug shows cognition- and memory-enhancing effects, neuroprotective effects, and antidepressant-like effects in preclinical research.[2][3][4] Its pharmacokinetics and pharmacodynamics have been evaluated in humans.[2][5] In terms of chemical structure, the drug is an indazole derivative.[6]

Development

Usmarapride is under development by Suven Life Sciences.[1] As of September 2023, no recent development has been reported for treatment of Alzheimer's disease and schizophrenia.[1] The drug has reached phase 1 clinical trials for both of these indications.[1]

References

  1. ↑ 1.0 1.1 1.2 1.3 1.4 "Usmarapride - Suven Life Sciences". 28 September 2023. https://adisinsight.springer.com/drugs/800043407. 
  2. ↑ 2.0 2.1 2.2 2.3 2.4 "Discovery and Preclinical Characterization of Usmarapride (SUVN-D4010): A Potent, Selective 5-HT4 Receptor Partial Agonist for the Treatment of Cognitive Deficits Associated with Alzheimer's Disease". J Med Chem 64 (15): 10641–10665. August 2021. doi:10.1021/acs.jmedchem.1c00703. PMID 34251799. 
  3. ↑ 3.0 3.1 3.2 "Usmarapride (SUVN-D4010), a 5-HT4 receptor partial agonist for the potential treatment of Alzheimer's disease: Behavioural, neurochemical and pharmacological profiling". Eur J Pharmacol 947. May 2023. doi:10.1016/j.ejphar.2023.175625. PMID 36997046. 
  4. ↑ "Usmarapride Oxalate (SUVN-D4010): A Serotonin-4 Receptor Partial Agonist for the Treatment of Cognitive Disorders". Alzheimer's & Dementia 18 (S10). 2022. doi:10.1002/alz.062167. ISSN 1552-5260. https://alz-journals.onlinelibrary.wiley.com/doi/10.1002/alz.062167. Retrieved 1 October 2025. 
  5. ↑ "First-in-Human Studies to Evaluate the Safety, Tolerability, and Pharmacokinetics of a Novel 5-HT4 Partial Agonist, SUVN-D4010, in Healthy Adult and Elderly Subjects". Clin Drug Investig 41 (5): 469–482. May 2021. doi:10.1007/s40261-021-01027-4. PMID 33788154. 
  6. ↑ "5-HT4R modulators: a patent landscape". Pharm Pat Anal 10 (4): 179–181. July 2021. doi:10.4155/ppa-2021-0017. PMID 34365797. 





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