Usmarapride
Selective 5-HT4 receptor partial agonist from Alzheimer's research; Phase 1 clinical-stage candidate.
Pharmacology
Contents
WHAT IS USMARAPRIDE?
Detailed overview
Usmarapride (development code SUVN-D4010) is a selective 5-HT4 receptor partial agonist developed by Suven Life Sciences and designed as a potential treatment for the cognitive deficits associated with Alzheimer's disease. Activating 5-HT4 receptors raises cortical acetylcholine release and nudges amyloid precursor protein cleavage toward the non-amyloidogenic (sAPP-alpha) pathway, which is theoretically neuroprotective. In animal models it showed procognitive and memory-enhancing effects together with neuroprotective and antidepressant-like activity. In humans it has reached first-in-human safety and pharmacokinetic studies, profiled for once-daily oral dosing; it is not an approved medicine and human efficacy data is not yet available.
Mechanism
5-HT4 partial agonist (cholinergic + sAPP-alpha)
Evidence
Preclinical + Phase 1 human PK/safety
Legal status
Unapproved clinical-stage candidate
Receptor profile
- 5-HT4 receptorsStrong
- Cortical acetylcholine releaseModerate
- Non-amyloidogenic sAPP-alpha processingModerate
- Hippocampal BDNF / neurogenesisModerate
Safety
Side effects, stop signs, contraindications
Side effects · 5
- Headache, also noted in early human testing
- Nausea and other gastrointestinal effects, a known class effect of 5-HT4 agonists
- Theoretical prokinetic gut effect of 5-HT4 agonists (diarrhea, abdominal cramping)
- Limited long-term human safety data: reached only Phase 1 trials
- Not an approved medicine; long-term tolerability unknown
Contraindications · 4
- Pregnancy and breastfeeding: safety not established, avoid
- Pre-existing cardiac arrhythmia: older 5-HT4 agonists warrant cardiac caution (though usmarapride is more selective)
- Active gastrointestinal disease where increased motility could be problematic
- Unapproved investigational clinical-stage compound; not recommended without medical supervision
Related Nootropics
Same therapeutic category
Studies
Related research and clinical findings
Usmarapride (SUVN-D4010), a 5-HT4 receptor partial agonist for the potential treatment of Alzheimer's disease
Nirogi R, Mohammed AR, Shinde AK, et al.
Discovery and Preclinical Characterization of Usmarapride (SUVN-D4010): A Potent, Selective 5-HT4 Receptor Partial Agonist for the Treatment of Cognitive Deficits
Nirogi R, Mohammed AR, Shinde AK, et al.
First-in-Human Studies to Evaluate the Safety, Tolerability, and Pharmacokinetics of a Novel 5-HT4 Partial Agonist, SUVN-D4010
Nirogi R, Kandikere V, Bhyrapuneni G, et al.
A selective and accurate liquid chromatography-tandem mass spectrometry method for the quantitation of the novel 5-HT4 receptor partial agonist SUVN-D4010
Nirogi R, Bhyrapuneni G, Kandikere V, et al.
FAQ
FAQ
Selective 5-HT4 receptor partial agonist from Alzheimer's research; Phase 1 clinical-stage candidate.
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Structure & chemistry
The information here is strictly for educational and scientific purposes. It does not replace medical advice or clinical consultation, and it does not encourage illegal substance or pharmaceutical use. Data is sourced. When in doubt, consult your doctor.