Drug intelligence / Profile preview

neramexane + clopidogrel

Development stage
Unknown
Lead developer
Merz
Modality
Small Molecules
Administration
Oral
01

Overview

Neramexane + clopidogrel is a combination therapy or clinical study regimen involving the NMDA receptor antagonist neramexane and the antiplatelet agent clopidogrel. Neramexane (MRZ 2/579) is a moderate-affinity, non-competitive antagonist of the N-methyl-D-aspartate (NMDA) receptor, which also exhibits antagonistic activity at alpha-9/alpha-10 nicotinic acetylcholine receptors and 5-HT3 receptors. Developed by Merz Pharmaceuticals, it was primarily investigated for Alzheimer's disease, vascular dementia, and tinnitus. Clopidogrel is a thienopyridine prodrug that, upon metabolic activation, irreversibly inhibits the P2Y12 adenosine diphosphate (ADP) receptor on platelets, thereby reducing platelet aggregation. The combination has been specifically evaluated in Phase 1 clinical trials (e.g., NCT00483106) to assess the pharmacokinetic impact of clopidogrel—a known inhibitor of CYP2C8—on the clearance of neramexane. Additionally, the combination has been explored in preclinical research for its potential to provide synergistic neuroprotection in the context of ischemic stroke and other cerebrovascular disorders.

Other names
neramexane and clopidogrelMRZ 2/579 + clopidogrel
02

Targets

NMDAR (Glutamate receptor ionotropic, NMDA)P2Y12 (Purinergic P2Y12 receptor)

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