Drug intelligence / Profile preview

memantine XR + pregabalin

Development stage
Unknown
Modality
Small Molecules
Administration
Oral
01

Overview

Memantine XR + pregabalin is a combination therapy consisting of extended-release memantine and pregabalin, proposed for the management of neuropathic pain conditions such as fibromyalgia syndrome (FMS) and chemotherapy-induced peripheral neuropathy (CIPN). Memantine is an N-methyl-D-aspartate receptor (NMDAR) antagonist that reduces excitotoxic neuronal activity by selectively blocking excessive glutamate signaling, thereby limiting pathological activation while sparing normal synaptic function. Pregabalin is a voltage-gated calcium channel (VGCC) blocker that decreases neurotransmitter release involved in pain transmission. The rationale for combining these agents lies in their complementary mechanisms—targeting both central sensitization via NMDAR inhibition and peripheral/central nociceptive signaling via VGCC blockade—to provide synergistic analgesia and potentially neuroprotective effects. This dual-drug approach aims to reduce chronic pain, slow gray matter atrophy associated with FMS, and improve quality of life in patients with neuropathic pain[1][2][8].

02

Targets

NMDAR (Glutamate receptor ionotropic, NMDA)α2δ (Voltage-gated calcium channel alpha-2-delta subunit)

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