Drug intelligence / Profile preview

pregabalin + toludesvenlafaxine

Development stage
Unknown
Lead developer
Beijing Tiantan Hospital
Modality
Small Molecules
Administration
Oral
01

Overview

Pregabalin + toludesvenlafaxine is a combination therapy being investigated by Beijing Tiantan Hospital for the treatment of fibromyalgia. This combination pairs pregabalin, a gabapentinoid that acts as a ligand for the alpha-2/delta subunit of voltage-gated calcium channels to reduce excitatory neurotransmitter release, with toludesvenlafaxine (LY03005), a serotonin-norepinephrine-dopamine reuptake inhibitor (SNDRI). While toludesvenlafaxine is primarily characterized as a selective serotonin and norepinephrine reuptake inhibitor (SNRI) in some clinical contexts, it also inhibits dopamine reuptake. The rationale for the combination is to provide synergistic pain relief by targeting both central sensitization (via pregabalin) and descending inhibitory pain pathways (via toludesvenlafaxine) associated with fibromyalgia.

Other names
pregabalin + desvenlafaxinepregabalin + LY03005pregabalin + Ruoxinlin
02

Targets

DAT (Dopamine plasma membrane transport protein)CACNA2D2 (α2δ-2)SERT (Sodium-dependent serotonin transporter)NET (Norepinephrine Transporter)CACNA2D1 (Voltage-gated calcium channel subunit alpha2/delta-1)

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