Drug intelligence / Profile preview

mephethofen hydrochloride

Development stage
Unknown
Lead developer
Yangtze River Pharmaceutical Group
Modality
Small Molecules
Administration
Intravenous
01

Overview

Mephethofen hydrochloride is a novel, non-opioid, centrally acting analgesic developed by Yangtze River Pharmaceutical Group and its subsidiary, Sichuan Hairong Pharmaceutical. As a structural derivative of nefopam, it functions as a multi-target inhibitor of monoamine reuptake—specifically targeting the serotonin, norepinephrine, and dopamine transporters—while also modulating voltage-gated sodium and calcium channels. This multi-modal mechanism provides potent analgesia for moderate to severe pain without the respiratory depression, sedation, or physical dependence typically associated with opioid therapy. Mephethofen hydrochloride has been primarily investigated in Phase III clinical trials in China for the management of postoperative pain following abdominal, orthopedic, and gynecological surgeries, where it is administered via intravenous injection or patient-controlled analgesia (PCA).

Other names
mephethofenmephethofenide盐酸美非替芬
02

Targets

NET (Norepinephrine Transporter)DAT (Dopamine plasma membrane transport protein)CaV (Voltage-gated calcium channel protein complex)SERT (Sodium-dependent serotonin transporter)NaV (Voltage-gated sodium channels)

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