Drug intelligence / Profile preview

cipepofol

Development stage
Approved
Lead developer
Haisco Pharmaceutical Group
Modality
Small Molecules
Administration
Intravenous
01

Overview

Cipepofol (also known as ciprofol or HSK3486) is a novel, short-acting, intravenous general anesthetic and sedative developed by Haisco Pharmaceutical Group. Structurally related to propofol, cipepofol is a chiral 2,6-disubstituted phenol derivative incorporating a cyclopropyl group that enhances its stereospecific binding and potency, making it approximately 4 to 5 times more potent than propofol. It acts as a positive allosteric modulator of the gamma-aminobutyric acid type A (GABA-A) receptor, facilitating chloride ion influx to hyperpolarize neuronal membranes and suppress central nervous system excitability. Cipepofol was first approved in China in December 2020 under the trade name Sishuning for sedation during gastrointestinal endoscopy, and its indications have since expanded to include bronchoscopy sedation, intensive care unit (ICU) sedation, and general anesthesia induction and maintenance. In May 2026, the U.S. FDA approved cipepofol under the brand name Cypsedo for the induction of general anesthesia in adults undergoing surgery. Compared to propofol, cipepofol offers clinical advantages such as improved hemodynamic stability, a lower risk of respiratory depression, and a significantly reduced incidence of injection-site pain.

Brand names
CypsedoSishuning
Other names
CiprofoCiprofol
02

Targets

GABRR (GABA-A receptor subunit rho)

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