Ciprofol

Ciprofol
INN: Cipepofol
Clinical data
Other names(R)-2-(1-cyclopropylethyl)-6-isopropylphenol
Pharmacokinetic data
MetabolismLiver glucuronidation
ExcretionKidney
Identifiers
  • 2-[(1R)-1-cyclopropylethyl]-6-isopropylphenol
CAS Number
PubChem CID
ChemSpider
UNII
Chemical and physical data
FormulaC14H20O
Molar mass204.313 g·mol−1
3D model (JSmol)
  • CC(C1=CC=CC([C@@H](C2CC2)C)=C1O)C
  • InChI=1S/C14H20O/c1-9(2)12-5-4-6-13(14(12)15)10(3)11-7-8-11/h4-6,9-11,15H,7-8H2,1-3H3/t10-/m1/s1 checkY
  • Key:BMEARIQHWSVDBS-SNVBAGLBSA-N checkY

Ciprofol (also known as cipepofol, or HSK3486) is a novel 2,6-disubstituted phenol derivative that is used for the intravenous induction of general anesthesia.[1][2] A short-acting and highly selective γ-aminobutyric acid agonist,[3] ciprofol is 4–6 times more potent than other phenol derivatives such as propofol or fospropofol.[4]

As of 2023, it is still an investigational drug.[5] Manufactured by Haisco Pharmaceutical Group of Chengdu, Sichuan, China, ciprofol has undergone phase I and II trials in Australia and China.[5][6][7] In these early studies, ciprofol appears to be comparable in efficacy to propofol and is associated with fewer adverse events.[2][4][8][9][10][11][12][13][14][15][excessive citations]

  1. ^ Wang X, Wang X, Liu J, Zuo YX, Zhu QM, Wei XC, et al. (March 2022). "Effects of ciprofol for the induction of general anesthesia in patients scheduled for elective surgery compared to propofol: a phase 3, multicenter, randomized, double-blind, comparative study". European Review for Medical and Pharmacological Sciences. 26 (5): 1607–1617. PMID 35302207.
  2. ^ a b Zeng Y, Wang DX, Lin ZM, Liu J, Wei XC, Deng J, et al. (February 2022). "Efficacy and safety of HSK3486 for the induction and maintenance of general anesthesia in elective surgical patients: a multicenter, randomized, open-label, propofol-controlled phase 2 clinical trial". European Review for Medical and Pharmacological Sciences. 26 (4): 1114–1124. PMID 35253166.
  3. ^ Liao J, Li M, Huang C, Yu Y, Chen Y, Gan J, et al. (2022). "Pharmacodynamics and Pharmacokinetics of HSK3486, a Novel 2,6-Disubstituted Phenol Derivative as a General Anesthetic". Frontiers in Pharmacology. 13: 830791. doi:10.3389/fphar.2022.830791. PMC 8851058. PMID 35185584.
  4. ^ a b Chen BZ, Yin XY, Jiang LH, Liu JH, Shi YY, Yuan BY (August 2022). "The efficacy and safety of ciprofol use for the induction of general anesthesia in patients undergoing gynecological surgery: a prospective randomized controlled study". BMC Anesthesiology. 22 (1): 245. doi:10.1186/s12871-022-01782-7. PMC 9347095. PMID 35922771.
  5. ^ a b Lu M, Liu J, Wu X, Zhang Z (2023). "Ciprofol: A Novel Alternative to Propofol in Clinical Intravenous Anesthesia?". BioMed Research International. 2023: 7443226. doi:10.1155/2023/7443226. PMC 9879693. PMID 36714027.
  6. ^ Qin L, Ren L, Wan S, Liu G, Luo X, Liu Z, et al. (May 2017). "Design, Synthesis, and Evaluation of Novel 2,6-Disubstituted Phenol Derivatives as General Anesthetics". Journal of Medicinal Chemistry. 60 (9): 3606–3617. doi:10.1021/acs.jmedchem.7b00254. PMID 28430430.
  7. ^ Nair A, Seelam S (2022). "Ciprofol- a game changing intravenous anesthetic or another experimental drug!". Saudi Journal of Anaesthesia. 16 (2): 258–259. doi:10.4103/sja.sja_898_21. PMC 9009555. PMID 35431734.
  8. ^ Man Y, Xiao H, Zhu T, Ji F (March 2023). "Study on the effectiveness and safety of ciprofol in anesthesia in gynecological day surgery: a randomized double-blind controlled study". BMC Anesthesiology. 23 (1): 92. doi:10.1186/s12871-023-02051-x. PMC 10039513. PMID 36964501.
  9. ^ Chen X, Guo P, Yang L, Liu Z, Yu D (2022). "Comparison and Clinical Value of Ciprofol and Propofol in Intraoperative Adverse Reactions, Operation, Resuscitation, and Satisfaction of Patients under Painless Gastroenteroscopy Anesthesia". Contrast Media & Molecular Imaging. 2022: 9541060. doi:10.1155/2022/9541060. PMC 9314164. PMID 35935320.
  10. ^ Zhong J, Zhang J, Fan Y, Zhu M, Zhao X, Zuo Z, et al. (May 2023). "Efficacy and safety of Ciprofol for procedural sedation and anesthesia in non-operating room settings". Journal of Clinical Anesthesia. 85: 111047. doi:10.1016/j.jclinane.2022.111047. PMID 36599219. S2CID 255468218.
  11. ^ Liang P, Dai M, Wang X, Wang D, Yang M, Lin X, et al. (June 2023). "Efficacy and safety of ciprofol vs. propofol for the induction and maintenance of general anaesthesia: A multicentre, single-blind, randomised, parallel-group, phase 3 clinical trial". European Journal of Anaesthesiology. 40 (6): 399–406. doi:10.1097/EJA.0000000000001799. PMC 10155686. PMID 36647565.
  12. ^ Luo Z, Tu H, Zhang X, Wang X, Ouyang W, Wei X, et al. (March 2022). "Efficacy and Safety of HSK3486 for Anesthesia/Sedation in Patients Undergoing Fiberoptic Bronchoscopy: A Multicenter, Double-Blind, Propofol-Controlled, Randomized, Phase 3 Study". CNS Drugs. 36 (3): 301–313. doi:10.1007/s40263-021-00890-1. PMC 8927014. PMID 35157236.
  13. ^ Hu C, Ou X, Teng Y, Shu S, Wang Y, Zhu X, et al. (November 2021). "Sedation Effects Produced by a Ciprofol Initial Infusion or Bolus Dose Followed by Continuous Maintenance Infusion in Healthy Subjects: A Phase 1 Trial". Advances in Therapy. 38 (11): 5484–5500. doi:10.1007/s12325-021-01914-4. PMC 8523013. PMID 34559359.
  14. ^ Teng Y, Ou M, Wang X, Zhang W, Liu X, Liang Y, et al. (September 2021). "Efficacy and safety of ciprofol for the sedation/anesthesia in patients undergoing colonoscopy: Phase IIa and IIb multi-center clinical trials". European Journal of Pharmaceutical Sciences. 164: 105904. doi:10.1016/j.ejps.2021.105904. PMID 34116176.
  15. ^ Zhu Q, Luo Z, Wang X, Wang D, Li J, Wei X, et al. (April 2023). "Efficacy and safety of ciprofol versus propofol for the induction of anesthesia in adult patients: a multicenter phase 2a clinical trial". International Journal of Clinical Pharmacy. 45 (2): 473–482. doi:10.1007/s11096-022-01529-x. PMC 10147789. PMID 36680620.