Lorotomidate

Lorotomidate
Identifiers
  • ethyl 1-[(1R)-1-phenylethyl]-4-fluoroimidazole-5-carboxylate
CAS Number
PubChem CID
ChemSpider
UNII
Chemical and physical data
FormulaC14H15FN2O2
Molar mass262.284 g·mol−1
3D model (JSmol)
  • CCOC(=O)C1=C(N=CN1[C@H](C)C2=CC=CC=C2)F
  • InChI=1S/C14H15FN2O2/c1-3-19-14(18)12-13(15)16-9-17(12)10(2)11-7-5-4-6-8-11/h4-10H,3H2,1-2H3/t10-/m1/s1
  • Key:LLTPWRDHXHDIIG-SNVBAGLBSA-N

Lorotomidate (EL-0052, NH600001, 4-fluoroetomidate) is an anesthetic drug derived from etomidate, which was developed in China as a replacement for etomidate with improved side effect profile. Lorotomidate is an analogue of etomidate substituted with a fluorine atom on the imidazole ring. This almost entirely eliminates the enzyme inhibitory activity which is responsible for most of the problematic side effects of etomidate, especially suppression of corticosteroid synthesis. Lorotomidate has been found to show similar sedative-hypnotic effects to etomidate in human clinical trials, and with a markedly improved side effect profile.

See also

References

  1. ↑ Jiang JH, Xu XQ, Jiang WG, Wang T, Liu X, Zeng LG, et al. (8 January 2021). "Discovery of the EL-0052 as a potential anesthetic drug". Computational and Structural Biotechnology Journal. 19: 710–718. doi:10.1016/j.csbj.2021.01.002. PMC 7817531. PMID 33510871.
  2. ↑ Xu X, Wei Y, Dong Y, Qiu Y, Mei Z, Wang K, et al. (December 2021). "A Novel Etomidate Analog EL-0052 Retains Potent Hypnotic Effect and Stable Hemodynamics without Suppressing Adrenocortical Function". The Journal of Pharmacology and Experimental Therapeutics. 379 (3): 324–330. doi:10.1124/jpet.121.000691. PMID 34521699.
  3. ↑ Liu Y, Kuang Y, Huang J, Jiang D, Cao Y, Gao Q, et al. (21 December 2024). "Pharmacokinetic-pharmacodynamic Modelling of NH600001 in Healthy Subjects and Patients Undergoing Gastroscopy". The AAPS Journal. 27 (1) 21. doi:10.1208/s12248-024-01004-7. PMID 39707020.
  4. ↑ Sun Y, Huang J, Duan K, Lin Y, Wu Q, Xie J, et al. (1 December 2025). "Safety, tolerability, and pharmacokinetics of 4-fluoroetomidate (NH600001) in healthy subjects: a first-in-human, randomised, controlled, phase I study". European Journal of Pharmaceutical Sciences. 215 107317. doi:10.1016/j.ejps.2025.107317. PMID 41076136.
  5. ↑ Cao YJ, Kuang Y, Gao Q, Deng KH, Pei Q, Liu YX, et al. (September 2026). "Population pharmacokinetic/pharmacodynamic modeling of NH600001 reveals age-related differences in sedation response and supports individualized dosing in elderly patients". Expert Opinion on Drug Metabolism & Toxicology. 22 (9): 735–743. doi:10.1080/17425255.2026.2733399. PMID 42728212.
  6. ↑ Zhou Y, Duan K, Luo S, Liu S, Li Q, Liu S, et al. (4 May 2026). "NH600001, an etomidate analogue, provides gastrointestinal endoscopy sedation/anesthesia and reduces adrenocortical depression: two randomized controlled trials". Nature Communications. 17 (1) 5972. Bibcode:2026NatCo..17.5972Z. doi:10.1038/s41467-026-72614-2. PMC 13342565. PMID 42082491.