Drug intelligence / Profile preview

lofentanil

Development stage
Preclinical
Lead developer
Janssen Pharmaceutica
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules
Administration
Intravenous (experimental/clinical Research), Epidural/extradural (studied In Clinical Trials)[2]
01

Overview

Lofentanil is an extremely potent synthetic opioid analgesic and a structural analog of fentanyl. It is most similar to carfentanil but is considered slightly more potent. Lofentanil acts primarily as a full agonist at the μ-opioid receptor, producing profound analgesia and anesthesia. It also acts as a full agonist at the κ-opioid receptor. The drug has a long duration of action and high lipophilicity compared to other fentanyl analogs, which limits its practical use in clinical settings due to increased risk of side effects such as respiratory depression and rapid development of tolerance. Its main application today is in research on opioid receptors rather than clinical medicine[1][2][3][5].

Other names
lofentanyl3-methylcarfentanil3-methyl-4-carbomethoxyfentanyl
02

Targets

MOR (Mu opioid receptor)KOR (Kappa opioid receptor)

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