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Summary

Etomoxir is the first drug candidate out of a new class of substances -oxirane carboxylic acids – that has been developed in two clinical indications – diabetes type 2 and heart insufficiency – until phase II of clinical development. The substance acts as a irreversible inhibitor of the mitochondrial carnitine palmitoyltransferase 1 (E.C. 2.3.1.21), a regulatory enzyme of long-chain fatty acid oxidation. The real inhibitor is the Coenzyme A ester of the substance that is built in the cells.

INN:Etomoxir (lat. etomixirum), Ethyl ( + )-2-[6-(parachlorphenoxy)hexyl]glycidat
or
( R )-( + )-2-[6-(4-Chlorphenoxy)hexyl]-oxiran-2-carbonsäure Ethylester
Mol. formula:C17H23CIO4
Mol. wt.:326,8

Mol. structure:

strukturformel-strichmodell
Indications:metabolic syndrome, heart insufficiency, diabetes type 2, ketoacidosis, hyperlipidemia, arteriosclerosis, coronary heart disease, inflammation, leukemia, dairy cow ketosis.
Status:phase II of clinical development.
Dosis:2 x 40 mg until 2 x 80 mg daily.
Drug form:wet gelatin capsule
Toxicology:Acute toxicity: (LD50, fasted mice, rats, p. o.): 270 mg/kg.
Sub acute toxicity: (LD50, rat, p. o.): > 125 mg/kg; (LD5, dog, p. o.): > 200 mg/kg.
No signs of mutagenicity, embryo-toxicity, and teratogenicity.