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Synonyms: 2-(difluoromethyl)ornithine (DMFO) | difluoromethylornithine | Ornidyl® | Vaniqa®
eflornithine is an approved drug (FDA (2000), EMA (2001))
Compound class: Synthetic organic
Comment: Eflornithine is an irreversible ornithine decarboxylase inhibitor [1,4] and is a partial inhibitor of arginase enzymes . Marketed formulations may contain eflornithine hydrochloride (PubChem CID 57004).
Eflornithine has recently been reported to provide neuroprotective effects in a mouse model of Alzheimer's disease (AD) . The authors identify microglial-induced arginine depletion as a causative factor in AD pathophysiology in their model, focussing on inhibition of arginine catabolising enzymes as a novel mechanism by which to halt the neurodegeneration observed in AD. These findings suggest that eflornithine could be used as a starting point for medicinal chemists to identify novel compounds with anti-arginase activity in humans.
Ligand Activity Visualisation Charts
These are box plot that provide a unique visualisation, summarising all the activity data for a ligand taken from ChEMBL and GtoPdb across multiple targets and species. Click on a plot to see the median, interquartile range, low and high data points. A value of zero indicates that no data are available. A separate chart is created for each target, and where possible the algorithm tries to merge ChEMBL and GtoPdb targets by matching them on name and UniProt accession, for each available species. However, please note that inconsistency in naming of targets may lead to data for the same target being reported across multiple charts.✖
1. Abeloff MD, Slavik M, Luk GD, Griffin CA, Hermann J, Blanc O, Sjoerdsma A, Baylin SB. (1984)
Phase I trial and pharmacokinetic studies of alpha-difluoromethylornithine--an inhibitor of polyamine biosynthesis.
J. Clin. Oncol., 2 (2): 124-30. [PMID:6422008]
Accessed on 23/01/2019. Modified on 23/01/2019. www.ema.europa.eu, https://www.ema.europa.eu/en/medicines/human/orphan-designations/eu3161679
3. Kan MJ, Lee JE, Wilson JG, Everhart AL, Brown CM, Hoofnagle AN, Jansen M, Vitek MP, Gunn MD, Colton CA. (2015)
Arginine deprivation and immune suppression in a mouse model of Alzheimer's disease.
J. Neurosci., 35 (15): 5969-82. [PMID:25878270]
4. Pepin J, Milord F, Guern C, Schechter PJ. (1987)
Difluoromethylornithine for arseno-resistant Trypanosoma brucei gambiense sleeping sickness.
Lancet, 2 (8573): 1431-3. [PMID:2891995]
5. Qu N, Ignatenko NA, Yamauchi P, Stringer DE, Levenson C, Shannon P, Perrin S, Gerner EW. (2003)
Inhibition of human ornithine decarboxylase activity by enantiomers of difluoromethylornithine.
Biochem. J., 375 (Pt 2): 465-70. [PMID:12859253]
6. Selamnia M, Mayeur C, Robert V, Blachier F. (1998)
Alpha-difluoromethylornithine (DFMO) as a potent arginase activity inhibitor in human colon carcinoma cells.
Biochem. Pharmacol., 55 (8): 1241-5. [PMID:9719479]