Eflornithine is a synthetic fluoroamino acid and an irreversible inhibitor of the enzyme ornithine decarboxylase (ODC). It is also known as α-difluoromethylornithine (DFMO) and has the chemical name 2,5-diamino-2-(difluoromethyl)pentanoic acid. Its molecular formula is C6H12F2N2O2 and its molecular weight is approximately 182.17 g/mol.
Eflornithine API is a pharmaceutical active ingredient used in different therapeutic applications. Its pharmacological activity is primarily associated with inhibition of ornithine decarboxylase, an enzyme involved in polyamine biosynthesis.
Eflornithine is associated with the treatment of human African trypanosomiasis and has also been used in topical formulations for unwanted facial hair growth. More recently, oral eflornithine was approved in the United States as maintenance therapy for patients with high-risk neuroblastoma who have responded to prior treatment.
Eflornithine is a fluoro-substituted amino acid structurally related to ornithine. The compound contains two fluorine atoms and two amino groups and is classified as a fluoroamino acid.
Chemical Name: 2,5-Diamino-2-(difluoromethyl)pentanoic acid
Molecular Formula: C6H12F2N2O2
Molecular Weight: 182.17 g/mol
CAS Number: 70052-12-9
Synonyms: Eflornithine, DFMO, α-Difluoromethylornithine
Eflornithine acts as an irreversible ornithine decarboxylase inhibitor. Ornithine decarboxylase participates in the biosynthesis of polyamines, which are important for cellular growth and proliferation. Inhibition of this enzyme reduces polyamine production and contributes to the pharmacological activity of eflornithine.
Eflornithine has been used as an active pharmaceutical ingredient in formulations associated with:
The particular application depends on the pharmaceutical formulation, regulatory approval and intended market.
Eflornithine API should be manufactured and tested according to the applicable approved product specification and relevant pharmaceutical quality requirements. Typical quality evaluation may include identity, assay, related substances, water content, residue on ignition and other applicable physicochemical and analytical parameters.
Note: Numerical acceptance criteria should be taken from the manufacturer's approved specification or Certificate of Analysis rather than using generic values.
| Parameter | Specification |
|---|---|
| Appearance | White to off-white crystalline powder |
| Identification | IR & HPLC compliant |
| Assay (HPLC) | 98.0% – 102.0% |
| Loss on Drying | NMT 1.0% |
| Heavy Metals | NMT 20 ppm |
| Individual Impurity | ≤ 0.5% |
| Total Impurities | NMT 2.0% |
| Water Content | NMT 1.0% |
| Melting Point | 150°C – 154°C |