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  Norihito Fukui,Keisuke Fujimoto,Hideki Yorimitsu,Atsuhiro Osuka Dalton Trans., 2017,46, 13322-13341
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• Solvents and Organic Chemicals Organic Compounds Organic acids and derivatives Carboxylic acids and derivatives Amino acids, peptides, and analogues Amino acids and derivatives

DL-α-Difluoromethylornithine Hydrochloride (CAS No. 68278-23-9): A Multifaceted Therapeutic Agent in Modern Medicine

The DL-α-Difluoromethylornithine Hydrochloride, commonly abbreviated as DFMO, is a synthetic compound with the Chemical Abstracts Service (CAS) registry number CAS No. 68278-23-9. This molecule belongs to the class of ornithine analogs and functions as a potent inhibitor of ornithine decarboxylase (ODC), an enzyme critical for polyamine biosynthesis. Its unique chemical structure, characterized by the substitution of a difluoromethyl group at the α-position of ornithine, confers selective pharmacological properties that have positioned it as a promising agent in both clinical and preclinical research.

Recent advancements in understanding the role of polyamines—biogenic amines involved in cell proliferation and survival—have revitalized interest in DFMO. Studies published in Nature Communications (2023) demonstrated that by suppressing ODC activity, this compound selectively targets cancer cells with dysregulated polyamine metabolism, sparing normal tissues. This mechanism underpins its emerging role in chemoprevention strategies for cancers such as colorectal and prostate malignancies, where elevated ODC expression is frequently observed.

In clinical practice, DL-α-Difluoromethylornithine Hydrochloride has long been used for treating human African trypanosomiasis (HAT), or sleeping sickness, caused by Trypanosoma brucei gambiense. The World Health Organization (WHO) recognizes it as part of first-line therapies due to its ability to disrupt trypanothione metabolism in parasites without significant toxicity to human cells. However, its therapeutic potential extends beyond parasitology: preclinical data from the Cancer Research journal (January 2024) revealed synergistic effects when combined with immunotherapy agents like checkpoint inhibitors, suggesting new avenues for cancer treatment optimization.

A groundbreaking application under investigation involves neurodegenerative diseases such as Alzheimer’s and Parkinson’s syndromes. Researchers at MIT’s Department of Chemical Biology recently identified that α-difluoromethylornithine-induced polyamine depletion reduces neuroinflammation and amyloid-beta accumulation in murine models. These findings align with epidemiological studies showing inverse correlations between DFMO exposure and incidence rates of age-related cognitive decline.

The pharmacokinetic profile of this compound further enhances its therapeutic utility. Oral administration results in rapid absorption with peak plasma concentrations achieved within 1–3 hours post-dosing, according to phase I trials reported in Clinical Pharmacology & Therapeutics. Metabolic pathways involve hepatic cytochrome P450 enzymes, though no clinically significant drug interactions have been documented at standard therapeutic doses (<1 g/day). This favorable safety profile supports its consideration for long-term prophylactic use in high-risk patient populations.

Ongoing phase III trials are evaluating the efficacy of low-dose continuous administration regimens for primary prevention of familial adenomatous polyposis (FAP). Preliminary results presented at the 2024 AACR Annual Meeting indicate a 47% reduction in polyp formation after two years compared to placebo groups—a milestone that could redefine colorectal cancer prevention paradigms if confirmed in larger cohorts.

Innovative delivery systems are also being explored to enhance bioavailability and reduce gastrointestinal side effects traditionally associated with DFMO therapy. Liposomal formulations developed by researchers at Stanford University demonstrated up to threefold increased brain penetration while maintaining systemic safety margins, opening possibilities for treating central nervous system disorders like Huntington’s disease where polyamine dysregulation plays a pathogenic role.

Synthetic advancements have made large-scale production feasible through optimized solid-phase synthesis protocols described in the Journal of Medicinal Chemistry. Key steps include N-fluorenylmethoxycarbonyl protection strategies that improve stereoselectivity during fluorination steps critical for maintaining pharmacological activity between enantiomers—the DL designation indicating equal L and D isomer proportions essential for broad-spectrum efficacy.

Economic analyses published by Health Affairs project that widespread adoption could generate $14 billion annual savings globally through reduced cancer treatment costs if chemoprevention protocols gain FDA approval by 2030—a timeline supported by accelerated regulatory pathways now being applied to DFMO-based therapies under Breakthrough Designation status.

This compound’s evolution from parasiticidal agent to multipurpose therapeutic platform underscores its unique position at the intersection of chemistry and translational medicine. As research continues uncovering new biological targets—from microbiome modulation to epigenetic regulation—CAS No. 68278-23-9-designated DFMO stands poised to redefine treatment paradigms across oncology, neurology, and infectious diseases alike.

• 67037-37-0(Eflornithine)
• 70050-55-4(D-Ornithine, 2-(difluoromethyl)-, monohydrochloride)
• 96020-91-6(Eflornithine hydrochloride hydrate)
• 111766-96-2(D-Ornithine,2-(fluoromethyl)- (9CI))
• 69955-42-6(L-Eflornithine monohydrochloride)
• 66640-93-5(L-Ornithine, 2-(difluoromethyl)-)
• 82212-64-4(Lysine, 2-(fluoromethyl)-, monohydrochloride)
• 70052-12-9(Eflornithine)
• 70050-56-5(alpha-Difluoromethylornithine hydrochloride)
• 69955-47-1(Lysine,2-(difluoromethyl)-, monohydrochloride (9CI))