Title: Eflornithine
CAS Registry Number: 67037-37-0
CAS Name: 2-(Difluoromethyl)-DL-ornithine
Synonyms: a-difluoromethylornithine; DFMO
Manufacturers' Codes: RMI-71782
Molecular Formula: C6H12F2N2O2
Molecular Weight: 182.17
Percent Composition: C 39.56%, H 6.64%, F 20.86%, N 15.38%, O 17.57%
Literature References: Irreversible inhibitor of ornithine decarboxylase, an enzyme involved in polyamine biosynthesis. Prepn: B. W. Metcalf
et al., J. Am. Chem. Soc. 100, 2551 (1978); P. Bey
et al., J. Org. Chem. 44, 2732 (1979). Effect on polyamine biosynthesis in trypanosomes: C. J. Bacchi
et al., Science 210, 332 (1980). Clinical pharmacokinetics: K. D. Haegele
et al., Clin. Pharmacol. Ther. 30, 210 (1981). Reviews of clinical experience in
Pneumocystis carinii pneumonia: J. Sahai, A. J. Berry,
Pharmacotherapy 9, 29-33 (1989); in cancer chemotherapy: F. L. Meyskens, Jr., E. W. Gerner,
Clin. Cancer Res. 5, 945-951 (1999); in trypanosomiasis: C. Burri, R. Brun,
Parasitol. Res. 90, S49-S52 (2003). Review of topical use in hirsutism: J. A. Barman Balfour, K. McClellen,
Am. J. Clin. Dermatol. 2, 197-201 (2001).
Derivative Type: Hydrochloride monohydrate
CAS Registry Number: 96020-91-6
Trademarks: Ornidyl (Aventis); Vaniqa (SkinMedica)
Molecular Formula: C6H12F2N2O2.HCl.H2O
Molecular Weight: 236.64
Percent Composition: C 30.45%, H 6.39%, F 16.06%, N 11.84%, O 20.28%, Cl 14.98%
Properties: Crystals from ethanol/water, mp 183°. Freely sol in water; sparingly sol in ethanol.
Melting point: mp 183°
Therap-Cat: Antineoplastic; antipneumocystic; antiprotozoal (Trypanosoma). In treatment of hirsutism.
Keywords: Antineoplastic; Antipneumocystic; Antiprotozoal (Trypanosoma).