Monograph number:
3564
Title:
Eflornithine
Specification
IHS (In House Specification)
Category
Antineoplastic, Antipneumocystic Antiprotozoal, To Remove excess facial hair
DMF Status
TP (Technical Package)
CAS Registry number:
[67037-37-0]
CAS name(s):
2-(Difluoromethyl)-DL-ornithine
Additional name(s):
alpha-difluoromethylornithine; DFMO
Drug Code(s):
RMI
Molecular formula:
C 6 H 12 F 2 N 2 O 2
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. Prepn: B. W. Metcalf et al., J. Am. Chem. Soc. 100, 2551 (1978); P. Bey et al., J. Org. Chem. 44, 2732 (1979). Antiproliferative effects on cultured tumor cells: P. S. Mamont et al., Biochem. Biophys. Res. Commun. 81, 58 (1978); on Ehrlich ascites cells in rats: L. Alhonen-Hon gis to et al., Acta Chem. Scand. B33, 559 (1979). Inhibition of polyamine biosynthesis: E. Houmllttauml et al., Biochem. J. 178, 109 (1979). Antitrypanosomal activity in mice: C. J. Bacchi et al., Science 210, 332 (1980). Pharmacokinetics in humans: K. D. Haegele et al., Clin. Pharmacol. Ther. 30, 210 (1981). Clinical evaluations in Pneumocystis carinii pneu monia: J. A. Golden et al., West. J. Med. 141, 613 (1984); in trypanosomiasis: S. Van Nieuwenhove et al., Trans. Royal Soc. Trop. Med. Hyg. 79, 692 (1985); in cancer chemotherapy: M. D. Abeloff et al., Cancer Treat. Rep. 70, 843 (1986); V. A. Levin et al., ibid. 71, 459 (1987).
Derivative
Hydro chloride monohydrade
Molecular Formula
C 6 H 12 F 2 N 2 O 2 .HCl.H 2O.
CAS Registry
[96020-91-6]
Trade name(s)
Or nidyl (HMR)
Properties:
Crystals from ethanol/water
Melting Point:
183