Title: L-Asparaginase
CAS Registry Number: 9015-68-3
Additional Names: L-Asparagine amidohydrolase; colaspase; L-asnase; EC
Manufacturers' Codes: MK-965; NSC-109229
Trademarks: Crasnitin (Bayer); Elspar (Merck & Co.); Kidrolase (RPR); Leunase (Kyowa)
Literature References: Enzyme which catalyzes the hydrolysis of L-asparagine to L-aspartic acid and ammonia. Inhibits the growth of tumor cells requiring exogenous asparagine. Widely distributed; occurs in bacteria, fungi, yeasts, plants, animal tissues and guinea pig serum. Commonly obtained from E. coli and Erwinia sp. Asparaginase from E. coli has a mol wt of ~136,000 and is composed of four identical subunits. Identification of antitumor activity: J. D. Broome, Nature 191, 1114 (1961); idem, J. Exp. Med. 118, 99 (1963). Purif, chemical properties of asparaginase from E. coli: D. H. Ho et al., J. Biol. Chem. 245, 3708 (1970). Structural studies: A. C. Greenquist, J. C. Wriston, Arch. Biochem. Biophys. 152, 280 (1972). Amino acid sequence: T. Maita et al., J. Biochem. 76, 1351 (1974). Pharmacology and clinical effects: R. H. Adamson, S. Fabro, Cancer Chemother. Rep. Part 1 52, 617 (1968); R. L. Capizzi et al., Annu. Rev. Med. 21, 433 (1970). Reviews: R. L. Capizzi, Leuk. Lymphoma 10, Suppl., 147-150 (1993); M. J. Keating et al., ibid. 153-157.
Properties: White crystalline powder. Freely sol in water where it appears to be global in shape. [a]D20 -30 to -32°. uv max (0.03M sodium phosphate, pH 7.3): 278 nm (A1%1cm 7.1 ±0.15). Active at pH 5-9. Practically insol in methanol, acetone, chloroform.
Optical Rotation: [a]D20 -30 to -32°
Absorption maximum: uv max (0.03M sodium phosphate, pH 7.3): 278 nm (A1%1cm 7.1 ±0.15)
Derivative Type: Compd with polyethylene glycol
CAS Registry Number: 130167-69-0
Additional Names: Pegaspargase; PEG-asparaginase; (monomethoxypolyethylene glycol succinimidyl)74-L-asparaginase
Trademarks: Oncaspar (RPR)
Literature References: L-Asparaginase from E. coli covalently coupled to polyethylene glycol moieties of mol wt ~5000 Da. Prepn: F. F. Davis et al., DE 2433883 (1976 to Research Corp.); eidem, US 4179337 (1979). Prepn, pharmacology and antitumor efficacy: A. Abuchowski et al., Cancer Biochem. Biophys. 7, 175 (1984). Toxicology: A. T. Viau et al., Am. J. Vet. Res. 47, 1398 (1986). Review of clinical experience: F. Fuertges, A. Abuchowski, J. Controlled Release 11, 139 (1990).
Therap-Cat: Antineoplastic (acute leukemia).
Keywords: Antineoplastic; Enzymes.

Others monographs:
TilmicosinMethylene BromidePassifloraGuanosine
MarrubiinMethyl RedLinseedEthopropazine
©2016 DrugLead US FDA&EMEA