Pharmacokinetics of KRM-1648, a new benzoxazinorifamycin, in rats and dogs

Antimicrobial Agents and Chemotherapy

Volumn 40, Issue 12, 1996, Pages 2749-2755

  Hosoe, Kazunori ^a   Mae, Tatsumasa ^a   Konishi, Eisaku ^a   Fujii, Kenji ^a   Yamashita, Katsuji ^a   Yamane, Takehiko ^a   Hidaka, Takayoshi ^a   Ohashi, Takehisa ^a  

^a KANEKA CORPORATION   (Japan)

Author keywords

[No Author keywords available]

Indexed keywords

RIFALAZIL; RIFAMYCIN DERIVATIVE;

ANIMAL EXPERIMENT; ANIMAL MODEL; ARTICLE; BACTEREMIA; BIOAVAILABILITY; BLOOD SAMPLING; CONTROLLED STUDY; DEACETYLATION; DOG; DRUG BLOOD LEVEL; DRUG ELIMINATION; DRUG HALF LIFE; DRUG METABOLISM; DRUG TISSUE LEVEL; INTRAVENOUS DRUG ADMINISTRATION; NONHUMAN; ORAL DRUG ADMINISTRATION; PRIORITY JOURNAL; PROTEIN BINDING;

EID: 0029828259     PISSN: 00664804     EISSN: None     Source Type: Journal    
DOI: 10.1128/aac.40.12.2749     Document Type: Article

References (35)

1. Allain, C. C., L. S. Poon, C. S. G. Chan, W. Richmond, and P. C. Fu. 1974. Enzymatic determination of total serum cholesterol. Clin. Chem. 20:470-475.
2. Bermudez, L. E., and L. S. Young. 1987. Intracellular killing of Mycobacterium avium complex by rifapentine and liposome-encapsulated amikacin. J. Infect. Dis. 156:510-513.
3. Chapman, M. J., S. Goldstein, D. Lagrange, and P. M. Laplaud. 1981. A density gradient ultracentrifugal procedure for the isolation of the major lipoprotein classes from human serum. J. Lipid Res. 22:339-358.
4. Dijkstra, C. D., and A. J. P. Veerman. 1990. Normal anatomy, histology, ultrastructure, rat, p. 185-193. In T. C. Jones, J. M. Ward, U. Mohr, and R. D. Hunt (ed.), Hematopoietic system. Springer-Verlag, Berlin.
5. Emori, M., H. Saito, K. Sato, H. Tomioka, T. Setogawa, and T. Hidaka. 1993. Therapeutic efficacy of benzoxazinorifamycin KRM-1648 against experimental Mycobacterium avium infection induced in rabbits. Antimicrob. Agents Chemother. 37:722-728.
6. Gabrielsson, J., and D. Weiner. 1994. Basic pharmacokinetic and dynamic concepts, p. 41-100. In Pharmacokinetics and pharmacodynamic data analysis: concepts and applications. Swedish Pharmaceutical Press, Stockholm.
7. Gibaldi, M., and D. Perrier. 1982. Apparent volume of distribution, p. 199-219. In Pharmacokinetics, 2nd ed. Marcel Dekker, Inc., New York.
8. 1-acid glycoprotein and lipoproteins. Biochem. Pharmacol. 31:831-835.
9. Hosoe, K., E. Konishi, T. Hidaka, T. Yamane, K. Yamashita, and T. Ohashi. 1994. High-performance liquid chromatographic determination of 3′-hydroxy-5′-(4-isobutyl-l-piperazinyl)benzoxazinorifamycin (KRM-1648) and its deacetyl metabolite in plasma, whole blood, urine and tissue samples in rats. J. Chromatogr. B 653:177-186.
10. Hosoe, K., T. Mae, K. Yamashita, K. Fujii, T. Yamane, T. Hidaka, and T. Ohashi. 1996. Identification and antimicrobial activity of urinary metabolites of a rifamycin derivative in dog. Xenobiotica 26:321-332.
11. Inderlied, C. B., L. Barbara-Burnham, M. Wu, L. S. Young, and L. E. Bermudez. 1994. Activity of the benzoxazinorifamycin KRM-1648 and ethambutol against Mycobacterium avium complex in vitro and macrophages. Antimicrob. Agents Chemother. 38:1838-1843.
12. ++ precipitation and enzymatic measurement. J. Jpn. Atherosclerosis Soc. 9:393-398. (In Japanese.)
13. Klemens, S. P., M. A. Grossi, and M. H. Cynamon. 1994. Activity of KRM-1648, a new benzoxazinorifamycin, against Mycobacterium tuberculosis in a murine model. Antimicrob. Agents Chemother. 38:2245-2248.
14. Klemens, S. P., M. A. Grossi, and M. H. Cynamon. 1996. Activity of KRM-1648 in combination with isoniazid against Mycobacterium tuberculosis in a murine model. Antimicrob. Agents Chemother. 40:298-3111.
15. Koch-Weser, J., and E. M. Sellers. 1976. Binding of drugs to serum albumin. N. Engl. J. Med. 294:311-316.
16. Kuze, F., T. Yamamoto, R. Amitani, and K. Suzuki. 1991. In vivo activities of new rifamycin derivatives against mycobacteria. Kekkaku 66:7-12. (In Japanese.)
17. Labaune, J. P. 1989. Tissue distribution, p. 176-206. In Handbook of pharmacokinetics, toxicity assessment of chemicals. Ellis Horwood Limited. Chichester, England.
18. Lemaire, M., and J. P. Tillement. 1982. Role of lipoproteins and crythrocytes in the in vitro binding and distribution of cyclosporin A in the blood. J. Pharm. Pharmacol. 34:715-718.
19. Lowry, O. H., N. J. Rosebrough, N. J. Farr, and R. J. Randall. 1951. Protein measurement with the Folin phenol reagent. J. Biol. Chem. 193:265-275.
20. Luna-Herrera, J., M. V. Reddy, and P. R. J. Gangadharam. 1995. In vitro activity of the benzoxazinorifamycin KRM-1648 against drug-susceptible and multidrug-resistant tubercle bacilli. Antimicrob. Agents Chemother. 39:440-444.
21. Nightingale, S. D., D. W. Cameron, F. M. Gordin, P. M. Sullam, U. L. Cohn, K. C. Chaisson, L. J. Eron, P. D. Sparti, B. Bihari, D. L. Kaufman, J. J. Stern, D. D. Pearce, W. G. Weinberg, A. LaMarca, and F. P. Siegal. 1993. Two controlled trials of rifabutin prophylaxis against Mycobacterium avium complex infection in AIDS. N. Engl. J. Med. 329:828-833.
22. Rudman, D., B. Hollins, T. J. Bixler II, and R. C. Mosteller. 1972. Transport of drugs, hormones and fatty acids in lipemic serum. J. Pharmacol. Exp. Ther. 180:797-810.
23. Saito, H., H. Tomioka, K. Sato, M. Emori, T. Yamane, K. Yamashita, K. Hosoe, and T. Hidaka. 1991. In vitro antimycobacterial activities of newly synthesized benzoxazinofifamycin. Antimicrob. Agents Chemother. 35:542-547.
24. Takayama, T., S. Itoh, T. Nagasaki, and I. Tanimizu. 1977. A new enzymatic method for determination of scrum choline-containing phospholipids. Clin. Chim. Acta 79:93-98.
25. Takebe, M., J. Azuma, A. Yafune, M. Tei, and S. Kishimoto. 1989. Evaluation of a new software PAG-CP for caluculation of pharmacokinetic parameters. Jpn. J. Clin. Pharmacol. Ther. 20:139-140. (In Japanese.)
26. Taniguchi, S., H. Yamashita, H. Hirakawa, and H. Yosizaki. 1974. Serum triglycerides measurement with glycero-3-phosphate oxidase. Jpn. J. Clin. Pathol. 27(Suppl.):47. (In Japanese.)
27. Tomioka, H., H. Saito, K. Sato, T. Yamane, K. Yamashita, K. Hosoe, K. Fujii, and T. Hidaka. 1992. Chemotherapeutic efficacy of a newly synthesized benzoxazinorifamycin, KRM-1648, against Mycobacterium avium complex infection induced in mice. Antimicrob. Agents Chemother. 36:387-393.
28. Traxler, P., W. A. Vischer, and O. Zak. 1988. New rifamycins. Drug Future 13:845-856.
29. Urien, S., P. Riant, E. Albengres, R. Brioude, and J. P. Tillement. 1984. In vitro studies on the distribution of probucol among human plasma lipoproteins. Mol. Pharmacol. 26:322-327.
30. Weinkan, R. J., A. Finn, V. A. Levin, and J. P. Kane. 1980. Lipophilic drugs and lipoproteins: partitioning effects on chlorocthylnitrosourca reaction rate in serum. J. Pharmacol. Exp. Ther. 214:318-323.
31. Woodley, C. L., and J. O. Kilburn. 1982. In vitro susceptibility of Mycobacterium avium complex and Mycobacterium tuberculosis strains to a spiropiperidyl rifamycin. Am. Rev. Respir. Dis. 126:586-587,
32. Yamamoto, T., R. Amitani, F. Kuze, and K. Suzuki. 1990. In vitro activities of new rifamycin derivatives against Mycobacterium tuberculosis and M. avium complex. Kekkaku 65:805-810. (In Japanese.)
33. Yamamoto, T., R. Amitani, K. Suzuki, E. Tanaka, T. Murayama, and F. Kuze. 1996. In vitro bactericidal and in vivo therapeutic activities of a new rifamycin derivative. KRM-1648. against Mycobacterium tuberculosis. Antimicrob. Agents Chemother. 40:426-428.
34. Yamamoto, T., R. Amitani, K. Suzuki, E. Tanaka, T. Murayama, and F. Kuze. 1996. Activity of KRM-1648 alone or in combination with both ethambutol and kanamycin or clarithromycin against Mycobacterium intracellulare infection in beige mice. Antimicrob. Agents Chemother. 40:429-432.
35. Yamane, T., T. Hashizume, K. Yamashita, E. Konishi, K. Hosoe, T. Hidaka, K. Watanabe, H. Kawaharada, T. Yamamoto, and F. Kuze. 1993. Synthesis and biological activity of 3′-hydroxy-5′-aminobenzoxazinorifamycin derivatives. Chem. Pharm. Bull. 41:148-155.