Penetration of GS4071, a novel influenza neuraminidase inhibitor, into rat bronchoalveolar lining fluid following oral administration of the prodrug GS4104

Antimicrobial Agents and Chemotherapy

Volumn 41, Issue 9, 1997, Pages 1949-1952

  Eisenberg, Eugene J ^a   Bidgood, Alison ^a   Cundy, Kenneth C ^a  

^a GILEAD SCIENCES   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

4 ACETAMIDO 5 AMINO 3 (1 ETHYLPROPOXY) 1 CYCLOHEXENE 1 CARBOXYLIC ACID; OSELTAMIVIR; SIALIDASE INHIBITOR; UNCLASSIFIED DRUG;

ANTIVIRAL ACTIVITY; AREA UNDER THE CURVE; ARTICLE; BRONCHUS MUCOSA; DRUG BIOAVAILABILITY; DRUG PENETRATION; DRUG POTENCY; DRUG UPTAKE; ENZYME INHIBITION; INFLUENZA; NONHUMAN; PRIORITY JOURNAL;

EID: 0030822685     PISSN: 00664804     EISSN: None     Source Type: Journal    
DOI: 10.1128/aac.41.9.1949     Document Type: Article

References (14)

1. Bend, J. R., C. J. Serabjit-Singh, and R. M. Philpot. 1985. The pulmonary uptake, accumulation and metabolism of xenobiotics. Annu. Rev. Pharmacol. Toxicol. 25:97-125.
2. Bergogne-Berezin, E. 1988. Pharmacokinetics of antibiotics in respiratory secretions, p. 608-631. In J. E. Pennington (ed.), Respiratory infections: diagnosis and management. Raven Press, New York, N.Y.
3. Brown, E. A. B. 1974. The localization, metabolism and effects of drugs and toxicants in lung. Drug Metab. Rev. 3:33-87.
4. Kim, C. U., W. Lew, M. Williams, L. Zhang, S. Swaminathan, N. Bischofberger, M. S. Chen, D. Mendel, W. Li, L. Tai, P. Escarpe, K. C. Cundy, E. J. Eisenberg, S. Lacy, R. W. Sidwell, R. C. Stevens, and W. G. Laver. 1996. New potent, orally active neuraminidase inhibitors as anti-influenza agents: in vitro and in vivo activity of GS4071 and analogs, abstr. H-44, p. 171. In Abstracts of the 36th Interscience Conference on Antimicrobial Agents and Chemotherapy. American Society for Microbiology, Washington, D.C.
5. Rennard, S., R. G. Basset, D. Lecossier, K. O'Donnell, P. Martin, and R. G. Crystal. 1986. Estimation of volume of epithelial lining fluid recovered by lavage using urea as marker of dilution. J. Appl. Physiol. 60:532-538.
6. Ryan, D. M., J. Ticehurst, M. H. Dempsey, and C. R. Penn. 1994. Inhibition of influenza virus replication in mice by GG167 is consistent with extracellular activity of viral neuraminidase (sialidase). Antimicrob. Agents Chemother. 38:2270-2275.
7. Taylor, G. 1990. The absorption and metabolism of xenobiotics in the lung. Adv. Drug Delivery Rev. 5:37-61.
8. Valke, Y., R. Pauwels, and M. Van der Straeten. 1990. Penetration of aminoglycosides into the alveolar lining fluid of rats. Am. Rev. Respir. Dis. 142:1099-1103.
9. Vestal, R. E., D. M. Kornhauser, and D. G. Shand. 1980. Active uptake of propranolol by isolated rabbit alveolar macrophages and its inhibition by other basic amines. J. Pharmacol. Exp. Ther. 214:106-111.
10. Von Itzstine, M., W.-Y. Wu, G. B. Kok, M. S. Pegg, J. C. Dyason, B. Jin, T. V. Phan, M. L. Smythe, H. F. White, S. W. Oliver, P. M. Colman, G. N. Varghese, D. M. Ryan, J. M. Woods, R. C. Bethell, V. J. Hotham, J. M. Cameron, and C. R. Penn. 1993. Rational design of potent sialidase-based inhibitors of influenza virus replication. Nature (London) 363:418-423.
11. Wilson, A. G. E. 1982. Toxicokinetics of uptake, accumulation and metabolism of chemicals by the lung, p. 161-185. In H. Witschi and P. Nettesheim (ed.), Mechanisms in respiratory toxicology, vol. 1. CRC Press, Inc., Boca Raton, Fla.
12. Wilson, A. G. E., R. D. Peckett, T. E. Eling, and M. W. Anderson. 1979. Studies on persistence of basic amines in the rabbit lung. Drug Metab. Dispos. 7:420-424.
13. Woods, J. M., R. C. Bethell, J. A. V. Coates, N. Healy, S. A. Hiscox, B. A. Pearson, D. M. Ryan, J. Ticehurst, J. Tilling, S. M. Walcott, and C. R. Penn. 1993. 4-Guanidino-2,4-dideoxy-2,3-dehydro-N-acetylneuraminic acid is a highly effective inhibitor both of the sialidase (neuraminidase) and of growth of a wide range of influenza A and B viruses in vitro. Antimicrob. Agents Chemother. 37:1473-1479.
14. Young, K. R., and H. Y. Reinolds. 1984. Bronchoalveolar lavage washings: proteins and cells from normal lungs, p. 157-173. In J. Beinestock (ed.), Immunology of the lung and upper respiratory tract. McGraw-Hill, New York, N.Y.