A prodrug strategy for the oral delivery of a poorly soluble HCV NS5B thumb pocket 1 polymerase inhibitor using self-emulsifying drug delivery systems (SEDDS).
作者： Pierre L. Beaulieu , Josie De Marte , Michel Garneau , Laibin Luo , Timothy Stammers
DOI: 10.1016/J.BMCL.2014.11.071
关键词: Chemistry 、 Hepatitis C virus 、 Self emulsifying 、 Biochemistry 、 NS5B 、 Pharmacology 、 Prodrug 、 Ns5b polymerase 、 Drug delivery 、 Polymerase inhibitor 、 Bioavailability
摘要: Abstract A prodrug approach was developed to address the low oral bioavailability of a poorly soluble (
elsevier.com
sci-hub.se 参考文章(25)
Gregory T Everson, Karen D Sims, Maribel Rodriguez-Torres, Christophe Hézode, Eric Lawitz, Marc Bourlière, Veronique Loustaud-Ratti, Vinod Rustgi, Howard Schwartz, Harvey Tatum, Patrick Marcellin, Stanislas Pol, Paul J Thuluvath, Timothy Eley, Xiaodong Wang, Shu-Pang Huang, Fiona McPhee, Megan Wind-Rotolo, Ellen Chung, Claudio Pasquinelli, Dennis M Grasela, David F Gardiner, None, Efficacy of an Interferon- and Ribavirin-Free Regimen of Daclatasvir, Asunaprevir, and BMS-791325 in Treatment-Naive Patients With HCV Genotype 1 Infection Gastroenterology. ,vol. 146, pp. 420- 429 ,(2014) , 10.1053/J.GASTRO.2013.10.057
Nathaniel A Brown, Progress towards improving antiviral therapy for hepatitis C with hepatitis C virus polymerase inhibitors. Part I: Nucleoside analogues. Expert Opinion on Investigational Drugs. ,vol. 18, pp. 709- 725 ,(2009) , 10.1517/13543780902854194
Stefan Zeuzem, Vincent Soriano, Tarik Asselah, Jean-Pierre Bronowicki, Ansgar W. Lohse, Beat Müllhaupt, Marcus Schuchmann, Marc Bourlière, Maria Buti, Stuart K. Roberts, Ed J. Gane, Jerry O. Stern, Richard Vinisko, George Kukolj, John-Paul Gallivan, Wulf-Otto Böcher, Federico J. Mensa, Faldaprevir and deleobuvir for HCV genotype 1 infection. The New England Journal of Medicine. ,vol. 369, pp. 630- 639 ,(2013) , 10.1056/NEJMOA1213557
Edward J. Gane, Catherine A. Stedman, Robert H. Hyland, Xiao Ding, Evguenia Svarovskaia, G. Mani Subramanian, William T. Symonds, John G. McHutchison, Phillip S. Pang, Efficacy of Nucleotide Polymerase Inhibitor Sofosbuvir Plus the NS5A Inhibitor Ledipasvir or the NS5B Non-Nucleoside Inhibitor GS-9669 Against HCV Genotype 1 Infection Gastroenterology. ,vol. 146, pp. 736- 743 ,(2014) , 10.1053/J.GASTRO.2013.11.007
E. Lawitz, C. Hezode, E. Gane, E. Tam, M. Lagging, L. Balart, L. Rossaro, R. Ghalib, M. Shaughnessy, P. Hwang, J. Wahl, M.N. Robertson, B. Haber, O61 EFFICACY AND SAFETY OF MK-5172 AND MK-8742 ± RIBAVIRIN IN HEPATITIS C GENOTYPE 1 INFECTED PATIENTS WITH CIRRHOSIS OR PREVIOUS NULL-RESPONSE: THE C-WORTHY STUDY Journal of Hepatology. ,vol. 60, ,(2014) , 10.1016/S0168-8278(14)60063-5
Gillian M. Keating, Asha Vaidya, Sofosbuvir: first global approval. Drugs. ,vol. 74, pp. 273- 282 ,(2014) , 10.1007/S40265-014-0179-7
C. Sarrazin, D. Hueppe, E. Zehnter, M. P. Manns, S. Zeuzem, T. Berg, B. Moeller, H. Hinrichsen, S. Mauss, H. Wedemeyer, Expert opinion on the treatment of patients with chronic hepatitis C Journal of Viral Hepatitis. ,vol. 16, pp. 75- 90 ,(2009) , 10.1111/J.1365-2893.2008.01012.X
Michael W. Fried, Mitchell L. Shiffman, K. Rajender Reddy, Coleman Smith, George Marinos, Fernando L. Gonçales, Dieter Häussinger, Moises Diago, Giampiero Carosi, Daniel Dhumeaux, Antonio Craxi, Amy Lin, Joseph Hoffman, Jian Yu, Peginterferon alfa-2a plus ribavirin for chronic hepatitis C virus infection. The New England Journal of Medicine. ,vol. 347, pp. 975- 982 ,(2002) , 10.1056/NEJMOA020047
Hans Bundgaard, Niels Mørk Nielsen, Glycolamide esters as a novel biolabile prodrug type for non-steroidal anti-inflammatory carboxylic acid drugs International Journal of Pharmaceutics. ,vol. 43, pp. 101- 110 ,(1988) , 10.1016/0378-5173(88)90064-6
Pierre L Beaulieu, Recent advances in the development of NS5B polymerase inhibitors for the treatment of hepatitis C virus infection. Expert Opinion on Therapeutic Patents. ,vol. 19, pp. 145- 164 ,(2009) , 10.1517/13543770802672598