Paritaprevir ( Paritaprevir , ABT-450 ) is an inhibitor of [1] NS3-4A serine protease [2] II wave of the 1st generation, manufactured by AbbVie Inc. [3] and used as a component of combined drugs for the treatment of hepatitis C under the brands Viekira Pak [4] , Technivie [5] , ViekiraX, ViekiraXR. This inhibitor has an average resistance barrier; its action is aimed at binding the site : resistance arises as a result of mutations at positions 155, 168 and some other positions of the non-structural NS3 viral protein [6] p. 248 . A serious drawback of paritaprevir is a rapid decrease in the concentration of the drug in the blood, forcing it to be used in conjunction with the pharmacokinetic enhancer ritonavir, which has hepatotoxicity and a poor profile of drug interactions. Like other NS3 / 4A inhibitors of the first generation, it does not have optimal virological activity for all genotypes. since 2018 in the list of Vital and Essential Drugs
| Paritaprevir | |
|---|---|
 | |
| Chemical compound | |
| IUPAC | (2 R , 6 S , 12 Z , 13a S , 14a R , 16a S ) - N - (Cyclopropylsulfonyl) -6 - {[(5-methyl-2-pyrazinyl) carbonyl] amino} -5,16-dioxo- 2- (6-phenanthridinyloxy) -1,2,3,6,7,8,9,90,11,13a, 14,15,16,16a-tetradecahydrocyclopropa [ e ] pyrrolo [1,2- a ] [1 , 4] diazacyclopentadecine-14a (5 H ) -carboxamide |
| Gross formula | C 40 H 43 N 7 O 7 S |
| Molar mass | 765.88 g / mol |
| Cas | |
| PubChem | |
| Drugbank | |
| Classification | |
| ATX | |
| Pharmacokinetics | |
| Bioavailable | not rated |
| Plasma Protein Binding | 97β98.6% |
| Metabolism | hepatic, CYP3A4 and CYP3A5 |
| The half-life. | 5.5 hours |
| Excretion | feces (88%), urine (8.8%) |
| Route of administration | |
| Oral | |
Notes
- β Hepatitis C: antiviral drug discovery and development / Seng-Lai Tan and Yupeng He. - Norfolk: Caister academic press, 2011 .-- P. 210. - ISBN 9781904455783 .
- β Hepatitis C / Donald Jensen, Nancy Reau. - New York: Oxford University Press, 2013 .-- P. 144. - ISBN 9780199844296 .
- β Abbott Announces Phase 3 Hepatitis C Program Details . Abbott company website . Abbott Laboratories. Date of treatment April 28, 2014.
- β FDA approves Viekira Pak to treat hepatitis C. FDA News Release . FDA (December 19, 2014) . Date of treatment February 9, 2016.
- β Technivie β’ (ombitasvir, paritaprevir and ritonavir) Tablets, for Oral Use. Full Prescribing Information unspecified . AbbVie Inc., North Chicago, IL 60064. Date accessed February 9, 2016.
- β Hepatology 2013 a clinical textbook / Stefan Mauss. - 4th. - DΓΌsseldorf: Flying Publisher, 2013 .-- ISBN 978-3-924774-90-5 . Archived April 29, 2014 on Wayback Machine
Links
- Compound Summary for CID 45110509 . Pubchem> Compound> Paritaprevir . National Center for Biotechnology Information . Date of treatment February 9, 2016.
- Paritaprevir (English) . Drugs.com. Date of treatment February 9, 2016.
- Dasabuvir; Ombitasvir + Paritaprevir + Ritonavir . Encyclopedia of medicines and pharmaceutical products . Radar Patent. - Instruction, application and formula.