1132935-63-7 Usage
Description
ABT-333 is a pyrimidone-based antiviral drug that is used in combination with other medications for the treatment of chronic hepatitis C virus (HCV) infection, particularly genotype 1. It is a member of the class of pyrimidone and works by inhibiting the HCV RNA-dependent RNA polymerase, thereby suppressing viral replication.
Uses
Used in Pharmaceutical Industry:
ABT-333 is used as an antiviral agent for the treatment of chronic hepatitis C virus genotype 1 infection. It is combined with other medications, such as ombitasvir, paritaprevir, and ritonavir, under the trade name Viekira Pak, to provide a comprehensive treatment regimen for patients with chronic HCV infection.
Additionally, ABT-333 is used in the treatment of liver cirrhosis, a severe liver disease that can be caused by chronic HCV infection. By effectively managing the viral infection, ABT-333 contributes to the improvement of liver function and the prevention of further liver damage in affected patients.
Clinical Use
Treatment of chronic hepatitis C infection
Drug interactions
Potentially hazardous interactions with other drugsAntibacterials: avoid concomitant use with
clarithromycin and telithromycin; concentration
possibly reduced by rifampicin - avoid.Antidepressants: concentration possibly reduced by
St John’s wort - avoid.Antiepileptics: concentration reduced by
carbamazepine - avoid; concentration possibly
reduced by fosphenytoin, phenobarbital, phenytoin
and primidone - avoid.Antifungals: concentration of both drugs increased
with ketoconazole and possibly itraconazole and
posaconazole - avoid.Diuretics: concentration of furosemide increased
(reduce furosemide dose).Immunosuppressants: increases concentration of
ciclosporin (reduce ciclosporin dose by a fifth);
everolimus (avoid); sirolimus and tacrolimus (reduce
dose and use only if benefit outweighs risk - see
SPC).Lipid-regulating drugs: avoid with atorvastatin,
gemfibrozil and simvastatin; concentration of
rosuvastatin increased (reduce dose of rosuvastatin).Oestrogens: avoid concomitant use with
ethinylestradiol.
Metabolism
Dasabuvir is mainly metabolised by CYP2C8 and to
a lesser extent by CYP3A. Seven metabolites were
identified in plasma. The most abundant plasma
metabolite was M1, which represented 21% of drugrelated radioactivity (AUC) in circulation following single
dose; it is formed via oxidative metabolism predominantly
by CYP2C8.Following a 400 mg 14C-dasabuvir dose, approximately
94% of the radioactivity was recovered in faeces with
limited radioactivity (approximately 2%) in urine.
Unchanged dasabuvir accounted for 26.2% and M1 for
31.5% of the total dose in faeces. M1 is mainly cleared
through direct biliary excretion with the contribution of
UGT-mediated glucuronidation and, to a small extent,
oxidative metabolism.
Check Digit Verification of cas no
The CAS Registry Mumber 1132935-63-7 includes 10 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 7 digits, 1,1,3,2,9,3 and 5 respectively; the second part has 2 digits, 6 and 3 respectively.
Calculate Digit Verification of CAS Registry Number 1132935-63:
(9*1)+(8*1)+(7*3)+(6*2)+(5*9)+(4*3)+(3*5)+(2*6)+(1*3)=137
137 % 10 = 7
So 1132935-63-7 is a valid CAS Registry Number.
1132935-63-7Relevant articles and documents
Discovery and Development of Metal-Catalyzed Coupling Reactions in the Synthesis of Dasabuvir, an HCV-Polymerase Inhibitor
Barnes, David M.,Shekhar, Shashank,Dunn, Travis B.,Barkalow, Jufang H.,Chan, Vincent S.,Franczyk, Thaddeus S.,Haight, Anthony R.,Hengeveld, John E.,Kolaczkowski, Lawrence,Kotecki, Brian J.,Liang, Guangxin,Marek, James C.,McLaughlin, Maureen A.,Montavon, Donna K.,Napier, James J.
supporting information, p. 4873 - 4892 (2019/02/05)
Dasabuvir (1) is an HCV polymerase inhibitor which has been developed as a part of a three-component direct-acting antiviral combination therapy. During the course of the development of the synthetic route, two novel coupling reactions were developed. First, the copper-catalyzed coupling of uracil with aryl iodides, employing picolinamide 16 as the ligand, was discovered. Later, the palladium-catalyzed sulfonamidation of aryl nonaflate 33 was developed, promoted by electron-rich palladium complexes, including the novel phosphine ligand, VincePhos (50). This made possible a convergent, highly efficient synthesis of dasabuvir that significantly reduced the mutagenic impurity burden of the process.
PROCESS FOR PREPARING ANTIVIRAL COMPOUNDS
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, (2012/02/01)
This disclosure is directed to: (a) processes for preparing a compound and salts thereof that, inter alia, are useful for inhibiting hepatitis C virus (HCV); (b) intermediates useful for the preparation of the compound and salts; (c) pharmaceutical compositions comprising the compound or salts; and (d) methods of use of such compositions.
ANTI-INFECTIVE PYRIMIDINES AND USES THEREOF
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Page/Page column 109, (2009/04/25)
This invention relates to: (a) compounds and salts thereof that, inter alia, inhibit HCV; (b) intermediates useful for the preparation of such compounds and salts; (c) compositions comprising such compounds and salts; (d) methods for preparing such intermediates, compounds, salts, and compositions; (e) methods of use of such compounds, salts, and compositions; and (f) kits comprising such compounds, salts, and compositions.
