Paritaprevir (ABT-450) is a potent, orally active and antiviral non-structural protein 3/4A (NS3/4A) protease inhibitor with EC50s of 1 and 0.21 nM against HCV 1a and 1b, respectively. Paritaprevir is also a SARS-CoV 3CLpro inhibitor with an IC50 of 1.31 μM. Paritaprevir is metabolized primarily by cytochrome P450 (CYP) 3A. The plasma concentration and half-life of Paritaprevir can be enhanced by Ritonavir (a CYP450 inhibitor)
产品描述：
Paritaprevir (ABT-450) is a potent, orally active and antiviral non-structural protein 3/4A (NS3/4A) protease inhibitor with EC50s of 1 and 0.21 nM against HCV 1a and 1b, respectively. Paritaprevir is also a SARS-CoV 3CLpro inhibitor with an IC50 of 1.31 μM. Paritaprevir is metabolized primarily by cytochrome P450 (CYP) 3A. The plasma concentration and half-life of Paritaprevir can be enhanced by Ritonavir (a CYP450 inhibitor)
Paritaprevir has in vitro antiviral activity against HCV GT1-4 and GT6 (EC50 range, 0.09 to 19 nM), with an EC50 of 0.09 nM against GT4a
体内研究：
The combination of Paritaprevir, Ritonavir, Ombitasvir (an NS5A protein inhibitor), and Dasabuvir (an NS5B non-nucleoside polymerase inhibitor) with or without RBV has been approved to treat HCV genotype 1 infections. The acute toxicity of Paritaprevir is considered to be low. Single oral doses of ≤600 mg/kg in rats and ≤100 mg/kg in dogs produces no mortality and were well tolerated. However, since Paritaprevir is administered without ritonavir as a PK enhancer, the exposures are low, especially in male rats (rat 600 mg/kg, males: Cmax 1.82 μg/mL, AUC0-24 8.89 μg·h/mL; dog 100 mg/kg, mean: Cmax 61.3 μg/mL, AUC0-24 285 μg·h/mL).
参考文献：
1. Smith MA,et al. Profile of paritaprevir/ritonavir/ombitasvir plus dasabuvir in the treatment of chronic hepatitis C virus genotype 1 infection. Drug Des Devel Ther. 2015 Nov 13;9:6083-94. 2. Schnell G, et al. Hepatitis C Virus Genotype 4 Resistance and Subtype Demographic Characterization of Patients Treated with Ombitasvir plus Paritaprevir/ritonavir. Antimicrob Agents Chemother. 2015 Aug 17. pii: AAC.01229-15. 3. Qi Sun, et al. Bardoxolone and bardoxolone methyl, two Nrf2 activators in clinical trials, inhibit SARS-CoV-2 replication and its 3C-like protease. Signal Transduct Target Ther. 2021 May 29;6(1):212. 4. Menon RM, et al. Drug-drug interaction profile of the all-oral anti-hepatitis C virus regimen of paritaprevir/ritonavir, ombitasvir, and dasabuvir. J Hepatol. 2015 Jul;63(1):20-9.
上海工商
危险品化学品经营许可证（不带存储）
营业执照(三证合一)
北京