Paritaprevir (ABT-450) 是一种有效且具有口服活性和抗病毒活性的非结构蛋白 3/4A (NS3/4A) 蛋白酶抑制剂，对 HCV 1a 和 1b 的 EC₅₀ 分别为 1 和 0.21 nM。Paritaprevir 也是一种 SARS-CoV 3CL^pro 抑制剂，IC₅₀ 为1.31 μM。Paritaprevir 主要由细胞色素 P450 (CYP) 3A 代谢。利托那韦 (Ritonavir，一种 CYP450 抑制剂) 可提高 Paritaprevir 的血浆浓度和半衰期。

Paritaprevir (ABT-450) is a potent, orally active and antiviral non-structural protein 3/4A (NS3/4A) protease inhibitor with EC 50 s of 1 and 0.21 nM against HCV 1a and 1b, respectively. Paritaprevir is also a SARS-CoV 3CL inhibitor with an IC 50 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).

Solid

EC50: 1 nM (HCV 1a), 0.21 nM (HCV 1b)
IC50: 1.31 μM (SARS-CoV 3CL)

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. has not independently confirmed the accuracy of these methods. They are for reference only.

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: C max 1.82 μg/mL, AUC 0-24 8.89 μg·h/mL; dog 100 mg/kg, mean: C max 61.3 μg/mL, AUC 0-24 285 μg·h/mL). has not independently confirmed the accuracy of these methods. They are for reference only.

Room temperature in continental US; may vary elsewhere.

4°C, sealed storage, away from moisture and light In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

[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.

In Vitro: DMSO : ≥ 125 mg/mL (163.21 mM)H₂O : ≥ 0.1 mg/mL (0.13 mM)