Paritaprevir dihydrate  (Synonyms: ABT-450 dihydrate; Veruprevir dihydrate)

Paritaprevir (ABT-450) dihydrate 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 dihydrate is also a SARS-CoV 3CL^pro inhibitor with an IC₅₀ of 1.31 μM. Paritaprevir dihydrate is metabolized primarily by cytochrome P450 (CYP) 3A. The plasma concentration and half-life of Paritaprevir dihydrate can be enhanced by Ritonavir (a CYP450 inhibitor)^[1][2][3][4].

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

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^[2].

MCE 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^[1][4].
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).

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

801.91

C₄₀H₄₇N₇O₉S

1456607-71-8

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [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.  [Content Brief]

  [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.  [Content Brief]

  [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.  [Content Brief]

  [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.  [Content Brief]