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].

MedChemExpress (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).

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

801.91

C₄₀H₄₇N₇O₉S

1456607-71-8

O=C([C@]1(NC([C@@]2([H])N3C[C@H](OC4=C(C=CC=C5)C5=C6C(C=CC=C6)=N4)C2)=O)[C@H](/C=C\CCCCC[C@H](NC(C7=NC=C(C)N=C7)=O)C3=O)C1)NS(=O)(C8CC8)=O.O.O

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]