|Description||In biochemical assays, MK-5172 was effective against a panel of major genotypes and variants engineered with common resistant mutations observed in clinical studies with other NS3/4a protease inhibitors. In the replicon assay, MK-5172 demonstrated subnanomolar to low-nanomolar EC50s against genotypes 1a, 1b, and 2a. In rats, MK-5172 showed a plasma clearance of 28 ml/min/kg and plasma half-life of 1.4 hr. When dosed p.o. at 5 mg/kg, the plasma exposure of MK-5172 was good with an AUC of 0.7 uM.hr. The liver exposure of the compound was quite good (23 uM at 4 hr), and MK-5172 remained in liver 24 hr after a single p.o. 5 mg/kg dose. At 24 hr, the liver concentration of MK-5172 was 0.2 uM, which was over 25-fold higher than the IC50 in the replicon assay with 50% NHS. When dosed to dogs, MK-5172 showed low clearance of 5 ml/min/kg and a 3 hr half-life after i.v. 2 mg/kg dosing and had good plasma exposure (AUC=0.4 uM.hr) after a p.o. 1 mg/kg dose.|
|Synonyms||Grazoprevir potassium salt; MK5172 potassium salt; MK 5172 potassium salt|
Danoprevir(ITMN-191;R7227; RO5190591;RG7227) is a peptidomimetic inhibitor of the NS3/4A protease of hepatitis C virus (HCV) with IC50 of 0.2-3.5 nM, inhibition...
Simeprevir plays an important role in HCV replication. Data from phase I and II clinical trials of TMC-435350 (TMC 435350; TMC 435; TMC-435350) to date have sho...
An NS3 serine protease inhibitor of hepatitis C virus, for the treatment of HCV infection.
PSI-7976 is an inhibitor of HCV RNA replication with EC50 value of 1.07μM. PSI-7851 is a phosphoramidate prodrug of PSI-7411 and has potent anti-hepatitis C vir...
Against JFH1/3a-NS5A, DCV was more potent (EC(50) = 0.52 nM) than GS-5885 (EC(50) = 141 nM). DCV sensitivity was increased against JFH1/3a-NS5A-M28V (EC50 = 0.0...
PSI-6206 (RO2433) is a selective HCV RNA polymerase inhibitor. It is the unphosphorylated parent compound of triphosphate analog PSI-7409, which is a potent inh...
Ribavirin is a guanosine (ribonucleic) analog used to stop viral RNA synthesis and viral mRNA capping, thus, it is a nucleoside inhibitor.
APC-6336 is a Hepatitis C virus NS3 protein inhibitor.
Alisporivir, also known as DEB-025, a non-immunosuppressive cyclosporine A derivative, is acyclophil ininhibitor molecule with potent anti-hepatitis C virus (HC...
Nesbuvir, a novel selective nonstructural protein 5B (NS5B) polymerase inhibitor, acts as candidate for HCV treatment. It was reduced across different isolates.
BMS-890068 is an acyclic P1 bi-cyclopropaneacylsulfonamidetripeptide that can be used as hepatitis C virus (HCV) NS3 protease inhibitor.
GSK-2818713 is a second-generation inhibitor of hepatitis C virus (HCV) NS5A replication. Compared to daclatasvir, a first-generation NS5A replication complex i...
Dasabuvir is an antiviral drug for the treatment of hepatitis C. It inhibits hepatitis C virus (HCV) non-nucleoside NS5B palm polymerase to suppress RNA replica...
VX-950 is a potent, selective, peptidomimetic inhibitor of the hepatitis C virus (HCV) NS3-4A serine protease, and it demonstrated excellent antiviral activity ...
Avidasvir is a second-generation Hepatitis C virus NS 5 protein inhibitor. In Sep 2016, Phase-II/III clinical trials in Hepatitis C in Malaysia was on-going.
Vedroprevir is a selective hepatitis C virus (HCV) NS3 protease inhibitor. It is a pharmaceutical drug that is used in the treatment of hepatitis C virus in pat...
In biochemical assays, MK-5172 was effective against a panel of major genotypes and variants engineered with common resistant mutations observed in clinical stu...
Anguizole is a small molecule inhibitor of HCV replication and alters NS4B's subcellular distribution.
Daclatasvir, inhibits the HCV protein NS5A, and thus can be used as a drug candidate for the treatment of hepatitis C (HCV).
Tegobuvir is a non-nucleoside nonstructural protein (NS)5B polymerase inhibitor.