"目录号: HY-15298B
Anti-infectionMetabolic Enzyme/Protease-
MK-5172是HCV NS3/4a蛋白酶抑制剂，已进入临床阶段。
相关产品
Asunaprevir-PSI-7977-Simeprevir-Daclatasvir-Paritaprevir-Telaprevir-Boceprevir-Ledipasvir-Ombitasvir-MK-5172-Elbasvir-ABT-333-Ribavirin-R-1479-Balapiravir-
生物活性
Description
MK-5172 is a novel P2-P4 quinoxaline macrocyclic HCV NS3/4a protease inhibitor currently in clinical development.IC50 Value: 7.4 nM and 7 nM for genotype 1b and 1a respectively, in replicon system [1]Target: HCV NS3/4a proteasein vitro: 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 [2].in vivo: 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 [1].Clinical trial: Evaluation of Hepatic Pharmacokinetics for MK-5172 in Participants With Chronic Hepatitis C . Phase1
Clinical Trial
Kyushu University-Merck Sharp & Dohme Corp.
Hepatitis C Viral-Chronic Kidney Disease stage3
April 1, 2017
Phase 4
University Hospital, Clermont-Ferrand-Merck Sharp & Dohme Corp.-LC2 PHARMA
Chronic HCV Infection
November 2016
Phase 3
Merck Sharp & Dohme Corp.
Chronic Hepatitis C
June 2014
Phase 3
Taoyuan General Hospital-Merck Sharp & Dohme Corp.
To Assess the Efficacy of Grazoprevir 100mg and Elbasvir 50mg by Determining the Proportion of Sustained Virological Response 12 Weeks After the End of Therapy
June 20, 2017
Phase 4
Kirby Institute
Hepatitis C
December 2016
Phase 4
Merck Sharp & Dohme Corp.
Hepatitis C
October 2013
Phase 1
Institute Of Cardiology & Internal Diseases, Kazakhstan-Schering-Plough-Synergy Research Group
Chronic Hepatitis C Genotype 1B-Metabolic Syndrome-Fibrosis, Liver-Cirrhoses, Liver
October 2017
Phase 3
Merck Sharp & Dohme Corp.
Hepatitis C
October 17, 2012
Erasmus Medical Center
Acute Hepatitis C-Human Immunodeficiency Virus-Hepatitis C
February 2016
Phase 3
Merck Sharp & Dohme Corp.
Chronic Hepatitis C
September 2, 2014
Phase 3
Merck Sharp & Dohme Corp.
Hepatitis C, Chronic
November 2011
Phase 2
University Hospital, Toulouse-MSD France
Hepatitis C-Chronic Kidney Diseases
June 2, 2017
Merck Sharp & Dohme Corp.
Hepatitis C
February 2010
Phase 1
Merck Sharp & Dohme Corp.
Hepatitis C Infection
June 2014
Phase 3
Merck Sharp & Dohme Corp.
Hepatitis C
January 28, 2015
Phase 3
Massachusetts General Hospital-Merck Sharp & Dohme Corp.
Renal Failure
February 1, 2017
Phase 4
Merck Sharp & Dohme Corp.
Hepatitis C
January 2013
Phase 2
Merck Sharp & Dohme Corp.
Hepatitis C
June 2014
Phase 2
University of Maryland
Hepatitis C-Renal Insufficiency, Chronic-Disorder of Transplanted Kidney
May 1, 2017
Phase 4
Merck Sharp & Dohme Corp.
Chronic Hepatitis C (CHC)
December 2012
Phase 2
Norte Study Group-Merck Sharp & Dohme Corp.
Chronic Hepatitis C
January 15, 2017
Phase 4
Merck Sharp & Dohme Corp.
Hepatitis C
July 2011
Phase 1
Institut de Médecine et d'Epidémiologie Appliquée - Fondation Internationale Léon M'Ba-Merck Sharp & Dohme Corp.-Institut National de la Santé Et de la Recherche Médicale, France
Acute Hepatitis C-HIV
May 24, 2017
Phase 2
Merck Sharp & Dohme Corp.
Hepatitis C
October 22, 2014
Phase 3
French National Institute for Health and Medical Research-French National Agency for Research on AIDS and Viral Hepatitis (Inserm-ANRS)
Hepatitis C
January 2016
Phase 2
Hepa C
Hepatitis C
March 31, 2017
Merck Sharp & Dohme Corp.
Hepatitis C Virus
March 2014
Phase 2-Phase 3
Raymond T. Chung, MD-Merck Sharp & Dohme Corp.-Massachusetts General Hospital
Cardiac Transplant Disorder-Hepatitis C
December 1, 2017
Phase 4
Merck Sharp & Dohme Corp.
Chronic Hepatitis C
May 2012
Phase 1
Merck Sharp & Dohme Corp.
Chronic Hepatitis C-Renal Impairment
September 2013
Phase 1
Merck Sharp & Dohme Corp.
Hepatitis C
October 2013
Phase 2
Merck Sharp & Dohme Corp.
Chronic Hepatitis C
May 2014
Phase 2-Phase 3
Merck Sharp & Dohme Corp.
Hepatitis C
November 2014
Phase 3
Merck Sharp & Dohme Corp.
Hepatitis C
February 27, 2015
Phase 3
Merck Sharp & Dohme Corp.
Chronic Hepatitis C Virus
June 2014
Phase 3
Merck Sharp & Dohme Corp.
Hepatitis C
January 2016
Phase 2
Merck Sharp & Dohme Corp.
Hepatitis C
August 2014
Phase 2-Phase 3
Tel-Aviv Sourasky Medical Center-Merck Sharp & Dohme Corp.
HCV, HCC
May 1, 2017
Merck Sharp & Dohme Corp.
Hepatitis C
February 2013
Phase 2
Merck Sharp & Dohme Corp.
Hepatitis C Virus
May 2014
Phase 2
Merck Sharp & Dohme Corp.
Hepatitis C
January 22, 2015
Phase 2
Merck Sharp & Dohme Corp.
Hepatitis C
January 28, 2015
Phase 2
Fundacion SEIMC-GESIDA
HCV
July 15, 2017
Phase 4
Merck Sharp & Dohme Corp.
Hepatitis C, Chronic
June 2011
Phase 2
University of Zurich
Hepatitis C-HIV
June 2016
Phase 3
Fundacion Clinic per a la Recerca Biomédica
Hepatitis C-HIV
September 2016
Phase 3
Fundacion Clinic per a la Recerca Biomédica
Liver Transplantation-Hepatitis C
September 2016
Phase 3
Oregon Health and Science University
Hepatitis C-Substance Use Disorders-Substance Abuse, Intravenous
May 30, 2017
Phase 4
