MK-5172 potassium salt

"目录号: HY-15298A

Anti-infectionMetabolic Enzyme/Protease-

MK-5172是HCV NS3/4a蛋白酶抑制剂,已进入临床阶段。

HCVHCV Protease

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

NCT03144635

Kyushu University-Merck Sharp & Dohme Corp.

Hepatitis C Viral-Chronic Kidney Disease stage3

April 1, 2017

Phase 4

NCT02973503

University Hospital, Clermont-Ferrand-Merck Sharp & Dohme Corp.-LC2 PHARMA

Chronic HCV Infection

November 2016

Phase 3

NCT02105662

Merck Sharp & Dohme Corp.

Chronic Hepatitis C

June 2014

Phase 3

NCT03098121

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

NCT02940691

Kirby Institute

Hepatitis C

December 2016

Phase 4

NCT01537900

Merck Sharp & Dohme Corp.

Hepatitis C

October 2013

Phase 1

NCT03222167

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

NCT01667081

Merck Sharp & Dohme Corp.

Hepatitis C

October 17, 2012

NCT02600325

Erasmus Medical Center

Acute Hepatitis C-Human Immunodeficiency Virus-Hepatitis C

February 2016

Phase 3

NCT02105688

Merck Sharp & Dohme Corp.

Chronic Hepatitis C

September 2, 2014

Phase 3

NCT01440595

Merck Sharp & Dohme Corp.

Hepatitis C, Chronic

November 2011

Phase 2

NCT03145623

University Hospital, Toulouse-MSD France

Hepatitis C-Chronic Kidney Diseases

June 2, 2017

NCT00998985

Merck Sharp & Dohme Corp.

Hepatitis C

February 2010

Phase 1

NCT02105701

Merck Sharp & Dohme Corp.

Hepatitis C Infection

June 2014

Phase 3

NCT02251990

Merck Sharp & Dohme Corp.

Hepatitis C

January 28, 2015

Phase 3

NCT02945150

Massachusetts General Hospital-Merck Sharp & Dohme Corp.

Renal Failure

February 1, 2017

Phase 4

NCT01716156

Merck Sharp & Dohme Corp.

Hepatitis C

January 2013

Phase 2

NCT02133131

Merck Sharp & Dohme Corp.

Hepatitis C

June 2014

Phase 2

NCT02902120

University of Maryland

Hepatitis C-Renal Insufficiency, Chronic-Disorder of Transplanted Kidney

May 1, 2017

Phase 4

NCT01710501

Merck Sharp & Dohme Corp.

Chronic Hepatitis C (CHC)

December 2012

Phase 2

NCT03022006

Norte Study Group-Merck Sharp & Dohme Corp.

Chronic Hepatitis C

January 15, 2017

Phase 4

NCT01390428

Merck Sharp & Dohme Corp.

Hepatitis C

July 2011

Phase 1

NCT02886624

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

NCT02252016

Merck Sharp & Dohme Corp.

Hepatitis C

October 22, 2014

Phase 3

NCT02647632

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

NCT03111966

Hepa C

Hepatitis C

March 31, 2017

NCT02092350

Merck Sharp & Dohme Corp.

Hepatitis C Virus

March 2014

Phase 2-Phase 3

NCT03026023

Raymond T. Chung, MD-Merck Sharp & Dohme Corp.-Massachusetts General Hospital

Cardiac Transplant Disorder-Hepatitis C

December 1, 2017

Phase 4

NCT01547312

Merck Sharp & Dohme Corp.

Chronic Hepatitis C

May 2012

Phase 1

NCT01937975

Merck Sharp & Dohme Corp.

Chronic Hepatitis C-Renal Impairment

September 2013

Phase 1

NCT01932762

Merck Sharp & Dohme Corp.

Hepatitis C

October 2013

Phase 2

NCT02115321

Merck Sharp & Dohme Corp.

Chronic Hepatitis C

May 2014

Phase 2-Phase 3

NCT02204475

Merck Sharp & Dohme Corp.

Hepatitis C

November 2014

Phase 3

NCT02358044

Merck Sharp & Dohme Corp.

Hepatitis C

February 27, 2015

Phase 3

NCT02105467

Merck Sharp & Dohme Corp.

Chronic Hepatitis C Virus

June 2014

Phase 3

NCT02601573

Merck Sharp & Dohme Corp.

Hepatitis C

January 2016

Phase 2

NCT02203149

Merck Sharp & Dohme Corp.

Hepatitis C

August 2014

Phase 2-Phase 3

NCT03110055

Tel-Aviv Sourasky Medical Center-Merck Sharp & Dohme Corp.

HCV, HCC

May 1, 2017

NCT01717326

Merck Sharp & Dohme Corp.

Hepatitis C

February 2013

Phase 2

NCT02105454

Merck Sharp & Dohme Corp.

Hepatitis C Virus

May 2014

Phase 2

NCT02332707

Merck Sharp & Dohme Corp.

Hepatitis C

January 22, 2015

Phase 2

NCT02332720

Merck Sharp & Dohme Corp.

Hepatitis C

January 28, 2015

Phase 2

NCT03105349

Fundacion SEIMC-GESIDA

HCV

July 15, 2017

Phase 4

NCT01353911

Merck Sharp & Dohme Corp.

Hepatitis C, Chronic

June 2011

Phase 2

NCT02785666

University of Zurich

Hepatitis C-HIV

June 2016

Phase 3

NCT02897596

Fundacion Clinic per a la Recerca Biomédica

Hepatitis C-HIV

September 2016

Phase 3

NCT02890719

Fundacion Clinic per a la Recerca Biomédica

Liver Transplantation-Hepatitis C

September 2016

Phase 3

NCT03093415

Oregon Health and Science University

Hepatitis C-Substance Use Disorders-Substance Abuse, Intravenous

May 30, 2017

Phase 4

你可能感兴趣的:(MK-5172 potassium salt)