MK-5172 sodium salt

作者: 莫小枫 | 来源:发表于2017-11-30 15:11 被阅读0次

    "目录号: HY-15298C

    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

    相关文章

      网友评论

        本文标题:MK-5172 sodium salt

        本文链接:https://www.haomeiwen.com/subject/xnmvbxtx.html