[CAS NO. 1370468-36-2] Elbasvir
PRODUCTS SPECIFICATIONS [1370468-36-2]
DESCRIPTION [1370468-36-2]
Overview
| MDL | MFCD30829850 |
|---|---|
| Molecular Weight | 882.02 |
| Molecular Formula | C49H55N9O7 |
| SMILES | O=C([C@H](C(C)C)NC(OC)=O)N(CCC1)[C@@H]1C(N2)=NC=C2C(C=C3)=CC4=C3C5=CC6=CC(C7=CN=C([C@H]8N(C([C@H](C(C)C)NC(OC)=O)=O)CCC8)N7)=CC=C6N5[C@H](C9=CC=CC=C9)O4 |
10 Publications Citing Use of MCE
- [1]Adv Sci (Weinh). 2022 Oct 18;e2203088.
- [2]Hepatology. 2019 May;69(5):1861-1872.
- [3]J Gastroenterol. 2019 May;54(5):449-458.
- [4]Sci Rep. 2019 Apr 5;9(1):5722.
- [5]Viruses. 2018 Aug 28;10(9). pii: E462.
- [6]J Pharmaceut Biomed. 2020 Jan 30;178:112964.
- [7]Hepatol Res. 2019 Nov;49(11):1275-1285.
- [8]J Chromatogr B Analyt Technol Biomed Life Sci. 2019 Mar 15;1110-1111:15-24.
- [9]Pharmaceuticals. 2022 Feb 18;15(2):242.
- [10]Chemrxiv. 2021, Jun 10.
Summary
Elbasvir (MK-8742) is a hepatitis C virus nonstructural protein 5A ( HCV NS5A ) inhibitor with EC 50 s of 4, 3 and 3 nM against genotype 1a, 1b, and 2a, respectively.
IC50 & Target
EC50: 4 nM (HCV 1a), 3 nM (HCV 1b), 3 nM (HCV 2a) [1]
In Vitro
Elbasvir shows potent activity against genotype 1a and 1b replicons, with EC 90 of 0.006 nM for both the wild-type 1a_H77 and 1b_con1 replicons. Elbasvir inhibits genotype 3 replicons with EC 90 of 0.12 nM. Elbasvir (0.06 nM, 0.6 nM, and 6 nM) demonstrates dose-dependent suppression of resistant genotype 1a replicons, illustrated by the reductions in colony counts at higher doses [1] . Elbasvir is highly potent against HCV replicons bearing NS5A sequences from GT1a, -1b, -2a(31L), -3a, -4a, -5a, and -6, with EC 50 s in the low-picomolar range [2] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date | Phase |
|---|---|---|---|---|
| NCT04063839 | University Hospital, Akershus |
Hepatitis C|Substance Use Disorders
|
January 2015 | |
| NCT04047680 | National Taiwan University Hospital |
Hepatitis C|Renal Disease|Viral Hepatitis C
|
February 2015 | |
| NCT02092350 | Merck Sharp & Dohme LLC |
Hepatitis C Virus
|
March 17, 2014 | Phase 2|Phase 3 |
| NCT01532973 | Merck Sharp & Dohme LLC |
Hepatitis, Viral, Human
|
February 16, 2012 | Phase 1 |
| NCT02203149 | Merck Sharp & Dohme LLC |
Hepatitis C
|
August 1, 2014 | Phase 2|Phase 3 |
| NCT03098121 | Taoyuan General Hospital|Merck Sharp & Dohme LLC |
Chronic Hepatitis C
|
October 20, 2017 | Phase 4 |
| NCT03823911 | University of Maryland, Baltimore|National Institutes of Health (NIH)|Merck Sharp & Dohme LLC |
Cardiovascular Diseases|Hepatitis C|Hiv
|
November 18, 2018 | Phase 4 |
| NCT02902120 | University of Maryland, Baltimore |
Hepatitis C|Renal Insufficiency, Chronic|Disorder of Transplanted Kidney
|
May 1, 2017 | Phase 4 |
| NCT02105701 | Merck Sharp & Dohme LLC |
Hepatitis C Infection
|
June 5, 2014 | Phase 3 |
| NCT03496233 | Azienda Ospedaliera Universitaria Policlinico Paolo Giaccone Palermo |
Chronic HCV Hepatitis
|
April 2018 | Phase 3 |
| NCT03365635 | University of Pennsylvania|Merck Sharp & Dohme LLC |
Hepatitis C|Hemodialysis|Nosocomial Infection
|
September 22, 2019 | Phase 4 |
| NCT02332707 | Merck Sharp & Dohme LLC |
Hepatitis C
|
January 22, 2015 | Phase 2 |
| NCT01717326 | Merck Sharp & Dohme LLC |
Hepatitis C
|
February 7, 2013 | Phase 2 |
| NCT02897596 | Fundacion Clinic per a la Recerca Biomédica |
Hepatitis C|HIV
|
April 28, 2017 | Phase 3 |
| NCT02105454 | Merck Sharp & Dohme LLC |
Hepatitis C Virus
|
May 23, 2014 | Phase 2 |
| NCT02332720 | Merck Sharp & Dohme LLC |
Hepatitis C
|
January 28, 2015 | Phase 2 |
| NCT03145623 | University Hospital, Toulouse|MSD France |
Hepatitis C|Chronic Kidney Diseases
|
June 2, 2017 | |
| NCT02945150 | Massachusetts General Hospital|Merck Sharp & Dohme LLC |
Renal Failure
|
February 1, 2017 | Phase 4 |
| NCT02105467 | Merck Sharp & Dohme LLC |
Chronic Hepatitis C Virus
|
June 5, 2014 | Phase 3 |
| NCT02333292 | Valme University Hospital|Hospital del SAS de Jerez|Hospital General Universitario Elche|Hospital La Línea de la Concepción|Complexo Hospitalario Universitario de A Coruña|Hospital de Figueres|Hospital Universitario Puerto Real|Hospital Universitario Virgen de la Victoria|Hospital Universitario de Canarias|Hospital General Universitario de Alicante|Hospital Universitario Araba|Hospital Royo Vilanova|Hospital Universitario de Burgos|Complejo Hospitalario Universitario de Huelva|Hospital Universitario Reina Sofia de Cordoba|Hospital Universitario Virgen Macarena|Complejo Hospitalario Universitario de Vigo|Clinica Universidad de Navarra, Universidad de Navarra|Hospital Clinico Universitario San Cecilio|Hospital Universitario La Fe|Hospital General Universitario de Valencia|Hospital Universitario Infanta Leonor|Hospital Universitario de Gran Canaria|Hospital General Universitario Santa Lucía|Centro Penitenciario Alicante 1|Hospital Regional Universitario Carlos Haya|Hospital Virgen de la Luz|Hospital General Universitario de Castellón|Hospital Parc Taulí, Sabadell |
Chronic Hepatitis C Infection
|
December 2014 | |
| NCT03026023 | Raymond T. Chung, MD|Merck Sharp & Dohme LLC|Massachusetts General Hospital |
Cardiac Transplant Disorder|Hepatitis C
|
August 1, 2018 | Phase 4 |
| NCT03379506 | Merck Sharp & Dohme LLC |
HCV Infection
|
January 25, 2018 | Phase 2 |
| NCT04546802 | Bayside Health|Merck Sharp & Dohme LLC|Austin Hospital, Melbourne Australia |
Hepatocellular Carcinoma|Hepatoma|Liver Cell Carcinoma|Hepatitis C
|
September 2019 | Phase 3 |
| NCT02890719 | Fundacion Clinic per a la Recerca Biomédica |
Liver Transplantation|Hepatitis C
|
May 2, 2017 | Phase 3 |
| NCT01937975 | Merck Sharp & Dohme LLC |
Chronic Hepatitis C|Renal Impairment
|
September 6, 2013 | Phase 1 |
| NCT03723824 | Taichung Veterans General Hospital|Merck Sharp & Dohme LLC |
Chronic Hepatitis c|Liver Transplant Infection|Kidney Transplant Infection
|
February 14, 2019 | Phase 4 |
| NCT01797536 | Merck Sharp & Dohme LLC|Celerion |
Hepatic Insufficiency
|
March 6, 2013 | Phase 1 |
| NCT03144635 | Kyushu University|Merck Sharp & Dohme LLC |
Hepatitis C Viral|Chronic Kidney Disease stage3
|
April 1, 2017 | Phase 4 |
| NCT03407703 | San Francisco Veterans Affairs Medical Center|Merck Sharp & Dohme LLC |
Hepatitis C
|
March 27, 2018 | |
| NCT01932762 | Merck Sharp & Dohme LLC |
Hepatitis C
|
October 1, 2013 | Phase 2 |
| NCT02115321 | Merck Sharp & Dohme LLC |
Chronic Hepatitis C
|
May 9, 2014 | Phase 2|Phase 3 |
| NCT02601573 | Merck Sharp & Dohme LLC |
Hepatitis C
|
January 5, 2016 | Phase 2 |
| NCT02252016 | Merck Sharp & Dohme LLC |
Hepatitis C
|
October 22, 2014 | Phase 3 |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : ≥ 50 mg/mL ( 56.69 mM )
* "≥" means soluble, but saturation unknown.
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 1.1338 mL | 5.6688 mL | 11.3376 mL |
| 5 mM | 0.2268 mL | 1.1338 mL | 2.2675 mL |
| 10 mM | 0.1134 mL | 0.5669 mL | 1.1338 mL |
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1.
References
- [1] Liu R, et al. Susceptibilities of genotype 1a, 1b, and 3 hepatitis C virus variants to the NS5A inhibitor Elbasvir. Antimicrob Agents Chemother. 2015 Nov;59(11):6922-6929.
- [2] Lahser FC, et al. The Combination of Grazoprevir, a Hepatitis C Virus (HCV) NS3/4A Protease Inhibitor, and Elbasvir, an HCV NS5A Inhibitor, Demonstrates a High Genetic Barrier to Resistance in HCV Genotype 1a Replicons. Antimicrob Agents Chemother. 2016 A
Synonyms