DOCSLIB.ORG

(12) Patent Application Publication (10) Pub. No.: US 2014/0275099 A1 Bernstein Et Al

Total Page：16

File Type：pdf, Size：1020Kb

Download full-text PDF Read full-text
(12) Patent Application Publication (10) Pub. No.: US 2014/0275099 A1 Bernstein Et Al US 20140275099A1 (19) United States (12) Patent Application Publication (10) Pub. No.: US 2014/0275099 A1 Bernstein et al. (43) Pub. Date: Sep. 18, 2014 (54) METHODS FOR TREATING HCV Publication Classification (71) Applicant: AbbVie Inc., North Chicago, IL (US) (51) Int. Cl. A613 L/4985 (2006.01) (72) Inventors: Barry M. Bernstein, Mequon, WI (US); A613 L/454 (2006.01) Sandeep Dutta, Lincolnshire, IL (US); (52) U.S. Cl. Wei Liu, Mundelein, IL (US); Thomas CPC ........... A6 IK3I/4985 (2013.01); A61 K3I/454 J. Podsadecki, Chicago, IL (US); (2013.01) Andrew L. Campbell, Lake Forest, IL USPC .......................................................... S14/250 (US); Rajeev M. Menon, Buffalo Grove, IL (US); Chih-Wei Lin, Vernon Hills, IL (57) ABSTRACT (US); Tianli Wang, Lake Bluff, IL (US); The present invention features interferon- and ribavirin-free Walid M.Awni, Green Oaks, IL (US) therapies for the treatment of HCV. Preferably, the treatment is over a shorter duration of treatment, such as no more than (21) Appl. No.: 14/210,870 12 weeks. In one aspect, the treatment comprises administer ing at least two direct acting antiviral agents without inter (22) Filed: Mar 14, 2014 feron and ribavirin to a subject with HCV infection, wherein the treatment lasts for 12 weeks, and said at least two direct Related U.S. Application Data acting antiviral agents comprise (a) Compound 1 or a phar (60) Provisional application No. 61/783,376, filed on Mar. maceutically acceptable salt thereofand (b) Compound 2 or a 14, 2013. pharmaceutically acceptable salt thereof. Patent Application Publication Sep. 18, 2014 Sheet 1 of 7 US 2014/0275099 A1 ax. i ~~~~~ 333. :38 33 ;: 3. if S 838 is: Patent Application Publication Sep. 18, 2014 Sheet 2 of 7 US 2014/0275099 A1 i 3. 3: 3: six 3. { & S : 88.ie Patent Application Publication Sep. 18, 2014 Sheet 3 of 7 US 2014/0275099 A1 x x: er s ex S. s : iS x 388 is Patent Application Publication Sep. 18, 2014 Sheet 4 of 7 US 2014/0275099 A1 if xS : pe Patent Application Publication Sep. 18, 2014 Sheet 5 of 7 US 2014/0275099 A1 i (i. 88: : * : if S - 388. Patent Application Publication Sep. 18, 2014 Sheet 6 of 7 US 2014/0275099 A1 i 3. 38 : ;: : : if S : 838 is Patent Application Publication Sep. 18, 2014 Sheet 7 of 7 US 2014/0275099 A1 s & s ss i k e At ptariocities US 2014/0275099 A1 Sep. 18, 2014 METHODS FOR TREATING HCV 0007. In any method described herein, the at least two DAAS comprise (a) Compound 1 or a pharmaceutically 0001. This application claims the benefit of U.S. Provi acceptable salt thereof, and (b) Compound 2 or a pharmaceu sional Application No. 61/783,376, filed Mar. 14, 2013, tically acceptable salt thereof. The at least two DAAs can also which is incorporated herein by reference in its entirety. optionally comprise another anti-HCV agent. The other optional anti-HCV agent can be selected from protease FIELD OF THE INVENTION inhibitors, nucleoside or nucleotide polymerase inhibitors, non-nucleoside polymerase inhibitors, NS3B inhibitors, 0002 The present invention relates to interferon-free and NS4A inhibitors, NS5A inhibitors, NS5B inhibitors, cyclo ribavirin-free treatment for hepatitis C virus (HCV). philin inhibitors, or combinations thereof. For example, in some embodiments, the DAAs used in a method of the present BACKGROUND OF THE INVENTION invention comprise or consist of (a) Compound 1 or a phar 0003. The HCV is an RNA virus belonging to the Hepa maceutically acceptable salt thereof, and (b) Compound 2 or civirus genus in the Flaviviridae family. The enveloped HCV a pharmaceutically acceptable salt thereof. For another virion contains a positive stranded RNA genome encoding all example, the DAAs used in a method of the present invention known virus-specific proteins in a single, uninterrupted, open comprise or consist of (a) Compound 1 or a pharmaceutically reading frame. The open reading frame comprises approxi acceptable salt thereof, (b) Compound 2 or a pharmaceuti mately 9500 nucleotides and encodes a single large polypro cally acceptable salt thereof, and (c) a HCV polymerase tein of about 3000 amino acids. The polyprotein comprises a inhibitor, wherein said HCV polymerase inhibitor can be a core protein, envelope proteins E1 and E2, a membrane nucleotide or nucleoside polymerase inhibitor or a non bound protein p7, and the non-structural proteins NS2. NS3, nucleoside or non-nucleotide polymerase inhibitor. NS4A, NS4B, NS5A and NS5B. 0008. Non-limiting examples of the other optional antic 0004 Chronic HCV infection is associated with progres HCV agent include PSI-7977 (sofosbuvir), PSI-938, BMS sive liver pathology, including cirrhosis and hepatocellular 790052 (daclatasvir), BMS-650032 (asunaprevir), BMS carcinoma. Chronic hepatitis C may be treated with peginter 791325, GS-5885 (ledipasvir), GS-9451 (tegobuvir), feron-alpha in combination with ribavirin. Substantial limi GS-9190, GS-9256, BI-201335. BI-27127, telaprevir, tations to efficacy and tolerability remain as many users Suffer VX-222, TMC-435 (simepravir), MK-5172, MK-7009 (vani from side effects, and viral elimination from the body is often previr), danoprevir, R7128 (mericitabine), and any combina incomplete. Therefore, there is a need for new therapies to tion thereof. treat HCV infection. 0009. In any method described herein, the DAAS can be administered in any effective dosing schemes and/or frequen BRIEF SUMMARY OF THE INVENTION cies; for example, they can each be administered daily. Each DAA can be administered either separately or in combina 0005 One aspect of the present invention features meth tion, and each DAA can be administered once a day, twice a ods for treating HCV infection in a subject in need of such day, or three times a day. Preferably, Compound 1 (or a treatment. The methods comprise administering at least two pharmaceutically acceptable salt thereof) and Compound 2 direct acting antiviral agents (DAAS) to the Subject for a (or a pharmaceutically acceptable salt thereof) are adminis duration of no more than 12 weeks, or for another duration as tered once daily. set forth herein. The at least two DAAs comprise Compound 0010 Preferably, Compound 1 (or a pharmaceutically 1 (or a pharmaceutically acceptable salt thereof) and Com acceptable salt thereof) is administered from 100 mg to 600 pound 2 (or a pharmaceutically acceptable salt thereof). Pref mg once daily, and Compound 2 (or a pharmaceutically erably, the duration of the treatment is 12 weeks. The duration acceptable salt thereof) is administered from 50 to 500 mg of the treatment can also be, for example, no more than 8 once daily. More preferably, Compound 1 (or a pharmaceu weeks. Preferably, the two or more DAAs are administered in tically acceptable salt thereof) is administered from 200 mg to amounts effective to provide a Sustained Virological response 600 mg once daily, and Compound 2 (or a pharmaceutically (SVR) or achieve another desired measure of effectiveness in acceptable salt thereof) is administered from 100 to 500 mg the subject. The subject is not administered ribavirin during once daily. Highly preferably, Compound 1 (or a pharmaceu the treatment regimen. The Subject is also not administered tically acceptable salt thereof) is administered from 400 mg to interferon during the treatment regimen. Put another way, the 600 mg once daily, and Compound 2 (or a pharmaceutically methods exclude the administration of interferon or ribavirin acceptable salt thereof) is administered from 100 to 500 mg to the subject, thereby avoiding the side effects associated once daily. For instance, Compound 1 (or a pharmaceutically with interferon and ribavirin. acceptable salt thereof) can be administered 400 mg once 0006 Another aspect of the present invention features daily, and Compound 2 (or a pharmaceutically acceptable salt methods for treating a population of subjects having HCV thereof) is administered 120 mg once daily. For another infection. The methods comprise administering at least two instance, Compound 1 (or a pharmaceutically acceptable salt DAAS to the subjects for a duration of no more than 12 weeks. thereof) can be administered 400 mg once daily, and Com The at least two DAAS comprise Compound 1 (or a pharma pound 2 (or a pharmaceutically acceptable salt thereof) can be ceutically acceptable salt thereof) and Compound 2 (or a administered 240 mg once daily. pharmaceutically acceptable salt thereof). Preferably, the at 0011. In yet another aspect, the present invention features least two DAAS are administered to the Subjects in amounts a combination of Compound 1 (or a pharmaceutically accept effective to result in SVR or another measure of effectiveness able Salt thereof) and Compound 2 (or a pharmaceutically in at least about 70% of the population, preferably at least acceptable salt thereof) for use to treat HCV infection. The about 80% of the population, or more preferably at least about treatment comprises administering the DAAS to a subject 90%/o of the population. infected with HCV. The duration of the treatment regimen is US 2014/0275099 A1 Sep. 18, 2014 no more than twelve weeks (e.g., the duration being 12 a null responder) infected with HCV genotype 1. In yet weeks; or the duration being 11, 10, 9, 8, 7, 6, 5, 4, or 3 another example, the treatment lasts for 8 weeks, and the weeks). Preferably, the duration of the treatment regimen is Subject being treated is a non-responder (e.g., a null twelve weeks. The duration of the treatment can also last, for responder) infected with HCV genotype 1. In yet another example, no more than eight weeks (e.g., the duration being 8 example, the treatment lasts for 12 weeks, and the Subject being treated is a non-responder (e.g., a null responder) weeks; or the duration being 7, 6, 5, 4, or 3 weeks).
Load more

Recommended publications
  • Assessment Report
    21 November 2013 EMA/CHMP/688774/2013 Committee for Medicinal Products for Human Use (CHMP) Assessment report Sovaldi International non-proprietary name: sofosbuvir Procedure No. EMEA/H/C/002798/0000 Note Assessment report as adopted by the CHMP with all information of a commercially confidential nature deleted. 7 Westferry Circus ● Canary Wharf ● London E14 4HB ● United Kingdom Telephone +44 (0)20 7418 8400 Facsimile +44 (0)20 7523 7455 E-mail [email protected] Website www.ema.europa.eu An agency of the European Union © European Medicines Agency, 2014. Reproduction is authorised provided the source is acknowledged. Table of contents 1. Background information on the procedure ............................................ 7 1.1. Submission of the dossier .................................................................................... 7 1.2. Manufacturers .................................................................................................... 8 1.3. Steps taken for the assessment of the product ....................................................... 8 2. Scientific discussion .............................................................................. 9 2.1. Introduction ....................................................................................................... 9 2.2. Quality aspects ................................................................................................ 14 2.2.1. Introduction .................................................................................................. 14 2.2.2.
    [Show full text]
  • HCV - - Leverages Gilead’S Infrastructure and Expertise in Antiviral Drug Development, Manufacturing and Commercialization
    UNITED STATES SECURITIES AND EXCHANGE COMMISSION WASHINGTON, D.C. 20549 FORM 8-K CURRENT REPORT Pursuant to Section 13 or 15(d) of the Securities Exchange Act of 1934 Date of Report (Date of Earliest Event Reported): November 21, 2011 Gilead Sciences, Inc. (Exact name of registrant as specified in its charter) Delaware 0-19731 94-3047598 (State or other jurisdiction (Commission (I.R.S. Employer of incorporation) File Number) Identification No.) 333 Lakeside Drive, Foster City, California 94404 (Address of principal executive offices) (Zip Code) Registrant’s telephone number, including area code (650) 574-3000 Not Applicable Former name or former address, if changed since last report Check the appropriate box below if the Form 8-K filing is intended to simultaneously satisfy the filing obligation of the registrant under any of the following provisions: ¨ Written communications pursuant to Rule 425 under the Securities Act (17 CFR 230.425) ¨ Soliciting material pursuant to Rule 14a-12 under the Exchange Act (17 CFR 240.14a-12) x Pre-commencement communications pursuant to Rule 14d-2(b) under the Exchange Act (17 CFR 240.14d-2(b)) ¨ Pre-commencement communications pursuant to Rule 13e-4(c) under the Exchange Act (17 CFR 240.13e-4(c)) Item 8.01 Other Events. On November 21, 2011, Gilead Sciences, Inc. (“Gilead”) announced that it had signed a definitive agreement under which Gilead will acquire Pharmasset, Inc. (“Pharmasset”) for $137 cash per Pharmasset share. The transaction, which values Pharmasset at approximately $11 billion, was unanimously approved by Pharmasset’s Board of Directors. A copy of the Press Release is attached as Exhibit 99.1 to this Current Report on Form 8-K and is incorporated herein by reference.
    [Show full text]
  • Review Resistance to Mericitabine, a Nucleoside Analogue Inhibitor of HCV RNA-Dependent RNA Polymerase
    Antiviral Therapy 2012; 17:411–423 (doi: 10.3851/IMP2088) Review Resistance to mericitabine, a nucleoside analogue inhibitor of HCV RNA-dependent RNA polymerase Jean-Michel Pawlotsky1,2*, Isabel Najera3, Ira Jacobson4 1National Reference Center for Viral Hepatitis B, C and D, Department of Virology, Hôpital Henri Mondor, Université Paris-Est, Créteil, France 2INSERM U955, Créteil, France 3Roche, Nutley, NJ, USA 4Weill Cornell Medical College, New York-Presbyterian Hospital, New York, NY, USA *Corresponding author e-mail: [email protected] Mericitabine (RG7128), an orally administered prodrug passage experiments. To date, no evidence of genotypic of PSI-6130, is the most clinically advanced nucleoside resistance to mericitabine has been detected by popula- analogue inhibitor of the RNA-dependent RNA poly- tion or clonal sequence analysis in any baseline or on- merase (RdRp) of HCV. This review describes what has treatment samples collected from >600 patients enrolled been learnt so far about the resistance profile of mericit- in Phase I/II trials of mericitabine administered as mon- abine. A serine to threonine substitution at position 282 otherapy, in combination with pegylated interferon/ (S282T) of the RdRp that reduces its replication capacity ribavirin, or in combination with the protease inhibitor, to approximately 15% of wild-type is the only variant danoprevir, for 14 days in the proof-of-concept study of that has been consistently generated in serial in vitro interferon-free therapy. Introduction The approval of boceprevir and telaprevir [1,2], the first HCV variants are selected and grow when the inter- inhibitors of the non-structural (NS) 3/4A (NS3/4A) feron response is inadequate [3,4,6].
    [Show full text]
  • Current and Future Therapies for Hepatitis C Virus Infection: from Viral Proteins to Host Targets
    Arch Virol DOI 10.1007/s00705-013-1803-7 BRIEF REVIEW Current and future therapies for hepatitis C virus infection: from viral proteins to host targets Muhammad Imran • Sobia Manzoor • Nasir Mahmood Khattak • Madiha Khalid • Qazi Laeeque Ahmed • Fahed Parvaiz • Muqddas Tariq • Javed Ashraf • Waseem Ashraf • Sikandar Azam • Muhammad Ashraf Received: 27 February 2013 / Accepted: 19 June 2013 Ó Springer-Verlag Wien 2013 Abstract Hepatitis C virus (HCV) infection is the most cell-targeting compounds, the most hopeful results have important problem across the world. It causes acute and been demonstrated by cyclophilin inhibitors. The current chronic liver infection. Different approaches are in use to SOC treatment of HCV infection is Peg-interferon, riba- inhibit HCV infection, including small organic compounds, virin and protease inhibitors (boceprevir or telaprevir). The siRNA, shRNA and peptide inhibitors. This review article future treatment of this life-threatening disease must summarizes the current and future therapies for HCV involve combinations of therapies hitting multiple targets infection. PubMed and Google Scholar were searched for of HCV and host factors. It is strongly expected that the articles published in English to give an insight into the near future, treatment of HCV infection will be a combi- current inhibitors against this life-threatening virus. HCV nation of direct-acting agents (DAA) without the involve- NS3/4A protease inhibitors and nucleoside/nucleotide ment of interferon to eliminate its side effects. inhibitors of NS5B polymerase are presently in the most progressive stage of clinical development, but they are linked with the development of resistance and viral Introduction breakthrough. Boceprevir and telaprevir are the two most important protease inhibitors that have been approved HCV is a major health burden affecting about 200 million recently for the treatment of HCV infection.
    [Show full text]
  • Curing Hepatitis C" by Gregory T
    6 ThE FUTURE of HCV TREATMENT Beyond Triple Therapy I am still on treatment and almost halfway through the trial. I do not have hepatitis C at the present time. I hope this treatment has cured it, and I hope I will not need future treatment. The results were immediate. Before I began the QUAD Therapy clinical trial, there were over four million copies of the virus per milliliter of my blood. After the first week, that was down to only 160 copies per milliliter, and, at week two, I tested negative for hepatitis C. The virus is still undetectable in my blood—hopefully, this is it, and I am cured. — Mark Tw e n ty year s ago, I treated patients with HCV genotype 1 infection with interferon monotherapy, and five percent achieved SVR. Results improved to an SVR of 45 percent with peginterferon/ribavirin. Now, the new standard of care of triple therapy is expected to raise SVR up to 75 percent. What’s next? In this chapter, I look to the future, focusing on the next generation of direct-acting antivirals: new protease inhibitors, polymerase inhibitors, From "Curing Hepatitis C" by Gregory T. Everson Reprinted with permission— 115 by Hatherleigh— Press ISBN: 978-1-57826-425-4 Available wherever books are sold 116 CUR in G H E PA titis C NS5A inhibitors, and others. The future for treating HCV is, indeed, bright. Hopefully, the time will soon arrive when nearly every person infected with HCV will have safe, tolerable, and effective options for treatment. The year 2011 marked the beginning of a new era in the treatment of the hepatitis C virus (HCV) with the introduction of telaprevir and boceprevir.
    [Show full text]
  • Stembook 2018.Pdf
    The use of stems in the selection of International Nonproprietary Names (INN) for pharmaceutical substances FORMER DOCUMENT NUMBER: WHO/PHARM S/NOM 15 WHO/EMP/RHT/TSN/2018.1 © World Health Organization 2018 Some rights reserved. This work is available under the Creative Commons Attribution-NonCommercial-ShareAlike 3.0 IGO licence (CC BY-NC-SA 3.0 IGO; https://creativecommons.org/licenses/by-nc-sa/3.0/igo). Under the terms of this licence, you may copy, redistribute and adapt the work for non-commercial purposes, provided the work is appropriately cited, as indicated below. In any use of this work, there should be no suggestion that WHO endorses any specific organization, products or services. The use of the WHO logo is not permitted. If you adapt the work, then you must license your work under the same or equivalent Creative Commons licence. If you create a translation of this work, you should add the following disclaimer along with the suggested citation: “This translation was not created by the World Health Organization (WHO). WHO is not responsible for the content or accuracy of this translation. The original English edition shall be the binding and authentic edition”. Any mediation relating to disputes arising under the licence shall be conducted in accordance with the mediation rules of the World Intellectual Property Organization. Suggested citation. The use of stems in the selection of International Nonproprietary Names (INN) for pharmaceutical substances. Geneva: World Health Organization; 2018 (WHO/EMP/RHT/TSN/2018.1). Licence: CC BY-NC-SA 3.0 IGO. Cataloguing-in-Publication (CIP) data.
    [Show full text]
  • Interferon-Combination Strategies for the Treatment of Chronic Hepatitis C
    30 Interferon-Combination Strategies for the Treatment of Chronic Hepatitis C Andrew Aronsohn, MD1 Donald Jensen, MD1 1 Center for Liver Disease, Section of Gastroenterology, Hepatology Address for correspondence Andrew Aronsohn, MD, Center for Liver and Nutrition, University of Chicago Medical Center, Chicago, Illinois Disease, Section of Gastroenterology, Hepatology and Nutrition, 5841 South Maryland Avenue, MC 7120, Chicago, IL 60637 Semin Liver Dis 2014;34:30–36. (e-mail: [email protected]). Abstract Direct acting antiviral agents have revolutionized hepatitis C (HCV) therapy. Many agents that are either currently available or undergoing investigation offer higher rates of sustained virologic response, reduced toxicity and shorter duration of therapy when compared to traditional treatment consisting of pegylated interferon and ribavirin. Keywords Although interferon free therapy may be a preferred option, some patients may still ► hepatitis C require an interferon based regimen to ensure efficacy. In this review, we discuss ► hepatitis C therapy therapeutic strategies which utilize various combinations of protease inhibitors, NS5A ► direct-acting antiviral inhibitors, nucleotide polymerase inhibitors and non-nucleoside polymerase inhibitors agents along with pegylated interferon in the treatment of chronic HCV. In 2011, the first direct-acting antiviral agents (DAAs) became complex is involved in decreasing activity of type 1 IFN available for use in the treatment of chronic hepatitis C. In though cleavage of IFN-B promoter
    [Show full text]
  • Review : Imunoterapi Penanganan Infeksi Virus
    Jurnal Mandala Pharmacon Indonesia, Vol 7.No.1 Juni 2021 Avaiable online at www.jurnal-pharmaconmw.com/jmpi p-ISSN : 2442-6032 e-ISSN : 2598-9979 Review : Imunoterapi Penanganan Infeksi Virus Usmar1, Andi Maqhfirah Nurul Fitri1, Dewi Yuliana2, Firzan Nainu1* 1Fakultas Farmasi, Universitas Hasanuddin, Makassar 2Fakultas Farmasi, Universitas Muslim Indonesia, Makassar ABSTRAK Penyakit menular akibat virus merupakan salah satu perkembangan yang pesat terutama dalam kondisi masalah kesehatan global yang mempengaruhi sistem pandemi COVID-19 yang dihadapi saat ini. Meskipun kesehatan masyarakat dan ekonomi di seluruh dunia. terapi dan obat-obatan yang digunakan dalam bidang Hal tersebut mendorong disusunnya artikel ini untuk imunofarmakologi masih terbatas serta banyak hal yang mendiskusikan relevansi dan pentingnya imunoterapi belum dapat ditemukan, namun teknologi baru dan dalam menentukan pilihan terapetik terkait infeksi kemajuan pesat dalam pengetahuan tentang regulasi virus, dengan menitikberatkan pembahasan pada sistem imun telah menjadikan imunoterapi sebagai ketersediaan pilihan vaksin dan obat yang telah bidang yang memiliki potensi besar dan menjanjikan ditemukan untuk membantu manusia melawan berbagai dalam penanganan infeksi virus maupun patogen lain. jenis infeksi yang disebabkan oleh virus. Penulisan Oleh karena itu, konsep imunoterapi serta relevansinya artikel review naratif ini dilakukan menggunakan dengan penyakit manusia merupakan salah satu solusi metode analisis pustaka primer maupun sekunder yang menawarkan pilihan baru
    [Show full text]
  • Repurposing of FDA Approved Drugs
    Antiviral Drugs (In Phase IV) ABACAVIR GEMCITABINE ABACAVIR SULFATE GEMCITABINE HYDROCHLORIDE ACYCLOVIR GLECAPREVIR ACYCLOVIR SODIUM GRAZOPREVIR ADEFOVIR DIPIVOXIL IDOXURIDINE AMANTADINE IMIQUIMOD AMANTADINE HYDROCHLORIDE INDINAVIR AMPRENAVIR INDINAVIR SULFATE ATAZANAVIR LAMIVUDINE ATAZANAVIR SULFATE LEDIPASVIR BALOXAVIR MARBOXIL LETERMOVIR BICTEGRAVIR LOPINAVIR BICTEGRAVIR SODIUM MARAVIROC BOCEPREVIR MEMANTINE CAPECITABINE MEMANTINE HYDROCHLORIDE CARBARIL NELFINAVIR CIDOFOVIR NELFINAVIR MESYLATE CYTARABINE NEVIRAPINE DACLATASVIR OMBITASVIR DACLATASVIR DIHYDROCHLORIDE OSELTAMIVIR DARUNAVIR OSELTAMIVIR PHOSPHATE DARUNAVIR ETHANOLATE PARITAPREVIR DASABUVIR PENCICLOVIR DASABUVIR SODIUM PERAMIVIR DECITABINE PERAMIVIR DELAVIRDINE PIBRENTASVIR DELAVIRDINE MESYLATE PODOFILOX DIDANOSINE RALTEGRAVIR DOCOSANOL RALTEGRAVIR POTASSIUM DOLUTEGRAVIR RIBAVIRIN DOLUTEGRAVIR SODIUM RILPIVIRINE DORAVIRINE RILPIVIRINE HYDROCHLORIDE EFAVIRENZ RIMANTADINE ELBASVIR RIMANTADINE HYDROCHLORIDE ELVITEGRAVIR RITONAVIR EMTRICITABINE SAQUINAVIR ENTECAVIR SAQUINAVIR MESYLATE ETRAVIRINE SIMEPREVIR FAMCICLOVIR SIMEPREVIR SODIUM FLOXURIDINE SOFOSBUVIR FOSAMPRENAVIR SORIVUDINE FOSAMPRENAVIR CALCIUM STAVUDINE FOSCARNET TECOVIRIMAT FOSCARNET SODIUM TELBIVUDINE GANCICLOVIR TENOFOVIR ALAFENAMIDE GANCICLOVIR SODIUM TENOFOVIR ALAFENAMIDE FUMARATE TIPRANAVIR VELPATASVIR TRIFLURIDINE VIDARABINE VALACYCLOVIR VOXILAPREVIR VALACYCLOVIR HYDROCHLORIDE ZALCITABINE VALGANCICLOVIR ZANAMIVIR VALGANCICLOVIR HYDROCHLORIDE ZIDOVUDINE Antiviral Drugs (In Phase III) ADEFOVIR LANINAMIVIR OCTANOATE
    [Show full text]
  • 1 Identification of Potent Drugs and Antiviral Agents for the Treatment Of
    1 Identification of Potent Drugs and Antiviral Agents for the Treatment of the SARS- CoV-2 Infection N.R. Jena* Discipline of Natural Sciences, Indian Institute of Information Technology, Design, and Manufacturing Dumna Airport Road, Jabalpur-482005, India *Corresponding author’s email address: [email protected] Abstract The recent outbreak of the SARS-CoV-2 infection has affected the lives and economy of more than 200 countries. The unavailability of vaccines and the virus-specific drugs has created an opportunity to repurpose existing drugs to examine their efficacy in controlling the virus activities. Here, the inhibition of the RdRp viral protein responsible for the replication of the virus in host cells is examined by evaluating the binding patterns of various approved and investigational antiviral, antibacterial, and anti-cancer drugs by using the molecular docking approach. Some of these drugs have been proposed to be effective against the SARS- Cov-2 virus infection. In an attempt to discover new antiviral agents, artificially expanded genetic alphabets (AEGIS) such as dP, dZ, dJ, dV, dX, dK, dB, dS, dP4, and dZ5 and different sequences of these nucleotides were also docked into the active site of the RdRp protein. It is found that among the various approved and investigational drugs, the Clevudine, N4-hydroxycytidine (EIDD-1931), 2'-C-methylcytidine, EIDD-2801, Uprifosbuvir, Balapiravir, Acalabrutinib, BMS-986094, Remdesivir (full drug), GS-6620, and Ceforanide would act as potent inhibitors of the RdRp protein. Similarly, among the AEGIS nucleotides, dB, dJ, dP, dK, dS, dV, and dZ are found to inhibit the RdRp protein efficiently.
    [Show full text]
  • Product Data Sheet
    Product data sheet MedKoo Cat#: 319769 Name: Mericitabine CAS#: 940908-79-2 Chemical Formula: C18H26FN3O6 Exact Mass: 399.1806 Molecular Weight: 399.4194 Product supplied as: Powder Purity (by HPLC): ≥ 98% Shipping conditions Ambient temperature Storage conditions: Powder: -20°C 3 years; 4°C 2 years. In solvent: -80°C 3 months; -20°C 2 weeks. 1. Product description: Mericitabine, also known as RG7128 and R-7128, is a HCV polymerase inhibitor. RG7128 is also a prodrug of PSI-6130, which shows potent antiviral efficacy in patients infected with hepatitis C virus (HCV) genotypes 1, 2, or 3. 2. CoA, QC data, SDS, and handling instruction SDS and handling instruction, CoA with copies of QC data (NMR, HPLC and MS analytical spectra) can be downloaded from the product web page under “QC And Documents” section. Note: copies of analytical spectra may not be available if the product is being supplied by MedKoo partners. Whether the product was made by MedKoo or provided by its partners, the quality is 100% guaranteed. 3. Solubility data Solvent Max Conc. mg/mL Max Conc. mM DMSO 100 250.36 4. Stock solution preparation table: Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg 1 mM 2.50 mL 12.52 mL 25.04 mL 5 mM 0.50 mL 2.50 mL 5.01 mL 10 mM 0.25 mL 1.25 mL 2.50 mL 50 mM 0.05 mL 0.25 mL 0.50 mL 5. Molarity Calculator, Reconstitution Calculator, Dilution Calculator Please refer the product web page under section of “Calculator” 6.
    [Show full text]
  • Product List
    PRODUCT LIST Active Pharma Ingredients API Acid Reflux Disorders Product Pharmacopoeia CAS No. Technical Document A Acotiamide Hydrochloride - 773092-05-0 - Almagate EP 66827-12-1 - Aluminum Hydroxide BP, USP 21645-51-2 - C Cimetidine - 51481-61-9 - D Dexlansoprazole - 138530-94-6 - Dexlansoprazole - 313640-86-7 DMF Sesquihydrate Dexrabeprazole Sodium - 171440-18-9 ODMF, Tech Pack E Ecabet Sodium - 86408-72-2 DMF Esomeprazole - 119141-88-7 - Esomeprazole Magneisum - 217087-10-0 - Dihydrate Esomeprazole Magnesium - 161973-10-0 - Esomeprazole Magnesium USP 217087-09-7 CEP, DMF Trihydrate Esomeprazole Potassium IHS 161796-84-5 DMF Esomeprazole Sodium - 161796-78-7 - Esomeprazole Zinc/ 793668-08-3, - - Base/Strontium 119141-88-7 F Famotidine - 76824-35-6 - E Glycopyrrolate - 596-51-0 - H Hydrotelcite BP 12304-65-3 - I Ilaprazole IHS, IP 172152-36-2 DMF Ilaprazole Sodium - 172152-50-0 ODMF, Tech Pack Itopride - 122898-67-3 - Itopride Hydrochloride IHS 122892-31-3 - Patent Disclaimer: Products protected by valid patents are not offered for sale in countries, where the sale of such products constitutes a patent infringement. The buyers should make their independent evaluation of the patent scenario for their respective markets and will be responsible for all patent related liabilities. 2021-01-11 © ExSyn Corp | All rights reserved. | www.exsyncorp.com 1 API Acid Reflux Disorders Product Pharmacopoeia CAS No. Technical Document L Lafutidine - 118288-08-7 - Lansoprazole - 103577-45-3 - Lansoprazole Sodium - 226904-00-3 - M Magaldrate USP 74978-16-8
    [Show full text]