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Drug Discovery Case History

The discovery of sofosbuvir: a revolution for therapy of chronic hepatitis C

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Read on this site (7)

Sara I. Aboras, Heba H. Abdine, Marwa A. A. Ragab & Mohamed A. Korany. (2022) A Review on Analytical Strategies for the Assessment of Recently Approved Direct Acting Antiviral Drugs. Critical Reviews in Analytical Chemistry 52:8, pages 1878-1900.
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Alberto E Maraolo, Riccardo Scotto, Emanuela Zappulo, Biagio Pinchera, Nicola Schiano Moriello, Salatore Nappa, Antonio Riccardo Buonomo & Ivan Gentile. (2020) Novel strategies for the management of bacterial and fungal infections in patients with liver cirrhosis: focus on new antimicrobials. Expert Review of Anti-infective Therapy 18:3, pages 191-202.
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Emanuela Zappulo, Riccardo Scotto, Antonio Riccardo Buonomo, Alberto Enrico Maraolo, Biagio Pinchera & Ivan Gentile. (2020) Efficacy and safety of a fixed dose combination tablet of asunaprevir + beclabuvir + daclatasvir for the treatment of Hepatitis C. Expert Opinion on Pharmacotherapy 21:3, pages 261-273.
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Guglielmo Borgia, Riccardo Scotto & Antonio Riccardo Buonomo. (2019) An update on recent developments in the search for hepatitis C virus therapies with pan-genotypic efficacy. Expert Opinion on Investigational Drugs 28:5, pages 395-397.
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Guglielmo Borgia, Alberto Enrico Maraolo, Salvatore Nappa, Ivan Gentile & Antonio Riccardo Buonomo. (2018) NS5B polymerase inhibitors in phase II clinical trials for HCV infection. Expert Opinion on Investigational Drugs 27:3, pages 243-250.
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Guglielmo Borgia, Alberto Enrico Maraolo, Antonio Riccardo Buonomo, Riccardo Scotto & Ivan Gentile. (2016) The therapeutic potential of new investigational hepatitis C virus translation inhibitors. Expert Opinion on Investigational Drugs 25:10, pages 1209-1214.
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Articles from other publishers (46)

S. V. Kondratiuk. (2023) The abuse of patentability conditions in the sphere of pharmacy in Ukraine and the EpO: upon the Example of polymorph sofosbuvir. Medicne pravo:2(32), pages 23-39.
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Kiran Shehzadi, Afsheen Saba, Mingjia Yu & Jianhua Liang. (2023) Structure-Based Drug Design of RdRp Inhibitors against SARS-CoV-2. Topics in Current Chemistry 381:5.
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Brittany M. Klootwyk, Amy E. Ryan, Arbil Lopez, Mitchell J. R. McCloskey, Chasity P. Janosko, Alexander Deiters & Paul E. Floreancig. (2023) Peroxide-Mediated Release of Organophosphates from Boron-Containing Phosphotriesters: A New Class of Organophosphate Prodrugs. Organic Letters 25:29, pages 5530-5535.
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David P. Rotella. (2023) Successes in antiviral drug discovery: a tribute to Nick Meanwell. Medicinal Chemistry Research 32:7, pages 1239-1248.
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Béatrice Roy, Valentin Navarro & Suzanne Peyrottes. (2023) Prodrugs of Nucleoside 5'-Monophosphate Analogues: Overview of the Recent Literature Concerning their Synthesis and Applications. Current Medicinal Chemistry 30:11, pages 1256-1303.
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Manojit Bhattacharya, Srijan Chatterjee, Sang-Soo Lee & Chiranjib Chakraborty. (2023) Therapeutic applications of nanobodies against SARS-CoV-2 and other viral infections: Current update. International Journal of Biological Macromolecules 229, pages 70-80.
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Ashley N. Brown, Yinzhi Lang, Jieqiang Zhou, Evelyn J. Franco, Kaley C. Hanrahan, Juergen B. Bulitta & George L. Drusano. (2022) Why Molnupiravir Fails in Hospitalized Patients. mBio 13:6.
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Ahmed Abdullah Al Awadh. (2022) Nucleotide and nucleoside-based drugs: past, present, and future. Saudi Journal of Biological Sciences 29:12, pages 103481.
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Pinar Mesci, Janaina S. de Souza, Laura Martin-Sancho, Angela Macia, Aurian Saleh, Xin Yin, Cedric Snethlage, Jason W. Adams, Simoni H. Avansini, Roberto H. Herai, Angels Almenar-Queralt, Yuan Pu, Ryan A. Szeto, Gabriela Goldberg, Patrick T. Bruck, Fabio Papes, Sumit K. Chanda & Alysson R. Muotri. (2022) SARS-CoV-2 infects human brain organoids causing cell death and loss of synapses that can be rescued by treatment with Sofosbuvir. PLOS Biology 20:11, pages e3001845.
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Lívia Victor, Renata Perez, Flávia Fernandes, Juliana Piedade, Cristiane A. Villela-Nogueira & Gustavo Pereira. (2022) Results of interferon-free treatment for HCV-infected patients with decompensated cirrhosis from a Brazilian real-life cohort. Medicine 101:35, pages e30097.
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Ameya Fulmali & Sonali S. Bharate. (2022) Phosphate moiety in FDA‐approved pharmaceutical salts and prodrugs. Drug Development Research 83:5, pages 1059-1074.
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Abanoub K. Wasef, Sara A. Wahdan, Noha M. Saeed & Ebtehal El‐Demerdash. (2022) Effects of aged garlic and ginkgo biloba extracts on the pharmacokinetics of sofosbuvir in rats. Biopharmaceutics & Drug Disposition 43:4, pages 152-162.
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Nadia Hanafy Metwally & Ahmed Sabri Abd-Elmoety. (2022) Novel fluorinated pyrazolo[1,5-a]pyrimidines: In a way from synthesis and docking studies to biological evaluation. Journal of Molecular Structure 1257, pages 132590.
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Ke Xing, Yang Cong, Cunbin Du, Yuchao Bian, Xiaoxuan Li & Mingliang Wang. (2022) Research on Solubility Measurement, Solvent Effects, Preferential Solvation, and Model Correlation of Sofosbuvir Form A in Different Pure and Binary Solvents. Journal of Chemical & Engineering Data 67:3, pages 748-760.
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Tommaso Felicetti, Maria Chiara Pismataro, Violetta Cecchetti, Oriana Tabarrini & Serena Massari. (2022) Triazolopyrimidine Nuclei: Privileged Scaffolds for Developing Antiviral Agents with a Proper Pharmacokinetic Profile. Current Medicinal Chemistry 29:8, pages 1379-1407.
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Sunil Taneja, Ajay Duseja, Manu Mehta, Arka De, Nipun Verma, Madhumita Premkumar, Radha K. Dhiman, Virendra Singh, Mini P. Singh, Radha K. Ratho, Raja Ramachandran, Vivek Kumar & Harbir S. Kohli. (2021) Sofosbuvir and Velpatasvir combination is safe and effective in treating chronic hepatitis C in end‐stage renal disease on maintenance haemodialysis. Liver International 41:4, pages 705-709.
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Anna Maria Spera. (2021) Are nucleotide inhibitors, already used for treating hepatitis C virus infection, a potential option for the treatment of COVID-19 compared with standard of care? A literature review. World Journal of Virology 10:2, pages 53-61.
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Manisha ThakurDr.Dr., Anurag ChauhanDr.Dr., Prashant JambunathanDr.Dr., Shikha AwasthiDr.Dr., Thilagavathi KDr.Dr. & Mujeeb VRDr.Dr.. (2021) EFFICACY OF SOFOSBUVIR AND DACLATASVIR IN COMPENSATED CHRONIC HEPATITIS C INFECTION: A SINGLE CENTER, OPEN-LABEL AND PROOF OF CONCEPT STUDY. GLOBAL JOURNAL FOR RESEARCH ANALYSIS, pages 27-30.
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Lei Tian, Taotao Qiang, Chengyuan Liang, Xiaodong Ren, Minyi Jia, Jiayun Zhang, Jingyi Li, Minge Wan, Xin YuWen, Han Li, Wenqiang Cao & Hong Liu. (2021) RNA-dependent RNA polymerase (RdRp) inhibitors: The current landscape and repurposing for the COVID-19 pandemic. European Journal of Medicinal Chemistry 213, pages 113201.
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Sjoerd Slagman & Wolf-Dieter Fessner. (2021) Biocatalytic routes to anti-viral agents and their synthetic intermediates. Chemical Society Reviews 50:3, pages 1968-2009.
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Michael S. Saporito. 2021. Remington. Remington 663 681 .
Tengiz Tsertsvadze, Amiran Gamkrelidze, Muazzam Nasrullah, Lali Sharvadze, Juliette Morgan, Shaun Shadaker, Lia Gvinjilia, Maia Butsashvili, David Metreveli, Vakhtang Kerashvili, Marina Ezugbaia, Nikoloz Chkhartishvili, Akaki Abutidze, Valeri Kvaratskhelia & Francisco Averhoff. (2020) Treatment outcomes of patients with chronic hepatitis C receiving sofosbuvir-based combination therapy within national hepatitis C elimination program in the country of Georgia. BMC Infectious Diseases 20:1.
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Babak Sayad, Mahsa Sobhani & Reza Khodarahmi. (2020) Sofosbuvir as Repurposed Antiviral Drug Against COVID-19: Why Were We Convinced to Evaluate the Drug in a Registered/Approved Clinical Trial?. Archives of Medical Research 51:6, pages 577-581.
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Tea L Laursen, Thomas D Sandahl, Konstantin Kazankov, Jacob George & Henning Grønbæk. (2020) Liver-related effects of chronic hepatitis C antiviral treatment. World Journal of Gastroenterology 26:22, pages 2931-2947.
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M. Kyle Hadden & Angela M. Zaino. (2020) Introduction to Medicinal Chemistry: A Five-Day Course for High School Students. Journal of Chemical Education 97:6, pages 1543-1548.
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Holger Hannemann. (2020) Viral replicons as valuable tools for drug discovery. Drug Discovery Today 25:6, pages 1026-1033.
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Deepti Chopra & Bharti Bhandari. (2020) Sofosbuvir: Really Meets the Unmet Needs for Hepatitis C Treatment?. Infectious Disorders - Drug Targets 20:1, pages 2-15.
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A. Chris Krueger, Hui-Ju Chen, John T. Randolph, Brian S. Brown, Geoff T. Halvorsen, Howard R. Heyman, Tongmei Li, Christopher C. Marvin, Jason P. Shanley, Eric A. Voight, Daniel A.J. Bow, Cecilia Van Handel, Vincent Peterkin, Robert A. Carr, DeAnne Stolarik, Tatyana Dekhtyar, Michelle L. Irvin, Preethi Krishnan, Rodger F. Henry, Rolf Wagner & David A. DeGoey. (2020) Synthesis and evaluation of 2′-dihalo ribonucleotide prodrugs with activity against hepatitis C virus. Bioorganic & Medicinal Chemistry 28:1, pages 115208.
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Nicola Coppola, Federica Portunato, Antonio Riccardo Buonomo, Laura Staiano, Riccardo Scotto, Biagio Pinchera, Stefania De Pascalis, Daniela Caterina Amoruso, Salvatore Martini, Mariantonietta Pisaturo, Carmine Coppola & Ivan Gentile. (2019) Interferon-free regimens improve kidney function in patients with chronic hepatitis C infection. Journal of Nephrology 32:5, pages 763-773.
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Riccardo Scotto, Antonio Riccardo Buonomo, Nicola Schiano Moriello, Alberto Enrico Maraolo, Emanuela Zappulo, Biagio Pinchera, Ivan Gentile & Guglielmo Borgia. (2019) Real-World Efficacy and Safety of Pangenotypic Direct-Acting Antivirals Against Hepatitis C Virus Infection. Reviews on Recent Clinical Trials 14:3, pages 173-182.
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Ivan Gentile, Riccardo Scotto, Carmine Coppola, Laura Staiano, Daniela Caterina Amoruso, Teresa De Simone, Federica Portunato, Stefania De Pascalis, Salvatore Martini, Margherita Macera, Giulio Viceconte, Grazia Tosone, Antonio Riccardo Buonomo, Guglielmo Borgia & Nicola Coppola. (2018) Treatment with direct-acting antivirals improves the clinical outcome in patients with HCV-related decompensated cirrhosis: results from an Italian real-life cohort (Liver Network Activity—LINA cohort). Hepatology International 13:1, pages 66-74.
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Michael J. Sofia & Phillip A. Furman. 2019. HCV: The Journey from Discovery to a Cure. HCV: The Journey from Discovery to a Cure 141 169 .
Suely da Silva, Daniel Oliveira Silva Martins & Ana Jardim. (2018) A Review of the Ongoing Research on Zika Virus Treatment. Viruses 10:5, pages 255.
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Alain Braillon. (2018) Adding care to cure for patients with liver disease: A cultural shift. Hepatology 67:3, pages 1172-1172.
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Pinar Mesci, Angela Macia, Spencer M. Moore, Sergey A. Shiryaev, Antonella Pinto, Chun-Teng Huang, Leon Tejwani, Isabella R. Fernandes, Nicole A. Suarez, Matthew J. Kolar, Sandro Montefusco, Scott C. Rosenberg, Roberto H. Herai, Fernanda R. Cugola, Fabiele B. Russo, Nicholas Sheets, Alan Saghatelian, Sujan Shresta, Jeremiah D. Momper, Jair L. Siqueira-Neto, Kevin D. Corbett, Patricia C. B. Beltrão-Braga, Alexey V. Terskikh & Alysson R. Muotri. (2018) Blocking Zika virus vertical transmission. Scientific Reports 8:1.
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Marco Fiore, Sebastiano Leone, Alberto Enrico Maraolo, Emilio Berti & Giovanni Damiani. (2018) Liver Illness and Psoriatic Patients. BioMed Research International 2018, pages 1-12.
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Yanling Wu, Shibo Jiang & Tianlei Ying. (2017) Single-Domain Antibodies As Therapeutics against Human Viral Diseases. Frontiers in Immunology 8.
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Ivan Gentile, Antonio Riccardo Buonomo, Riccardo Scotto, Emanuela Zappulo & Guglielmo Borgia. (2017) Infections worsen prognosis of patients with cirrhosis irrespective of the liver disease stage. European Journal of Internal Medicine 46, pages e45-e47.
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Zhe Chen, Bryan D. Cox, Ethel C. Garnier-Amblard, Tamara R. McBrayer, Steven J. Coats, Raymond F. Schinazi & Franck Amblard. (2017) Synthesis and anti-HCV activity of a series of β- d -2′-deoxy-2′-dibromo nucleosides and their corresponding phosphoramidate prodrugs. Bioorganic & Medicinal Chemistry Letters 27:23, pages 5296-5299.
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Jarkko Rautio, Jussi Kärkkäinen & Kenneth B. Sloan. (2017) Prodrugs – Recent approvals and a glimpse of the pipeline. European Journal of Pharmaceutical Sciences 109, pages 146-161.
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Raoul Walther, Jarkko Rautio & Alexander N. Zelikin. (2017) Prodrugs in medicinal chemistry and enzyme prodrug therapies. Advanced Drug Delivery Reviews 118, pages 65-77.
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Mauro Safir Filho, Anthony R. Martin & Rachid Benhida. (2017) Assessment of new triplet forming artificial nucleobases as RNA ligands directed towards HCV IRES IIId loop. Bioorganic & Medicinal Chemistry Letters 27:8, pages 1780-1783.
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Pablo Olivera, Silvio Danese & Laurent Peyrin-Biroulet. (2017) Next generation of small molecules in inflammatory bowel disease. Gut 66:2, pages 199-209.
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Autumn Bagwell & Cody A. Chastain. (2016) Hepatitis C Treatment in HIV Coinfection: Approaches, Challenges, and Future Opportunities. Current Treatment Options in Infectious Diseases 8:4, pages 379-399.
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Michael J. Sofia. 2016. Successful Drug Discovery. Successful Drug Discovery 163 188 .
Mohammad Taher Bahrami, Bahareh Mohammadi, Shahram Miraghaei, Atefeh Babaei, Matin Ghaheri & Gholamreza Bahrami. (2016) Quantification of sofosbuvir in human serum by liquid chromatography with negative ionization mass spectrometry using the parent peak and its source-induced fragment: Application to a bioequivalence study. Journal of Separation Science 39:14, pages 2702-2709.
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