I-Daclatasvir Dihydrochloride
Incazelo
I-Daclatasvir dihydrochloride (BMS-790052 dihydrochloride) inamandla futhi isebenza ngomlomo.Iphrotheni ye-HCV NS5Ainhibitor ngeEC50s uhla 9-146 pM foreziningi ze-HCV replicon genotypes. I-Daclatasvir dihydrochloride nayo iyi-ai-organic anion transporting polypeptide 1B (OATP1B)futhiI-OATP1B3inhibitor ngeIC50s ka-1.5 µM no-3.27 µM, ngokulandelanayo.
IC50& Okuqondiwe
EC50: 50 pM (HCV replicon genotype 1a), 9 pM (HCV replicon genotype 1b), 71 pM (HCV replicon genotype 2a), 146 pM (HCV replicon genotype 3a), 12 pM (HCV replicon genotype 3pM) I-HCV replicon genotype 5a)[1]
I-Kd: 8 nM (NS5A33-202) kanye ne-210 nM (NS5A26-202)[2]
I-IC50: 1.5 µM (OATP1B) kanye ne-3.27 µM (OATP1B3)[3]
Ku-Vitro
I-Daclatasvir (BMS-790052) ibonisa umsebenzi onamandla wokuvimbela kuwo wonke ama-genotypes ahloliwe, nge-EC50amanani asuka ku-9pm kuye ku-146 pM. I-Daclatasvir ivimbela i-HCV replicon genotype 1a, 1b, 2a, 3a, 4a kanye no-5a nge-EC50amanani 50 pM, 9 pM, 71 pM, 146 pM, 12 pM kanye 33 pM, ngokulandelana. I-Daclatasvir iyi-inhibitor enamandla ye-JFH-1 genotype 2a igciwane elithathelwanayo eliphindaphinda isiko lamaseli (EC50=28 pM)[1]. I-Daclatasvir (BMS-790052) ibophezela ngokuqinile ku-NS5A33-202 kanye ne-NS5A26-202 ne-Kds ka-8 nM no-210 nM, ngokulandelana[2].
Isitoreji
| Impushana | -20°C | 3 iminyaka |
| 4°C | iminyaka engu-2 | |
| Ku-solvent | -80°C | 6 izinyanga |
| -20°C | Inyanga engu-1 |
Ukuhlolwa Komtholampilo
| Inombolo ye-NCT | Umxhasi | Isimo | Usuku okuqalwa ngalo | Isigaba |
| I-NCT03369327 | I-Tehran University of Medical Sciences|RojanPharma Pharmaceutical Company | Ukutheleleka Ngegciwane Le-Hepatitis C, Ukusabela Ekwelashweni Kwe-|Human Immunodeficiency Virus | Januwari 1, 2017 | Isigaba 3 |
| I-NCT03485846 | R-Pharm|Almedis | I-Chronic Hepatitis C Genotype 1b | Novemba 27, 2017 | Isigaba 2 |
| I-NCT01016912 | Bristol-Myers Squibb | Ukutheleleka kwe-Hepatitis C | Disemba 2009 | Isigaba 2 |
| I-NCT01629732 | Bristol-Myers Squibb | I-Hepatitis C Virus | Mashi 2013 | Isigaba 2 |
| I-NCT01497834 | Bristol-Myers Squibb | I-Hepatitis C | Januwari 2012 | Isigaba 3 |
| I-NCT01973049 | Bristol-Myers Squibb | I-Hepatitis C | Disemba 2013 | Isigaba 3 |
| I-NCT00663208 | Bristol-Myers Squibb | I-Hepatitis C Engamahlalakhona | Meyi 2008 | Isigaba 2 |
| I-NCT02576314 | Humanity and Health Research Centre|Beijing 302 Hospital | Ukutheleleka Kwe-Hepatitis C Okungapheli | May 2015 | Isigaba 3 |
| I-NCT02756936 | I-Genuine Research Center, Egypt|Zeta Pharma Pharmaceutical Industries | Unempilo | February 2016 | Isigaba 1 |
| I-NCT02771405 | I-National Hepatology & Tropical Medicine Research Institute|Cairo University | I-Hepatitis C, Engamahlalakhona | I-Hepatocellular Carcinoma | Mashi 2016 | Isigaba 3 |
| I-NCT03706898 | I-Viriom | HIV-1-infection|Hepatic Impairment | Okthoba 1, 2018 | Isigaba 1 |
| I-NCT02319031 | Bristol-Myers Squibb | I-Hepatitis C | February 2015 | Isigaba 3 |
| I-NCT02124044 | Izikhungo Zikazwelonke Zesikhungo Sezempilo Sezempilo (CC)|Isikhungo Sikazwelonke Sokungezwani Nezifo Nezifo Ezithathelwanayo (NIAID)|Bristol-Myers Squibb | I-HIV-HCV | February 2014 | Isigaba 2 |
| I-NCT02551861 | Bristol-Myers Squibb | I-Hepatitis C | Disemba 2015 | Isigaba 2 |
| I-NCT00859053 | Bristol-Myers Squibb | Ukungasebenzi Kwesibindi | Mashi 2009 | Isigaba 1 |
| I-NCT01257204 | Bristol-Myers Squibb | I-Hepatitis C Virus | Disemba 2010 | Isigaba 2 |
| I-NCT03063879 | I-Tehran University of Medical Sciences|Ahvaz Jundishapur University of Medical Sciences|Shiraz University of Medical Sciences|Hamadan University of Medical Science | I-Hepatitis C, Okungamahlalakhona|Ukwehluleka Kwezinso Okungapheli | Ephreli 1, 2017 | Isigaba 4 |
| I-NCT01017575 | Bristol-Myers Squibb | Ukutheleleka kwe-Hepatitis C | Disemba 2009 | Isigaba 2 |
| I-NCT02865369 | Sang Gyune Kim|Seoul National University Boramae Hospital|Severance Hospital|Inha University Hospital|Korea University|Gachon University Gil Medical Center|Hanyang University Seoul Hospital|Ewha Womans University Mokdong Hospital|Bristol-Myers Squibb|Soonchunhyang University Hospital | I-Hepatitis C Engamahlalakhona | Septhemba 2016 |
|
| I-NCT04070235 | I-Nanjing Sanhome Pharmaceutical, Co., Ltd. | I-Hepatitis C, Engamahlalakhona | Mashi 29, 2019 | Isigaba 2|Isigaba 3 |
| I-NCT03487848 | Bristol-Myers Squibb | I-Hepatitis C | I-Hepatitis Engapheli | Meyi 18, 2018 | Isigaba 2 |
| I-NCT00904059 | Bristol-Myers Squibb | I-Hepatitis C | Meyi 2009 | Isigaba 1 |
| I-NCT02107365 | I-French National Institute for Health and Medical Research-Isikhungo Sikazwelonke SaseFrance Socwaningo Lwengculazi kanye Nesifo Sesibindi Esibangelwa Amagciwane (Inserm-ANRS)|Bristol-Myers Squibb | I-Hepatitis C Virus Genotype 4 Infection | Novemba 2013 | Isigaba 2 |
| I-NCT02397395 | Janssen R&D Ireland | Ukukhubazeka Kwezinso|Isifo Sezinso Sokuphela | May 2015 | Isigaba 2 |
| I-NCT03169348 | Inyuvesi yase-Assiut | I-Hepatitis C | Novemba 1, 2017 | Akufaneleki |
| I-NCT02323594 | Bristol-Myers Squibb | Ukutheleleka kwe-Hepatitis C | Disemba 2014 | Isigaba 1 |
| I-NCT03537196 | I-French National Institute for Health and Medical Research-Isikhungo Sikazwelonke SaseFrance Socwaningo Lwengculazi kanye ne-Viral Hepatitis (Inserm-ANRS) | I-Hepatitis C|Ukusetshenziswa Kwezidakamizwa|I-Viral Hepatitis C | Novemba 13, 2018 | Isigaba 4 |
| I-NCT02103569 | Bristol-Myers Squibb | I-Hepatitis C | Ephreli 2014 | Isigaba 1 |
| I-NCT02772744 | Inyuvesi yaseZagazig | Inyuvesi yaseCairo | I-Hepatitis C | Novemba 1, 2017 |
|
| I-NCT01718158 | Bristol-Myers Squibb | I-Hepatitis C | Januwari 2013 | Isigaba 3 |
| I-NCT02496078 | Bristol-Myers Squibb | I-Hepatitis C | Agasti 2015 | Isigaba 3 |
| I-NCT01425970 | Bristol-Myers Squibb | I-Hepatitis C | Meyi 2012 | Isigaba 2 |
| I-NCT01471574 | Bristol-Myers Squibb | I-Hepatitis C, i-Genotype 1 | Disemba 2011 | Isigaba 3 |
| I-NCT01573351 | Bristol-Myers Squibb | I-Hepatitis C Virus | Meyi 2012 | Isigaba 3 |
| I-NCT01938625 | Janssen R&D Ireland | I-Hepatitis C, Engamahlalakhona | Disemba 12, 2013 | Isigaba 2 |
| I-NCT01492426 | Bristol-Myers Squibb | I-Hepatitis C | Januwari 2012 | Isigaba 3 |
| I-NCT03480932 | Johns Hopkins Bloomberg School of Public Health|National Institute on Drug Abuse (NIDA)|YR Gaitonde Centre for AIDS Research and Education | I-Hepatitis C, Engamahlalakhona | Februwari 2, 2018 | Isigaba 2|Isigaba 3 |
| I-NCT03163849 | Inyuvesi yase-Assiut | Isifo Sesibindi Esingapheli c | Septhemba 1, 2019 | Isigaba 3 |
| I-NCT01581203 | Bristol-Myers Squibb | I-Hepatitis C Virus | Meyi 2012 | Isigaba 3 |
| I-NCT01492504 | Bristol-Myers Squibb | I-Hepatitis C | Februwari 7, 2012 |
|
| I-NCT03686722 | Mohamed Raslan|Ain Shams University|Isikhungo Sokucwaninga Ngezidakamizwa, eCairo, Egypt | Isifo sikashukela i-mellitus, Uhlobo 2|Hepatitis C|Ukusebenzelana Nezidakamizwa | Septhemba 9, 2017 | Isigaba 1 |
| I-NCT02262728 | Janssen Research & Development, LLC | I-Hepatitis C, Engamahlalakhona | Septhemba 30, 2014 | Isigaba 2 |
| I-NCT02349048 | Janssen Research & Development, LLC | I-Hepatitis C Virus | Januwari 2015 | Isigaba 2 |
| I-NCT03882307 | Inyuvesi yase-Assiut | I-Hepatitis C, Engamahlalakhona | Meyi 2020 | Isigaba sokuqala 1 |
| I-NCT02758509 | I-Parc de Salut Mar | I-Chronic Hepatitis C|Cirrhosis | Januwari 1, 2010 |
|
| I-NCT01795911 | Bristol-Myers Squibb | I-Hepatitis C | Mashi 2013 | Isigaba 2 |
| I-NCT03549832 | I-Assiut University|Sohag University|South Valley University | I-HCV Coinfection | Januwari 1, 2018 | Akufaneleki |
| I-NCT02161939 | Bristol-Myers Squibb | I-Hepatitis C Engamahlalakhona |
| |
| I-NCT01309932 | Bristol-Myers Squibb | I-Hepatitis C | Mashi 2011 | Isigaba 2 |
| I-NCT01995266 | Bristol-Myers Squibb | I-Hepatitis C | Februwari 28, 2014 | Isigaba 3 |
| I-NCT02640157 | AbbVie | I-Chronic Hepatitis C|Virus ye-Hepatitis C|Genotype 3 Igciwane Le-Hepatitis C | Disemba 2015 | Isigaba 3 |
| I-NCT02032875 | Bristol-Myers Squibb | I-Hepatitis C | Mashi 2014 | Isigaba 3 |
| I-NCT02624063 | I-Federal University yaseSão Paulo | I-Hepatitis C, Engamahlalakhona | Disemba 2015 | Isigaba 4 |
| I-NCT00546715 | Bristol-Myers Squibb | I-Hepatitis C Engamahlalakhona | Novemba 2007 | Isigaba 1|Isigaba 2 |
| I-NCT01718145 | Bristol-Myers Squibb | Ukutheleleka nge-Hepatitis C Virus | Novemba 2012 | Isigaba 3 |
| I-NCT01616524 | Bristol-Myers Squibb | I-Hepatitis C Virus (HCV) | Julayi 2012 | Isigaba 3 |
| I-NCT02032901 | Bristol-Myers Squibb | I-Hepatitis C | Januwari 2014 | Isigaba 3 |
| I-NCT03540212 | Inyuvesi yase-Ain Shams | Ukutheleleka kwe-HCV okungapheli | Disemba 10, 2017 | Isigaba 2|Isigaba 3 |
| I-NCT02097966 | Bristol-Myers Squibb | I-Hepatitis C Engamahlalakhona |
| |
| I-NCT02596880 | I-Tehran University of Medical Sciences | I-Hepatitis C | I-Cirrhosis | Septhemba 2015 | Isigaba 3 |
| I-NCT04019717 | Inkampani Atea Pharmaceuticals, Inc. | I-Hepatitis C|Hepatitis C, Engalapheki|I-Hepatitis C Engapheli|Ukutheleleka Ngegciwane Le-Hepatitis C|Ukutheleleka kwe-HCV | Juni 20, 2019 | Isigaba 2 |
| I-NCT02992457 | Inyuvesi yaseTanta | I-Hepatitis C | Januwari 2015 | Isigaba 4 |
| I-NCT03547895 | Inyuvesi yaseZagazig | I-Decompensated Cirrhosis | Juni 1, 2015 | Akufaneleki |
| I-NCT03004625 | Isibhedlela sase-Kaohsiung Medical University i-Chung-Ho Memorial Hospital|Isibhedlela i-Chang Gung Memorial|Isibhedlela Sikazwelonke sase-Taiwan University|Isibhedlela Sikazwelonke Sase-Taipei Veterans, e-Taiwan|Isibhedlela sase-China Medical University|Isibhedlela Sikazwelonke sase-Cheng-Kung University | I-Hepatitis C | Novemba 2016 | Isigaba 3 |
| I-NCT01051414 | Bristol-Myers Squibb | Ukutheleleka kwe-Hepatitis C | Ephreli 2010 | Isigaba 2 |
| I-NCT02309450 | I-French National Institute for Health and Medical Research-Isikhungo Sikazwelonke SaseFrance Socwaningo Lwengculazi kanye Nesifo Sesibindi Esibangelwa Amagciwane (Inserm-ANRS)|Bristol-Myers Squibb | I-Hepatitis C Virus Genotype 4 Infection | Disemba 2014 | Isigaba 2 |
| I-NCT01628692 | Bristol-Myers Squibb|Janssen Research & Development, LLC | I-Hepatitis C Virus | Julayi 2012 | Isigaba 2 |
| I-NCT03186313 | Isibhedlela sesibindi sase-Egypt | Isibhedlela i-Wadi El Nil | I-Hepatitis C | Septhemba 2016 | Isigaba 3 |
| I-NCT03063723 | Isibhedlela Sesithathu Esihlobene, i-Sun Yat-Sen University | I-Hepatitis C Engamahlalakhona (Isifo) | Januwari 1, 2016 |
|
| I-NCT00983957 | Bristol-Myers Squibb | I-Hepatitis C Engamahlalakhona | Okthoba 2009 | Isigaba 1 |
| I-NCT01725542 | I-French National Institute for Health and Medical Research-Isikhungo Sikazwelonke SaseFrance Socwaningo Lwengculazi kanye Nesifo Sesibindi Esibangelwa Amagciwane (Inserm-ANRS)|Bristol-Myers Squibb | I-HCV-HIV Co-Infection | Disemba 2012 | Isigaba 2 |
| I-NCT02282709 | Isisekelo Socwaningo Lwesibindi | I-Hepatitis C Engamahlalakhona | February 2014 | Isigaba 3 |
| I-NCT02032888 | Bristol-Myers Squibb | I-Hepatitis C | February 2014 | Isigaba 3 |
| I-NCT03247296 | Inyuvesi ye-MTI | I-Hepatitis C | February 28, 2017 |
|
| I-NCT01389323 | Bristol-Myers Squibb | I-Hepatitis C | Septhemba 2011 | Isigaba 3 |
| I-NCT02556086 | Bristol-Myers Squibb | I-Hepatitis C | Disemba 2015 | Isigaba 2 |
| I-NCT01741545 | Bristol-Myers Squibb | I-Hepatitis C Virus | Mashi 31, 2013 | Isigaba 3 |
| I-NCT01866930 | Bristol-Myers Squibb | Ukutheleleka Kwe-Hepatitis C Okungapheli | Julayi 11, 2013 | Isigaba 3 |
| I-NCT02268864 | Ukulinganisa kwenkampani Janssen-Cilag International NV | I-Hepatitis C, Engamahlalakhona | Januwari 2015 | Isigaba 2 |
| I-NCT01797848 | Bristol-Myers Squibb | I-Hepatitis C | Juni 2014 | Isigaba 3 |
| I-NCT03166280 | Eman Sayed Hassan Abd Allah|Assiut University | I-Hepatitis C | Juni 2017 |
|
| I-NCT02159352 | Bristol-Myers Squibb | I-Hepatitis C | Juni 2014 | Isigaba 1 |
| I-NCT01125189 | Bristol-Myers Squibb | I-Hepatitis C Virus | Julayi 2010 | Isigaba 2 |
| I-NCT03748745 | I-Nanjing Sanhome Pharmaceutical, Co., Ltd. | Ukusebenzisana Kwezidakamizwa | Novemba 19, 2018 | Isigaba 1 |
| I-NCT01012895 | Bristol-Myers Squibb | I-Hepatitis C Engamahlalakhona | Disemba 2009 | Isigaba 2 |
| I-NCT02565888 | Inyuvesi yaseRadboud | I-Hepatitis C | I-HIV | Novemba 2015 | Isigaba 1 |
| I-NCT02555943 | Humanity and Health Research Centre|Beijing 302 Hospital|Nanfang Hospital of Southern Medical University | Ukutheleleka Kwe-Hepatitis C Okungapheli|I-HBV Coinfection|Ukuvuselelwa Kwe-Hepatitis B | February 2015 | Isigaba 2|Isigaba 3 |
| I-NCT02304159 | Tarek I. Hassanein, MD, FACP, FAG, AGAF|Southern California Research Center | I-Hepatitis C | I-Cirrhosis | Januwari 2015 | Isigaba 4 |
| I-NCT02580474 | Myeong Jun Song|Bristol-Myers Squibb|Soonchunhyang University Hospital|Dankook University|Chungnam National University Hospital|Konyang University Hospital|Eulji University Hospital|Saint Vincent's Hospital, Korea|Konkuk University Hospital|Cheongju St. Mary's Hospital, Cheongju , Korea|Severance Hospital|Korea University Guro Hospital|Eulji General Hospital|The Catholic University of Korea | I-Hepatitis C | February 2016 | Isigaba 4 |
| I-NCT02104843 | Bristol-Myers Squibb | I-Hepatitis C | Ephreli 2014 | Isigaba 1 |
| I-NCT01428063 | Bristol-Myers Squibb | Ukutheleleka nge-Hepatitis C Virus | Septhemba 2011 | Isigaba 2 |
| I-NCT02123654 | Bristol-Myers Squibb | Ukutheleleka nge-Hepatitis C Virus | Ephreli 2014 | Isigaba 3 |
| I-NCT02565862 | Inyuvesi yaseRadboud | IHepatitis C|Diabetes Mellitus|Ukumelana ne-insulin | Januwari 2016 | Isigaba 1 |
| I-NCT04211844 | Inyuvesi yase-Ain Shams | I-Hepatitis C Engamahlalakhona | Okthoba 1, 2019 |
|
| I-NCT00874770 | Bristol-Myers Squibb | Ukutheleleka kwe-Hepatitis C | Juni 2009 | Isigaba 2 |
| I-NCT03883698 | I-Sanjay Gandhi Postgraduate Institute of Medical Sciences | Ukwehluleka Kwezinso, Okungapheli|I-Hepatitis C | Mashi 15, 2019 | Isigaba 3 |
| I-NCT01448044 | Bristol-Myers Squibb | I-Hepatitis C | Disemba 2011 | Isigaba 3 |
| I-NCT01359644 | I-Bristol-Myers Squibb|Pharmasset | I-Hepatitis C Engamahlalakhona | Juni 2011 | Isigaba 2 |
| I-NCT01842451 | I-Vertex Pharmaceuticals Incorporated | IHepatitis C|CHC|HCV|Hepatitis C | Juni 2013 | Isigaba 2 |
| I-NCT02762448 | Isibhedlela sikaMasipala waseTainan | I-Hepatitis c | Julayi 2016 |
|
| I-NCT02473211 | Humanity and Health Research Centre|Beijing 302 Hospital | Ukutheleleka Kwe-Hepatitis C Okungapheli | Januwari 2015 | Isigaba 2|Isigaba 3 |
| I-NCT01455090 | Bristol-Myers Squibb | I-Hepatitis C Engamahlalakhona | Novemba 30, 2011 | Isigaba 2 |
| I-NCT03490097 | Inyuvesi yase-Ain Shams | IHepatitis C|Metabolic Syndrome | Disemba 1, 2017 | Isigaba 2|Isigaba 3 |
| I-NCT01170962 | Bristol-Myers Squibb | I-Hepatitis C Virus | Agasti 2010 | Isigaba 2 |
| I-NCT02333292 | Isibhedlela i-Valme University|Isibhedlela del SAS de Jerez|Isibhedlela I-General Universitario Elche|Isibhedlela La Línea de la Concepción|Complexo Hospitalario Universitario de A Coruña|Isibhedlela de Figueres|Isibhedlela Universitario Puerto Real|Isibhedlela Universitario Virgen de laversitare Isibhedlela Jikelele Universitario de Alicante|Isibhedlela Universitario Araba|Isibhedlela Royo Vilanova|Isibhedlela Universitario de Burgos|Complejo Hospitalario Universitario de Huelva|Isibhedlela Universitario Reina Sofia de Cordoba|Isibhedlela Universitario Virgen Macarena|Complejo Hospitalario Universitario de Huelva|Isibhedlela Universitario Reina Sofia de Cordoba|Isibhedlela Universitario Virgen Macarena|Complejo Hospitalario Universitario de Huelva Navarra, Universidad de Navarra|Hospital Clinico Universitario San Cecilio|Isibhedlela Universitario La Fe|Isibhedlela Jikelele Universitario de Valencia|Isibhedlela Universitario Infanta Leonor|Isibhedlela Universitario de Gran Canaria|Isibhedlela Universitario Santa Alinaria Universitario Carlos Haya|Isibhedlela Virgen de la Luz|Isibhedlela I-General Universitario de Castellón|Isibhedlela uParc Taulí, Sabadell | Ukutheleleka Kwe-Hepatitis C Okungapheli | Disemba 2014 |
|
| I-NCT03200184 | I-Tehran University of Medical Sciences | I-Hepatitis C | Septhemba 1, 2016 | Isigaba 4 |
| I-NCT03188276 | Isibhedlela Sesithathu Esihlobene, i-Sun Yat-Sen University | I-Hepatitis C Engamahlalakhona | Februwari 1, 2016 | Isigaba sokuqala 1 |
| I-NCT01830205 | Bristol-Myers Squibb | I-Hepatitis C | Septhemba 2012 | Isigaba 1 |
Isiphakamiso18Amaphrojekthi Wokuhlola Ukuvumelana Kwekhwalithi asegunyaziwe4, futhi6amaphrojekthi angaphansi kokugunyazwa.
Uhlelo lokuphatha ikhwalithi yamazwe ngamazwe oluthuthukile lwenze isisekelo esiqinile sokuthengisa.
Ukugadwa kwekhwalithi kusebenza kuwo wonke umjikelezo wempilo womkhiqizo ukuze kuqinisekiswe ikhwalithi nomphumela wokwelapha.
Ithimba Lezindaba Zokulawula Ochwepheshe lisekela izimfuno zekhwalithi ngesikhathi sokufaka isicelo nokubhaliswa.
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