| 词条 | Celgosivir |
| 释义 |
| drug_name = | INN = | IUPAC_name = [(1S,6S,7S,8R,8aR)-1,7,8-Trihydroxy-1,2,3,5,6,7,8,8a-octahydroindolizin-6-yl] butanoate | image = Celgosivir.svg | alt = | caption = | pronounce = | tradename = | Drugs.com = | MedlinePlus = | pregnancy_AU = | pregnancy_AU_comment = | pregnancy_US = | pregnancy_category= | routes_of_administration = | legal_AU = | legal_AU_comment = | legal_CA = | legal_DE = | legal_NZ = | legal_UK = | legal_US = | legal_UN = | legal_status = Investigational | bioavailability = | protein_bound = | metabolism = | metabolites = | onset = | elimination_half-life = | duration_of_action = | excretion = | index_label = | index2_label = | CAS_number = | ATCvet = | ATC_prefix = | ATC_suffix = | PubChem = 60734 | PubChem2 = 3033824 | DrugBank = | synonyms = 6-O-Butanoylcastanospermine; MDL-28574; MX-3253 | ChemSpiderID = 54737 | C=12 | H=21 | N=1 | O=5 | StdInChI=1S/C12H21NO5/c1-2-3-9(15)18-8-6-13-5-4-7(14)10(13)12(17)11(8)16/h7-8,10-12,14,16-17H,2-6H2,1H3/t7-,8-,10+,11+,12+/m0/s1 | StdInChIKey=HTJGLYIJVSDQAE-VWNXEWBOSA-N | smiles = CCCC(=O)O[C@H]1CN2CC[C@@H]([C@@H]2[C@H]([C@@H]1O)O)O }}Celgosivir, in development by Migenix for the treatment of hepatitis C virus (HCV) infection, is an oral prodrug of the natural product castanospermine that inhibits alpha-glucosidase I, an enzyme that plays a critical role in viral maturation by initiating the processing of the N-linked oligosaccharides of viral envelope glycoproteins. Celgosivir is well absorbed in vitro and in vivo, and is rapidly converted to castanospermine. Celgosivir has a novel mechanism of action (preventing the glycosylation of viral proteins by the host), and demonstrates broad antiviral activity in vitro.[1] Clinical trialsCelgosivir is not efficient as a monotherapy for the treatment of HCV, but has demonstrated a synergistic effect in combination with pegylated interferon alfa-2b plus ribavirin, both in vitro and in phase II clinical trials that last up to 1 year in patients with chronic HCV infection. Celgosivir may prove to be a valuable component for combination therapy and may help to prevent the apparition of drug resistance. Long-term toxicity studies are necessary to confirm the safety of celgosivir in humans.[1] Although generally safe and well tolerated, celgosivir does not seem to reduce viral load or fever burden in patients with dengue fever.[2] References1. ^1 {{cite journal | pmid=19649930 | year=2009 | author1=Durantel | first1=D | title=Celgosivir, an alpha-glucosidase I inhibitor for the potential treatment of HCV infection | journal=Current Opinion in Investigational Drugs | volume=10 | issue=8 | pages=860–70 }} 2. ^{{cite journal | doi = 10.1016/S1473-3099(14)70730-3| pmid = 24877997| title = Efficacy and safety of celgosivir in patients with dengue fever (CELADEN): A phase 1b, randomised, double-blind, placebo-controlled, proof-of-concept trial| journal = The Lancet Infectious Diseases| volume = 14| issue = 8| pages = 706| year = 2014| last1 = Low| first1 = Jenny G| last2 = Sung| first2 = Cynthia| last3 = Wijaya| first3 = Limin| last4 = Wei| first4 = Yuan| last5 = Rathore| first5 = Abhay P S| last6 = Watanabe| first6 = Satoru| last7 = Tan| first7 = Boon Hian| last8 = Toh| first8 = Liying| last9 = Chua| first9 = Lian Tee| last10 = Hou| first10 = Yan'an| last11 = Chow| first11 = Angelia| last12 = Howe| first12 = Shiqin| last13 = Chan| first13 = Wing Ki| last14 = Tan| first14 = Kah Hin| last15 = Chung| first15 = Jasmine S| last16 = Cherng| first16 = Benjamin P| last17 = Lye| first17 = David C| last18 = Tambayah| first18 = Paul A| last19 = Ng| first19 = Lee Ching| last20 = Connolly| first20 = John| last21 = Hibberd| first21 = Martin L| last22 = Leo| first22 = Yee Sin| last23 = Cheung| first23 = Yin Bun| last24 = Ooi| first24 = Eng Eong| last25 = Vasudevan| first25 = Subhash G}} External links
5 : Antivirals|Iminosugars|Butyrate esters|Triols|Indolizidines |
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