词条 | Zoliflodacin |
释义 |
| drug_name = | INN = | type = | IUPAC_name = | image = Zoliflodacin.svg | alt = | caption = | pronounce = | tradename = | Drugs.com = | MedlinePlus = | licence_EU = | licence_US = | pregnancy_AU = | pregnancy_AU_comment = | pregnancy_US = | pregnancy_category = Not classified yet | routes_of_administration = Oral | legal_AU = | legal_AU_comment = | legal_BR = | legal_BR_comment = | legal_CA = | legal_DE = | legal_NZ = | legal_UK = | legal_US = IND | legal_UN = | legal_status = Investigational | bioavailability = 97.8% | protein_bound = | metabolism = Hepatic | metabolites = | onset = {{ubl|Fasted: 1.5–2.3 h|Fed: 4 h}} | elimination_half-life = 5.3–6.3 h | duration_of_action = | excretion = {{ubl|Faeces (79.6%)|Urine (18.2%)}} | CAS_number = 1620458-09-4 | class = Antibiotic | ATCvet = | ATC_prefix = | ATC_suffix = | PubChem = 76685216 | DrugBank = 12817 | UNII = FWL2263R77 | synonyms = AZD0914; ETX0914 | C = 22 | H = 22 | F = 1 | N = 5 | O = 7 | smiles = C[C@@H]1CN2[C@H]([C@@H](O1)C)C3(CC4=C2C(=C5C(=C4)C(=NO5)N6[C@H](COC6=O)C)F)C(=O)NC(=O)NC3=O | StdInChI = 1S/C22H22FN5O7/c1-8-7-33-21(32)28(8)17-12-4-11-5-22(18(29)24-20(31)25-19(22)30)16-10(3)34-9(2)6-27(16)14(11)13(23)15(12)35-26-17/h4,8-10,16H,5-7H2,1-3H3,(H2,24,25,29,30,31)/t8-,9+,10-,16+/m0/s1 | StdInChIKey = ZSWMIFNWDQEXDT-ZESJGQACSA-N }}Zoliflodacin (development codes AZD0914 and ETX0914) is an experimental antibiotic that is being studied for the treatment of infection with Neisseria gonorrhoeae (gonorrhea).[1] It has a novel mechanism of action which involves inhibition of bacterial type II topoisomerases.[2] It is being developed by Entasis Therapeutics and is currently in Phase II clinical trials.[3] References1. ^{{cite journal | doi = 10.1056/NEJMoa1706988| pmid = 30403954| title = Single-Dose Zoliflodacin (ETX0914) for Treatment of Urogenital Gonorrhea| journal = New England Journal of Medicine| volume = 379| issue = 19| pages = 1835–1845| year = 2018| last1 = Taylor| first1 = Stephanie N.| last2 = Marrazzo| first2 = Jeanne| last3 = Batteiger| first3 = Byron E.| last4 = Hook| first4 = Edward W.| last5 = Seña| first5 = Arlene C.| last6 = Long| first6 = Jill| last7 = Wierzbicki| first7 = Michael R.| last8 = Kwak| first8 = Hannah| last9 = Johnson| first9 = Shacondra M.| last10 = Lawrence| first10 = Kenneth| last11 = Mueller| first11 = John}} 2. ^{{Cite journal | doi = 10.1038/srep11827| pmid = 26168713| pmc = 4501059| title = Responding to the challenge of untreatable gonorrhea: ETX0914, a first-in-class agent with a distinct mechanism-of-action against bacterial Type II topoisomerases| journal = Scientific Reports| volume = 5| pages = 11827| year = 2015| last1 = Basarab| first1 = Gregory S.| last2 = Kern| first2 = Gunther H.| last3 = McNulty| first3 = John| last4 = Mueller| first4 = John P.| last5 = Lawrence| first5 = Kenneth| last6 = Vishwanathan| first6 = Karthick| last7 = Alm| first7 = Richard A.| last8 = Barvian| first8 = Kevin| last9 = Doig| first9 = Peter| last10 = Galullo| first10 = Vincent| last11 = Gardner| first11 = Humphrey| last12 = Gowravaram| first12 = Madhusudhan| last13 = Huband| first13 = Michael| last14 = Kimzey| first14 = Amy| last15 = Morningstar| first15 = Marshall| last16 = Kutschke| first16 = Amy| last17 = Lahiri| first17 = Sushmita D.| last18 = Perros| first18 = Manos| last19 = Singh| first19 = Renu| last20 = Schuck| first20 = Virna J. A.| last21 = Tommasi| first21 = Ruben| last22 = Walkup| first22 = Grant| last23 = Newman| first23 = Joseph V.}} 3. ^{{cite web | url = http://www.entasistx.com/pipeline | title = Pipeline | publisher = Entasis Therapeutics}} 6 : Experimental drugs|Antibiotics|Oxazolidinones|Isoxazoles|Fluoroarenes|Imides |
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