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词条 Zoliflodacin
释义

  1. References

{{Infobox drug
| 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]

References

1. ^{{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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