Acorafloxacin(Acorafloxacin) - 药物靶点：Bacterial DNA gyrase x Top II x Topoisomerase IV_在研适应症：社区获得性细菌性肺炎，复杂皮肤和皮肤结构感染_专利_临床

概要

基本信息

药物类型

小分子化药

别名

Acorafloxacin (USAN)、Acorafloxacin Hydrochloride、Avarofloxacin

+ [4]

靶点

Bacterial DNA gyrase x Top II x Topoisomerase IV

作用机制

细菌DNA旋转酶复合体抑制剂、Top II抑制剂(拓扑异构酶II抑制剂)、拓扑异构酶 IV抑制剂

+ [1]

治疗领域

感染呼吸系统疾病皮肤和肌肉骨骼疾病

在研适应症

社区获得性细菌性肺炎复杂皮肤和皮肤结构感染

非在研适应症

复杂的皮肤和软组织感染

原研机构

Janssen Global Services LLC

在研机构

Johnson & Johnson Pharmaceutical Research & Development LLC

非在研机构

Furiex Pharmaceuticals, Inc.

Janssen Global Services LLCJanssen, Inc.

最高研发阶段临床前

首次获批日期-

最高研发阶段(中国)-

特殊审评-

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结构

分子式C21H23F2N3O4

InChIKeyVMKVDAAFMQKZJS-LFIBNONCSA-N

CAS号878592-87-1

关联

4

项与 Acorafloxacin 相关的临床试验

EUCTR2010-021574-11-DE / Not yet recruitingN/A

A Randomized, Controlled, Double-Blind, Multicenter, Phase 2 Study of the Safety/Tolerability and Efficacy of JNJ-32729463 Compared With Moxifloxacin for the Treatment of Subjects Requiring Hospitalization for Community-Acquired Bacterial Pneumonia (CABP) With a PORT Score of II or Greater

开始日期2011-01-24

申办/合作机构

Furiex Pharmaceuticals, Inc.

NCT01198626 / Terminated临床2期

A Randomized, Controlled, Double Blind, Multicenter, Phase 2 Study of the Safety/Tolerability and Efficacy of JNJ-32729463 Compared With Moxifloxacin for the Treatment of Subjects Requiring Hospitalization for Community-Acquired Bacterial Pneumonia (CABP) With a PORT Score of II or Greater

The purpose of this study is to determine the efficacy, safety and tolerability of JNJ-32729463 compared to moxifloxacin for the treatment of subjects requiring hospitalization for Community-Acquired Bacterial Pneumonia (CABP).

开始日期2010-10-01

申办/合作机构

Furiex Pharmaceuticals, Inc.

NCT01128530 / Completed临床2期

A Randomized, Controlled, Double-Blind, Double Dummy, Multicenter Phase 2 Study of the Safety/Tolerability and Efficacy of JNJ-32729463 Compared With Linezolid (Zyvox) for the Treatment of Complicated Skin and Skin Structure Infection

The purpose of this study is to determine the clinical efficacy, safety, and tolerability of a 250 mg BID oral dose of JNJ-32729463 compared with linezolid in subjects with complicated skin and skin structure infections (cSSSIs).

开始日期2010-06-01

申办/合作机构

Furiex Pharmaceuticals, Inc.

100 项与 Acorafloxacin 相关的临床结果

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100 项与 Acorafloxacin 相关的转化医学

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100 项与 Acorafloxacin 相关的专利（医药）

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22

项与 Acorafloxacin 相关的文献（医药）

2022-07-01·BMJ Open Ophthalmology

Potential new fluoroquinolone treatments for suspected bacterial keratitis

Review

作者: Herbert, Rose ; Kaye, Stephen B ; Somerville, Tobi ; Caddick, Mary ; McLean, Keri ; Czanner, Gabriela ; Neal, Timothy ; Tuft, Stephen ; Herwitker, Shakeel

Topical fluoroquinolones (FQs) are an established treatment for suspected microbial keratitis. An increased FQ resistance in some classes of bacterial pathogens is a concern. Some recently developed FQs have an extended spectrum of activity, making them a suitable alternative for topical ophthalmic use. For example, the new generation FQs, avarofloxacin, delafloxacin, finafloxacin, lascufloxacin, nadifloxacin, levonadifloxacin, nemonoxacin and zabofloxacin have good activity against the common ophthalmic pathogens such asStaphylococcus aureus,Pseudomonas aeruginosa,Streptococcus pneumoniaeand several of theEnterobacteriaceae. However, because there are no published ophthalmic break-point concentrations, the susceptibility of an isolated micro-organism to a topical FQ is extrapolated from systemic break-point data and wild type susceptibility. The purpose of this review is to compare the pharmacokinetics and pharmacodynamics of the FQs licensed for topical ophthalmic use with the same parameters for new generation FQs. We performed a literature review of the FQs approved for topical treatment and the new generation FQs licensed to treat systemic infections. We then compared the minimum inhibitory concentrations (MIC) of bacterial isolates and the published concentrations that FQs achieved in the cornea and aqueous. We also considered the potential suitability of new generation FQs for topical use based on their medicinal properties. Notably, we found significant variation in the reported corneal and aqueous FQ concentrations so that reliance on the reported mean concentration may not be appropriate, and the first quartile concentration may be more clinically relevant. The provision of the MIC for the microorganism together with the achieved lower (first) quartile concentration of a FQ in the cornea could inform management decisions such as whether to continue with the prescribed antimicrobial, increase the frequency of application, use a combination of antimicrobials or change treatment.

2022-05-04·Expert Review of Anti-infective Therapy2区 · 医学

Anti-MRSA quinolones for acute bacterial skin and skin structure infection: a systematic review and meta-analysis of randomized controlled trials

2区 · 医学

Review

作者: Chao, Chien-Ming ; Lin, Wei-Ting ; Weng, Teng-Song ; Chen, Yu-Hung ; Lai, Chih-Cheng

OBJECTSThis study compared the clinical efficacy and safety of anti-methicillin-resistant Staphylococcus aureus (MRSA) quinolones for treating acute bacterial skin and skin structure infections (ABSSSIs).METHODSPubMed, Embase, and the Cochrane Central Register of Controlled Trials were searched for relevant articles from inception to 21 July 2021. RCTs comparing the clinical efficacy and safety of anti-MRSA quinolones with other antibiotics for treating adult patients with ABSSSIs were included.RESULTSSix RCTs were included. A total of 1,264 and 1,307 participants received the anti-MRSA quinolone-based study group and the control group. In the study group receiving anti-MRSA quinolone-based treatment, 935, 246, and 83 patients received delafloxacin, levonadifloxacin, and acorafloxacin, respectively. No significant difference was observed in the clinical cure rate at test of cure between the study and control groups (OR, 1.08; 95% CI, 0.91-1.29; I² = 0%). In patients with MRSA-associated ABSSSIs, the clinical cure rate (OR, 1.09; 95% CI, 0.71-1.65; I² = 0%) and microbiological response rate (OR, 1.24; 95% CI, 0.48-3.21; I² = 0%) of anti-MRSA quinolones were similar to those of other antibiotics.CONCLUSIONSThe efficacy of anti-MRSA quinolone-based treatment is comparable to that of other anti-MRSA antibiotics for treating ABSSSIs.

2021-06-24·Journal of Medicinal Chemistry1区 · 医学

Design, Synthesis, and Biological Evaluation of Novel Pyrimido[4,5-b]indole Derivatives Against Gram-Negative Multidrug-Resistant Pathogens

1区 · 医学

Article

作者: Meng, Xin ; Xue, Yaru ; Wang, Ting ; Pan, Wei ; Luo, Cheng ; Xu, Heng ; Zhang, Shuhua ; Kong, Qidi ; Guo, Bin ; Yang, Yushe

Due to the poor permeability across Gram-negative bacterial membranes and the troublesome bacterial efflux mechanism, only a few GyrB/ParE inhibitors with potent activity against Gram-negative pathogens have been reported. Among them, pyrimido[4,5-b]indole derivatives represented by GP-1 demonstrated excellent broad-spectrum antibacterial activity against both Gram-positive and Gram-negative bacteria but were limited by hERG inhibition and poor pharmacokinetics profile. To improve their drug-like properties, we designed a series of novel pyrimido[4,5-b]indole derivatives based on the tricyclic scaffold of GP-1 and the C-7 moiety of acorafloxacin. These efforts have culminated in the discovery of a promising compound 18r with reduced hERG liability and an improved PK profile. Compound 18r exhibited superior broad-spectrum in vitro antibacterial activity compared to GP-1, including a variety of clinical multidrug G^- pathogens, especially Acinetobacter baumannii, and the in vivo efficacy was also demonstrated in a neutropenic mouse thigh model of infection with multidrug-resistant A. baumannii.

100 项与 Acorafloxacin 相关的药物交易

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外链

KEGG	Wiki	ATC	Drug Bank
D10435	Acorafloxacin	-	-

研发状态

10 条进展最快的记录,

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适应症	最高研发状态	国家/地区	公司	日期
社区获得性细菌性肺炎	临床3期	匈牙利	Furiex Pharmaceuticals, Inc.	2010-10-01
社区获得性细菌性肺炎	临床3期	加拿大	Furiex Pharmaceuticals, Inc.	2010-10-01
社区获得性细菌性肺炎	临床3期	哥伦比亚	Furiex Pharmaceuticals, Inc.	2010-10-01
社区获得性细菌性肺炎	临床3期	波兰	Furiex Pharmaceuticals, Inc.	2010-10-01
社区获得性细菌性肺炎	临床3期	德国	Furiex Pharmaceuticals, Inc.	2010-10-01
社区获得性细菌性肺炎	临床3期	美国	Furiex Pharmaceuticals, Inc.	2010-10-01
复杂的皮肤和软组织感染	临床3期	美国	Furiex Pharmaceuticals, Inc.	-
肺炎	临床3期	-	Janssen Global Services LLC	-
皮肤和皮肤结构感染	临床3期	-	Janssen Global Services LLC	-
复杂皮肤和皮肤结构感染	药物发现	美国	Furiex Pharmaceuticals, Inc.	2010-06-01