那氟沙星(Nadifloxacin) - 药物靶点：Bacterial DNA gyrase x Topoisomerase IV_在研适应症：毛囊炎，脓疱疮，寻常痤疮_专利_临床

概要

基本信息

药物类型

小分子化药

别名

Nadifloxacin (JAN/INN)、Nadixa

+ [6]

靶点

Bacterial DNA gyrase x Topoisomerase IV

作用机制

细菌DNA旋转酶复合体抑制剂、拓扑异构酶 IV抑制剂

治疗领域

感染皮肤和肌肉骨骼疾病

在研适应症

毛囊炎脓疱疮寻常痤疮

非在研适应症-

原研机构

Otsuka Pharmaceutical Co., Ltd.

在研机构

湖南中威制药有限公司

Otsuka Pharmaceutical Co., Ltd.Ferrer Internacional SA

非在研机构-

最高研发阶段批准上市

首次获批日期

日本 (1993-09-14),

寻常痤疮

最高研发阶段(中国)批准上市

特殊审评-

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结构

分子式C19H21FN2O4

InChIKeyJYJTVFIEFKZWCJ-UHFFFAOYSA-N

CAS号124858-35-1

关联

7

项与那氟沙星相关的临床试验

DRKS00014231 / CompletedN/A

Comparative Investigation on the in vitro susceptibility of Propionibacterium acnes (P. acnes) against nadifloxacin, erythromycin, clindamycin and tetracycline - P343

开始日期2018-03-05

申办/合作机构-

CTRI/2017/08/009280 / Completed临床4期IIT

Efficacy and safety of Nadifloxacin and Benzoyl peroxide versus Adapalene and Benzoyl Peroxide in acene vulgaris : A Randomized open label phase IV clinical trial

开始日期2017-08-09

申办/合作机构-

CTRI/2018/03/012411 / Completed临床4期IIT

An open label, randomized, parallel group, comparative evaluation of safety and efficacy of Nadifloxacin 1% ointment versus Mupirocin 2% ointment in children with skin and soft tissue infection.

开始日期2017-07-19

申办/合作机构-

100 项与那氟沙星相关的临床结果

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100 项与那氟沙星相关的转化医学

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100 项与那氟沙星相关的专利（医药）

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101

项与那氟沙星相关的文献（医药）

2024-09-01·The Journal of Dermatology

Ozenoxacin suppresses sebum production by inhibiting mTORC1 activation in differentiated hamster sebocytes

Article

作者: Matsumoto, Tatsumi ; Kitano, Takamichi ; Koiwai, Toshikazu ; Mori, Sachi ; Fujikawa, Koki ; Sato, Takashi

AbstractAcne vulgaris is a complex condition involving factors that affect the pilosebaceous unit. A primary manifestation of acne pathology is the development of comedones, often linked to the overproduction of sebum resulting from 5α‐dihydrotestosterone (5α‐DHT) and insulin activity. Ozenoxacin is a topical quinolone that exhibits potent antibacterial activity against Cutibacterium acnes (C. acnes). It is commonly used to treat acne associated with this bacterium; however, its effect on sebum production within the sebaceous glands remains unclear. In this study, the effects of ozenoxacin on sebum production were examined using insulin‐ and 5α‐DHT‐differentiated hamster sebocytes. Ozenoxacin showed a dose‐dependent inhibition of lipid droplet formation and triacylglycerol (TG) production, which is a major component of sebum. In addition, it suppressed the expression of diacylglycerol acyltransferase 1, stearoyl‐CoA desaturase‐1, and perilipin‐1 mRNA, all important factors involved in sebum synthesis, in a dose‐dependent manner. Moreover, ozenoxacin decreased phosphorylated 40S ribosomal protein S6 levels downstream of the mechanistic/mammalian target of rapamycin complex 1 (mTORC1), without altering the phosphorylation of Akt, an upstream regulator of mTORC1, in both insulin‐ and 5α‐DHT‐treated hamster sebocytes. Interestingly, nadifloxacin, but not clindamycin, exhibited a similar suppression of sebum production, albeit with lesser potency compared with ozenoxacin. Furthermore, a topical application of a 2% ozenoxacin‐containing lotion to the auricle skin of hamsters did not affect the size of the sebaceous glands or epidermal thickness. Notably, it decreased the amount of TG on the skin surface. The results provide novel insights into the sebum‐inhibitory properties of ozenoxacin, indicating its potential efficacy in controlling microbial growth and regulating sebum production for acne management.

2024-01-01·Spectrochimica Acta Part A: Molecular and Biomolecular Spectroscopy

Photoluminescence detection of nadifloxacin: Adopts switching off photoinduced electron transfer (PET)

Article

作者: Mohamed, Abobakr A ; Derayea, Sayed M ; Omar, Mahmoud A ; Mostafa, Islam M ; Elsayed, Mohamed Ahmed

A new fluorimetric sensing method for the selective and sensitive quantification of nadifloxacin (antibacterial agent, NDF) was established for the first time. The introduced method relies on blocking the photoinduced electron transfer (PET) effect of the nitrogen atom presented on the piperidine ring in NDF by fine-tuning the pH of the surrounding medium through its protonation using 0.5 M acetic acid. This protonation turns the weak fluorescence of NDF into stronger fluorescence intensity, allowing its selective and sensitive detection in its pure state as well as cream pharmaceutical formulation without any obstruction from the common excipients. The developed method has shown an NDF detection limit of 1.72 ng mL^-1 and a quantification limit of 5.20 ng mL^-1.

2023-09-06·Molecules (Basel, Switzerland)

Rapid Limit Test of Eight Quinolone Residues in Food Based on TLC-SERS, a New Limit Test Method.

Article

作者: Zhang, Min ; Ren, Qiyong ; Wang, Yuanrui ; Xu, Feng ; Dong, Wei ; Xu, Tao ; Liu, Jicheng ; Li, Li ; Zhang, Honglian

Residual quinolones in food that exceed their maximum residue limit (MRL) are harmful to human health. However, the existing methods used for testing these residues have limitations; so, we developed a new limit test method called TLC-SERS to rapidly determine the levels of residues of the following: enrofloxacin (A), ciprofloxacin (B), ofloxacin (C), fleroxacin (D), sparfloxacin (E), enoxacin (F), gatifloxacin (G), and nadifloxacin (H). The residues ware preliminarily separated via TLC. The tested compounds' position on a thin-layer plate were labeled using their relative R_f under 254 nm ultraviolet light, and an appropriate amount of nanometer silver solution was added to the position. The silver on the plate was irradiated with a 532 nm laser to obtain the SERSs of the compounds. The results show significant differences in the SERS of the eight quinolones: the LODs of H, A, D, E, C, G, F, and B were 9.0, 12.6, 8.9, 19.0, 8.0, 8.7, 19.0, and 12.6 ng/mL, respectively; and the RSD was ≤4.9% for the SERS of each quinolone. The limit test results of 20 samples are consistent with those obtained via UPLC-MS/MS. The results indicate that TLC-SERS is a specific, sensitive, stable, and accurate method, providing a new reference for the rapid limit test of harmful residues in foods.

100 项与那氟沙星相关的药物交易

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外链

KEGG	Wiki	ATC	Drug Bank
D01147	那氟沙星	D10AF05	DB12447

研发状态

10 条最早获批的记录,

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适应症	国家/地区	公司	日期
毛囊炎	中国	湖南中威制药有限公司	2008-01-01
脓疱疮	中国	湖南中威制药有限公司	2008-01-01
寻常痤疮	日本	Otsuka Pharmaceutical Co., Ltd.	1993-09-14