Delving into the Latest Updates on Sitafloxacin Hydrate with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Gracevit, Sitafloxacin, Sitafloxacin (USAN)

+ [6]

Target

Bacterial DNA gyrase x Bacterial top IV

Action

inhibitors

Mechanism

Bacterial DNA gyrase inhibitors(Bacterial DNA gyrase inhibitors), Bacterial top IV inhibitors(Bacterial topoisomerase IV inhibitors)

Therapeutic Areas

Infectious DiseasesMouth and Tooth DiseasesRespiratory Diseases+ [3]

Active Indication

Bacterial InfectionsGingivitisInfectious Diseases+ [20]

Inactive Indication

Acute pharyngitisAcute tonsillitisCommunity Acquired Pneumonia+ [4]

Originator Organization

Daiichi Sankyo Co., Ltd.

Active Organization

Nanjing Zhenhua Pharmaceutical Technology Development Co Ltd

Shenzhen Salubris Pharmaceuticals Co., Ltd.

Daiichi Sankyo Co., Ltd.

+ [3]

Inactive Organization

Shanghai Pharmaceuticals Holding Co., Ltd.

Hainan Hualon Pharmaceutical Co., Ltd.

Nanjing Yoko Pharmaceutical Group Co. Ltd.

+ [1]

Drug Highest PhaseApproved

First Approval Date

Japan (25 Jan 2008),

GingivitisInfectious DiseasesRespiratory Tract Infections+ [1]

RegulationPriority Review (China)

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Structure/Sequence

Molecular FormulaC19H18ClF2N3O3

InChIKeyPNUZDKCDAWUEGK-CYZMBNFOSA-N

CAS Registry127254-12-0

View All Structures (2)

This study is a single-center, open-label clinical trial designed to evaluate the early bactericidal activity (EBA) of sitafloxacin against Mycobacterium abscessus disease. Patients with Mycobacterium abscessus disease were enrolled and treated with sitafloxacin monotherapy for 14 days. Colony forming units (CFU) and time to positivity (TTP) in sputum cultures were analyzed and compared. By assessing the impact of sitafloxacin monotherapy on the bacteria in the sputum of patients with Mycobacterium abscessus disease, the early bactericidal activity of sitafloxacin was evaluated, providing a basis for the selection of new drugs for the treatment of Mycobacterium abscessus disease.

Start Date28 Jan 2025

Sponsor / Collaborator

Beijing Chest Hospital

ChiCTR2400092355

/ RecruitingPhase 1IIT

Ultra-short treatment by advancing new regimens based on sitafloxacin and pyrazinamide for drug-susceptible pulmonary tuberculosis (UltraStar-SZ): A multi-arm, multi-stage, adaptive, multi-centre, randomised, controlled, open-label, non-inferiority trial

Start Date19 Aug 2023

Sponsor / Collaborator-

CTR20223292

/ CompletedNot Applicable

浙江麒正药业有限公司研制的西他沙星片与持证商为Daiichi Sankyo Co., Ltd的西他沙星片（商品名：格雷必妥®/GRACEVIT®）在中国健康受试者中进行的随机、开放、单剂量、两周期、双交叉、空腹及餐后状态下的生物等效性研究

[Translation] A randomized, open-label, single-dose, two-period, double-crossover, fasting and fed bioequivalence study of sitafloxacin tablets developed by Zhejiang Qizheng Pharmaceutical Co., Ltd. and sitafloxacin tablets (trade name: GRACEVIT®) from Daiichi Sankyo Co., Ltd in healthy Chinese subjects

以浙江麒正药业有限公司研制的西他沙星片（规格：50 mg）为受试制剂，以持证商为Daiichi Sankyo Co., Ltd的西他沙星片（商品名：格雷必妥®/GRACEVIT®，规格：50 mg）为参比制剂，考察两制剂在空腹及餐后状态下单次给药的药代动力学参数及相对生物利用度，评价两制剂是否具有生物等效性；同时评价两种制剂在健康人体中的安全性和耐受性。

[Translation]

Sitafloxacin tablets (specification: 50 mg) developed by Zhejiang Qizheng Pharmaceutical Co., Ltd. were used as the test preparation, and Sitafloxacin tablets (trade name: GRACEVIT®/GRACEVIT®, specification: 50 mg) from Daiichi Sankyo Co., Ltd were used as the reference preparation. The pharmacokinetic parameters and relative bioavailability of the two preparations after single administration in the fasting and postprandial states were investigated to evaluate whether the two preparations were bioequivalent; at the same time, the safety and tolerability of the two preparations in healthy humans were evaluated.

Start Date07 Feb 2023

Sponsor / Collaborator

Zhejiang Qizheng Pharmaceutical Co., Ltd

100 Clinical Results associated with Sitafloxacin Hydrate

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100 Translational Medicine associated with Sitafloxacin Hydrate

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100 Patents (Medical) associated with Sitafloxacin Hydrate

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709

Literatures (Medical) associated with Sitafloxacin Hydrate

01 Apr 2025·Journal of Infection and Chemotherapy

Mycobacterium goodii pulmonary disease in an immunocompetent patient: A case report and literature review

Article

Author: Chikamatsu, Kinuyo ; Mitarai, Satoshi ; Nunomura, Yasuhito ; Shiratori, Toshihiro ; Tanaka, Hisashi ; Kurose, Akira ; Taima, Kageaki ; Itoga, Masamichi ; Tasaka, Sadatomo ; Makiguchi, Tomonori

Mycobacterium goodii is a rapidly growing non-tuberculosis mycobacterium, which is known to cause skin, bone and soft tissue infections, but there are a few reports of respiratory infections due to M. goodii. A 67-year-old man had suffered from productive cough, shortness of breath and weight loss for 6 months. He had a history of total gastrectomy for gastric ulcer perforation. Computed tomography (CT) showed dense consolidation in the right lower lobe and nodular lesions in both lungs. Transbronchial cryobiopsy was performed on a lesion in the right lower lobe and granulomatous lesions were observed pathologically. Because M. goodii was identified from two sputum samples using matrix-assisted laser desorption ionization-time of flight mass spectrometry (MALDI-TOF MS), we made a diagnosis of M. goodii pulmonary disease. To confirm the diagnosis, whole genome sequencing analysis was performed, which showed average nucleotide identity of 99.18%. The patient was responded well to the initial therapy with amikacin, imipenem/cilastatin, doxycycline, sulfamethoxazole/ trimethoprim, and clarithromycin, followed by 18 months of ambulatory treatment with doxycycline, sulfamethoxazole/ trimethoprim, clarithromycin, and sitafloxacin. The sputum culture remained negative and CT findings also significantly improved 6 months after the introduction of treatment. In this case, the development of M. goodii pulmonary disease is might be associated with the history of gastrectomy. For identifying the pathogen, MALDI-TOF MS and whole genome sequencing analysis were useful and the intensive initial treatment in accordance with the drug susceptibility testing was successful.

03 Mar 2025·Journal of Antimicrobial Chemotherapy

Reply: prolonged sitafloxacin and doxycycline combination regimen for treating infections by highly resistant Mycoplasma genitalium

Article

Author: Ando, Naokatsu ; Gatanaga, Hiroyuki ; Mizushima, Daisuke

01 Mar 2025·Journal of Infection and Chemotherapy

Non-tuberculous mycobacterial shoulder arthritis with acute exacerbation soon after initiation of immune checkpoint inhibitor: A case report

Article

Author: Nomura, Toshihito ; Kitagawa, Hiroki ; Inada, Shugo ; Ohge, Hiroki ; Hattori, Noboru ; Omori, Keitaro ; Shigemoto, Norifumi

Immune checkpoint inhibitors (ICIs) have been approved for treating various cancers; however, they can cause immune-related adverse events. Generally, ICIs are not associated with an increased risk of infection, however, several reports demonstrated infections caused by non-tuberculous mycobacterium (NTM) during ICI therapy. Here, we report a case of NTM shoulder arthritis with acute exacerbation immediately after ICI initiation. A 75-year-old man was diagnosed with left shoulder arthritis caused by Mycobacterium intracellulare eight months before receiving ICI treatment and was treated with clarithromycin and ethambutol. However, the mild redness, swelling, heat, and shoulder pain persisted. The patient was diagnosed with hepatocellular carcinoma and atezolizumab and bevacizumab treatment was initiated; one day after the initiation of therapy, the patient presented with a fever and worsened shoulder symptoms. Considering the suspected worsening of NTM arthritis, sitafloxacin was additionally administered, and surgical debridement was performed. M. intracellulare was isolated through culturing shoulder synovial tissue; immunohistochemical staining analysis revealed programmed death-1 (PD-1) and programmed death ligand-1 (PD-L1) expression in granulation tissue cells. After the arthritis symptoms decreased, atezolizumab plus bevacizumab was resumed and continued with no recurrence of arthritis. The NTM exacerbation on the day after ICI administration suggests the potential involvement of the PD-1/PD-L1 pathway in the pathogenesis of NTM; moreover, adverse inflammatory reactions to NTM were possibly triggered through the blockade of this pathway.

100 Deals associated with Sitafloxacin Hydrate

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External Link

KEGG	Wiki	ATC	Drug Bank
D02475	Sitafloxacin Hydrate	J01MA21	DB13261

R&D Status

Approved

10 top approved records.

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Indication	Country/Location	Organization	Date
Bacterial Infections	Japan	Daiichi Sankyo Co., Ltd.	02 Jun 2008
Gingivitis	Japan	Daiichi Sankyo Co., Ltd.	25 Jan 2008
Infectious Diseases	Japan	Daiichi Sankyo Co., Ltd.	25 Jan 2008
Respiratory Tract Infections	Japan	Daiichi Sankyo Co., Ltd.	25 Jan 2008
Urinary Tract Infections	Japan	Daiichi Sankyo Co., Ltd.	25 Jan 2008

Developing

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Acute Bronchitis	Phase 1	China	Hainan Hualon Pharmaceutical Co., Ltd.	23 Oct 2015
Bronchitis, Chronic	Phase 1	China	Hainan Hualon Pharmaceutical Co., Ltd.	23 Oct 2015
Cystitis	Phase 1	China	Hainan Hualon Pharmaceutical Co., Ltd.	23 Oct 2015
Urinary Tract Infections	Phase 1	China	Hainan Hualon Pharmaceutical Co., Ltd.	23 Oct 2015
Acute urinary tract infection	Phase 1	China	CMIC CMO Co., Ltd.	08 Dec 2012
Acute urinary tract infection	Phase 1	China	Daiichi Sankyo Co., Ltd.	08 Dec 2012
Complicated urinary tract infection	Phase 1	China	Daiichi Sankyo Co., Ltd.	08 Dec 2012
Complicated urinary tract infection	Phase 1	China	CMIC CMO Co., Ltd.	08 Dec 2012
Pneumonia	Phase 1	China	CMIC CMO Co., Ltd.	02 Dec 2012
Pneumonia	Phase 1	China	Daiichi Sankyo Co., Ltd.	02 Dec 2012

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Clinical Result

Indication

Phase

Evaluation

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


IAS2022	Not Applicable	Mycoplasma genitalium infection	114	Sitafloxacin 200 mg	(zcchayltnh) = xaztcfbftz ctigxskpzx (qzoyzxsdgd )	-	01 Jan 2022
ASN2012	Not Applicable	Infectious Diseases Maintenance	-	Sitafloxacin 50 mg	mytomxnwfz(nvjbdrrroj) = tccdrbqvrl qjalbbxovu (mfgwdjhpxn ) View more	Positive	30 Oct 2012
ASN2012	Not Applicable	Infectious Diseases Maintenance	-	Levofloxacin 500 mg/250 mg	mytomxnwfz(nvjbdrrroj) = mvsskocgto qjalbbxovu (mfgwdjhpxn ) View more	Positive	30 Oct 2012