Delving into the Latest Updates on Cefotiam hexetil hydrochloride with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

CTM-HE, Cefotiam hexetil hydrochloride (JP17)

+ [5]

Target

α2A-AR

Mechanism

α2A-AR agonists(Alpha-2a adrenergic receptor agonists)

Therapeutic Areas

Infectious DiseasesEye DiseasesMouth and Tooth Diseases+ [5]

Active Indication

AbscessBurn infectionsCystitis+ [14]

Inactive Indication

Acute BronchitisCorneal UlcerHordeolum+ [7]

Originator Organization

Takeda Pharmaceutical Co., Ltd.

Active Organization

Takeda Pharmaceutical Co., Ltd.

Beijing Boshi Antai Technology Development Co., Ltd.

Inactive Organization-

Drug Highest PhaseApproved

First Approval Date

JP (01 Jan 1990),

AbscessBurn infectionsCystitis+ [13]

Regulation-

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Structure

Molecular FormulaC27H37N9O7S3

InChIKeyVVFDMWZLBPUKTD-ZKRNHDOASA-N

CAS Registry95761-91-4

View All Structures (2)

考察健康志愿者空腹口服由成都倍特药业有限公司开发的100mg 规格（受试制剂）及200mg 规格（参比制剂）的盐酸头孢替安酯片后血药浓度经时变化过程，估算相应的药代动力学参数，评价受试制剂的相对生物利用度，判断其与参比制剂是否具有生物等效性，指导临床用药。

[Translation]

To investigate the time-dependent changes in blood drug concentrations of healthy volunteers after oral administration of 100mg (test preparation) and 200mg (reference preparation) of ceftriaxone hydrochloride tablets developed by Chengdu Beite Pharmaceutical Co., Ltd. on an empty stomach, estimate the corresponding pharmacokinetic parameters, evaluate the relative bioavailability of the test preparation, determine whether it is bioequivalent to the reference preparation, and guide clinical drug use.

Start Date22 May 2015

Sponsor / Collaborator

Shandong Chuangxin Pharmaceutical Research & Development Co., Ltd.

[+1]

CTR20140697 / CompletedPhase 1

盐酸头孢替安酯片人体药代动力学试验

[Translation] Pharmacokinetic study of ceftriaxone hydrochloride tablets in humans

考察健康志愿者单次或多次空腹口服成都倍特药业有限公司生产的盐酸头孢替安酯片后体内头孢替安的血药浓度经时变化过程，估算相应的药代动力学参数，评价盐酸头孢替安在人体内的药代动力学特征，为盐酸头孢替安酯片II期临床试验方案制定提供试验依据，同时为临床用药的给药剂量和给药方法提供依据。

[Translation]

To investigate the time-dependent changes in the blood concentration of ceftriaxone in healthy volunteers after single or multiple oral administrations of ceftriaxone hydrochloride tablets produced by Chengdu Beite Pharmaceutical Co., Ltd. on an empty stomach, estimate the corresponding pharmacokinetic parameters, evaluate the pharmacokinetic characteristics of ceftriaxone hydrochloride in humans, provide an experimental basis for the formulation of the Phase II clinical trial plan of ceftriaxone hydrochloride tablets, and provide a basis for the dosage and method of clinical medication.

Start Date01 Mar 2015

Sponsor / Collaborator

Shandong Chuangxin Pharmaceutical Research & Development Co., Ltd.

[+1]

100 Clinical Results associated with Cefotiam hexetil hydrochloride

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100 Translational Medicine associated with Cefotiam hexetil hydrochloride

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100 Patents (Medical) associated with Cefotiam hexetil hydrochloride

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25

Literatures (Medical) associated with Cefotiam hexetil hydrochloride

01 Jul 2023·Redox Biology

Development of an assay pipeline for the discovery of novel small molecule inhibitors of human glutathione peroxidases GPX1 and GPX4

Article

Author: Cheng, Qing ; Travers, Jameson ; Klumpp-Thomas, Carleen ; Guo, Hui ; Cheff, Dorian M ; Arnér, Elias S J ; Hall, Matthew D ; Shen, Min

Selenoprotein glutathione peroxidases (GPX), like ubiquitously expressed GPX1 and the ferroptosis modulator GPX4, enact antioxidant activities by reducing hydroperoxides using glutathione. Overexpression of these enzymes is common in cancer and can be associated with the development of resistance to chemotherapy. GPX1 and GPX4 inhibitors have thus shown promise as anti-cancer agents, and targeting other GPX isoforms may prove equally beneficial. Existing inhibitors are often promiscuous, or modulate GPXs only indirectly, so novel direct inhibitors identified through screening against GPX1 and GPX4 could be valuable. Here, we developed optimized glutathione reductase (GR)-coupled GPX assays for the biochemical high-throughput screen (HTS) of almost 12,000 compounds with proposed mechanisms of action. Initial hits were triaged using a GR counter-screen, assessed for isoform specificity against an additional GPX isoform, GPX2, and were assessed for general selenocysteine-targeting activity using a thioredoxin reductase (TXNRD1) assay. Importantly, 70% of the GPX1 inhibitors identified in the primary screen, including several cephalosporin antibiotics, were found to also inhibit TXNRD1, while auranofin, previously known as a TXNRD1 inhibitor, also inhibited GPX1 (but not GPX4). Additionally, every GPX1 inhibitor identified (including omapatrilat, tenatoprazole, cefoxitin and ceftibuten) showed similar inhibitory activity against GPX2. Some compounds inhibiting GPX4 but not GPX1 or GPX2, also inhibited TXNRD1 (26%). Compounds only inhibiting GPX4 included pranlukast sodium hydrate, lusutrombopag, brilanestrant, simeprevir, grazoprevir (MK-5172), paritaprevir, navitoclax, venetoclax and VU0661013. Two compounds (metamizole sodium and isoniazid sodium methanesulfate) inhibited all three GPXs but not TXNRD1, while 2,3-dimercaptopropanesulfonate, PI4KIII beta inhibitor 3, SCE-2174 and cefotetan sodium inhibited all tested selenoproteins (but not GR). The detected overlaps in chemical space suggest that the counter screens introduced here should be imperative for identification of specific GPX inhibitors. With this approach, we could indeed identify novel GPX1/GPX2- or GPX4-specific inhibitors, thus presenting a validated pipeline for future identification of specific selenoprotein-targeting agents. Our study also identified GPX1/GPX2, GPX4 and/or TXNRD1 as targets for several previously developed pharmacologically active compounds.

01 May 2013·Sichuan da xue xue bao. Yi xue ban = Journal of Sichuan University. Medical science edition

[Determination of unknown impurities in cefotiam hexetil by HPLC-MS/MS].

Article

Author: Liao, Lin-Chuan ; Wang, Zhi-Hui ; Ye, Yi ; Zhan, Lan-Fen ; Yan, You-Yi ; Liu, Ming-Dong ; Tang, Qun-Xing

OBJECTIVETo detect unknown impurities in raw drug material of cefotiam hexetil.METHODSHigh performance liquid chromatography-tandem mass spectrometry (HPLC-MS/MS) was employed for the determination of impurities in cefotiam hexetil. Agilent SB-C18 column (150 mm x 2.1 mm i. d. , 3.5 microm particles) was used for chromatographic separations of cofotiam hexetil dissolved in deionized water, with mobile phase consisting of (A) 0.1% formic acid and (B) acetonitrile and timed gradient program T (min)/B (%): 0/3, 5/3, 15/20, 20/40, 30/60, 40/80. The flow rate was set at 0. 3 mL/min with DAD detector wavelength fixed at 254 nm. Electrospray ionization source was applied and operated in positive ion MRM mode. The source voltage was kept at 4 kV and cone voltage was 100 V with the mass range m/z 50-1000. Nitrogen was used as nebulizing gas and the nebulizer pressure was 40 psi. The drying gas temperature was 350 degrees C and the drying gas flow was 10 L/min. Results Unknown impurities of cefotiam hexetil were identified. Substance 1 was delta3-isomer of cefotiam hexetil. The structures of 3 other substances were also determined.CONCLUSIONThe method is sensitive, rapid and credible for the analysis of cefotiam hexetil and its related impurities, which can be applied in quality control of cefotiam hexetil.

01 Jan 2013·Nihon Jinzo Gakkai shi

[A case of tuberculous peritonitis in a hemodialysis patient revealed by severe diarrhea and stomachache].

Article

Author: Hatta, Tsuguru ; Hara, Masayuki ; Segawa, Hiroyoshi ; Ohtani, Mai ; Sawada, Katsunori ; Ueno, Risa

A 53-year-old woman was admitted to our hospital due to abdominal pain, diarrhea, and shunt occlusion caused by dehydration. She had undergone hemodialysis due to diabetic nephropathy over a ten-year period. She was hospitalized again with fever and a persistent high serum CRP level. We started antibiotic administration using cefotiam hexetil hydrochloride because of ascites and peritoneum thickening observed by abdominal computed tomography. Although her symptoms, such as abdominal pain and diarrhea, improved after the administration of antibiotics, the ascites and the peritoneum thickening did not improve. On the fourth hospital day, we attempted ascites aspiration to investigate the etiology of the peritonitis. Cytological examination suggested tuberculous peritonitis because of predominant macrophage cell proliferation, a high level of ADA concentration, and a high level of CA125 of ascites. Although QuantiFERON-tuberculosis (QFT) and the Gaffky scale were negative, we started multidrug therapy (isoniazid + rifampicin + pyrazinamide + ethambutol) on the 20th hospital day. She was finally diagnosed as mycobacterium tuberculous peritonitis based on biopsy of the tissue of the ileum and the results of colonoscopy. Administration of antituberculosis chemotherapy improved abdominal fullness and ascites and the patient was discharged on the 97th hospital day. Moreover Kuno et al. reported that serum soluble interleukin-2 receptor(sIL-2R) and CA-125 levels can be used to monitor the response to anti-tuberculosis treatment. In this case, we use these markers to monitor the response to treatment. We experienced a case of tuberculous peritonitis undergoing hemodialysis. Tuberculosis should be suspected when patients undergoing dialysis have long-term fever of unknown etiology. There are many reports stating that the sensitivity and specificity of QuantiFERON-tuberculosis (QFT) and sputum culture are low in latent tuberculosis infection of dialysis patients. Accordingly it is necessary to diagnose mycobacterium tuberculous peritonitis comprehensively by the clinical symptoms and image analysis.

100 Deals associated with Cefotiam hexetil hydrochloride

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External Link

KEGG	Wiki	ATC	Drug Bank
D01415	Cefotiam hexetil hydrochloride	J01DC07	-

R&D Status

Approved

10 top approved records.

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Indication	Country/Location	Organization	Date
Abscess	JP	Takeda Pharmaceutical Co., Ltd.	01 Jan 1990
Burn infections	JP	Takeda Pharmaceutical Co., Ltd.	01 Jan 1990
Cystitis	JP	Takeda Pharmaceutical Co., Ltd.	01 Jan 1990
Dacryocystitis	JP	Takeda Pharmaceutical Co., Ltd.	01 Jan 1990
Escherichia Coli Infections	JP	Takeda Pharmaceutical Co., Ltd.	01 Jan 1990
Haemophilus Infections	JP	Takeda Pharmaceutical Co., Ltd.	01 Jan 1990
Keratitis	JP	Takeda Pharmaceutical Co., Ltd.	01 Jan 1990
Otitis Media	JP	Takeda Pharmaceutical Co., Ltd.	01 Jan 1990
Pneumococcal Infections	JP	Takeda Pharmaceutical Co., Ltd.	01 Jan 1990
Pneumonia	JP	Takeda Pharmaceutical Co., Ltd.	01 Jan 1990
Pyelonephritis	JP	Takeda Pharmaceutical Co., Ltd.	01 Jan 1990
Sinusitis	JP	Takeda Pharmaceutical Co., Ltd.	01 Jan 1990
Skin Diseases, Infectious	JP	Takeda Pharmaceutical Co., Ltd.	01 Jan 1990
Staphylococcal Infections	JP	Takeda Pharmaceutical Co., Ltd.	01 Jan 1990
Stomatitis	JP	Takeda Pharmaceutical Co., Ltd.	01 Jan 1990
Tonsillitis	JP	Takeda Pharmaceutical Co., Ltd.	01 Jan 1990

Developing

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Bacterial Infections	Phase 3	CN	Beijing Boshi Antai Technology Development Co., Ltd.	11 Sep 2015
Cystitis	Phase 3	CN	Beijing Boshi Antai Technology Development Co., Ltd.	04 Sep 2014
Dacryocystitis	Phase 3	CN	Beijing Boshi Antai Technology Development Co., Ltd.	04 Sep 2014
Hordeolum	Phase 3	CN	Beijing Boshi Antai Technology Development Co., Ltd.	04 Sep 2014
Laryngitis	Phase 3	CN	Beijing Boshi Antai Technology Development Co., Ltd.	04 Sep 2014
Lymphadenitis	Phase 3	CN	Beijing Boshi Antai Technology Development Co., Ltd.	04 Sep 2014
Otitis Media	Phase 3	CN	Beijing Boshi Antai Technology Development Co., Ltd.	04 Sep 2014
Perianal abscess	Phase 3	CN	Beijing Boshi Antai Technology Development Co., Ltd.	04 Sep 2014
Pyelonephritis	Phase 3	CN	Beijing Boshi Antai Technology Development Co., Ltd.	04 Sep 2014
Pyoderma	Discovery	CN	Beijing Boshi Antai Technology Development Co., Ltd.	04 Sep 2014