Delving into the Latest Updates on Arbekacin Sulfate with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

ABK, Arbekacin, Arbekacin sulfate (JP17)

+ [5]

Target

30S subunit

Mechanism

30S subunit inhibitors(30S ribosomal subunit inhibitors)

Therapeutic Areas

Infectious DiseasesRespiratory DiseasesOther Diseases

Active Indication

Hemorrhagic SepticemiaPneumonia

Inactive Indication

VABP

Originator Organization

Meiji Seika Pharma Co., Ltd.

Active Organization

Meiji Seika Pharma Co., Ltd.

Inactive Organization-

Drug Highest PhaseApproved

First Approval Date

JP (28 Sep 1990),

Hemorrhagic SepticemiaPneumonia

Regulation-

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Structure

Molecular FormulaC22H44N6O10

InChIKeyMKKYBZZTJQGVCD-XTCKQBCOSA-N

CAS Registry51025-85-5

View All Structures (2)

This study is a randomized, open-label phase I study. The primary objective of this study is to assess the pharmacokinetic (PK) profile of ME1100 in subjects with mechanically ventilated bacterial pneumonia (MVBP). The secondary objective of this study is to assess the safety and tolerability of ME1100 for the treatment of subjects with MVBP to assess the safety and tolerability of ME1100.

Start Date01 Sep 2015

Sponsor / Collaborator

Meiji Seika Pharma Co., Ltd.

NCT01961830 / CompletedPhase 1

An Open-label, Single Dose Study to Assess Intrapulmonary Pharmacokinetics of ME1100 Inhalation Solution Administered to Healthy Volunteers

This is a single-center, open-label, single-dose study. The primary objective is to determine Epithelial Lining Fluid (ELF) levels of ME1100 after a single orally inhaled dose. The secondary objectives are to determine systemic exposure to inhaled ME1100 and to assess tolerability and safety of a single dose of ME1100 inhalation solution.

Start Date01 Sep 2013

Sponsor / Collaborator

Meiji Seika Pharma Co., Ltd.

JPRN-jRCT1091220134 / CompletedPhase 2IIT

Phase II study of nonsense readthrough compound NPC-14 (Arbekacin sulfate) to explore safety, tolerability, and efficacy in Duchenne muscular dystrophy patients (NORTH POLE DMD study) - NORTH POLE DMD study

Start Date14 Aug 2013

Sponsor / Collaborator-

100 Clinical Results associated with Arbekacin Sulfate

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100 Translational Medicine associated with Arbekacin Sulfate

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100 Patents (Medical) associated with Arbekacin Sulfate

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454

Literatures (Medical) associated with Arbekacin Sulfate

31 May 2024·The Journal of Biochemistry

Direct visualization of ribosomes in the cell-free system revealed the functional evolution of aminoglycoside

Article

Author: Asano, Kosuke ; Suzuki, Masato ; Tanaka, Yoshikazu ; Tomono, Junta ; Igarashi, Masayuki ; Takahashi, Yoshiaki ; Chiashi, Takuma ; Yokoyama, Takeshi

AbstractThe rapid emergence of multi-drug-resistant bacteria has raised a serious public health concern. Therefore, new antibiotic developments have been highly desired. Here, we propose a new method to visualize antibiotic actions on translating ribosomes in the cell-free system under macromolecular crowding conditions by cryo-electron microscopy, designated as the DARC method: the Direct visualization of Antibiotic binding on Ribosomes in the Cell-free translation system. This new method allows for acquiring a more comprehensive understanding of the mode of action of antibiotics on the translation inhibition without ribosome purification. Furthermore, with the direct link to biochemical analysis at the same condition as cryo-EM observation, we revealed the evolution of 2-DOS aminoglycosides from dibekacin (DBK) to arbekacin (ABK) by acquiring the synthetic tailored anchoring motif to lead to stronger binding affinity to ribosomes. Our cryo-EM structures of DBK and ABK bound ribosomes in the cell-free environment clearly depicted a synthetic tailored γ-amino-α-hydroxybutyryl (HABA) motif formed additional interactions with the ribosome enhancing antibiotic bindings. This new approach would be valuable for understanding the function of antibiotics for more efficient drug development.

06 Feb 2024·ACS Omega

Experimental Determination of the pK_a Values of Clinically Relevant Aminoglycoside Antibiotics: Toward Establishing pK_a─Activity Relationships

Article

Author: Gysin, Marina ; Crich, David ; Hobbie, Sven N. ; Haldimann, Klara ; Muhamadejevs, Ruslans ; Jaudzems, Kristaps

Investigating the relationship between individual pK_a values and the efficacy of aminoglycosides is essential for the development of more effective and targeted therapies. In this work, we measured the pK_a values for individual amino groups of the six clinically relevant aminoglycoside antibiotics gentamicin, tobramycin, amikacin, arbekacin, plazomicin, and apramycin using ¹⁵N-¹H heteronuclear multiple-bond correlation and ¹H NMR experiments. For arbekacin and plazomicin, the pK_a values are reported for the first time. These pK_a values were used to calculate the net charges of the aminoglycosides and the protonation levels of amino groups under various pH conditions. The results were analyzed in relation to the mode of interaction and inhibition to establish pK_a relationships for rRNA binding, inhibitory activity, and the pH dependence of the uptake into bacterial cells.

27 Nov 2023·Cureus

A Comparison of the Minimum Inhibitory Concentration of Antibiotics in Staphylococcus Species Isolated From Orthopedic and Respiratory Medicine Infections

Article

Author: Higashihira, Shota ; Yukizawa, Yohei ; Inaba, Yutaka ; Kobayashi, Naomi ; Takagawa, Shu ; Kumagai, Ken ; Choe, Hyonmin ; Tomoyama, Akito ; Ike, Hiroyuki

INTRODUCTIONAntibiotic susceptibility is very important for the successful treatment of orthopedic infections, particularly for implant-related infections. While the minimum inhibitory concentrations (MICs) of Staphylococcus species were well investigated for the isolates from the respiratory tract, investigations for orthopedic pathogens are very limited. We investigated the antibiotic MIC values of Staphylococcus species isolated from orthopedic infections and compared them with those of respiratory medicine isolates used as a control.METHODSThe MICs of vancomycin (VCM), arbekacin (ABK), teicoplanin (TEIC), linezolid (LZD), and rifampicin (RFP) of a total of consecutive 259 (89 orthopedic and 170 respiratory) Staphylococcus speciesisolated in our laboratory from January 2013 to July 2016 were retrospectively reviewed. Differences between the MICs of each antibiotic in orthopedic and respiratory samples were determined.RESULTSThe number of methicillin-sensitive Staphylococcus aureus (MSSA) with a VCM MIC of <0.5 μg/mL among respiratory isolates was significantly higher than that among orthopedic isolates, while those with a MIC of 2 μg/mL were significantly lower (P = 0.0078). The proportion of methicillin-resistant coagulase-negative staphylococci (MRCNS) isolates with a VCM MIC of 2 μg/mL was significantly higher in orthopedic samples than that of methicillin-resistant Staphylococcus aureus (MRSA) (P < 0.001) in respiratory isolates. The proportion of MRCNS orthopedic isolates with an RFP MIC of >2 μg/mL was significantly higher (P = 0.0058) than that of other orthopedic staphylococci.CONCLUSIONSThe VCM MICs of Staphylococcus species from orthopedic infections were higher than those of respiratory samples, particularly MRCNS from implant-related samples.

100 Deals associated with Arbekacin Sulfate

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