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Arbekacin
Published in Anton C. de Groot, Monographs in Contact Allergy, 2021
Arbekacin is a semisynthetic aminoglycoside antibiotic derived from dibekacin with activity against both grampositive and gram-negative bacteria. Arbekacin is most commonly used in the treatment of multi-resistant bacterial infections such as methicillin-resistant Staphylococcus aureus (MRSA). In pharmaceutical products, arbekacin is employed as arbekacin sulfate (CAS number 104931-87-5, EC number not available, molecular formula C22H46N6O14S) (1).
Comparing the pharmacokinetics and organ/tissue distribution of anti-methicillin-resistant Staphylococcus aureus agents using a rat model of sepsis
Published in Xenobiotica, 2022
Shinji Kobuchi, Naoya Kanda, Taichi Okumi, Yuma Kano, Himawari Tachi, Yukako Ito, Toshiyuki Sakaeda
For patients infected with methicillin-resistant Staphylococcus aureus (MRSA), glycopeptide vancomycin (VCM) is empirically the first-line drug; however, various anti-MRSA agents, including aminoglycoside arbekacin (ABK), oxazolidinone linezolid (LZD), and lipopeptide daptomycin (DAP) are available. VCM is also prescribed for treating sepsis or septic shock because of its extensive clinical use. However, dose modification is essential to achieve effective plasma VCM concentrations with minimal side effects, such as renal failure. Clinical studies have shown that decreased susceptibility of MRSA to VCM is associated with treatment failure and poor prognosis (Holmes et al. 2012; Britt et al. 2017; Egi et al. 2021; Hort et al. 2021). Therefore, pharmacokinetic and pharmacodynamic/toxicodynamic information on drugs other than VCM is required to expand the treatment selection for sepsis.
The discovery and development of transmembrane serine protease 2 (TMPRSS2) inhibitors as candidate drugs for the treatment of COVID-19
Published in Expert Opinion on Drug Discovery, 2022
Christiana Mantzourani, Sofia Vasilakaki, Velisaria-Eleni Gerogianni, George Kokotos
Baby et al. used the human plasma kallikrein (PDB ID: 5TJX), identified with BLAST tool, as the template to build the homology model of TMPRSS2 protein. Schrödinger Prime Module was employed for the construction of the model, which further modified with Refine Loops software and evaluated accordingly [103]. Schrödinger’s High Throughput Virtual Screening was employed to dock ~2800 FDA-acquiesced molecules in TMPRSS2 and ACE2, for which the receptor grid was created based on the co-crystalized ligand. Their calculations resulted in a number of drugs that demonstrated a promising binding mode, including valrubicin, lopinavir, fleroxacin, alvimopan, arbekacin, and dequalinium. For these compounds, molecular dynamics in Maestro Desmond was accomplished and suggested a superiority of valrubicin and lopinavir in their formation of a stable complex with the proteins. The main interactions formed in these complexes were hydrophobic and hydrophilic with residues such as Trp461, Trp461, Lys300.