keyword
MENU ▼
Read by QxMD icon Read
search

Solithromycin

keyword
https://www.readbyqxmd.com/read/29107789/overcoming-the-challenges-of-low-drug-solubility-in-the-intravenous-formulation-of-solithromycin
#1
Daniel Evans, Samuel Yalkowsky, Sara Wu, David Pereira, Prabha Fernandes
Solithromycin is a fluoro-ketolide (a fourth-generation macrolide) antibiotic that has been undergoing clinical trials for the treatment of community acquired bacterial pneumonia. In this study, development of the tri-amino acid buffered solithromycin intravenous (IV) formulation was performed to minimize the occurrence of infusion associated local adverse events (infusion site pain or phlebitis) observed in patients who received the tartaric acid buffered IV formulation with a lower buffered capacity during Phase I clinical trials...
October 28, 2017: Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/29068158/development-of-an-adult-physiologically-based-pharmacokinetic-model-of-solithromycin-in-plasma-and-epithelial-lining-fluid
#2
Sara N Salerno, Andrea Edginton, Michael Cohen-Wolkowiez, Christoph P Hornik, Kevin M Watt, Brian D Jamieson, Daniel Gonzalez
Solithromycin is a fluoroketolide antibiotic under investigation for community-acquired bacterial pneumonia (CABP). We developed a whole-body physiologically based pharmacokinetic (PBPK) model for solithromycin in adults using PK-Sim and MoBi version 6.2, which incorporated time-dependent CYP3A4 auto-inhibition. The model was developed and evaluated using plasma and epithelial lining fluid (ELF) concentration data from 100 healthy subjects and 22 patients with CABP (1,966 plasma, 30 ELF samples). We performed population simulations and calculated the number of observations falling outside the 90% prediction interval...
October 25, 2017: CPT: Pharmacometrics & Systems Pharmacology
https://www.readbyqxmd.com/read/28979150/mycoplasma-genitalium-infections-current-treatment-options-and-resistance-issues
#3
REVIEW
Sunil Sethi, Kamran Zaman, Neha Jain
Mycoplasma genitalium is one of the important causes of non-gonococcal urethritis. Rising incidence and emerging antimicrobial resistance are a major concern these days. The poor clinical outcomes with doxycycline therapy led to the use of azithromycin as the primary drug of choice. Single-dose azithromycin regimen over a period of time was changed to extended regimen following studies showing better clinical cures and less risk of resistance development. However, emerging macrolide resistance, either due to transmission of resistance or drug pressure has further worsened the management of this infection...
2017: Infection and Drug Resistance
https://www.readbyqxmd.com/read/28838073/new-horizons-in-mycoplasma-genitalium-treatment
#4
REVIEW
Catriona S Bradshaw, Jorgen S Jensen, Ken B Waites
Mycoplasmagenitalium is an important sexually transmitted pathogen responsible for both male and female genital tract disease. Appreciation of its significance in human disease has been hampered by its slow growth in culture, difficulty in isolating it, and lack of commercial molecular-based tests for rapid detection. Comparatively few in vitro data on antimicrobial susceptibility are available due to the scarcity of clinical isolates and difficulty in performing susceptibility tests to determine minimum inhibitory concentrations for M...
July 15, 2017: Journal of Infectious Diseases
https://www.readbyqxmd.com/read/28762839/new-treatment-options-for-lower-respiratory-tract-infections
#5
Bela Kocsis, Dora Szabo
Community-acquired pneumonia (CAP) and acute exacerbation of chronic obstructive pulmonary disease (AECOPD) are among the most frequent lower respiratory tract infections (LRTIs). They represent an increased morbidity and mortality rate in adults. Areas covered: This review describes recent advances regarding solithromycin, zabofloxacin and delafoxacin antibacterial agents that have been recently developed for treatment of CAP and in AECOPD. All of them have been introduced into phase III clinical trials. We will be summarising chemical structures, pharmacokinetics, antibacterial efficacy and toxicity of these agents...
September 2017: Expert Opinion on Pharmacotherapy
https://www.readbyqxmd.com/read/28668674/16-membered-macrolide-antibiotics-a-review
#6
REVIEW
Biljana Arsic, Jill Barber, Ana Čikoš, Milan Mladenovic, Nevena Stankovic, Predrag Novak
Mainly used in veterinary medicine, the 16-membered macrolide antibiotics (e.g. tylosin A and josamycin) are much less studied than their 14- and 15-membered erythromycin-based cousins. Even though they share similar antibacterial profile (they are active primarily against Gram-positive and a limited range of Gram-negative organisms), the 16-membered macrolides show some advantages, including better gastrointestinal tolerance, lack of drug-drug interactions and activity against some resistant strains with additional interactions by extending the peptide tunnel reach...
June 28, 2017: International Journal of Antimicrobial Agents
https://www.readbyqxmd.com/read/28625123/role-of-the-n-acetylation-polymorphism-in-solithromycin-metabolism
#7
David W Hein, Mark A Doll
AIM: Solithromycin is a new macrolide antibiotic for the potential treatment of bacterial pneumonia. MATERIALS & METHODS: Solithromycin N-acetylation by human NAT1 and NAT2 was investigated following recombinant expression in yeast and in cryopreserved human hepatocytes from rapid, intermediate and slow acetylators. RESULTS: Solithromycin exhibited over twofold higher affinity for recombinant human NAT2 than NAT1. Apparent maximum velocities for the N-acetylation of solithromycin catalyzed by the NAT2 allozyme associated with rapid acetylators were significantly (p < 0...
June 2017: Pharmacogenomics
https://www.readbyqxmd.com/read/28598693/managing-community-acquired-pneumonia-in-the-elderly-the-next-generation-of-pharmacotherapy-on-the-horizon
#8
REVIEW
B Amalakuhan, K L Echevarria, M I Restrepo
Community acquired pneumonia (CAP) is associated with high rates of morbidity and mortality, especially among the elderly. Antibiotic treatment for CAP in the elderly is particularly challenging for many reasons, including compliance issues, immunosuppression, polypharmacy and antimicrobial resistance. There are few available antibiotics that are able to address these concerns. Areas covered: After a systematic review of the current literature, we describe seven novel antibiotics that are currently in advanced stages of development (phase 3 and beyond) and show promise for the treatment of CAP in those over the age of 65...
August 2017: Expert Opinion on Pharmacotherapy
https://www.readbyqxmd.com/read/28490220/solithromycin-cem-101-a-new-fluoroketolide-antibiotic-and-its-role-in-the-treatment-of-gonorrhea
#9
Alexandra M Mancuso, Mona A Gandhi, Judianne Slish
Solithromycin is a macrolide antibiotic that has undergone review for the treatment of community-acquired bacterial pneumonia. Solithromycin is also being investigated and has shown promise for the treatment of gonorrhea. With increasing antibiotic resistance, the development of novel antibiotics to combat infections is essential. The unique ribosome-binding stability of solithromycin and mild side effect profile make this a promising new antibiotic. This article will provide an overview on the mechanism of action, clinical efficacy, and safety of this drug for the treatment of gonorrhea...
January 1, 2017: Journal of Pharmacy Practice
https://www.readbyqxmd.com/read/28483717/surveillance-of-the-activity-of-solithromycin-cem-101-against-bacteria-from-respiratory-tract-infections
#10
Stephen Hawser, Ian Morrissey, Barbara Lemos, Kara Keedy, Prabhavathi Fernandes
The activity of solithromycin, a fourth-generation macrolide and novel fluoroketolide, was evaluated by determining its minimum inhibitory concentration (MIC) (via Clinical and Laboratory Standards Institute broth microdilution) against 2797 contemporary clinical respiratory tract isolates collected from North America, Europe, Asia-Pacific and other regions of the world in 2012-13. Solithromycin was very active against Streptococcus pneumoniae and Streptococcus pyogenes, with MIC90 of 0.25 and 0.12 µg/mL, respectively...
May 5, 2017: International Journal of Antimicrobial Agents
https://www.readbyqxmd.com/read/28432048/solithromycin-a-novel-ketolide-antibiotic
#11
REVIEW
Michael J Buege, Jack E Brown, Samuel L Aitken
PURPOSE: The pharmacology, pharmacokinetics, pharmacodynamics, antimicrobial activity, clinical safety, and current regulatory status of solithromycin are reviewed. SUMMARY: Solithromycin is a novel ketolide antibiotic developed for the treatment of community-acquired bacterial pneumonia (CABP). Its pharmacologic, pharmacokinetic, and pharmacodynamic properties provide activity against a broad range of intracellular organisms, including retained activity against pathogens displaying various mechanisms of macrolide resistance...
June 15, 2017: American Journal of Health-system Pharmacy: AJHP
https://www.readbyqxmd.com/read/28314920/-new-antibiotics-standstill-or-progress
#12
J Rademacher, T Welte
The development of resistance to antibiotics has been ignored for a long time. But nowadays, increasing resistance is an important topic. For a decade no new antibiotics had been developed and it is not possible to quickly close this gap of new resistance and no new drugs. This work presents six new antibiotics (ceftaroline, ceftobiprole, solithromycin, tedizolid, ceftolozane/tazobactam, ceftazidime/avibactam). In part, only expert opinions are given due to lack of study results.The two 5th generation cephalosporins ceftaroline and ceftobiprole have beside their equivalent efficacy to ceftriaxone (ceftaroline) and cefipim (ceftobiprole) high activity against MRSA...
April 2017: Medizinische Klinik, Intensivmedizin und Notfallmedizin
https://www.readbyqxmd.com/read/28267725/solithromycin-rejection-chills-antibiotic-sector
#13
Brian Owens
No abstract text is available yet for this article.
March 7, 2017: Nature Biotechnology
https://www.readbyqxmd.com/read/27909995/solithromycin-a-novel-fluoroketolide-for-the-treatment-of-community-acquired-bacterial-pneumonia
#14
REVIEW
George G Zhanel, Erika Hartel, Heather Adam, Sheryl Zelenitsky, Michael A Zhanel, Alyssa Golden, Frank Schweizer, Bala Gorityala, Philippe R S Lagacé-Wiens, Andrew J Walkty, Alfred S Gin, Daryl J Hoban, Joseph P Lynch, James A Karlowsky
Solithromycin is a novel fluoroketolide developed in both oral and intravenous formulations to address increasing macrolide resistance in pathogens causing community-acquired bacterial pneumonia (CABP). When compared with its macrolide and ketolide predecessors, solithromycin has several structural modifications which increase its ribosomal binding and reduce its propensity to known macrolide resistance mechanisms. Solithromycin, like telithromycin, affects 50S ribosomal subunit formation and function, as well as causing frame-shift errors during translation...
December 2016: Drugs
https://www.readbyqxmd.com/read/27899792/nature-nurtures-the-design-of-new-semi-synthetic-macrolide-antibiotics
#15
REVIEW
Prabhavathi Fernandes, Evan Martens, David Pereira
Erythromycin and its analogs are used to treat respiratory tract and other infections. The broad use of these antibiotics during the last 5 decades has led to resistance that can range from 20% to over 70% in certain parts of the world. Efforts to find macrolides that were active against macrolide-resistant strains led to the development of erythromycin analogs with alkyl-aryl side chains that mimicked the sugar side chain of 16-membered macrolides, such as tylosin. Further modifications were made to improve the potency of these molecules by removal of the cladinose sugar to obtain a smaller molecule, a modification that was learned from an older macrolide, pikromycin...
May 2017: Journal of Antibiotics
https://www.readbyqxmd.com/read/27798210/solithromycin-a-novel-macrolide-does-not-prolong-cardiac-repolarization-a-randomized-three-way-crossover-study-in-healthy-subjects
#16
RANDOMIZED CONTROLLED TRIAL
Borje Darpo, Philip T Sager, Prabhavathi Fernandes, Brian D Jamieson, Kara Keedy, Meijian Zhou, David Oldach
BACKGROUND: Macrolide antibiotics may cause QT prolongation. OBJECTIVES: To study the QT effect of a novel macrolide, solithromycin. METHODS: This was a thorough QT study with a three-way crossover design performed in healthy male and female subjects to evaluate the ECG effects of a novel macrolide, solithromycin. Forty-eight subjects were randomized to receive 800 mg of intravenous (iv) solithromycin, 400 mg of oral moxifloxacin and placebo in three separate treatment periods...
February 2017: Journal of Antimicrobial Chemotherapy
https://www.readbyqxmd.com/read/27753516/solithromycin-for-the-treatment-of-community-acquired-bacterial-pneumonia
#17
Diego Viasus, Oscar Ramos, Leidy Ramos, Antonella F Simonetti, Jordi Carratalà
Community-acquired pneumonia is a major public health problem worldwide. In recent years, there has been an increase in the frequency of resistance to the antimicrobials such as β-lactams or macrolides which have habitually been used against the causative pathogens. Solithromycin, a next-generation macrolide, is the first fluoroketolide with activity against most of the frequently isolated bacteria in community-acquired pneumonia, including typical and atypical bacteria as well as macrolide-resistant Streptococcus pneumoniae...
January 2017: Expert Review of Respiratory Medicine
https://www.readbyqxmd.com/read/27725229/in-vitro-activity-of-solithromycin-against-anaerobic-bacteria-from-the-normal-intestinal-microbiota
#18
Andrej Weintraub, Mamun-Ur Rashid, Carl Erik Nord
Solithromycin is a novel fluoroketolide with high activity against bacteria associated with community-acquired respiratory tract infections as well as gonorrhea. However, data on the activity of solithromycin against anaerobic bacteria from the normal intestinal microbiota are scarce. In this study, 1024 Gram-positive and Gram-negative anaerobic isolates from the normal intestinal microbiota were analyzed for in-vitro susceptibility against solithromycin and compared to azithromycin, amoxicillin/clavulanic acid, ceftriaxone, metronidazole and levofloxacin by determining the minimum inhibitory concentration (MIC)...
December 2016: Anaerobe
https://www.readbyqxmd.com/read/27646933/current-and-upcoming-pharmacotherapy-for-non-alcoholic-fatty-liver-disease
#19
REVIEW
Yaron Rotman, Arun J Sanyal
Given the high prevalence and rising incidence of non-alcoholic fatty liver disease (NAFLD), the absence of approved therapies is striking. Although the mainstay of treatment of NAFLD is weight loss, it is hard to maintain, prompting the need for pharmacotherapy as well. A greater understanding of disease pathogenesis in recent years was followed by development of new classes of medications, as well as potential repurposing of currently available agents. NAFLD therapies target four main pathways. The dominant approach is targeting hepatic fat accumulation and the resultant metabolic stress...
January 2017: Gut
https://www.readbyqxmd.com/read/27620481/in-vitro-activity-of-solithromycin-against-bordetella-pertussis-an-emerging-respiratory-pathogen
#20
Dwight J Hardy, David Vicino, Prabhavathi Fernandes
There has been an increase in the number of pertussis cases reported since the introduction of the acellular pertussis vaccine. While children that present with pertussis have a characteristic whooping cough, adults can simply have a persistent, nonspecific cough and remain undiagnosed. Macrolide antibiotics, such as azithromycin, are the currently recommended treatment for pertussis. Solithromycin is a new macrolide and the first fluoroketolide with broad activity against a wide spectrum of bacterial pathogens and has completed clinical development for community-acquired bacterial pneumonia...
December 2016: Antimicrobial Agents and Chemotherapy
keyword
keyword
42067
1
2
Fetch more papers »
Fetching more papers... Fetching...
Read by QxMD. Sign in or create an account to discover new knowledge that matter to you.
Remove bar
Read by QxMD icon Read
×

Search Tips

Use Boolean operators: AND/OR

diabetic AND foot
diabetes OR diabetic

Exclude a word using the 'minus' sign

Virchow -triad

Use Parentheses

water AND (cup OR glass)

Add an asterisk (*) at end of a word to include word stems

Neuro* will search for Neurology, Neuroscientist, Neurological, and so on

Use quotes to search for an exact phrase

"primary prevention of cancer"
(heart or cardiac or cardio*) AND arrest -"American Heart Association"