Untitled

Heimbach, Tycho; Oh, Doo-Man; Li, Lilian Y.; Forsberg, Markus; Savolainen, Jouko; Leppänen, Jukka; Matsunaga, Yasushi; Flynn, Gordon L.; Fleisher, David

doi:10.1023/a:1023827017224

Cited by 73 publications

(14 citation statements)

References 28 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…Oral tedizolid phosphate is converted into its active moiety, tedizolid, though apical alkaline phosphatases, which allows intestinal absorption 29. Tedizolid exhibits excellent bioavailability (about 92%), although lower values of 83%–86% have been reported in Chinese and Japanese patients 11.…”

Section: Methodsmentioning

confidence: 99%

<p>Tedizolid phosphate for the treatment of acute bacterial skin and skin-structure infections: an evidence-based review of its place in therapy</p>

Bassetti¹,

Castaldo²,

Carnelutti³

et al. 2019

View full text Add to dashboard Cite

Introduction Tedizolid phosphate is an oxazolidinone approved for the treatment of acute bacterial skin and skin-structure infections (ABSSSIs) and active against methicillin-resistant Staphylococcus aureus . Aims The objective of this article was to review the evidence for the efficacy and safety of tedizolid phosphate for the treatment of ABSSSI. Evidence review Approval of tedizolid phosphate for the treatment of ABSSSI was based on the results of two phase III randomized controlled trials, ESTABLISH-1 (NCT01170221) and ESTABLISH-2 (NCT01421511), comparing 6-day once-daily tedizolid vs 10-day twice-daily linezolid. In ESTABLISH-1, noninferiority was met with early clinical response rates of 79.5% and 79.4% in tedizolid and linezolid groups, respectively (difference 0.1%, 95% CI –6.1% to 6.2%, with a 10% noninferiority margin). In ESTABLISH-2, noninferiority was met with 85% and 83% rates of early clinical response in tedizolid and linezolid groups, respectively (difference 2.6%, 95% CI –3.0% to 8.2%). Pooled data from ESTABLISH-1 and ESTABLISH-2 indicated a lower frequency of thrombocytopenia in tedizolid-treated than in linezolid-treated patients. Conclusion Tedizolid offers the option of an intravenous to oral switch, allows once-daily administration, and presents lower risk of myelotoxicity when a 6-day course is used for the treatment of ABSSSI. Greater economic cost associated with this antibiotic could be offset by its shorter treatment duration and possibility of oral administration in routine clinical practice, although either sponsored or nonsponsored postmarketing observational experience remains essential for ultimately confirming the effectiveness and tolerability of tedizolid outside clinical trials.

show abstract

Section: Methodsmentioning

confidence: 99%

<p>Tedizolid phosphate for the treatment of acute bacterial skin and skin-structure infections: an evidence-based review of its place in therapy</p>

Bassetti¹,

Castaldo²,

Carnelutti³

et al. 2019

View full text Add to dashboard Cite

show abstract

“…HC, a 11β-hydroxyl compound corresponding chemically to 11β,17α,21-trihydroxypregn-4-ene-3,20-dione (formula C 21 H 30 O 5 ; molecular weight of 362.5 g/mol/l), is highly permeable with a gastrointestinal rate of absorption, without hepatic bioactivation, of about 93–96% for an oral dose of 20 mg. 43–45 After intravenous administration, the distribution phase of HC has an 8-min half-life, whereas the half-life of HC is 90 min after oral administration. 46 The absorption of HC is equivalent regardless of the route of administration (intravenous, intramuscular, gastric, sublingual).…”

Section: Standard Glucocorticoid Therapymentioning

confidence: 99%

Novel insights into glucocorticoid replacement therapy for pediatric and adult adrenal insufficiency

Oprea

Bonnet

Pollé

et al. 2019

Therapeutic Advances in Endocrinology

View full text Add to dashboard Cite

Adrenal insufficiency is defined as impaired adrenocortical hormone synthesis. According to its source, the deficit is classified as primary (adrenal steroidogenesis impairment), secondary (pituitary adrenocorticotropic hormone deficit) or tertiary (hypothalamic corticotropin-releasing hormone deficit). The management of adrenal insufficiency resides primarily in physiological replacement of glucocorticoid secretion. Standard glucocorticoid therapy is shrouded in several controversies. Along the difficulties arising from the inability to accurately replicate the pulsatile circadian cortisol rhythm, come the uncertainties of dose adjustment and treatment monitoring (absence of reliable biomarkers). Furthermore, side effects of inadequate replacement significantly hinder the quality of life of patients. Therefore, transition to circadian hydrocortisone therapy gains prominence. Recent therapeutic advancements consist of oral hydrocortisone modified-release compounds (immediate, delayed and sustained absorption formulations) or continuous subcutaneous hydrocortisone infusion. In addition to illustrating the current knowledge on conventional glucocorticoid regimens, this review outlines the latest research outcomes. We also describe the management of pediatric patients and suggest a novel strategy for glucocorticoid replacement therapy in adults.

show abstract

“…These include salt formation, determination of the proper polymorph, introduction of a prodrug moiety, utilization of co-solvents, cocrystals, or surfactants. [1,[3][4][5][6] A useful way to enhance water solubility is to form suitable bioisosteres via an introduction of a heteroatom into a molecule. For instance, the decrease of log P from 3.36 to 0.77 can be achieved by replacing the CH 2 (X) group for oxygen atom in the RCH 2 -X-CH 2 R segment.…”

Section: Introductionmentioning

confidence: 99%

Polysubstituted Pyrimidines as Potent Inhibitors of Prostaglandin E₂ Production: Increasing Aqueous Solubility

et al. 2021

View full text Add to dashboard Cite

Water solubility is one of the key features of potential therapeutic agents. In order to enhance the low water solubility of the parent 5-butyl-4-(4-methoxyphenyl)-6-phenylpyrimidin-2amine, a potent inhibitor of prostaglandin E 2 (PGE 2 ) production, we synthesized and evaluated a new series of derivatives in which the butyl group at the C5 position of the pyrimidine ring was replaced with a less lipophilic substituent, preferably with a hydrophilic aliphatic moiety. Except for the 5-cyanopyrimidine derivative, all target compounds exhibited increased (2.7-87fold) water solubility relative to the parent compound.Although nontoxic in mouse peritoneal cells, the prepared compounds were either equipotent or weaker inhibitors of PGE 2 production than the parent compound. The most promising compound from the series was found to be the 5-(2,5,8,11tetraoxadodecyl)pyrimidine derivative (with three polyethylene glycol units at the C5 position), which exhibited 32-fold higher water solubility and only slightly weaker inhibitory activity (22 % of remaining PGE 2 production) compared with the parent compound (15 % of remaining PGE 2 production).

show abstract

Untitled

Cited by 73 publications

References 28 publications

<p>Tedizolid phosphate for the treatment of acute bacterial skin and skin-structure infections: an evidence-based review of its place in therapy</p>

<p>Tedizolid phosphate for the treatment of acute bacterial skin and skin-structure infections: an evidence-based review of its place in therapy</p>

Novel insights into glucocorticoid replacement therapy for pediatric and adult adrenal insufficiency

Polysubstituted Pyrimidines as Potent Inhibitors of Prostaglandin E₂ Production: Increasing Aqueous Solubility

Contact Info

Product

Resources

About

Untitled

Cited by 73 publications

References 28 publications

<p>Tedizolid phosphate for the treatment of acute bacterial skin and skin-structure infections: an evidence-based review of its place in therapy</p>

<p>Tedizolid phosphate for the treatment of acute bacterial skin and skin-structure infections: an evidence-based review of its place in therapy</p>

Novel insights into glucocorticoid replacement therapy for pediatric and adult adrenal insufficiency

Polysubstituted Pyrimidines as Potent Inhibitors of Prostaglandin E2 Production: Increasing Aqueous Solubility

Contact Info

Product

Resources

About

Polysubstituted Pyrimidines as Potent Inhibitors of Prostaglandin E₂ Production: Increasing Aqueous Solubility