Alexander Treiber
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View article: Second-line temozolomide in first recurrent MGMT-methylated glioblastoma after lomustine/temozolomide: Efficacy and safety
Second-line temozolomide in first recurrent MGMT-methylated glioblastoma after lomustine/temozolomide: Efficacy and safety Open
Background The optimal salvage therapy for recurrent MGMT-methylated glioblastoma (GBM), IDH wildtype, remains undefined. While lomustine is often used in clinical trials and considered standard-of-care, cumulative toxicity precludes its u…
View article: Evaluating the efficacy of the selective orexin 1 receptor antagonist nivasorexant in an animal model of binge‐eating disorder
Evaluating the efficacy of the selective orexin 1 receptor antagonist nivasorexant in an animal model of binge‐eating disorder Open
Objective Test the efficacy of the selective orexin 1 receptor (OX1R) antagonist (SO1RA) nivasorexant in an animal model of binge‐eating disorder (BED) and study its dose–response relationship considering free brain concentrations and calc…
View article: The metabolism of the orexin-1 selective receptor antagonist nivasorexant
The metabolism of the orexin-1 selective receptor antagonist nivasorexant Open
Nivasorexant was the first orexin-1 selective receptor antagonist entering clinical development. Despite encouraging preclinical evidence in animal models, a proof-of-concept trial in binge-eating patients recently failed to demonstrate it…
View article: Pyrazole derivatives as selective orexin-2 receptor antagonists (2-SORA): synthesis, structure–activity–relationship, and sleep-promoting properties in rats
Pyrazole derivatives as selective orexin-2 receptor antagonists (2-SORA): synthesis, structure–activity–relationship, and sleep-promoting properties in rats Open
Medicinal chemistry efforts starting from the GPCR agonist HTS hit 1 led to the discovery of the potent, selective, brain-penetrating, orally active orexin 2 receptor antagonists 43 that induced sleep in rats.
View article: Effect of nivasorexant (<scp>ACT</scp>‐539313), a selective orexin‐1‐receptor antagonist, on multiple cytochrome <scp>P450</scp> probe substrates in vitro and in vivo using a cocktail approach in healthy subjects
Effect of nivasorexant (<span>ACT</span>‐539313), a selective orexin‐1‐receptor antagonist, on multiple cytochrome <span>P450</span> probe substrates in vitro and in vivo using a cocktail approach in healthy subjects Open
Nivasorexant, a selective orexin‐1‐receptor antagonist, has recently been assessed in the treatment of humans with binge‐eating disorder. Herein, the inhibitory potential of nivasorexant on cytochromes P450 (CYPs) 2C9, 2C19, and 3A4 was ev…
View article: Front Cover: The Quest for the Best Dual Orexin Receptor Antagonist (Daridorexant) for the Treatment of Insomnia Disorders (ChemMedChem 23/2020)
Front Cover: The Quest for the Best Dual Orexin Receptor Antagonist (Daridorexant) for the Treatment of Insomnia Disorders (ChemMedChem 23/2020) Open
The Front Cover illustrates a circadian rhythm accompanied by daridorexant, Idorsia′s dual orexin receptor antagonist (DORA), investigated for the treatment of insomnia. It represents the quest for a DORA that would provide the next-day be…
View article: The endothelin receptor antagonist macitentan for the treatment of pulmonary arterial hypertension: A cross‐species comparison of its cytochrome P450 induction pattern
The endothelin receptor antagonist macitentan for the treatment of pulmonary arterial hypertension: A cross‐species comparison of its cytochrome P450 induction pattern Open
The dual endothelin receptor antagonist macitentan was approved in 2013 for the treatment of pulmonary arterial hypertension. Macitentan is an inducer of cytochrome P450 expression in vivo in animal species but not in man. In rat and dog, …
View article: Cover Picture: Discovery of Highly Potent Dual Orexin Receptor Antagonists via a Scaffold‐Hopping Approach (ChemMedChem 19/2016)
Cover Picture: Discovery of Highly Potent Dual Orexin Receptor Antagonists via a Scaffold‐Hopping Approach (ChemMedChem 19/2016) Open
The front cover picture shows the successful application of a scaffold-hopping approach starting from the upper model structure and replacing the central core with different bicyclic diamine templates (some representative templates are dep…