Safety, Tolerability, Pharmacokinetics and Pharmacodynamics of Multiple Rising Oral Doses (5 to 100 mg q.d. for 14 Days) of BI 135585 XX in Patients With Type 2 Diabetes Mellitus (Randomized, Double-blind Placebo-controlled Within Dose Groups)

The objective of this study is to investigate safety, tolerability, pharmacokinetics and pharmacodynamics of BI 135585 XX following multiple dose administration over 14 days

开始日期2011-02-01

申办/合作机构

Boehringer Ingelheim GmbH

NCT01291732 / Completed临床1期

Safety, Tolerability, Pharmacokinetics and Pharmacodynamics of Single Rising Oral Doses (12.5 mg, 50 mg, 200 mg) of BI 135585 XX (Tablet) in Chinese and Japanese Healthy Male Volunteers (Randomised, Double-blind,Placebo-controlled Within Dose Groups)

The Aim of the study is to evaluate safety, tolerability, pharmacokinetics and pharmacodynamics in Asian healthy males administered a single dose of BI 135585.

开始日期2011-02-01

申办/合作机构

Boehringer Ingelheim GmbH

100 项与 BI-135585 相关的临床结果

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100 项与 BI-135585 相关的转化医学

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100 项与 BI-135585 相关的专利（医药）

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项与 BI-135585 相关的文献（医药）

2017-07-01·Bioorganic & medicinal chemistry3区 · 医学

Discovery of BI 135585, an in vivo efficacious oxazinanone-based 11β hydroxysteroid dehydrogenase type 1 inhibitor

3区 · 医学

Article

作者: Bukhtiyarov, Yuri ; Meng, Shi ; Zhao, Yi ; Guo, Rong ; Leftheris, Katerina ; Krosky, Paula M ; Zhao, Wei ; Tice, Colin M ; Lala, Deepak ; Zhuang, Linghang ; Claremon, David A ; Howard, Lamont ; Panemangalore, Reshma ; Johnson, Judith A ; Gregg, Richard ; McKeever, Brian M ; McGeehan, Gerard M ; Himmelsbach, Frank ; Singh, Suresh B ; Schauerte, Heike ; Hamilton, Bradford ; Xu, Zhenrong ; Ye, Yuan-Jie ; Guo, Joan ; Schuler-Metz, Annette ; Kruk, Barbara A ; Cacatian, Salvacion ; Lindblom, Peter

A potent, in vivo efficacious 11β hydroxysteroid dehydrogenase type 1 (11β HSD1) inhibitor (11j) has been identified. Compound 11j inhibited 11β HSD1 activity in human adipocytes with an IC₅₀ of 4.3nM and in primary human adipose tissue with an IC₈₀ of 53nM. Oral administration of 11j to cynomolgus monkey inhibited 11β HSD1 activity in adipose tissue. Compound 11j exhibited >1000× selectivity over other hydroxysteroid dehydrogenases, displays desirable pharmacodynamic properties and entered human clinical trials in 2011.

2015-01-01·European journal of pharmacology3区 · 医学

Pharmacological characterization of the selective 11β-hydroxysteroid dehydrogenase 1 inhibitor, BI 135585, a clinical candidate for the treatment of type 2 diabetes

3区 · 医学

Article

作者: Guo, Rong ; Krosky, Paula ; Schuler-Metz, Annette ; Nar, Herbert ; Hamilton, Bradford S ; McGeehan, Gerard M ; Zhuang, Linghang ; Himmelsbach, Frank ; Meng, Shi ; Zhao, Yi ; Claremon, David A ; Guo, Joan ; Lala, Deepak S

To combat the increased morbidity and mortality associated with the developing diabetes epidemic new therapeutic interventions are desirable. Inhibition of intracellular cortisol generation from cortisone by blocking 11β-hydroxysteroid dehydrogenase 1 (11β-HSD1) has been shown to ameliorate the risk factors associated with the metabolic syndrome. A challenge in developing 11β-HSD1 inhibitors has been the species selectivity of small molecules, as many compounds are primate specific. Here we describe our strategy to identify potent selective 11β-HSD1 inhibitors while ensuring target engagement in key metabolic tissues, liver and fat. This strategy enabled the identification of the clinical candidate, BI 135585.

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