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Original Research

Clinical profile of the functionally selective glucocorticoid receptor agonist BI 653048 in healthy male subjects

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Pages 489-496 | Received 03 Dec 2018, Accepted 22 Mar 2019, Published online: 09 Apr 2019

References

  • Singh JA , Saag KG, Bridges SL Jr., et al. 2015 American College of Rheumatology guideline for the treatment of rheumatoid arthritis. Arthritis Rheumatol. 2016;68(1):1–26.
  • Gordon C, Amissah-Arthur MB, Gayed M, et al. The British Society for Rheumatology guideline for the management of systemic lupus erythematosus in adults. Rheumatology (Oxford). 2018;57(1):e1–e45.
  • Gomollon F, Dignass A, Annese V, et al. 3rd European Evidence-Based Consensus on the diagnosis and management of Crohn‘s disease 2016: part 1: diagnosis and medical management. J Crohns Colitis. 2017;11(1):3–25.
  • Weinstein RS. Clinical practice. Glucocorticoid-induced bone disease. N Engl J Med. 2011;365(1):62–70.
  • Clark AR, Belvisi MG. Maps and legends: the quest for dissociated ligands of the glucocorticoid receptor. Pharmacol Ther. 2012;134(1):54–67.
  • Reichardt HM , Kaestner KH, Tuckermann J, et al. DNA binding of the glucocorticoid receptor is not essential for survival. Cell. 1998;93(4):531–541.
  • Schacke H , Schottelius A, Docke WD, et al. Dissociation of transactivation from transrepression by a selective glucocorticoid receptor agonist leads to separation of therapeutic effects from side effects. Proc Natl Acad Sci USA. 2004;101(1):227–232.
  • Desmet SJ , De Bosscher K. Glucocorticoid receptors: finding the middle ground. J Clin Invest. 2017;127(4):1136–1145.
  • Strehl C , van der Goes MC, Bijlsma JW, et al. Glucocorticoid-targeted therapies for the treatment of rheumatoid arthritis. Expert Opin Investig Drugs. 2017;26(2):187–195.
  • Stock T, Fleishaker D, Wang X, et al. Improved disease activity with fosdagrocorat (PF-04171327), a partial agonist of the glucocorticoid receptor, in patients with rheumatoid arthritis: a phase 2 randomized study. Int J Rheum Dis. 2017;20(8):960–970.
  • ZK-245186 . ClinicalTrials.gov [cited 2018 Mar 27]. Available from: https://clinicaltrials.gov/ct2/results?cond=&term=ZK-245186+&cntry1=&state1=&recrs=
  • Wigger-Alberti W , Williams R, von Mackensen YL, et al. Comparison of occlusive and open application in a psoriasis plaque test design, exemplarily using investigations of mapracorat 0.1% ointment versus vehicle and reference drugs. Skin Pharmacol Physiol. 2017;30(2):102–114.
  • Riether D , Harcken C, Razavi H, et al. Nonsteroidal dissociated glucocorticoid agonists containing azaindoles as steroid A-ring mimetics. J Med Chem. 2010;53(18):6681–6698.
  • Harcken C, Riether D, Kuzmich D, et al. Identification of highly efficacious glucocorticoid receptor agonists with a potential for reduced clinical bone side effects. J Med Chem. 2014;57(4):1583–1598.
  • Harcken C, Riether D, Liu P, et al. Optimization of drug-like properties of nonsteroidal glucocorticoid mimetics and identification of a clinical candidate. ACS Med Chem Lett. 2014;5(12):1318–1323.

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