Mapracorat

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Mapracorat
File:BOL-303242-X skeletal.svg
Systematic (IUPAC) name
(2R)-1,1,1-trifluoro-4-(5-fluoro-2,3-dihydro-1-benzofuran-7-yl)-4-methyl-2-[[(2-methylquinolin-5-yl)amino]methyl]pentan-2-ol
Clinical data
Routes of
administration		 Topical (ointment, eye drops)
Legal status
Legal status
  • Investigational
Identifiers
CAS Number 887375-26-0
ATC code none
PubChem CID 24795088
Chemical data
Formula C25H26F4N2O2
Molar mass 462.479 g/mol[[Script error: No such module "String".]]
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Mapracorat (code names BOL-303242-X, ZK 245186[1]) is an anti-inflammatory drug belonging to the experimental class of selective glucocorticoid receptor agonists (SEGRAs). It is in clinical trials for the topical treatment of atopic dermatitis[2] and inflammation following cataract surgery[3]. Preliminary investigation for the treatment of keratoconjunctivitis sicca has been conducted in cellular models.[1]

Clinical trials

Phase II clinical trials with mapracorat started in summer 2009. One trial is a dose finding study for an ointment against atopic dermatitis. It is testing concentrations of 0.01%, 0.03% and 0.1% versus placebo over four weeks; the total number of patients will be around 64. This trial is conducted by Intendis, a part of Bayer HealthCare Pharmaceuticals specialized on dermatology, and is expected to end sometime in 2010.[2] The other trial is evaluating an ophthalmic suspension for the treatment of inflammation following cataract surgery. Various concentrations and dosing schemes are tested versus placebo in about 550 patients. The study is conducted by Bausch & Lomb and will be running until December 2010.[3]

References

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  1. ↑ 1.0 1.1 Cavet, ME; Harrington, KL; Ward, KW; Zhang, JZ (2010). "Mapracorat, a novel selective glucocorticoid receptor agonist, inhibits hyperosmolar-induced cytokine release and MAPK pathways in human corneal epithelial cells". Molecular vision. 16: 1791–800. PMC 2932489 Freely accessible. PMID 20824100.  edit
  2. ↑ 2.0 2.1 ClinicalTrials.gov NCT00944632 Dose Escalation of Different Concentrations of ZK 245186 in Atopic Dermatitis
  3. ↑ 3.0 3.1 ClinicalTrials.gov NCT00905450 Evaluation of BOL-303242-X Versus Vehicle for the Treatment of Inflammation Following Cataract Surgery
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