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Mapracorat

From Wikipedia, the free encyclopedia
Type of selective glucocorticoid receptor agonist
Pharmaceutical compound
Mapracorat
Clinical data
Routes of
administration
Topical (ointment,eye drops)
ATC code
  • none
Legal status
Legal status
  • Investigational
Identifiers
  • (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
CAS Number
PubChemCID
ChemSpider
UNII
KEGG
CompTox Dashboard(EPA)
ECHA InfoCard100.217.969Edit this at Wikidata
Chemical and physical data
FormulaC25H26F4N2O2
Molar mass462.489 g·mol−1
3D model (JSmol)
  • c14OCCc4cc(F)cc1C(C)(C)CC(O)(C(F)(F)F)CNc(cccc2n3)c2ccc3C
  • InChI=1S/C25H26F4N2O2/c1-15-7-8-18-20(5-4-6-21(18)31-15)30-14-24(32,25(27,28)29)13-23(2,3)19-12-17(26)11-16-9-10-33-22(16)19/h4-8,11-12,30,32H,9-10,13-14H2,1-3H3/t24-/m1/s1 ☒N
  • Key:VJGFOYBQOIPQFY-XMMPIXPASA-N ☒N
 ☒NcheckY (what is this?)  (verify)

Mapracorat (INN, code namesBOL-303242-X,ZK-245186[1]) is ananti-inflammatory drug belonging to the experimental class ofselective glucocorticoid receptor agonists (SEGRAs). It is inclinical trials for the topical treatment ofatopic dermatitis,[2] inflammation followingcataract surgery,[3] andallergic conjunctivitis.[4] Preliminary investigation for the treatment ofkeratoconjunctivitis sicca has been conducted in cellular models.[1]

Clinical trials

[edit]

Phase II clinical trials with mapracorat started in summer 2009. One trial was adouble blind dose finding study for anointment against atopic dermatitis. It tested concentrations of 0.01%, 0.03% and 0.1% versusplacebo over four weeks in around 64 patients. This trial was conducted by Intendis, a part ofBayer HealthCare Pharmaceuticals specialized ondermatology, and completed in September or October 2010.[2] The other trial, also with a double blind design, evaluated anophthalmicsuspension for the treatment of inflammation following cataract surgery. Various concentrations and dosing schemes were tested versus placebo in about 550 patients. The study was conducted byBausch & Lomb and completed in September 2010.[3] Its successor study, a phase III trial, started in November 2010 and completed in August 2011.[5]

As of January 2017[update] no study results are available.

See also

[edit]

References

[edit]
  1. ^abCavet ME, Harrington KL, Ward KW, Zhang JZ (September 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.PMID 20824100.
  2. ^abClinical trial numberNCT00944632 for "Dose Escalation of Different Concentrations of ZK 245186 in Atopic Dermatitis" atClinicalTrials.gov
  3. ^abClinical trial numberNCT00905450 for "Evaluation of BOL-303242-X Versus Vehicle for the Treatment of Inflammation Following Cataract Surgery" atClinicalTrials.gov
  4. ^Clinical trial numberNCT01289431 for "Mapracorat Ophthalmic Formulation in Subjects With Allergic Conjunctivitis" atClinicalTrials.gov
  5. ^Clinical trial numberNCT01230125 for "Mapracorat Ophthalmic Suspension for the Treatment of Ocular Inflammation Following Cataract Surgery" atClinicalTrials.gov
Glucocorticoids
Natural
Synthetic
Antiglucocorticoids
Synthesis modifiers
GRTooltip Glucocorticoid receptor
Agonists
Mixed
(SEGRMsTooltip Selective glucocorticoid receptor agonists)
Antagonists
Others
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