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Revision as of 13:27, 6 January 2011 editAnypodetos (talk | contribs)Autopatrolled, Extended confirmed users, Pending changes reviewers, Rollbackers39,350 edits Phase III study started← Previous edit Latest revision as of 20:00, 22 January 2023 edit undoEntranced98 (talk | contribs)Extended confirmed users, Pending changes reviewers, Rollbackers172,831 edits Importing Wikidata short description: "Type of selective glucocorticoid receptor agonist"Tag: Shortdesc helper 
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{{Short description|Type of selective glucocorticoid receptor agonist}}
{{Drugbox {{Drugbox
| Verifiedfields = changed
⚫ | IUPAC_name = (2''R'')-1,1,1-trifluoro-4-(5-fluoro-2,3-dihydro-1-benzofuran-7-yl)-4-methyl-2-<nowiki>methyl]pentan-2-ol
| verifiedrevid = 406275524
| image = BOL-303242-X skeletal.svg
⚫ | IUPAC_name = (2''R'')-1,1,1-trifluoro-4-(5-fluoro-2,3-dihydro-1-benzofuran-7-yl)-4-methyl-2-<nowiki>methyl]pentan-2-ol
⚫ | CAS_number = 887375-26-0
| image = Mapracorat_skeletal.svg
| CAS_supplemental =
| width = 250
⚫ | ATC_prefix = none

⚫ | ATC_suffix =
<!--Clinical data-->
⚫ | ATC_supplemental =
| tradename =
⚫ | PubChem = 24795088
| DrugBank = | pregnancy_AU = <!-- A / B1 / B2 / B3 / C / D / X -->
⚫ | pregnancy_US = <!-- A / B / C / D / X -->
⚫ | chemical_formula =
⚫ | pregnancy_category =
⚫ | C=25 | H=26 | F=4 | N=2 | O=2
⚫ | legal_AU = <!-- S2, S3, S4, S5, S6, S7, S8, S9 or Unscheduled-->
| molecular_weight = 462.479 g/mol
⚫ | legal_CA = <!-- Schedule I, II, III, IV, V, VI, VII, VIII -->
⚫ | smiles = c14OCCc4cc(F)cc1C(C)(C)CC(O)(C(F)(F)F)CNc(cccc2n3)c2ccc3C
⚫ | legal_UK = <!-- GSL, P, POM, CD, or Class A, B, C -->
⚫ | bioavailability =
⚫ | legal_US = <!-- OTC / Rx-only / Schedule I, II, III, IV, V -->
⚫ | protein_bound =
⚫ | legal_status = Investigational
⚫ | metabolism =
⚫ | elimination_half-life =
⚫ | excretion =
| pregnancy_AU = <!-- A / B1 / B2 / B3 / C / D / X -->
⚫ | pregnancy_US = <!-- A / B / C / D / X -->
⚫ | pregnancy_category=
⚫ | legal_AU = <!-- S2, S3, S4, S5, S6, S7, S8, S9 or Unscheduled-->
⚫ | legal_CA = <!-- Schedule I, II, III, IV, V, VI, VII, VIII -->
⚫ | legal_UK = <!-- GSL, P, POM, CD, or Class A, B, C -->
⚫ | legal_US = <!-- OTC / Rx-only / Schedule I, II, III, IV, V -->
⚫ | legal_status = Investigational
| routes_of_administration = Topical (], ]) | routes_of_administration = Topical (], ])

<!--Pharmacokinetic data-->
⚫ | bioavailability =
⚫ | protein_bound =
⚫ | metabolism =
⚫ | elimination_half-life =
⚫ | excretion =

<!--Identifiers-->
| CAS_number_Ref = {{cascite|correct|??}}
⚫ | CAS_number = 887375-26-0
⚫ | ATC_prefix = none
⚫ | ATC_suffix =
⚫ | ATC_supplemental =
⚫ | PubChem = 24795088
| DrugBank_Ref = {{drugbankcite|correct|drugbank}}
| DrugBank =
| KEGG = D10136
| KEGG_Ref = {{keggcite|changed|kegg}}
| ChemSpiderID_Ref = {{chemspidercite|changed|chemspider}}
| ChemSpiderID = 25104194
| UNII_Ref = {{fdacite|changed|FDA}}
| UNII = 145V79YBVP

<!--Chemical data-->
⚫ | chemical_formula =
⚫ | C=25 | H=26 | F=4 | N=2 | O=2
⚫ | smiles = c14OCCc4cc(F)cc1C(C)(C)CC(O)(C(F)(F)F)CNc(cccc2n3)c2ccc3C
| StdInChI_Ref = {{stdinchicite|changed|chemspider}}
| StdInChI = 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
| StdInChIKey_Ref = {{stdinchicite|changed|chemspider}}
| StdInChIKey = VJGFOYBQOIPQFY-XMMPIXPASA-N
}} }}

'''Mapracorat''' (], code names '''BOL-303242-X''', '''ZK 245186'''<ref name="pmid20824100">{{pmid|20824100}}</ref>) is an ] belonging to the experimental class of ]s (SEGRAs). It is in ]s for the topical treatment of ]<ref name="NCT00944632">{{ClinicalTrialsGov|NCT00944632|Dose Escalation of Different Concentrations of ZK 245186 in Atopic Dermatitis}}</ref> and inflammation following ]<ref name="NCT00905450">{{ClinicalTrialsGov|NCT00905450|Evaluation of BOL-303242-X Versus Vehicle for the Treatment of Inflammation Following Cataract Surgery}}</ref>. Preliminary investigation for the treatment of ] has been conducted in cellular models.<ref name="pmid20824100" /> '''Mapracorat''' (], code names '''BOL-303242-X''', '''ZK-245186'''<ref name="pmid20824100">{{cite journal | vauthors = Cavet ME, Harrington KL, Ward KW, Zhang JZ | title = Mapracorat, a novel selective glucocorticoid receptor agonist, inhibits hyperosmolar-induced cytokine release and MAPK pathways in human corneal epithelial cells | journal = Molecular Vision | volume = 16 | pages = 1791–800 | date = September 2010 | pmid = 20824100 | pmc = 2932489 }}</ref>) is an ] belonging to the experimental class of ]s (SEGRAs). It is in ]s for the topical treatment of ],<ref name="NCT00944632">{{ClinicalTrialsGov|NCT00944632|Dose Escalation of Different Concentrations of ZK 245186 in Atopic Dermatitis}}</ref> inflammation following ],<ref name="NCT00905450">{{ClinicalTrialsGov|NCT00905450|Evaluation of BOL-303242-X Versus Vehicle for the Treatment of Inflammation Following Cataract Surgery}}</ref> and ].<ref>{{ClinicalTrialsGov|NCT01289431|Mapracorat Ophthalmic Formulation in Subjects With Allergic Conjunctivitis}}</ref> Preliminary investigation for the treatment of ] has been conducted in cellular models.<ref name="pmid20824100" />


== Clinical trials== == Clinical trials==
Phase II clinical trials with mapracorat started in summer 2009. One trial was a ] dose finding study for an ] against atopic dermatitis. It tested concentrations of 0.01%, 0.03% and 0.1% versus ] over four weeks in around 64 patients. This trial was conducted by ], a part of ] specialized on ], and completed in September or October 2010.<ref name="NCT00944632" /> The other trial, also with a double blind design, evaluated an ] ] 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 by ] and completed in September 2010.<ref name="NCT00905450" /> Its successor study, a phase III trial, started in November 2010 and is scheduled to run until February 2012.<ref name="NCT01230125">{{ClinicalTrialsGov|NCT01230125|Mapracorat Ophthalmic Suspension for the Treatment of Ocular Inflammation Following Cataract Surgery}}</ref> Phase II clinical trials with mapracorat started in summer 2009. One trial was a ] dose finding study for an ] against atopic dermatitis. It tested concentrations of 0.01%, 0.03% and 0.1% versus ] over four weeks in around 64 patients. This trial was conducted by Intendis, a part of ] specialized on ], and completed in September or October 2010.<ref name="NCT00944632" /> The other trial, also with a double blind design, evaluated an ] ] 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 by ] and completed in September 2010.<ref name="NCT00905450" /> Its successor study, a phase III trial, started in November 2010 and completed in August 2011.<ref name="NCT01230125">{{ClinicalTrialsGov|NCT01230125|Mapracorat Ophthalmic Suspension for the Treatment of Ocular Inflammation Following Cataract Surgery}}</ref>


{{as of|2011|1}} no study results are available. {{as of|2017|1}} no study results are available.


==References== == See also ==
* ]
⚫ {{Reflist}}
* ]
* ]

== References ==
⚫ {{Reflist|2}}

{{Glucocorticoids and antiglucocorticoids}}
{{Glucocorticoid receptor modulators}}


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