Mapracorat: Difference between revisions

| IUPAC_name = (2''R'')-1,1,1-trifluoro-4-(5-fluoro-2,3-dihydro-1-benzofuran-7-yl)-4-methyl-2-<nowiki>[[</nowiki>(2-methylquinolin-5-yl)amino]methyl]pentan-2-ol

| image = BOL-303242-X skeletal.svg

| CAS_number = 887375-26-0

| CAS_supplemental =

| ATC_prefix = none

| ATC_suffix =

| ATC_supplemental =

| PubChem = 24795088

| DrugBank =

| chemical_formula =

| C=25 | H=26 | F=4 | N=2 | O=2

| molecular_weight = 462.479 g/mol

| smiles = c14OCCc4cc(F)cc1C(C)(C)CC(O)(C(F)(F)F)CNc(cccc2n3)c2ccc3C

| bioavailability =

| protein_bound =

| 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

'''Mapracorat''' ([[International Nonproprietary Name|INN]], code names '''BOL-303242-X''', '''ZK 245186'''<ref name="pmid20824100">{{pmid|20824100}}</ref>) is an [[anti-inflammatory drug]] belonging to the experimental class of [[selective glucocorticoid receptor agonist]]s (SEGRAs). It is in [[clinical trial]]s for the topical treatment of [[atopic dermatitis]]<ref name="NCT00944632">{{ClinicalTrialsGov|NCT00944632|Dose Escalation of Different Concentrations of ZK 245186 in Atopic Dermatitis}}</ref> and inflammation following [[cataract surgery]]<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 [[keratoconjunctivitis sicca]] has been conducted in cellular models.<ref name="pmid20824100" />

Phase II clinical trials with mapracorat started in summer 2009. One trial was a [[double blind]] dose finding study for an [[ointment]] against atopic dermatitis. It tested concentrations of 0.01%, 0.03% and 0.1% versus [[placebo]] over four weeks in around 64 patients. This trial was conducted by [[Intendis]], a part of [[Bayer HealthCare Pharmaceuticals]] specialized on [[dermatology]], and completed in September or October 2010.<ref name="NCT00944632" /> The other trial, also with a double blind design, evaluated an [[Ophthalmology|ophthalmic]] [[suspension]] 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 [[Bausch & Lomb]] 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>

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

==References==

{{Reflist}}