{"database":"biostudies-literature","file_versions":[],"scores":null,"additional":{"omics_type":["Unknown"],"volume":["83(12)"],"submitter":["Miller BE"],"pubmed_abstract":["<h4>Aims</h4>Cathepsin C (CTSC) is necessary for the activation of several serine proteases including neutrophil elastase (NE), cathepsin G and proteinase 3. GSK2793660 is an oral, irreversible inhibitor of CTSC that is hypothesized to provide an alternative route to achieve NE inhibition and was tested in a Phase I study.<h4>Methods</h4>Single escalating oral doses of GSK2793660 from 0.5 to 20 mg or placebo were administered in a randomized crossover design to healthy male subjects; a separate cohort received once daily doses of 12 mg or placebo for 21 days. Data were collected on safety, pharmacokinetics, CTSC enzyme inhibition and blood biomarkers.<h4>Results</h4>Single, oral doses of GSK2793660 were able to dose-dependently inhibit whole blood CTSC activity. Once daily dosing of 12 mg "],"journal":["British journal of clinical pharmacology"],"pagination":["2813-2820"],"full_dataset_link":["https://www.ebi.ac.uk/biostudies/studies/S-EPMC5698569"],"repository":["biostudies-literature"],"pubmed_title":["Epithelial desquamation observed in a phase I study of an oral cathepsin C inhibitor (GSK2793660)."],"pmcid":["PMC5698569"],"pubmed_authors":["Goyal N","Mayer RJ","Lazaar AL","Heslop T","Boyce M","Bal J","Carpenter D","Miller BE","Churchill A","Dallow N"],"additional_accession":[]},"is_claimable":false,"name":"Epithelial desquamation observed in a phase I study of an oral cathepsin C inhibitor (GSK2793660).","description":"<h4>Aims</h4>Cathepsin C (CTSC) is necessary for the activation of several serine proteases including neutrophil elastase (NE), cathepsin G and proteinase 3. GSK2793660 is an oral, irreversible inhibitor of CTSC that is hypothesized to provide an alternative route to achieve NE inhibition and was tested in a Phase I study.<h4>Methods</h4>Single escalating oral doses of GSK2793660 from 0.5 to 20 mg or placebo were administered in a randomized crossover design to healthy male subjects; a separate cohort received once daily doses of 12 mg or placebo for 21 days. Data were collected on safety, pharmacokinetics, CTSC enzyme inhibition and blood biomarkers.<h4>Results</h4>Single, oral doses of GSK2793660 were able to dose-dependently inhibit whole blood CTSC activity. Once daily dosing of 12 mg ","dates":{"release":"2017-01-01T00:00:00Z","publication":"2017 Dec","modification":"2026-04-29T07:14:15.502Z","creation":"2019-03-27T00:09:13Z"},"accession":"S-EPMC5698569","cross_references":{"pubmed":["28800383"],"doi":["10.1111/bcp.13398"]}}