{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2026,9,17]],"date-time":"2026-09-17T17:22:37Z","timestamp":1789665757203,"version":"4.0.1"},"reference-count":36,"publisher":"Wiley","issue":"11","license":[{"start":{"date-parts":[[2013,6,12]],"date-time":"2013-06-12T00:00:00Z","timestamp":1370995200000},"content-version":"vor","delay-in-days":0,"URL":"http:\/\/onlinelibrary.wiley.com\/termsAndConditions#vor"}],"content-domain":{"domain":[],"crossmark-restriction":false},"short-container-title":["Diabetes Obesity Metabolism"],"published-print":{"date-parts":[[2013,11]]},"abstract":"<jats:sec>\n                    <jats:title>Aims<\/jats:title>\n                    <jats:p>\n                      This clinical trial assessed whether a potent, selective\n                      <jats:styled-content style=\"fixed-case\">GPR109A<\/jats:styled-content>\n                      agonist,\n                      <jats:styled-content style=\"fixed-case\">GSK256073<\/jats:styled-content>\n                      , could, through inhibition of lipolysis, acutely improve glucose homeostasis in subjects with type 2 diabetes mellitus.\n                    <\/jats:p>\n                  <\/jats:sec>\n                  <jats:sec>\n                    <jats:title>Methods<\/jats:title>\n                    <jats:p>\n                      Thirty\u2010nine diabetic subjects were enrolled in the randomized, single\u2010blind, placebo\u2010controlled, three\u2010period crossover trial. Each subject received placebo and two of four regimens of\n                      <jats:styled-content style=\"fixed-case\">GSK256073<\/jats:styled-content>\n                      for 2 days.\n                      <jats:styled-content style=\"fixed-case\">GSK256073<\/jats:styled-content>\n                      was dosed 5\u2009mg every 12\u2009h before breakfast and supper (\n                      <jats:styled-content style=\"fixed-case\">BID<\/jats:styled-content>\n                      ), 10\u2009mg every 24\u2009h before breakfast (\n                      <jats:styled-content style=\"fixed-case\">QD<\/jats:styled-content>\n                      ), 25\u2009mg\n                      <jats:styled-content style=\"fixed-case\">BID<\/jats:styled-content>\n                      and 50\u2009mg\n                      <jats:styled-content style=\"fixed-case\">QD<\/jats:styled-content>\n                      .\n                    <\/jats:p>\n                  <\/jats:sec>\n                  <jats:sec>\n                    <jats:title>Results<\/jats:title>\n                    <jats:p>\n                      The change from baseline weighted mean glucose concentration for an interval from 24 to 48\u2009h after the initial drug dose was significantly reduced for all\n                      <jats:styled-content style=\"fixed-case\">GSK256073<\/jats:styled-content>\n                      regimens, reaching a maximum of \u22120.87\u2009mmol\/l (\u22121.20, \u22120.52) with the 25\u2009mg\n                      <jats:styled-content style=\"fixed-case\">BID<\/jats:styled-content>\n                      dose. Sustained suppression of non\u2010esterified fatty acid (\n                      <jats:styled-content style=\"fixed-case\">NEFA<\/jats:styled-content>\n                      ) and glycerol concentrations was observed with all\n                      <jats:styled-content style=\"fixed-case\">GSK256073<\/jats:styled-content>\n                      doses throughout the 48\u2010h dosing period. Serum insulin and C\u2010peptide concentrations fell in concert with glucose concentrations and calculated\n                      <jats:styled-content style=\"fixed-case\">HOMA\u2010IR<\/jats:styled-content>\n                      scores decreased 27\u201347%, consistent with insulin sensitization. No marked differences were evident between either 10 and 50\u2009mg total daily doses or\n                      <jats:styled-content style=\"fixed-case\">QD<\/jats:styled-content>\n                      versus\n                      <jats:styled-content style=\"fixed-case\">BID<\/jats:styled-content>\n                      dosing.\n                    <\/jats:p>\n                  <\/jats:sec>\n                  <jats:sec>\n                    <jats:title>Conclusions<\/jats:title>\n                    <jats:p>\n                      Administration of a\n                      <jats:styled-content style=\"fixed-case\">GPR109A<\/jats:styled-content>\n                      agonist for 2 days significantly decreased serum\n                      <jats:styled-content style=\"fixed-case\">NEFA<\/jats:styled-content>\n                      and glucose concentrations in diabetic subjects. Glucose improvements were associated with decreased insulin concentrations and measures of enhanced insulin sensitivity. Improved glucose control occurred with\n                      <jats:styled-content style=\"fixed-case\">GSK256073<\/jats:styled-content>\n                      doses that were generally safe and not associated with events of flushing or gastrointestinal disturbances.\n                    <\/jats:p>\n                  <\/jats:sec>","DOI":"10.1111\/dom.12132","type":"journal-article","created":{"date-parts":[[2013,5,22]],"date-time":"2013-05-22T17:23:39Z","timestamp":1369243419000},"page":"1013-1021","source":"Crossref","is-referenced-by-count":31,"title":["<scp>GSK256073<\/scp>\n                    , a selective agonist of G\u2010protein coupled receptor 109A (GPR109A) reduces serum glucose in subjects with type 2 diabetes mellitus"],"prefix":"10.1111","volume":"15","author":[{"given":"R. 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