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Volumn 17, Issue 4, 2015, Pages 414-422

Short-term administration of the glucagon receptor antagonist LY2409021 lowers blood glucose in healthy people and in those with type 2 diabetes

Author keywords

Diabetes care; Glucagon antagonist; Pharmacokinetics; Pharmacology

Indexed keywords

ALANINE AMINOTRANSFERASE; ALKALINE PHOSPHATASE; ASPARTATE AMINOTRANSFERASE; BILIRUBIN; C PEPTIDE; GLUCAGON; GLUCAGON RECEPTOR; GLUCOSE; GLYCOSYLATED HEMOGLOBIN; HIGH DENSITY LIPOPROTEIN CHOLESTEROL; HORMONE RECEPTOR BLOCKING AGENT; LOW DENSITY LIPOPROTEIN CHOLESTEROL; LY 2409021; METFORMIN; ORAL ANTIDIABETIC AGENT; UNCLASSIFIED DRUG; ADOMEGLIVANT; ANTIDIABETIC AGENT; BIPHENYL DERIVATIVE; HEMOGLOBIN A1C PROTEIN, HUMAN;

EID: 84924670428     PISSN: 14628902     EISSN: 14631326     Source Type: Journal    
DOI: 10.1111/dom.12446     Document Type: Article
Times cited : (100)

References (26)
  • 1
    • 0014608994 scopus 로고
    • Effects of starvation on plasma pancreatic glucagon in normal man
    • Aguilar-Parada E, Eisentraut AM, Unger RH. Effects of starvation on plasma pancreatic glucagon in normal man. Diabetes 1969; 18: 717-723.
    • (1969) Diabetes , vol.18 , pp. 717-723
    • Aguilar-Parada, E.1    Eisentraut, A.M.2    Unger, R.H.3
  • 3
    • 0020066592 scopus 로고
    • Glucose modulation of insulin and glucagon secretion in nondiabetic and diabetic man
    • Hollander PM, Asplin CM, Palmer JP. Glucose modulation of insulin and glucagon secretion in nondiabetic and diabetic man. Diabetes 1982; 31: 489-495.
    • (1982) Diabetes , vol.31 , pp. 489-495
    • Hollander, P.M.1    Asplin, C.M.2    Palmer, J.P.3
  • 4
    • 0021357826 scopus 로고
    • Prolonged infusion of somatostatin with glucagon replacement increases plasma glucose and glucose turnover in man
    • Ward WK, Best JD, Halter JB, Porte D Jr. Prolonged infusion of somatostatin with glucagon replacement increases plasma glucose and glucose turnover in man. J Clin Endocrinol Metab 1984; 58: 449-453.
    • (1984) J Clin Endocrinol Metab , vol.58 , pp. 449-453
    • Ward, W.K.1    Best, J.D.2    Halter, J.B.3    Porte Jr, D.4
  • 5
    • 34250854205 scopus 로고    scopus 로고
    • The role of alpha-cell dysregulation in fasting and postprandial hyperglycemia in type 2 diabetes and therapeutic implications
    • Dunning BE, Gerich JE. The role of alpha-cell dysregulation in fasting and postprandial hyperglycemia in type 2 diabetes and therapeutic implications. Endocr Rev 2007; 28: 253-283.
    • (2007) Endocr Rev , vol.28 , pp. 253-283
    • Dunning, B.E.1    Gerich, J.E.2
  • 6
    • 0033890616 scopus 로고    scopus 로고
    • Influence of obesity and type 2 diabetes on gluconeogenesis and glucose output in humans: a quantitative study
    • Gastaldelli A, Baldi S, Pettiti M et al. Influence of obesity and type 2 diabetes on gluconeogenesis and glucose output in humans: a quantitative study. Diabetes 2000; 49: 1367-1373.
    • (2000) Diabetes , vol.49 , pp. 1367-1373
    • Gastaldelli, A.1    Baldi, S.2    Pettiti, M.3
  • 7
    • 0034524938 scopus 로고    scopus 로고
    • Lack of suppression of glucagon contributes to postprandial hyperglycemia in subjects with type 2 diabetes mellitus
    • Shah P, Vella A, Basu A, Basu R, Schwenk WF, Rizza RA. Lack of suppression of glucagon contributes to postprandial hyperglycemia in subjects with type 2 diabetes mellitus. J Clin Endocrinol Metab 2000; 85: 4053-4059.
    • (2000) J Clin Endocrinol Metab , vol.85 , pp. 4053-4059
    • Shah, P.1    Vella, A.2    Basu, A.3    Basu, R.4    Schwenk, W.F.5    Rizza, R.A.6
  • 8
    • 0029133235 scopus 로고
    • Metabolic effects of metformin in non-insulin-dependent diabetes mellitus
    • Stumvoll M, Nurjhan N, Perriello G, Dailey G, Jerich GE. Metabolic effects of metformin in non-insulin-dependent diabetes mellitus. N Engl J Med 1995; 333: 550-554.
    • (1995) N Engl J Med , vol.333 , pp. 550-554
    • Stumvoll, M.1    Nurjhan, N.2    Perriello, G.3    Dailey, G.4    Jerich, G.E.5
  • 9
    • 4043101702 scopus 로고    scopus 로고
    • Separate contribution of diabetes, total fat mass, and fat topography to glucose production, gluconeogenesis, and glucogenolysis
    • Gastaldelli A, Miyazaki Y, Pettiti M et al. Separate contribution of diabetes, total fat mass, and fat topography to glucose production, gluconeogenesis, and glucogenolysis. J Clin Endocrinol Metab 2004; 89: 3914-3921.
    • (2004) J Clin Endocrinol Metab , vol.89 , pp. 3914-3921
    • Gastaldelli, A.1    Miyazaki, Y.2    Pettiti, M.3
  • 11
    • 79961176667 scopus 로고    scopus 로고
    • Novel insight into glucagon receptor action: lessons from knockout and transgenic mouse models
    • Vuguin PM, Charron MJ. Novel insight into glucagon receptor action: lessons from knockout and transgenic mouse models. Diabetes Obes Metab 2011; 13(Suppl. 1): 144-150.
    • (2011) Diabetes Obes Metab , vol.13 , pp. 144-150
    • Vuguin, P.M.1    Charron, M.J.2
  • 12
    • 0029760864 scopus 로고    scopus 로고
    • Evidence for a major role for glucagon in regulation of plasma glucose in conscious, nondiabetic, and alloxan-induced diabetic rabbits
    • Brand CL, Jorgensen PN, Svendsen I, Holst JJ. Evidence for a major role for glucagon in regulation of plasma glucose in conscious, nondiabetic, and alloxan-induced diabetic rabbits. Diabetes 1996; 45: 1076-1083.
    • (1996) Diabetes , vol.45 , pp. 1076-1083
    • Brand, C.L.1    Jorgensen, P.N.2    Svendsen, I.3    Holst, J.J.4
  • 13
    • 85047693695 scopus 로고    scopus 로고
    • Hepatic and glucagon-like peptide-1-mediated reversal of diabetes by glucagon receptor antisense oligonucleotide inhibitors
    • Sloop KW, Cao X-C, Siesky AM. Hepatic and glucagon-like peptide-1-mediated reversal of diabetes by glucagon receptor antisense oligonucleotide inhibitors. J Clin Invest 2004; 113: 1571-1581.
    • (2004) J Clin Invest , vol.113 , pp. 1571-1581
    • Sloop, K.W.1    Cao, X.-C.2    Siesky, A.M.3
  • 14
    • 73349089955 scopus 로고    scopus 로고
    • Long-term inhibition of the glucacon receptor with a monoclonal antibody in mice causes sustained improvement in glycemic control, with reversible alpha-cell hyperplasia and hyperglucagonemia
    • Gu W, Yan H, Winters A et al. Long-term inhibition of the glucacon receptor with a monoclonal antibody in mice causes sustained improvement in glycemic control, with reversible alpha-cell hyperplasia and hyperglucagonemia. J Pharmacol Exp Ther 2009; 331: 871-881.
    • (2009) J Pharmacol Exp Ther , vol.331 , pp. 871-881
    • Gu, W.1    Yan, H.2    Winters, A.3
  • 15
    • 79551600048 scopus 로고    scopus 로고
    • Glucagon receptor knockout prevents insulin-deficient type 1 diabetes in mice
    • Lee Y, Wang MY, Du XQ, Charron MJ, Unger RH. Glucagon receptor knockout prevents insulin-deficient type 1 diabetes in mice. Diabetes 2011; 60: 391-397.
    • (2011) Diabetes , vol.60 , pp. 391-397
    • Lee, Y.1    Wang, M.Y.2    Du, X.Q.3    Charron, M.J.4    Unger, R.H.5
  • 16
    • 80054699140 scopus 로고    scopus 로고
    • Chronic treatment with a glucagon receptor antagonist lowers glucose and moderately raises circulating glucagon and glucagon-like peptide 1 without severe alpha cell hypertrophy in diet-induced obese mice
    • Mu J, Jiang G, Brady E et al. Chronic treatment with a glucagon receptor antagonist lowers glucose and moderately raises circulating glucagon and glucagon-like peptide 1 without severe alpha cell hypertrophy in diet-induced obese mice. Diabetologia 2011; 54: 2381-2391.
    • (2011) Diabetologia , vol.54 , pp. 2381-2391
    • Mu, J.1    Jiang, G.2    Brady, E.3
  • 17
    • 84869805184 scopus 로고    scopus 로고
    • Anti-diabetic efficacy and impact on amino acid metabolism of GRA1, a novel small-molecule glucagon receptor antagonist
    • Mu J, Qureshi SA, Brady EJ et al. Anti-diabetic efficacy and impact on amino acid metabolism of GRA1, a novel small-molecule glucagon receptor antagonist. PLoS One 2012; 7: e49572.
    • (2012) PLoS One , vol.7 , pp. e49572
    • Mu, J.1    Qureshi, S.A.2    Brady, E.J.3
  • 18
    • 0035195977 scopus 로고    scopus 로고
    • Effects of a novel glucagon receptor antagonist (Bay 27-9955) on glucagon-stimulated glucose production in humans
    • Petersen KF, Sullivan JT. Effects of a novel glucagon receptor antagonist (Bay 27-9955) on glucagon-stimulated glucose production in humans. Diabetologia 2001; 44: 2018-2024.
    • (2001) Diabetologia , vol.44 , pp. 2018-2024
    • Petersen, K.F.1    Sullivan, J.T.2
  • 19
    • 84924652626 scopus 로고    scopus 로고
    • Effects of potent CYP inhibitors on the PK of LY2409021, a selective antagonist of the human glucagon receptor, and evaluation of QTc effects at supra-therapeutic exposures
    • AAPS Annual Meeting, San Diego, 2-6 November
    • Chappell J, Satonin, DK, Lam E, Tang C, Garhyan P. Effects of potent CYP inhibitors on the PK of LY2409021, a selective antagonist of the human glucagon receptor, and evaluation of QTc effects at supra-therapeutic exposures. AAPS Annual Meeting, San Diego, 2-6 November 2014.
    • (2014)
    • Chappell, J.1    Satonin, D.K.2    Lam, E.3    Tang, C.4    Garhyan, P.5
  • 20
    • 85011788628 scopus 로고    scopus 로고
    • Pharmacokinetics of LY2409021, a glucagon receptor antagonist: metabolism, disposition and effect of food
    • Satonin DK, Chappell JC, Lam C etal. Pharmacokinetics of LY2409021, a glucagon receptor antagonist: metabolism, disposition and effect of food. Clin Pharmacol Ther 2013; 93(Suppl. 1): S105-106.
    • (2013) Clin Pharmacol Ther , vol.93 , pp. S105-S106
    • Satonin, D.K.1    Chappell, J.C.2    Lam, C.3
  • 21
    • 0037417984 scopus 로고    scopus 로고
    • Lower blood glucose, hyperglucagonemia, and pancreatic alpha cell hyperplasia in glucagon receptor knockout mice
    • Gelling RW, Du XQ, Dichmann DS et al. Lower blood glucose, hyperglucagonemia, and pancreatic alpha cell hyperplasia in glucagon receptor knockout mice. Proc Natl Acad Sci U S A 2003; 100: 1438-1443.
    • (2003) Proc Natl Acad Sci U S A , vol.100 , pp. 1438-1443
    • Gelling, R.W.1    Du, X.Q.2    Dichmann, D.S.3
  • 22
    • 70350666371 scopus 로고    scopus 로고
    • Homozygous P86S mutation of the human glucagon receptor is associated with hyperglucagonemia, alpha cell hyperplasia, and islet cell tumor
    • Zhou C, Dhall D, Nissen NN, Chen CR, Yu R. Homozygous P86S mutation of the human glucagon receptor is associated with hyperglucagonemia, alpha cell hyperplasia, and islet cell tumor. Pancreas 2009; 38: 941-946.
    • (2009) Pancreas , vol.38 , pp. 941-946
    • Zhou, C.1    Dhall, D.2    Nissen, N.N.3    Chen, C.R.4    Yu, R.5
  • 23
    • 80555157690 scopus 로고    scopus 로고
    • Processing of proglucagon to GLP-1 in pancreatic alpha-cells: is this a paracrine mechanism enabling GLP-1 to act on beta-cells?
    • Whalley NM, Pritchard LE, Smith DM, White A. Processing of proglucagon to GLP-1 in pancreatic alpha-cells: is this a paracrine mechanism enabling GLP-1 to act on beta-cells? J Endocrinol 2011; 211: 99-106.
    • (2011) J Endocrinol , vol.211 , pp. 99-106
    • Whalley, N.M.1    Pritchard, L.E.2    Smith, D.M.3    White, A.4
  • 24
    • 33845919110 scopus 로고    scopus 로고
    • Glucagon receptor knockout mice are resistant to diet-induced obesity and streptozotocin-mediated beta cell loss and hyperglycaemia
    • Conarello SL, Jiang G, Mu J et al. Glucagon receptor knockout mice are resistant to diet-induced obesity and streptozotocin-mediated beta cell loss and hyperglycaemia. Diabetologia 2007; 50: 142-150.
    • (2007) Diabetologia , vol.50 , pp. 142-150
    • Conarello, S.L.1    Jiang, G.2    Mu, J.3
  • 25
    • 54849431792 scopus 로고    scopus 로고
    • The glucagon receptor is required for the adaptive metabolic response to fasting
    • Longuet C, Sinclair EM, Maida A et al. The glucagon receptor is required for the adaptive metabolic response to fasting. Cell Metab 2008; 8: 359-371.
    • (2008) Cell Metab , vol.8 , pp. 359-371
    • Longuet, C.1    Sinclair, E.M.2    Maida, A.3
  • 26
    • 0842288445 scopus 로고    scopus 로고
    • Reduction in glucagon receptor expression by an antisense oligonucleotide ameliorates diabetic syndrome in db/db mice
    • Liang Y, Osborne MC, Monia BP et al. Reduction in glucagon receptor expression by an antisense oligonucleotide ameliorates diabetic syndrome in db/db mice. Diabetes 2004; 53: 410-417.
    • (2004) Diabetes , vol.53 , pp. 410-417
    • Liang, Y.1    Osborne, M.C.2    Monia, B.P.3


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.