메뉴 건너뛰기




Volumn 10, Issue 3, 2015, Pages

Pharmacokinetics (PK), pharmacodynamics (PD) and integrated PK/PD modeling of a novel long acting FGF21 clinical candidate PF-05231023 in diet-induced obese and leptin-deficient obese mice

Author keywords

[No Author keywords available]

Indexed keywords

FIBROBLAST GROWTH FACTOR 21; PF 05231023; UNCLASSIFIED DRUG; FIBROBLAST GROWTH FACTOR; GLUCOSE BLOOD LEVEL; LEPTIN; MONOCLONAL ANTIBODY; PF-05231023;

EID: 84925708565     PISSN: None     EISSN: 19326203     Source Type: Journal    
DOI: 10.1371/journal.pone.0119104     Document Type: Article
Times cited : (56)

References (38)
  • 2
    • 84883481988 scopus 로고    scopus 로고
    • The effects of LY2405319, an FGF21 analog, in obese human subjects with type 2 diabetes
    • PMID: 24011069
    • Gaich G, Chien JY, Fu H, Glass LC, Deeg MA, Holland WL, et al. The effects of LY2405319, an FGF21 analog, in obese human subjects with type 2 diabetes. Cell Metab. 2013; 18: 333-340. doi: 10.1016/j.cmet.2013.08.005 PMID: 24011069
    • (2013) Cell Metab , vol.18 , pp. 333-340
    • Gaich, G.1    Chien, J.Y.2    Fu, H.3    Glass, L.C.4    Deeg, M.A.5    Holland, W.L.6
  • 3
    • 84901821975 scopus 로고    scopus 로고
    • FGF21-based pharmacotherapy - Potential utility for metabolic disorders
    • Gimeno RE, Moller DE FGF21-based pharmacotherapy - potential utility for metabolic disorders. Trends Endocrinol Metab. 2014;
    • (2014) Trends Endocrinol Metab
    • Gimeno, R.E.1    Moller, D.E.2
  • 4
    • 57349098220 scopus 로고    scopus 로고
    • Fibroblast growth factor 21 corrects obesity in mice
    • PMID: 18687777
    • Coskun T, Bina HA, Schneider MA, Dunbar JD, Hu CC, Chen Y, et al. Fibroblast growth factor 21 corrects obesity in mice. Endocrinology. 2008; 149: 6018-6027. doi: 10.1210/en.2008-0816 PMID: 18687777
    • (2008) Endocrinology , vol.149 , pp. 6018-6027
    • Coskun, T.1    Bina, H.A.2    Schneider, M.A.3    Dunbar, J.D.4    Hu, C.C.5    Chen, Y.6
  • 5
    • 84870359606 scopus 로고    scopus 로고
    • Treating diabetes and obesity with an FGF21-mimetic antibody activating the betaKlotho/FGFR1c receptor complex
    • PMID: 23197570
    • Foltz IN, Hu S, King C, Wu X, Yang C, Wang W, et al. Treating diabetes and obesity with an FGF21-mimetic antibody activating the betaKlotho/FGFR1c receptor complex. Sci Transl Med. 2012; 4: 162ra153. doi: 10.1126/scitranslmed.3004690 PMID: 23197570
    • (2012) Sci Transl Med , vol.4 , pp. 162ra153
    • Foltz, I.N.1    Hu, S.2    King, C.3    Wu, X.4    Yang, C.5    Wang, W.6
  • 6
    • 84880426480 scopus 로고    scopus 로고
    • Development of a Novel Long-Acting Antidiabetic FGF21 Mimetic by Targeted Conjugation to a Scaffold Antibody
    • PMID: 23720456
    • Huang J, Ishino T, Chen G, Rolzin P, Osothprarop TF, Retting K, et al. Development of a Novel Long-Acting Antidiabetic FGF21 Mimetic by Targeted Conjugation to a Scaffold Antibody. J Pharmacol Exp Ther. 2013; 346: 270-280. doi: 10.1124/jpet.113.204420 PMID: 23720456
    • (2013) J Pharmacol Exp Ther , vol.346 , pp. 270-280
    • Huang, J.1    Ishino, T.2    Chen, G.3    Rolzin, P.4    Osothprarop, T.F.5    Retting, K.6
  • 7
    • 84874903440 scopus 로고    scopus 로고
    • Rational design of a fibroblast growth factor 21-based clinical candidate, LY2405319
    • PMID: 23536797
    • Kharitonenkov A, Beals JM, Micanovic R, Strifler BA, Rathnachalam R, Wroblewski VJ, et al. Rational design of a fibroblast growth factor 21-based clinical candidate, LY2405319. PLoS One. 2013; 8: e58575. doi: 10.1371/journal.pone.0058575 PMID: 23536797
    • (2013) PLoS One , vol.8 , pp. e58575
    • Kharitonenkov, A.1    Beals, J.M.2    Micanovic, R.3    Strifler, B.A.4    Rathnachalam, R.5    Wroblewski, V.J.6
  • 8
    • 61649127208 scopus 로고    scopus 로고
    • Fibroblast growth factor 21 reverses hepatic steatosis, increases energy expenditure, and improves insulin sensitivity in diet-induced obese mice
    • PMID: 18840786
    • Xu J, Lloyd DJ, Hale C, Stanislaus S, Chen M, Sivits G, et al. Fibroblast growth factor 21 reverses hepatic steatosis, increases energy expenditure, and improves insulin sensitivity in diet-induced obese mice. Diabetes. 2009; 58: 250-259. doi: 10.2337/db08-0392 PMID: 18840786
    • (2009) Diabetes , vol.58 , pp. 250-259
    • Xu, J.1    Lloyd, D.J.2    Hale, C.3    Stanislaus, S.4    Chen, M.5    Sivits, G.6
  • 9
    • 84865741904 scopus 로고    scopus 로고
    • betaKlotho is required for fibroblast growth factor 21 effects on growth and metabolism
    • PMID: 22958921
    • Ding X, Boney-Montoya J, Owen BM, Bookout AL, Coate KC, Mangelsdorf DJ, et al. betaKlotho is required for fibroblast growth factor 21 effects on growth and metabolism. Cell Metab. 2012; 16: 387-393. doi: 10.1016/j.cmet.2012.08.002 PMID: 22958921
    • (2012) Cell Metab , vol.16 , pp. 387-393
    • Ding, X.1    Boney-Montoya, J.2    Owen, B.M.3    Bookout, A.L.4    Coate, K.C.5    Mangelsdorf, D.J.6
  • 10
    • 84862017269 scopus 로고    scopus 로고
    • Dynamics and Distribution of Klothobeta (KLB) and fibroblast growth factor receptor-1 (FGFR1) in living cells reveal the fibroblast growth factor-21 (FGF21)-induced receptor complex
    • PMID: 22523080
    • Ming AY, Yoo E, Vorontsov EN, Altamentova SM, Kilkenny DM, Rocheleau JV Dynamics and Distribution of Klothobeta (KLB) and fibroblast growth factor receptor-1 (FGFR1) in living cells reveal the fibroblast growth factor-21 (FGF21)-induced receptor complex. J Biol Chem. 2012; 287: 19997-20006. doi: 10.1074/jbc.M111.325670 PMID: 22523080
    • (2012) J Biol Chem , vol.287 , pp. 19997-20006
    • Ming, A.Y.1    Yoo, E.2    Vorontsov, E.N.3    Altamentova, S.M.4    Kilkenny, D.M.5    Rocheleau, J.V.6
  • 11
    • 34247565954 scopus 로고    scopus 로고
    • Molecular insights into the klotho-dependent, endocrine mode of action of fibroblast growth factor 19 subfamily members
    • PMID: 17339340
    • Goetz R, Beenken A, Ibrahimi OA, Kalinina J, Olsen SK, Eliseenkova AV, et al. Molecular insights into the klotho-dependent, endocrine mode of action of fibroblast growth factor 19 subfamily members. Mol Cell Biol. 2007; 27: 3417-3428. PMID: 17339340
    • (2007) Mol Cell Biol , vol.27 , pp. 3417-3428
    • Goetz, R.1    Beenken, A.2    Ibrahimi, O.A.3    Kalinina, J.4    Olsen, S.K.5    Eliseenkova, A.V.6
  • 12
    • 84875421249 scopus 로고    scopus 로고
    • Exploring mechanisms of FGF signalling through the lens of structural biology
    • PMID: 23403721
    • Goetz R, Mohammadi M Exploring mechanisms of FGF signalling through the lens of structural biology. Nat Rev Mol Cell Biol. 2013; 14: 166-180. doi: 10.1038/nrm3528 PMID: 23403721
    • (2013) Nat Rev Mol Cell Biol , vol.14 , pp. 166-180
    • Goetz, R.1    Mohammadi, M.2
  • 13
    • 84874616515 scopus 로고    scopus 로고
    • Differential enzyme-linked immunosorbent assay and ligand-binding mass spectrometry for analysis of biotransformation of protein therapeutics: Application to various FGF21 modalities
    • PMID: 23373459
    • Hager T, Spahr C, Xu J, Salimi-Moosavi H, Hall M Differential enzyme-linked immunosorbent assay and ligand-binding mass spectrometry for analysis of biotransformation of protein therapeutics: application to various FGF21 modalities. Anal Chem. 2013; 85: 2731-2738. doi: 10.1021/ac303203y PMID: 23373459
    • (2013) Anal Chem , vol.85 , pp. 2731-2738
    • Hager, T.1    Spahr, C.2    Xu, J.3    Salimi-Moosavi, H.4    Hall, M.5
  • 14
    • 62149139387 scopus 로고    scopus 로고
    • Different roles of N- and C- termini in the functional activity of FGF21
    • PMID: 19117008
    • Micanovic R, Raches DW, Dunbar JD, Driver DA, Bina HA, Dickinson CD, et al. Different roles of N- and C- termini in the functional activity of FGF21. J Cell Physiol. 2009; 219: 227-234. doi: 10.1002/jcp. 21675 PMID: 19117008
    • (2009) J Cell Physiol , vol.219 , pp. 227-234
    • Micanovic, R.1    Raches, D.W.2    Dunbar, J.D.3    Driver, D.A.4    Bina, H.A.5    Dickinson, C.D.6
  • 15
    • 57849155278 scopus 로고    scopus 로고
    • FGF21 N- and C-termini play different roles in receptor interaction and activation
    • PMID: 19059246
    • Yie J, Hecht R, Patel J, Stevens J, Wang W, Hawkins N, et al. FGF21 N- and C-termini play different roles in receptor interaction and activation. FEBS Lett. 2009; 583: 19-24. doi: 10.1016/j.febslet.2008.11.023 PMID: 19059246
    • (2009) FEBS Lett , vol.583 , pp. 19-24
    • Yie, J.1    Hecht, R.2    Patel, J.3    Stevens, J.4    Wang, W.5    Hawkins, N.6
  • 16
    • 84865442538 scopus 로고    scopus 로고
    • Long-acting FGF21 has enhanced efficacy in diet-induced obese mice and in obese rhesus monkeys
    • PMID: 22798348
    • Veniant MM, Komorowski R, Chen P, Stanislaus S, Winters K, Hager T, et al. Long-acting FGF21 has enhanced efficacy in diet-induced obese mice and in obese rhesus monkeys. Endocrinology. 2012; 153: 4192-4203. doi: 10.1210/en.2012-1211 PMID: 22798348
    • (2012) Endocrinology , vol.153 , pp. 4192-4203
    • Veniant, M.M.1    Komorowski, R.2    Chen, P.3    Stanislaus, S.4    Winters, K.5    Hager, T.6
  • 17
    • 84863011453 scopus 로고    scopus 로고
    • FGF21 analogs of sustained action enabled by orthogonal biosynthesis demonstrate enhanced antidiabetic pharmacology in rodents
    • PMID: 22210323
    • Mu J, Pinkstaff J, Li Z, Skidmore L, Li N, Myler H, et al. FGF21 analogs of sustained action enabled by orthogonal biosynthesis demonstrate enhanced antidiabetic pharmacology in rodents. Diabetes. 2012; 61: 505-512. doi: 10.2337/db11-0838 PMID: 22210323
    • (2012) Diabetes , vol.61 , pp. 505-512
    • Mu, J.1    Pinkstaff, J.2    Li, Z.3    Skidmore, L.4    Li, N.5    Myler, H.6
  • 18
    • 84883482471 scopus 로고    scopus 로고
    • FGF21 mimetic shows therapeutic promise
    • PMID: 24011067
    • Reitman ML FGF21 mimetic shows therapeutic promise. Cell Metab. 2013; 18: 307-309. doi: 10.1016/j.cmet.2013.08.014 PMID: 24011067
    • (2013) Cell Metab , vol.18 , pp. 307-309
    • Reitman, M.L.1
  • 19
    • 84884821893 scopus 로고    scopus 로고
    • NCoR repression of LXRs restricts macrophage biosynthesis of insulin-sensitizing omega 3 fatty acids
    • PMID: 24074869
    • Li P, Spann NJ, Kaikkonen MU, Lu M, Oh da Y, Fox JN, et al. NCoR repression of LXRs restricts macrophage biosynthesis of insulin-sensitizing omega 3 fatty acids. Cell. 2013; 155: 200-214. doi: 10.1016/j.cell.2013.08.054 PMID: 24074869
    • (2013) Cell , vol.155 , pp. 200-214
    • Li, P.1    Spann, N.J.2    Kaikkonen, M.U.3    Lu, M.4    Oh Da, Y.5    Fox, J.N.6
  • 20
    • 84876256827 scopus 로고    scopus 로고
    • Neuronal Sirt1 deficiency increases insulin sensitivity in both brain and peripheral tissues
    • PMID: 23457303
    • Lu M, Sarruf DA, Li P, Osborn O, Sanchez-Alavez M, Talukdar S, et al. Neuronal Sirt1 deficiency increases insulin sensitivity in both brain and peripheral tissues. J Biol Chem. 2013; 288: 10722-10735. doi: 10.1074/jbc.M112.443606 PMID: 23457303
    • (2013) J Biol Chem , vol.288 , pp. 10722-10735
    • Lu, M.1    Sarruf, D.A.2    Li, P.3    Osborn, O.4    Sanchez-Alavez, M.5    Talukdar, S.6
  • 21
    • 70349675659 scopus 로고    scopus 로고
    • Estimating the continuous-time dynamics of energy and fat metabolism in mice
    • PMID: 19763167
    • Guo J, Hall KD Estimating the continuous-time dynamics of energy and fat metabolism in mice. PLoS Comput Biol. 2009; 5: e1000511. doi: 10.1371/journal.pcbi.1000511 PMID: 19763167
    • (2009) PLoS Comput Biol , vol.5 , pp. e1000511
    • Guo, J.1    Hall, K.D.2
  • 22
    • 40949154815 scopus 로고    scopus 로고
    • What is the required energy deficit per unit weight loss?
    • PMID: 17848938
    • Hall KD What is the required energy deficit per unit weight loss? Int J Obes (Lond). 2008; 32: 573-576. PMID: 17848938
    • (2008) Int J Obes (Lond) , vol.32 , pp. 573-576
    • Hall, K.D.1
  • 24
    • 84863012022 scopus 로고    scopus 로고
    • FGF21 regulates PGC-1alpha and browning of white adipose tissues in adaptive thermogenesis
    • PMID: 22302939
    • Fisher FM, Kleiner S, Douris N, Fox EC, Mepani RJ, Verdeguer F, et al. FGF21 regulates PGC-1alpha and browning of white adipose tissues in adaptive thermogenesis. Genes Dev. 2012; 26: 271-281. doi: 10.1101/gad.177857.111 PMID: 22302939
    • (2012) Genes Dev , vol.26 , pp. 271-281
    • Fisher, F.M.1    Kleiner, S.2    Douris, N.3    Fox, E.C.4    Mepani, R.J.5    Verdeguer, F.6
  • 25
    • 79954525448 scopus 로고    scopus 로고
    • Circulating FGF21 levels are progressively increased from the early to end stages of chronic kidney diseases and are associated with renal function in Chinese
    • PMID: 21525989
    • Lin Z, Zhou Z, Liu Y, Gong Q, Yan X, Xiao J, et al. Circulating FGF21 levels are progressively increased from the early to end stages of chronic kidney diseases and are associated with renal function in Chinese. PLoS One. 2011; 6: e18398. doi: 10.1371/journal.pone.0018398 PMID: 21525989
    • (2011) PLoS One , vol.6 , pp. e18398
    • Lin, Z.1    Zhou, Z.2    Liu, Y.3    Gong, Q.4    Yan, X.5    Xiao, J.6
  • 26
    • 64549152937 scopus 로고    scopus 로고
    • Serum levels of the adipokine FGF21 depend on renal function
    • PMID: 18840768
    • Stein S, Bachmann A, Lossner U, Kratzsch J, Bluher M, Stumvoll M, et al. Serum levels of the adipokine FGF21 depend on renal function. Diabetes Care. 2009; 32: 126-128. doi: 10.2337/dc08-1054 PMID: 18840768
    • (2009) Diabetes Care , vol.32 , pp. 126-128
    • Stein, S.1    Bachmann, A.2    Lossner, U.3    Kratzsch, J.4    Bluher, M.5    Stumvoll, M.6
  • 27
    • 79952103793 scopus 로고    scopus 로고
    • FGF21 reloaded: Challenges of a rapidly growing field
    • PMID: 21194964
    • Kharitonenkov A, Larsen P FGF21 reloaded: challenges of a rapidly growing field. Trends Endocrinol Metab. 2011; 22: 81-86. doi: 10.1016/j.tem.2010.11.003 PMID: 21194964
    • (2011) Trends Endocrinol Metab , vol.22 , pp. 81-86
    • Kharitonenkov, A.1    Larsen, P.2
  • 28
    • 77957376253 scopus 로고    scopus 로고
    • Research resource: Comprehensive expression atlas of the fibroblast growth factor system in adult mouse
    • PMID: 20667984
    • Fon Tacer K, Bookout AL, Ding X, Kurosu H, John GB, Wang L, et al. Research resource: Comprehensive expression atlas of the fibroblast growth factor system in adult mouse. Mol Endocrinol. 2010; 24: 2050-2064. doi: 10.1210/me.2010-0142 PMID: 20667984
    • (2010) Mol Endocrinol , vol.24 , pp. 2050-2064
    • Fon Tacer, K.1    Bookout, A.L.2    Ding, X.3    Kurosu, H.4    John, G.B.5    Wang, L.6
  • 29
    • 84863637593 scopus 로고    scopus 로고
    • FGF21 promotes metabolic homeostasis via white adipose and leptin in mice
    • PMID: 22792234
    • Veniant MM, Hale C, Helmering J, Chen MM, Stanislaus S, Busby J, et al. FGF21 promotes metabolic homeostasis via white adipose and leptin in mice. PLoS One. 2012; 7: e40164. doi: 10.1371/journal. pone.0040164 PMID: 22792234
    • (2012) PLoS One , vol.7 , pp. e40164
    • Veniant, M.M.1    Hale, C.2    Helmering, J.3    Chen, M.M.4    Stanislaus, S.5    Busby, J.6
  • 30
    • 74049108945 scopus 로고    scopus 로고
    • Fibroblast growth factor 21: From pharmacology to physiology
    • PMID: 19906798
    • Kliewer SA, Mangelsdorf DJ Fibroblast growth factor 21: from pharmacology to physiology. Am J Clin Nutr. 2010; 91: 254S-257S. doi: 10.3945/ajcn.2009.28449B PMID: 19906798
    • (2010) Am J Clin Nutr , vol.91 , pp. 254S-257S
    • Kliewer, S.A.1    Mangelsdorf, D.J.2
  • 31
    • 84877272187 scopus 로고    scopus 로고
    • An FGF21-adiponectin-ceramide axis controls energy expenditure and insulin action in mice
    • PMID: 23663742
    • Holland WL, Adams AC, Brozinick JT, Bui HH, Miyauchi Y, Kusminski CM, et al. An FGF21-adiponectin-ceramide axis controls energy expenditure and insulin action in mice. Cell Metab. 2013; 17: 790-797. doi: 10.1016/j.cmet.2013.03.019 PMID: 23663742
    • (2013) Cell Metab , vol.17 , pp. 790-797
    • Holland, W.L.1    Adams, A.C.2    Brozinick, J.T.3    Bui, H.H.4    Miyauchi, Y.5    Kusminski, C.M.6
  • 32
    • 84877260638 scopus 로고    scopus 로고
    • Adiponectin mediates the metabolic effects of FGF21 on glucose homeostasis and insulin sensitivity in mice
    • PMID: 23663741
    • Lin Z, Tian H, Lam KS, Lin S, Hoo RC, Konishi M, et al. Adiponectin mediates the metabolic effects of FGF21 on glucose homeostasis and insulin sensitivity in mice. Cell Metab. 2013; 17: 779-789. doi: 10.1016/j.cmet.2013.04.005 PMID: 23663741
    • (2013) Cell Metab , vol.17 , pp. 779-789
    • Lin, Z.1    Tian, H.2    Lam, K.S.3    Lin, S.4    Hoo, R.C.5    Konishi, M.6
  • 33
    • 77954277205 scopus 로고    scopus 로고
    • Fibroblast growth factor 21 action in the brain increases energy expenditure and insulin sensitivity in obese rats
    • PMID: 20357365
    • Sarruf DA, Thaler JP, Morton GJ, German J, Fischer JD, Ogimoto K, et al. Fibroblast growth factor 21 action in the brain increases energy expenditure and insulin sensitivity in obese rats. Diabetes. 2010; 59: 1817-1824. doi: 10.2337/db09-1878 PMID: 20357365
    • (2010) Diabetes , vol.59 , pp. 1817-1824
    • Sarruf, D.A.1    Thaler, J.P.2    Morton, G.J.3    German, J.4    Fischer, J.D.5    Ogimoto, K.6
  • 34
    • 84879187565 scopus 로고    scopus 로고
    • LY2405319, an Engineered FGF21 Variant, Improves the Metabolic Status of Diabetic Monkeys
    • PMID: 23823755
    • Adams AC, Halstead CA, Hansen BC, Irizarry AR, Martin JA, Myers SR, et al. LY2405319, an Engineered FGF21 Variant, Improves the Metabolic Status of Diabetic Monkeys. PLoS One. 2013; 8: e65763. PMID: 23823755
    • (2013) PLoS One , vol.8 , pp. e65763
    • Adams, A.C.1    Halstead, C.A.2    Hansen, B.C.3    Irizarry, A.R.4    Martin, J.A.5    Myers, S.R.6
  • 35
    • 84861657962 scopus 로고    scopus 로고
    • Fundamentals of FGF19 & FGF21 action in vitro and in vivo
    • PMID: 22675463
    • Adams AC, Coskun T, Rovira AR, Schneider MA, Raches DW, Micanovic R, et al. Fundamentals of FGF19 & FGF21 action in vitro and in vivo. PLoS One. 2012; 7: e38438. doi: 10.1371/journal.pone.0038438 PMID: 22675463
    • (2012) PLoS One , vol.7 , pp. e38438
    • Adams, A.C.1    Coskun, T.2    Rovira, A.R.3    Schneider, M.A.4    Raches, D.W.5    Micanovic, R.6
  • 36
    • 84883151328 scopus 로고    scopus 로고
    • Fibroblast growth factor 21 improves insulin resistance and ameliorates renal injury in db/db mice
    • PMID: 23825123
    • Kim HW, Lee JE, Cha JJ, Hyun YY, Kim JE, Lee MH, et al. Fibroblast growth factor 21 improves insulin resistance and ameliorates renal injury in db/db mice. Endocrinology. 2013; 154: 3366-3376. doi: 10.1210/en.2012-2276 PMID: 23825123
    • (2013) Endocrinology , vol.154 , pp. 3366-3376
    • Kim, H.W.1    Lee, J.E.2    Cha, J.J.3    Hyun, Y.Y.4    Kim, J.E.5    Lee, M.H.6
  • 37
    • 79952803104 scopus 로고    scopus 로고
    • FGF19 regulates cell proliferation, glucose and bile acid metabolism via FGFR4-dependent and independent pathways
    • PMID: 21437243
    • Wu AL, Coulter S, Liddle C, Wong A, Eastham-Anderson J, French DM, et al. FGF19 regulates cell proliferation, glucose and bile acid metabolism via FGFR4-dependent and independent pathways. PLoS One. 2011; 6: e17868. doi: 10.1371/journal.pone.0017868 PMID: 21437243
    • (2011) PLoS One , vol.6 , pp. e17868
    • Wu, A.L.1    Coulter, S.2    Liddle, C.3    Wong, A.4    Eastham-Anderson, J.5    French, D.M.6
  • 38


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.