Roxadustat in the treatment of anaemia in chronic kidney disease

References

• Kausz AT, Levey AS. The care of patients with chronic kidney disease. J Gen Intern Med. 2002;17:658–662.
   PubMed Web of Science ®Google Scholar
• Pisoni RL, Bragg-Gresham JL, Young EW, et al. Anemia management and outcomes from 12 countries in the dialysis outcomes and practice patterns study (DOPPS). Am J Kidney Dis. 2004;44(1):94–111.
   PubMed Web of Science ®Google Scholar
• De Nicola L, Minutolo R, Chiodini P, et al. Prevalence and prognosis of mild anemia in non-dialysis chronic kidney disease: a prospective cohort study in outpatient renal clinics. Am J Nephrol. 2010;32(6):533–540.
   PubMed Web of Science ®Google Scholar
• Eriksson D, Goldsmith D, Teitsson S, et al. Cross-sectional survey in CKD patients across Europe describing the association between quality of life and anaemia. BMC Nephrol. 2016;17(1):97.
   PubMedGoogle Scholar
• Pfeffer MA, Burdmann EA, Chen CY, et al. A trial of darbepoetin alfa in type 2 diabetes and chronic kidney disease. N Engl J Med. 2009;361(21):2019–2032.
   PubMed Web of Science ®Google Scholar
• Semenza GL, Nejfelt MK, Chi SM, et al. Hypoxia-inducible nuclear factors bind to an enhancer element located 3’ to the human erythropoietin gene. Proc Natl Acad Sci U S A. 1991;88(13):5680–5684.
   PubMed Web of Science ®Google Scholar
• Wang GL, Semenza GL. Purification and characterization of hypoxia-inducible factor 1. J Biol Chem. 1995;270(3):1230–1237.
   PubMed Web of Science ®Google Scholar
• Safran M, Kim WY, O’Connell F, et al. Mouse model for noninvasive imaging of HIF prolyl hydroxylase activity: assessment of an oral agent that stimulates erythropoietin production. Proc Natl Acad Sci USA. 2006;103:105–110.
   PubMed Web of Science ®Google Scholar
• Bernhardt WM, Wiesener MS, Scigalla P, et al. Inhibition of prolyl hydroxylases increases erythropoietin production in ESRD. J Am Soc Nephrol. 2010;21(12):2151–2156.
   PubMed Web of Science ®Google Scholar
• Webb JD, Coleman ML, Pugh CW. Hypoxia, hypoxia-inducible factors (HIF), HIF hydroxylases and oxygen sensing. Cell Mol Life Sci. 2009;66(22):3539–3554.
   PubMed Web of Science ®Google Scholar
• Semenza GL. Hypoxia-inducible factors in physiology and medicine. Cell. 2012;148(3):399–408.
   PubMed Web of Science ®Google Scholar
• Kapitsinou PP, Liu Q, Unger TL, et al. Hepatic HIF-2 regulates erythropoietic responses to hypoxia in renal anemia. Blood. 2010;116(16):3039–3048.
   PubMed Web of Science ®Google Scholar
• Scortegagna M, Ding K, Zhang Q, et al. HIF-2alpha regulates murine hematopoietic development in an erythropoietin-dependent manner. Blood. 2005;105(8):3133–3140.
   PubMed Web of Science ®Google Scholar
• Mastrogiannaki M, Matak P, Keith B, et al. HIF-2alpha, but not HIF-1alpha, promotes iron absorption in mice. J Clin Invest. 2009;119(5):1159–1166.
   PubMed Web of Science ®Google Scholar
• Duan C. Hypoxia-inducible factor 3 biology: complexities and emerging themes. Am J Physiol Cell Physiol. 2016;310:C260–9.
   PubMed Web of Science ®Google Scholar
• Lisy K, Peet DJ. Turn me on: regulating HIF transcriptional activity. Cell Death Differ. 2008;15:642–649.
   PubMed Web of Science ®Google Scholar
• Palazon A, Goldrath AW, Nizet V, et al. HIF transcription factors, inflammation, and immunity. Immunity. 2014;41(4):518–528.
   PubMed Web of Science ®Google Scholar
• Maxwell PH, Wiesener MS, Chang GW, et al. The tumour suppressor protein VHL targets hypoxia-inducible factors for oxygen-dependent proteolysis. Nature. 1999;399:271–275.
   PubMed Web of Science ®Google Scholar
• Majmundar AJ, Wong WJ, Simon MC. Hypoxia-inducible factors and the response to hypoxic stress. Mol Cell. 2010;40(2):294–309.
   PubMed Web of Science ®Google Scholar
• Kim SY, Yang EG. Recent advances in developing inhibitors for hypoxia-inducible factor prolyl hydroxylases and their therapeutic implications. Molecules. 2015;20(11):20551–20568.
   PubMed Web of Science ®Google Scholar
• Takeda K, Cowan A, Fong G. Essential role for prolyl hydroxylase domain protein 2 in oxygen homeostasis of the adult vascular system. Circulation. 2007;116:774–781.
   PubMed Web of Science ®Google Scholar
• Percy MJ, Furlow PW, Beer PA, et al. A novel erythrocytosis-associated PHD2 mutation suggests the location of a HIF binding groove. Blood. 2007;110(6):2193–2196.
   PubMed Web of Science ®Google Scholar
• Oliver K, Taylor C, Cummins E. Hypoxia regulation of NF_B signalling during inflammation: the role of hydroxylases. Arthritis Res Therapy. 2009;11:215.
   PubMed Web of Science ®Google Scholar
• Zhang Q, Gu J, Li L, et al. Control of cyclin D1 and breast tumorigenesis by the EglN2 prolyl hydroxylase. Cancer Cell. 2009;16:413–424.
   PubMed Web of Science ®Google Scholar
• Place TL, Domann FE. Prolyl-hydroxylase 3: evolving roles for an ancient signaling protein. Hypoxia. 2013;1:13–17.
   PubMedGoogle Scholar
• Barrett TD, Palomino HL, Brondstetter TI, et al. Pharmacological characterization of 1-(5-chloro-6-(trifluoromethoxy)-1H-benzoimidazol-2-yl)-1H-pyrazole-4-carboxylic acid (JNJ-42041935), a potent and selective hypoxia-inducible factor prolyl hydroxylase inhibitor. Mol Pharmacol. 2011;79:910–920.
   PubMed Web of Science ®Google Scholar
• Souma T, Nezu M, Nakano D, et al. Erythropoietin synthesis in renal myofibroblasts is restored by activation of hypoxia signaling. J Am Soc Nephrol. 2016;27(2):428–438.
   PubMed Web of Science ®Google Scholar
• Tojo Y, Sekine H, Hirano I, et al. Hypoxia signaling cascade for erythropoietin production in hepatocytes. Mol Cell Biol. 2015;35(15):2658–2672.
   PubMed Web of Science ®Google Scholar
• Koury MJ, Haase VH. Anaemia in kidney disease: harnessing hypoxia responses for therapy. Nat Rev Nephrol. 2015;11(7):394–410.
   PubMed Web of Science ®Google Scholar
• Nicolas G, Chauvet C, Viatte L, et al. The gene encoding the iron regulatory peptide hepcidin is regulated by anemia, hypoxia, and inflammation. J Clin Invest. 2002;110:1037–1044.
   PubMed Web of Science ®Google Scholar
• Peyssonnaux C, Zinkernagel AS, Schuepbach RA, et al. Regulation of iron homeostasis by the hypoxia-inducible transcription factors (HIFs). J Clin Invest. 2007;117:1926–1932.
   PubMed Web of Science ®Google Scholar
• Mastrogiannaki M, Matak P, Mathieu JR, et al. Hepatic hypoxia-inducible factor-2 down-regulates hepcidin expression in mice through an erythropoietin-mediated increase in erythropoiesis. Haematologica. 2012;97:827–834.
   PubMed Web of Science ®Google Scholar
• Liu Q, Davidoff O, Niss K, et al. Hypoxia-inducible factor regulates hepcidin via erythropoietin-induced erythropoiesis. J Clin Invest. 2012;122:4635–4644.
   PubMed Web of Science ®Google Scholar
• Schodel J, Oikonomopoulos S, Ragoussis J, et al. High-resolution genome-wide mapping of HIF-binding sites by ChIP-seq. Blood. 2011;117:e207–e217.
   PubMed Web of Science ®Google Scholar
• Kautz L, Jung G, Nemeth E, et al. Erythroferrone contributes to recovery from anemia of inflammation. Blood. 2014;124:2569–2574.
   PubMed Web of Science ®Google Scholar
• Seeley TW. Novel and beneficial pharmacodynamic properties of endogenous EPO and ‘complete erythropoiesis’ induced by selective HIF prolyl hydroxylase inhibitors [abstract]. J Am Soc Nephrol. 2005;16:761A.
   Google Scholar
• Groenendaal-Van De Meent D, Adel MD, Noukens J, et al. Effect of moderate hepatic impairment on the pharmacokinetics and pharmacodynamics of roxadustat, an oral hypoxia-inducible factor prolyl hydroxylase inhibitor. Clin Drug Investig. 2016;36(9):743–751.
   PubMed Web of Science ®Google Scholar
• Groenendaal-Van De Meent D, Den Adel M, Rijnders S, et al. The hypoxia-inducible factor prolyl-hydroxylase inhibitor roxadustat (fg-4592) and warfarin in healthy volunteers: a pharmacokinetic and pharmacodynamic drug-drug interaction study. Clin Ther. 2016;38(4):918–928.
   PubMed Web of Science ®Google Scholar
• Besarab A, Provenzano R, Hertel J, et al. Randomized placebo-controlled dose-ranging and pharmacodynamics study of roxadustat (FG-4592) to treat anemia in nondialysis-dependent chronic kidney disease (NDD-CKD) patients. Nephrol Dial Transplant. 2015;30(10):1665–1673.
   PubMed Web of Science ®Google Scholar
• Provenzano R, Besarab A, Sun CH, et al. Oral hypoxia-inducible factor prolyl hydroxylase inhibitor roxadustat (fg-4592) for the treatment of anemia in patients with CKD. Clin J Am Soc Nephrol. 2016;11(6):982–991.
   PubMed Web of Science ®Google Scholar
• Provenzano R, Besarab A, Wright S, et al. Roxadustat (fg-4592) versus epoetin alfa for anemia in patients receiving maintenance hemodialysis: a phase 2, randomized, 6- to 19-week, open-label, active-comparator, dose-ranging, safety and exploratory efficacy study. Am J Kidney Dis. 2016;67:912–924.
   PubMed Web of Science ®Google Scholar
• Besarab A, Chernyavskaya E, Motylev I, et al. Roxadustat (FG-4592): correction of anemia in incident dialysis patients. J Am Soc Nephrol. 2016;27:1225–1233.
   PubMed Web of Science ®Google Scholar
• Chen N, Qian J, Chen J, et al. Phase 2 studies of oral hypoxia-inducible factor prolyl hydroxylase inhibitor FG-4592 for treatment of anemia in China. Nephrol Dial Transplant. 2017;32(8):1373–1386.
   PubMed Web of Science ®Google Scholar
• Szczech LH, Besarab A, Saikali KG, et al. TH-OR039 anemia correction with roxadustat improves health related quality of life (HRQOL) in chronic kidney disease (CKD) patients [abstract]. J Am Soc Nephrol. 2015;Supplement 26:11.
   Google Scholar
• cited 2017 Oct 26. Available from: https://globenewswire.com/news-release/2017/01/30/911927/0/en/FibroGen-s-Roxadustat-FG-4592-Meets-Primary-Endpoints-in-Two-Phase-3-Anemia-Studies-in-China.html
   Google Scholar
• Thomas B, Matsushita K, Abate KH, et al. Global cardiovascular and renal outcomes of reduced GFR. J Am Soc Nephrol. 2017;28(7):2167–2179.
   PubMed Web of Science ®Google Scholar
• cited 2017 Oct 26. Available from: https://globenewswire.com/news-release/2017/10/18/1149112/0/en/FibroGen-Announces-Acceptance-by-China-FDA-of-Roxadustat-New-Drug-Application-NDA-for-Treatment-of-Anemia-Associated-With-Dialysis-and-Non-Dialysis-Chronic-Kidney-Disease-CKD.html
   Google Scholar
• Baigent C, Landray MJ, Reith C, et al. The effects of lowering LDL cholesterol with simvastatin plus ezetimibe in patients with chronic kidney disease (Study of heart and renal protection): a randomised placebo-controlled trial. Lancet. 2011;377(9784):2181–2192.
   PubMed Web of Science ®Google Scholar
• Gale DP, Harten SK, Reid CD, et al. Autosomal dominant erythrocytosis and pulmonary arterial hypertension associated with an activating HIF2 alpha mutation. Blood. 2008;112(3):919–921.
   PubMed Web of Science ®Google Scholar
• Yeh TL, Leissing TM, Abboud MI, et al. Molecular and cellular mechanisms of HIF prolyl hydroxylase inhibitors in clinical trials. Chem Sci. 2017;8:7651.
   PubMed Web of Science ®Google Scholar
• Chowdhury R, Leung IKH, Tian HM, et al. Structural basis for oxygen degradation domain selectivity of the HIF prolyl hydroxylases. Nat Commun. 2016;7:12673.
   PubMed Web of Science ®Google Scholar