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Roxadustat

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https://www.readbyqxmd.com/read/27470678/hypoxia-inducible-factor-1-plays-a-role-in-phosphate-induced-vascular-smooth-muscle-cell-calcification
#1
Sophie Mokas, Richard Larivière, Laurent Lamalice, Stéphane Gobeil, David N Cornfield, Mohsen Agharazii, Darren E Richard
Medial vascular calcification is a common complication of chronic kidney disease (CKD). Although elevated inorganic phosphate stimulates vascular smooth muscle cell (VSMC) osteogenic transdifferentiation and calcification, the mechanisms involved in their calcification during CKD are not fully defined. Because hypoxic gene activation is linked to CKD and stimulates bone cell osteogenic differentiation, we used in vivo and in vitro rodent models to define the role of hypoxic signaling during elevated inorganic phosphate-induced VSMC calcification...
September 2016: Kidney International
https://www.readbyqxmd.com/read/27352308/effect-of-moderate-hepatic-impairment-on-the-pharmacokinetics-and-pharmacodynamics-of-roxadustat-an-oral-hypoxia-inducible-factor-prolyl-hydroxylase-inhibitor
#2
Dorien Groenendaal-van de Meent, Martin den Adel, Jan Noukens, Sanne Rijnders, Axel Krebs-Brown, Lyudmila Mateva, Assen Alexiev, Marloes Schaddelee
BACKGROUND AND OBJECTIVE: Roxadustat is a hypoxia-inducible factor prolyl hydroxylase inhibitor in phase III development for the treatment of anaemia associated with chronic kidney disease. This study evaluated the effects of moderate hepatic impairment on roxadustat pharmacokinetics, pharmacodynamics and tolerability. METHODS: This was an open-label study in which eight subjects with moderate hepatic impairment (liver cirrhosis Child-Pugh score 7-9) and eight subjects with normal hepatic function (matched for body mass index, age and sex) received a single oral 100 mg roxadustat dose under fasted conditions...
September 2016: Clinical Drug Investigation
https://www.readbyqxmd.com/read/27122198/investigational-therapies-for-renal-disease-induced-anemia
#3
Holger Schmid, Wolfgang Jelkmann
INTRODUCTION: The main pillars for the treatment of chronic kidney disease (CKD) associated anemia are peptidic erythropoiesis stimulating agents (ESAs) and iron preparations. Both approaches benefit from long-term efficacy and safety data but are surrounded by clinical and economic concerns, driving the search for novel anti-anemic drugs. AREAS COVERED: By answering pivotal questions, the authors describe the recent developments of next generation ESAs, introduce cutting-edge iron formulations and focus on investigational approaches that interact with pathways involved in erythropoietin (Epo) synthesis and myeloid hematopoiesis...
August 2016: Expert Opinion on Investigational Drugs
https://www.readbyqxmd.com/read/27094610/oral-hypoxia-inducible-factor-prolyl-hydroxylase-inhibitor-roxadustat-fg-4592-for-the-treatment-of-anemia-in-patients-with-ckd
#4
Robert Provenzano, Anatole Besarab, Chao H Sun, Susan A Diamond, John H Durham, Jose L Cangiano, Joseph R Aiello, James E Novak, Tyson Lee, Robert Leong, Brian K Roberts, Khalil G Saikali, Stefan Hemmerich, Lynda A Szczech, Kin-Hung Peony Yu, Thomas B Neff
BACKGROUND AND OBJECTIVES: Roxadustat (FG-4592), an oral hypoxia-inducible factor prolyl hydroxylase inhibitor that stimulates erythropoiesis, regulates iron metabolism, and reduces hepcidin, was evaluated in this phase 2b study for safety, efficacy, optimal dose, and dose frequency in patients with nondialysis CKD. DESIGN, SETTING, PARTICIPANTS, & MEASUREMENTS: The 145 patients with nondialysis CKD and hemoglobin ≤10.5 g/dl were randomized into one of six cohorts of approximately 24 patients each with varying roxadustat starting doses (tiered weight and fixed amounts) and frequencies (two and three times weekly) followed by hemoglobin maintenance with roxadustat one to three times weekly...
June 6, 2016: Clinical Journal of the American Society of Nephrology: CJASN
https://www.readbyqxmd.com/read/27091985/comparative-systems-pharmacology-of-hif-stabilization-in-the-prevention-of-retinopathy-of-prematurity
#5
George Hoppe, Suzy Yoon, Banu Gopalan, Alexandria R Savage, Rebecca Brown, Kelsey Case, Amit Vasanji, E Ricky Chan, Randi B Silver, Jonathan E Sears
Retinopathy of prematurity (ROP) causes 100,000 new cases of childhood blindness each year. ROP is initiated by oxygen supplementation necessary to prevent neonatal death. We used organ systems pharmacology to define the transcriptomes of mice that were cured of oxygen-induced retinopathy (OIR, ROP model) by hypoxia-inducible factor (HIF) stabilization via HIF prolyl hydroxylase inhibition using the isoquinolone Roxadustat or the 2-oxoglutarate analog dimethyloxalylglycine (DMOG). Although both molecules conferred a protective phenotype, gene expression analysis by RNA sequencing found that Roxadustat can prevent OIR by two pathways: direct retinal HIF stabilization and induction of aerobic glycolysis or indirect hepatic HIF-1 stabilization and increased serum angiokines...
May 3, 2016: Proceedings of the National Academy of Sciences of the United States of America
https://www.readbyqxmd.com/read/26947173/the-hypoxia-inducible-factor-prolyl-hydroxylase-inhibitor-roxadustat-fg-4592-and-warfarin-in-healthy-volunteers-a-pharmacokinetic-and-pharmacodynamic-drug-drug-interaction-study
#6
Dorien Groenendaal-van de Meent, Martin den Adel, Sanne Rijnders, Axel Krebs-Brown, Virginie Kerbusch, Georg Golor, Marloes Schaddelee
PURPOSE: Roxadustat is a small-molecule hypoxia-inducible factor prolyl-hydroxylase inhibitor in late-stage clinical development for the treatment of anemia in patients with chronic kidney disease (CKD). Warfarin is an oral anticoagulant with a narrow therapeutic window that is often prescribed to treat coexisting cardiovascular diseases in patients with CKD. This clinical trial was designed to evaluate the effect of roxadustat on warfarin pharmacokinetic and pharmacodynamic parameters...
April 2016: Clinical Therapeutics
https://www.readbyqxmd.com/read/26846333/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
#7
Robert Provenzano, Anatole Besarab, Steven Wright, Sohan Dua, Steven Zeig, Peter Nguyen, Lona Poole, Khalil G Saikali, Gopal Saha, Stefan Hemmerich, Lynda Szczech, K H Peony Yu, Thomas B Neff
BACKGROUND: Roxadustat (FG-4592) is an oral hypoxia-inducible factor prolyl-hydroxylase inhibitor that promotes erythropoiesis through increasing endogenous erythropoietin, improving iron regulation, and reducing hepcidin. STUDY DESIGN: Phase 2, randomized (3:1), open-label, active-comparator, safety and efficacy study. SETTING & PARTICIPANTS: Patients with stable end-stage renal disease treated with hemodialysis who previously had hemoglobin (Hb) levels maintained with epoetin alfa...
June 2016: American Journal of Kidney Diseases: the Official Journal of the National Kidney Foundation
https://www.readbyqxmd.com/read/26494833/roxadustat-fg-4592-correction-of-anemia-in-incident-dialysis-patients
#8
RANDOMIZED CONTROLLED TRIAL
Anatole Besarab, Elena Chernyavskaya, Igor Motylev, Evgeny Shutov, Lalathaksha M Kumbar, Konstantin Gurevich, Daniel Tak Mao Chan, Robert Leong, Lona Poole, Ming Zhong, Khalil G Saikali, Marietta Franco, Stefan Hemmerich, Kin-Hung Peony Yu, Thomas B Neff
Safety concerns with erythropoietin analogues and intravenous (IV) iron for treatment of anemia in CKD necessitate development of safer therapies. Roxadustat (FG-4592) is an orally bioavailable hypoxia-inducible factor (HIF) prolyl hydroxylase inhibitor that promotes coordinated erythropoiesis through HIF-mediated transcription. We performed an open-label, randomized hemoglobin (Hb) correction study in anemic (Hb≤10.0 g/dl) patients incident to hemodialysis (HD) or peritoneal dialysis (PD). Sixty patients received no iron, oral iron, or IV iron while treated with roxadustat for 12 weeks...
April 2016: Journal of the American Society of Nephrology: JASN
https://www.readbyqxmd.com/read/26238121/randomized-placebo-controlled-dose-ranging-and-pharmacodynamics-study-of-roxadustat-fg-4592-to-treat-anemia-in-nondialysis-dependent-chronic-kidney-disease-ndd-ckd-patients
#9
RANDOMIZED CONTROLLED TRIAL
Anatole Besarab, Robert Provenzano, Joachim Hertel, Raja Zabaneh, Stephen J Klaus, Tyson Lee, Robert Leong, Stefan Hemmerich, Kin-Hung Peony Yu, Thomas B Neff
BACKGROUND: Roxadustat (FG-4592) is an oral hypoxia-inducible factor prolyl hydroxylase inhibitor that stimulates erythropoiesis. This Phase 2a study tested efficacy (Hb response) and safety of roxadustat in anemic nondialysis-dependent chronic kidney disease (NDD-CKD) subjects. METHODS: NDD-CKD subjects with hemoglobin (Hb) ≤11.0 g/dL were sequentially enrolled into four dose cohorts and randomized to roxadustat or placebo two times weekly (BIW) or three times weekly (TIW) for 4 weeks, in an approximate roxadustat:placebo ratio of 3:1...
October 2015: Nephrology, Dialysis, Transplantation
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