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DRUG:

Evrenzo (roxadustat)

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Other names: FG-4592, ASP1517, ASP 1517, ASP-1517, FG4592, FG 4592, AZD9941, AZD 9941, AZD-9941
Associations
Trials
Company:
Astellas, AstraZeneca, Kyntra Bio
Drug class:
Hypoxia-inducible factor prolyl hydroxylase inhibitor
Associations
Trials
2ms
Roxadustat induces erythroid differentiation of erythroleukemia cells through the hypoxia inducible factor-α / GATA binding protein 1 axis. (PubMed, Cell Signal)
Roxadustat induces erythropoiesis in erythroleukemia primarily by targeting HIF-2α and was partially GATA1-dependent. Besides upregulating erythropoietin, our study revealed the HIF-α/GATA1 axis as another critical regulatory mechanism for hypoxia-driven erythropoiesis.
Journal
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HIF1A (Hypoxia inducible factor 1, alpha subunit) • EPAS1 (Endothelial PAS domain protein 1) • GATA1 (GATA Binding Protein 1)
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imatinib • Jakafi (ruxolitinib) • Evrenzo (roxadustat)
2ms
Lactic acid promotes an MDSC-like phenotype via HIF1α stabilization with impact on prognosis in renal cell carcinoma. (PubMed, Cancer Lett)
In line, the HIF1α-stabilizing drug Roxadustat increased the number of CD14+ HLA-DR low cells...Our data dissect the intratumoral network of RCC and show that tumor-derived lactate promotes a pro-tumorigenic myeloid phenotype with low MHC-II but high immune-checkpoint, LOX-1 and S100A8/9 expression. Blocking MCT disrupts this interplay, offering a promising strategy to re-educate tumor-associated myeloid cells and enhance tumor immune surveillance.
Journal
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IL6 (Interleukin 6) • HIF1A (Hypoxia inducible factor 1, alpha subunit) • S100A8 (S100 Calcium Binding Protein A8) • CD14 (CD14 Molecule)
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Evrenzo (roxadustat)
3ms
New trial
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Evrenzo (roxadustat)
3ms
Concerns from bench and insights from bedside: the puzzle of Roxadustat in cancer patients with chemotherapy-induced anemia. (PubMed, Front Pharmacol)
Consequently, Roxadustat poses a clinical dilemma: its efficacy in CIA offers a promising ESAs alternative, but its HIF-driven oncogenic potential necessitates long-term safety assessment in cancer patients. Future studies must prioritize longitudinal monitoring to define the benefit-risk profile.
Review • Journal
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HIF1A (Hypoxia inducible factor 1, alpha subunit)
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Evrenzo (roxadustat)
3ms
A Study of Roxadustat to Treat Anemia in Children and Teenagers With Chronic Kidney Disease (clinicaltrials.gov)
P3, N=100, Recruiting, Astellas Pharma Global Development, Inc. | Trial completion date: Sep 2026 --> Oct 2027 | Trial primary completion date: Nov 2025 --> Oct 2027
Trial completion date • Trial primary completion date
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Evrenzo (roxadustat)
4ms
Genetic variation in targets of roxadustat and risk of common cancers: A Mendelian randomization analysis. (PubMed, Clin Nephrol)
Our findings support a potential causal relationship between the inhibition of EGLN1 and EGLN2 and the development of specific cancer types.
Journal
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ER (Estrogen receptor) • HIF1A (Hypoxia inducible factor 1, alpha subunit) • EGLN1 (Egl-9 Family Hypoxia Inducible Factor 1)
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Evrenzo (roxadustat)
4ms
Panaxadiol inhibits the proliferation and immune evasion of esophageal squamous cell carcinoma cells by suppressing HIF-1α/STAT3/PD-L1 pathway. (PubMed, Gene)
Panaxadiol suppresses cell proliferation, immunological evasion, and tumor formation in ESCC by inhibiting PD-L1 expression through the suppression of HIF-1α and STAT3.
Journal • PD(L)-1 Biomarker • IO biomarker
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MYC (V-myc avian myelocytomatosis viral oncogene homolog) • CD8 (cluster of differentiation 8) • PD-1 (Programmed cell death 1) • CCND1 (Cyclin D1) • IFNG (Interferon, gamma) • HIF1A (Hypoxia inducible factor 1, alpha subunit) • IL10 (Interleukin 10) • IL4 (Interleukin 4)
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PD-L1 expression • LDH elevation
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Evrenzo (roxadustat)
5ms
PANGU-stepup: Pegmolesatide Treatment for Anemia in Patients Undergoing Long-term Dialysis (clinicaltrials.gov)
P4, N=240, Recruiting, Chinese PLA General Hospital | Not yet recruiting --> Recruiting
Enrollment open
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Evrenzo (roxadustat)
6ms
New P4 trial
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Evrenzo (roxadustat)
7ms
Observation of the Impact of Hypoxia - Inducible Factor Prolyl Hydroxylase Inhibitors on Sarcopenia in Hemodialysis Patients (ChiCTR2500106730)
P4, N=60, Not yet recruiting, Department of Nephrology, Tianjin Medical University General Hospital; Department of Nephrology, Tianjin Medical University General Hospital
New P4 trial
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Evrenzo (roxadustat)
7ms
Post-marketing Surveillance of EVRENZO® Tablets (Roxadustat) in Patients With Renal Anemia (clinicaltrials.gov)
P=N/A, N=2104, Completed, Astellas Pharma Inc | Active, not recruiting --> Completed
Trial completion • Real-world evidence
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Evrenzo (roxadustat)
7ms
Prolyl Hydroxylase Inhibitor-Mediated HIF Activation Drives Transcriptional Reprogramming in Retinal Pigment Epithelium: Relevance to Chronic Kidney Disease. (PubMed, Cells)
Overall, Roxadustat triggered complex gene expression changes without promoting inflammation or oxidative stress in RPE cells. Despite these findings, ophthalmologic monitoring is advised during PHI treatment in CKD patients receiving HIF-PHIs.
Journal
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IL6 (Interleukin 6) • TNFA (Tumor Necrosis Factor-Alpha) • CXCL8 (Chemokine (C-X-C motif) ligand 8) • SLC2A1 (Solute Carrier Family 2 Member 1)
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Evrenzo (roxadustat)