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- | Retrospective data, Journal: Hypoxia-Inducible Factor Prolyl Hydroxylase Inhibitors for Anemia in Non-Dialysis Dependent Chronic Kidney Disease: Systematic Review and Meta-Analysis of Randomized Controlled Trials. (Pubmed Central) - Mar 10, 2025
Broadly, HIF-PHI molecules exhibited little difference when compared to other alternatives like erythropoietin stimulating agents (ESAs), but the evidence is not of high certainty. Our meta-analysis provides evidence on the use of HIF-PHIs as an alternative to ESAs for anemia in NDD-CKDs.
- | Retrospective data, Journal: Hypoxia-Inducible Factor Prolyl Hydroxylase Inhibitors for Anemia in Dialysis-Dependent Chronic Kidney Disease: Systematic Review and Meta-Analysis of Randomized Controlled Trials. (Pubmed Central) - Mar 10, 2025
Roxadustat increased treatment-emergent adverse events up to 6-52 weeks as compared to ESAs [OR: 1.45 (95% CI 1.08-1.96); p = 0.01; six studies; 1715 participants; moderate certainty evidence]. The study provided evidence on the use of HIF-PHIs for treating renal anemia in DD-CKD patients as an alternative to ESAs.
- | Journal: Bioanalysis, Analysis, Chemistry, and Pharmacological Aspects of Hypoxia-Inducible Factor Prolyl Hydroxylase Inhibitors. (Pubmed Central) - Jan 12, 2025
Research indicates that most studies concentrate on hyphenated methodologies for drug estimation in various biological fluids. Consequently, this study assesses the biological efficacy of HIF-PHIs and elucidates the analytical methodologies currently employed for measurement across various matrices.
- | Journal: The comparison of four hypoxia-inducible factor prolyl hydroxylase inhibitors on drug potency and cost for treatment in patients with renal anemia. (Pubmed Central) - Nov 16, 2024
The difference in dose escalation for anemia treatment among HIF-PHIs is due to differences in drug potency, where the HPI significantly differs among HIF-PHIs. The disparity between the HPI and the cost of the initial dose accounts for the variance in the daily costs of renal anemia treatment among HIF-PHIs.
- ||||| Musredo (molidustat) / Bayer
Enrollment closed: A Study to Learn More About the Long-term Safety and Effectiveness of Molidustat as a Treatment for Japanese Men and Women With Renal Anemia (clinicaltrials.gov) - Sep 20, 2024
P=N/A, N=1081, Active, not recruiting, Sponsor: Bayer
The disparity between the HPI and the cost of the initial dose accounts for the variance in the daily costs of renal anemia treatment among HIF-PHIs. Recruiting --> Active, not recruiting
- | Musredo (molidustat) / Bayer, Evrenzo (roxadustat) / FibroGen
Journal: Pharmacological induction of the hypoxia response pathway in Huh7 hepatoma cells limits proliferation but increases resilience under metabolic stress. (Pubmed Central) - Jul 30, 2024
This was accompanied by a higher resistance to the inhibition of mitochondrial respiration by antimycin A, a phenotype confirmed in Roxadustat-treated Huh7 cells and Molidustat-treated hepatoblastoma cells (Huh6 and HepG2). Overall, this study shows that HIF-inducing drugs increase the metabolic resilience of liver cancer cells to metabolic stressors, arguing for careful monitoring of patients treated with HIF-inducing drugs, especially when they are at risk of liver cancer.
- | Journal: A Prospective Randomized Controlled Clinical Study to Investigate the Efficacy and Safety of Hypoxia-Inducible Factor-Prolyl Hydroxylase Inhibitors in Non-Dialysis Patients with Chronic Heart Failure and Renal Anemia Switched from Continuous Erythropoietin Receptor Activator Treatment. (Pubmed Central) - May 25, 2024
The individual HIF-PH inhibitors appear to have different effects on anemia and thyroid function. However, because this was a single-center study with a limited sample size, the efficacy and potential limitations of HIF-PH inhibitors need to be further clarified.
- || Musredo (molidustat) / Bayer
Retrospective data, Review, Journal: The efficacy and safety of molidustat for anemia in dialysis-dependent and non-dialysis-dependent chronic kidney disease patients: A systematic review and meta-analysis. (Pubmed Central) - May 20, 2024
There was no significant difference in the incidence of severe adverse events (SAEs), death, and cardio-related adverse events between molidustat and the ESAs groups. Moricizine can effectively improves Hb levels in NDD patients and corrects anemia in DD patients without increasing adverse event incidence.
- | Preclinical, Journal: The drug-specific properties of hypoxia-inducible factor-prolyl hydroxylase inhibitors in mice reveal a significant contribution of the kidney compared to the liver to erythropoietin induction. (Pubmed Central) - Apr 13, 2024
Renal EPO induction is the major target of HIF-PH inhibitors for their therapeutic effects on erythropoiesis. Additionally, the drug-specific properties of HIF-PH inhibitors in EPO induction and iron metabolism have been shown in mice, providing useful information for selecting the proper HIF-PH inhibitor for each renal anemia patient.
- | Journal: New Therapeutic Strategies in the Treatment of CKD Anemia: Hypoxia-Induced Factor Prolyl-Hydroxylase Inhibitors (Pubmed Central) - Dec 1, 2023
The drugs currently produced are roxadustat, daprodustat, vadadustat, molidustat, desidustat, and enarodustat; among these only roxadustat is currently approved and usable in Italy. The possibility of oral intake, pleiotropic activity on martial and lipidic metabolism, and the non-inferiority compared to erythropoietins make these drugs a valid alternative to the treatment of anemia associated with chronic kidney disease in the nephrologist practice.
- | Musredo (molidustat) / Bayer
Journal: Use of molidustat, a hypoxia-inducible factor prolyl hydroxylase inhibitor, in chronic kidney disease-associated anemia in cats. (Pubmed Central) - Sep 23, 2023
Daily PO molidustat administration may stimulate a clinically relevant erythropoietic response in anemic cats with CKD. This HIF-PH inhibitor may be an alternative for managing anemia in cats compared to recombinant EPO treatment.
- || Retrospective data, Review: Safety of HIF prolyl hydroxylase inhibitors for anemia in dialysis patients: a systematic review and network meta-analysis. (Pubmed Central) - Jun 9, 2023
Although HIF-PHIs did not show significant differences from ESAs in terms of overall AEs and SAEs, statistical differences in gastrointestinal disorder, hypertension, and vascular-access complications were observed between HIF-PHIs, which deserved to be noted in clinical decision making. Systematic review registration: This study is registered with PROSPERO (registration number CRD42022312252).
- | Musredo (molidustat) / Bayer, Aranesp (darbepoetin alfa) / Amgen, Kyowa Kirin
Retrospective data, Journal: Treatment satisfaction with molidustat in CKD-related anemia in non-dialysis patients: a post-hoc analysis of two clinical trials. (Pubmed Central) - May 7, 2023
P3
Systematic review registration: This study is registered with PROSPERO (registration number CRD42022312252). These patient-reported satisfaction outcomes support the use of molidustat as a patient-centered treatment option for CKD-related anemia.
- HIFS AND BUTS : A NETWORK META-ANALYSIS OF HIF-PH INHIBITORS & ESAS IN NDD-CKD PATIENTS WITH ANEMIA COMPARING THEIR SAFETY AND EFFICACY (Focussed Oral Room 8) - May 4, 2023 - Abstract #ERAEDTA2023ERA_EDTA_1234;
These patient-reported satisfaction outcomes support the use of molidustat as a patient-centered treatment option for CKD-related anemia. Compared to ESA, all HIF-PHIs increased risk for SAEs (daprodustat of RR, 1.21[95 % CI, 0.825
- CHARACTERISTICS OF PATIENTS WITH CKD WHO USE HYPOXIA-INDUCIBLE FACTOR PROLYL HYDROXYLASE INHIBITORS: A JAPAN MEDICAL DATA CENTER DATABASE STUDY (Focussed Oral Room 8) - May 4, 2023 - Abstract #ERAEDTA2023ERA_EDTA_1084;
Our analysis found most patients initiating on HIF-PHIs were male, had previous rhEPO use, and had history of hypertension and diabetes. Understanding patient profiles in a real-world setting may guide treatment decisions in clinical practice.
- | Retrospective data, Journal: A network meta-analysis of the efficacy of hypoxia-inducible factor prolyl-hydroxylase inhibitors in dialysis chronic kidney disease. (Pubmed Central) - Apr 10, 2023
When administering roxadustat and daprodustat, clinicians should check ferritin to assess iron storage. Lower TSAT in patients receiving HIF-PHIs and ESAs treatment suggests intravenous iron supplements are needed.
- | Journal: New developments in anaemia treatment - erythropoietin versus prolyl hydroxylase inhibitors? (Pubmed Central) - Nov 21, 2022
The first of these, roxadustat, is currently reimbursed also in the Czech Republic. Other molecules affecting anaemia, such as sotatercept, have also been confirmed to be effective in phase 1 and 2 clinical trials and are awaiting results from larger randomised trials.
- || Musredo (molidustat) / Bayer
Trial completion date, Trial primary completion date: A Study to Learn More About the Long-term Safety and Effectiveness of Molidustat as a Treatment for Japanese Men and Women With Renal Anemia (clinicaltrials.gov) - Nov 15, 2022
P=N/A, N=1500, Recruiting, Sponsor: Bayer
Other molecules affecting anaemia, such as sotatercept, have also been confirmed to be effective in phase 1 and 2 clinical trials and are awaiting results from larger randomised trials. Trial completion date: Sep 2026 --> Sep 2027 | Trial primary completion date: Jun 2026 --> Jun 2027
- Aranesp (darbepoetin alfa) / Amgen, Kyowa Kirin
Efficacy and Safety of Hypoxia-Inducible Factor Prolyl Hydroxylase Inhibitors for Treatment of Anaemia of Chronic Kidney Disease: A Systematic Literature Review (Virtual) - Sep 1, 2022 - Abstract #ISPOREU2022ISPOR_EU_1058;
Of these, 12 assessed roxadustat, 7 daprodustat, 6 vadadustat, and 3 molidustat; comparators included darbepoetin alfa (DA), epoetin alfa (EA), methoxy polyethylene glycol–epoetin beta (MPG-EPO), and placebo... Based on a qualitative assessment, efficacy of HIF-PHIs appeared comparable to that of ESAs, while safety profiles were similar between these drug classes.
- | Musredo (molidustat) / Bayer
Preclinical, Journal: EPO synthesis induced by HIF-PHD inhibition is dependent on myofibroblast transdifferentiation and colocalizes with non-injured nephron segments in murine kidney fibrosis. (Pubmed Central) - Jul 28, 2022
Based on a qualitative assessment, efficacy of HIF-PHIs appeared comparable to that of ESAs, while safety profiles were similar between these drug classes. Our studies suggest that HIF-PHIs do not reactivate Epo transcription in interstitial myofibroblasts and that their efficacy in inducing kidney EPO in CKD is dependent on the degree of myofibroblast formation, the preservation of renal parenchyma and the level of residual renal function.
- | Musredo (molidustat) / Bayer
Journal: The Prolyl hydroxylase inhibitor molidustat fails to restore erythropoietin production in the fibrotic kidney. (Pubmed Central) - Jul 28, 2022
Our studies suggest that HIF-PHIs do not reactivate Epo transcription in interstitial myofibroblasts and that their efficacy in inducing kidney EPO in CKD is dependent on the degree of myofibroblast formation, the preservation of renal parenchyma and the level of residual renal function. No abstract available
- Musredo (molidustat) / Bayer, Evrenzo (roxadustat) / Astellas, AstraZeneca, FibroGen
Investigating the role of EGLN1 in non-small cell lung cancer 2D cultures and in patient-derived 3D spheroids (Poster Area) - Jun 28, 2022 - Abstract #EACR2022EACR_1125;
Conclusion EGLN1 plays a fundamental role in KRAS-mutated NSCLC and EGLN1 inhibitors represent a valuable possibility that can become part of future therapeutic strategies for this tumor. Preliminary evidence suggest that patient-derived 3D cultures may be useful to asses ex-vivo the response to the molidustat treatment, thus acquiring both a screening and a prognostic meaning.
- | Musredo (molidustat) / Bayer
Journal: HIF-PH Encoded by EGLN1 Is a Potential Therapeutic Target for Chronic Lymphocytic Leukemia. (Pubmed Central) - Jun 25, 2022
We further identified synergistic cytotoxicity of molidustat in combination with ibrutinib on the MEC-1 and HG3 cell lines at certain concentrations. Therefore, molidustat is a potential therapeutic option for CLL.
- | cyclophosphamide / Generic mfg.
Journal: Inhibition of hypoxia-inducible factor-prolyl hydroxylation protects from cyclophosphamide-induced bladder injury and urinary dysfunction. (Pubmed Central) - Jun 24, 2022
Void spot analysis to examine bladder function quantitatively demonstrated that HIF-PHI administration normalized micturition patterns and protected against CYP-induced alteration of urinary frequency and micturition patterns. Our studies highlight the therapeutic potential of HIF-activating small molecule compounds for the prevention or therapy of bladder injury and urinary dysfunction due to blood-urine barrier disruption.
- | Musredo (molidustat) / Bayer
Journal: Isoliquiritin apioside relieves intestinal ischemia/reperfusion-induced acute lung injury by blocking Hif-1α-mediated ferroptosis. (Pubmed Central) - Jun 22, 2022
And Hif-1α activation increased the mRNA levels of Ptgs2 and Acsl4 but decreased the mRNA level of Gpx4 in H/R-induced MLE-2 cells treated with IA. Taken together, our study unveiled IA could protect against intestinal I/R-induced ALI by decreasing lung epithelial ferroptosis in a Hif-1α-dependent manner.
- | Musredo (molidustat) / Bayer, Evrenzo (roxadustat) / Astellas, AstraZeneca, FibroGen, Vafseo (vadadustat) / Akebia Therap, Otsuka, Mitsubishi Tanabe
Journal: Mannose Binding Lectin Is Hydroxylated by Collagen Prolyl-4-hydroxylase and Inhibited by Some PHD Inhibitors. (Pubmed Central) - Apr 8, 2022
Reduced MBL activity is likely to be an off-target effect of some, but not all, prolyl hydroxylase domain (PHD) inhibitors. There may be advantages in selective PHD inhibitors that would not interfere with MBL production.
- || Review, Journal: Clinical Potential of Hypoxia Inducible Factors Prolyl Hydroxylase Inhibitors in Treating Nonanemic Diseases. (Pubmed Central) - Mar 15, 2022
Since HIFs are involved in many physiological and pathological conditions, efforts have been made to extend the potential usage of HIF-PHIs beyond anemia. This paper reviewed the progress of preclinical and clinical research on clinically available HIF-PHIs in pathological conditions other than CKD anemia.
- ||| Musredo (molidustat) / Bayer, Aranesp (darbepoetin alfa) / Amgen, Kyowa Kirin
Clinical, P3 data, Journal: Molidustat for Renal Anemia in Nondialysis Patients Previously Treated with Erythropoiesis-Stimulating Agents: A Randomized, Open-Label, Phase 3 Study. (Pubmed Central) - Mar 11, 2022
Molidustat was noninferior to darbepoetin and maintained Hb levels in the prespecified target range in patients with renal anemia not undergoing dialysis and previously treated with ESA. Molidustat was well tolerated, and no new safety signal was observed.
- ||| Musredo (molidustat) / Bayer, Aranesp (darbepoetin alfa) / Amgen, Kyowa Kirin
Clinical, P3 data, Journal: Efficacy and Safety of Molidustat for Anemia in ESA-Naive Nondialysis Patients: A Randomized, Phase 3 Trial. (Pubmed Central) - Mar 11, 2022
Molidustat was well tolerated, and no new safety signal was observed. In the MIYABI ND-C study, molidustat appeared to be an efficacious and generally well-tolerated alternative to darbepoetin for the treatment of renal anemia in Japanese patients who were not undergoing dialysis and were not receiving ESA treatment.
- ||| Musredo (molidustat) / Bayer
Clinical, P3 data, Journal: Molidustat for the treatment of anemia in Japanese patients undergoing peritoneal dialysis: A single-arm, open-label, phase 3 study. (Pubmed Central) - Mar 4, 2022
No deaths were reported. Molidustat maintained hemoglobin levels in the prespecified range in more than half the patients and was well tolerated.
- | Musredo (molidustat) / Bayer
Journal: Structural Basis of Prolyl Hydroxylase Domain Inhibition by Molidustat. (Pubmed Central) - Feb 17, 2022
The inhibitors bind to the active site metal in a bidentate manner via their pyrazolone and pyrimidine nitrogens, with the triazole π-π-stacking with Tyr303 in the 2OG binding pocket. Comparison of the new structures with other PHD inhibitor complexes reveals differences in the conformations of Tyr303, Tyr310, and a mobile loop linking β2-β3, which are involved in dynamic substrate binding/product release.
- ||| Musredo (molidustat) / Bayer
Clinical, P3 data, Journal: Molidustat for anemia correction in Japanese patients undergoing hemodialysis: a single-arm, phase 3 study. (Pubmed Central) - Feb 5, 2022
P3
No adverse events of special interest were reported. Treatment with dose-titrated molidustat for 24 weeks was well tolerated in Japanese patients undergoing hemodialysis, and no new safety signal was observed.
- | Musredo (molidustat) / Bayer
Journal: Activation of HIF1α Rescues the Hypoxic Response and Reverses Metabolic Dysfunction in the Diabetic Heart. (Pubmed Central) - Dec 31, 2021
In vivo this corrected the abnormal metabolic phenotype and impaired post-ischaemic recovery of the diabetic heart. Therefore, molidustat may be an effective compound to further explore the clinical translatability of HIF1α activation in the diabetic heart.
- | Retrospective data, Journal: Long-term efficacy and safety of hypoxia-inducible factor prolyl hydroxylase inhibitors in anaemia of chronic kidney disease: A meta-analysis including 13,146 patients. (Pubmed Central) - Dec 16, 2021
HIF-PHD inhibitors treatment effectively increased haemoglobin levels and promoted iron utilization in anaemic patients with CKD, and they were well tolerated for long-term use. In order to avoid unfavourable effects of excessive iron consumption, it was appropriate to administer HIF-PHD inhibitors in combination with iron supplements for long-term treatment.
- | Musredo (molidustat) / Bayer
Journal: Targeting HIF-α for robust prevascularization of human cardiac organoids. (Pubmed Central) - Dec 16, 2021
Lastly, we showed that Molidustat treatment improves survival of cardiac organoids when exposed to both hypoxic and ischemic conditions in vitro. For the first time, we demonstrate that targeted HIF-α stabilization provides a robust strategy to improve endothelial expression and lumen formation in cardiac microtissues, which will provide a powerful framework for prevascularization of various microtissues in developing successful cell transplantation therapies.
- | Journal: Sensing an Oxygen Sensor: Development and Application of Activity-Based Assays Directly Monitoring HIF Heterodimerization. (Pubmed Central) - Nov 11, 2021
Applicability was demonstrated using a panel of PHD inhibitors, including roxadustat, molidustat, daprodustat, desidustat, vadadustat, and FG-2216, for which concentration-response curves were generated, allowing for the derivation of potency (EC) and efficacy (E) data. The broad applicability of the biosensors was established via applying hypoxia mimetic CoCl, iron chelator desferrioxamine, proteasome inhibitor MG-132, and 2-OG mimetic dimethyloxalylglycine on the assays, indicating concentration-dependent effects.
- | Musredo (molidustat) / Bayer
Journal: Stabilization of Hypoxia-Inducible Factor Promotes Antimicrobial Activity of Human Macrophages Against Mycobacterium tuberculosis. (Pubmed Central) - Oct 28, 2021
Treatment of Mtb-infected macrophages with the prolyl-hydroxylase inhibitor Molidustat reduced the release of TNFα and IL-10, two key cytokines involved in the immune response in tuberculosis...Consequently, these immunological effects resulted in reduced proliferation of virulent Mtb in human macrophages. Therefore, HIFs may be attractive new candidates for host-directed therapies against infectious diseases caused by intracellular bacteria, including tuberculosis.
- | Musredo (molidustat) / Bayer
Preclinical, Journal: Effects of molidustat, a hypoxia-inducible factor prolyl hydroxylase inhibitor, on sodium dynamics in hypertensive subtotally nephrectomized rats. (Pubmed Central) - Oct 22, 2021
Furthermore, molidustat had no significant effect on urinary sodium excretion or concentration in response to acute oral salt loading (1 g/kg). In conclusion, molidustat did not affect distribution or excretion of salt in rats subjected to a model of nephron loss.
- || Musredo (molidustat) / Bayer, Aranesp (darbepoetin alfa) / Amgen, Kyowa Kirin
Clinical, Journal: Molidustat for Japanese Patients With Renal Anemia Receiving Dialysis. (Pubmed Central) - Oct 9, 2021
In line with published literature, and as expected in this patient population, most participants had ≥1 treatment-emergent adverse event. Molidustat maintained Hb levels throughout the trial in patients receiving dialysis and previously treated with erythropoiesis-stimulating agents, and was noninferior to darbepoetin.
- | Musredo (molidustat) / Bayer
Journal: Drug-drug interaction of atazanavir on UGT1A1-mediated glucuronidation of molidustat in human. (Pubmed Central) - Oct 6, 2021
Baseline-corrected increase of EPO was 14% and 34% for C and AUC (calculated over 24 hours), respectively. Coadministration of molidustat and atazanavir was well tolerated.
- | Musredo (molidustat) / Bayer, Evrenzo (roxadustat) / Astellas, AstraZeneca, FibroGen
Journal: Pharmacologic HIF-PHD inhibition reduces renovascular resistance and increases glomerular filtration by stimulating nitric oxide generation. (Pubmed Central) - Sep 12, 2021
Coadministration of molidustat and atazanavir was well tolerated. Our data provide mechanistic insights into dose-dependent effects of short-term pharmacologic HIF activation on renal hemodynamics, glomerular filtration and O metabolism and identify NO as a major mediator of these effects.
- | Musredo (molidustat) / Bayer, Evrenzo (roxadustat) / Astellas, AstraZeneca, FibroGen
Preclinical, Journal: Get use to the -dustats: Roxadustat and molidustat, members of the hypoxia-inducible factor (HIF) Prolyl hydroxylase (PHD) inhibitor drug class promote kidney function, perfusion and oxygenation in rats through nitric oxide. (Pubmed Central) - Sep 12, 2021
Oxygen sensing is a fundamental process of most living organisms and it can now be targeted pharmacologically. Burmakin et al show in a preclinical approach with rats that systemic administration of 2 different drugs, roxa- and molidustat, lowers blood pressure, increases renal plasma flow and GFR.
- ||| Musredo (molidustat) / Bayer
Enrollment open: A Study to Learn More About the Long-term Safety and Effectiveness of Molidustat as a Treatment for Japanese Men and Women With Renal Anemia (clinicaltrials.gov) - Aug 16, 2021
P=N/A, N=1500, Recruiting, Sponsor: Bayer
Burmakin et al show in a preclinical approach with rats that systemic administration of 2 different drugs, roxa- and molidustat, lowers blood pressure, increases renal plasma flow and GFR. Not yet recruiting --> Recruiting
- | Musredo (molidustat) / Bayer
Preclinical, Journal: The HIF-PHI BAY 85-3934 (Molidustat) improves anemia and is associated with reduced levels of circulating FGF23 in a CKD mouse model. (Pubmed Central) - Aug 11, 2021
In vitro, differentiated osteocyte-like cells exposed to an iron chelator to simulate iron depletion/hypoxia increased FGF23; repletion with holo-transferrin completely suppressed FGF23 and normalized Tfrc1. Collectively, these results support that resolving anemia using a HIF-PHI during CKD was associated with lower BUN and reduced FGF23, potentially through direct restoration of iron utilization, thus providing modifiable outcomes beyond improving anemia for this patient population.
- || Retrospective data, Review, Journal: Efficacy and safety of HIF prolyl-hydroxylase inhibitor vs epoetin and darbepoetin for anemia in chronic kidney disease patients not undergoing dialysis: a network meta-analysis. (Pubmed Central) - Jul 8, 2021
In conclusion, these HIF-PHIs are effective and relatively tolerant for treating anemia patients with CKD not undergoing dialysis. Further research should consider the limitations of our study to evaluate the value of these HIF-PHIs in clinical settings.
- |||||| Musredo (molidustat) / Bayer
New trial: A Study to Learn More About the Long-term Safety and Effectiveness of Molidustat as a Treatment for Japanese Men and Women With Renal Anemia (clinicaltrials.gov) - May 23, 2021
P, N=1500, Not yet recruiting, Sponsor: Bayer
- molidustat (BAY85-3934) / Bayer, Evrenzo (roxadustat) / Astellas, AstraZeneca, FibroGen, Duvroq (daprodustat) / GSK, Kyowa Hakko Kirin
[VIRTUAL] EXPANDING THE POTENTIAL BENEFIT OF HYPOXIA-INDUCIBLE FACTOR PROLYL HYDROXYLASE INHIBITORS FOR IMPROVING DYSLIPIDEMIA IN ANEMIA OF CHRONIC KIDNEY DISEASE PATIENTS: META-ANALYSIS OF RANDOMIZED CONTROLLED TRIALS () - Apr 17, 2021 - Abstract #ISNWCN2021ISN-WCN_857;
Conclusions Hypoxia-inducible factor prolyl hydroxylase inhibitor gives more significant dyslipidemia improvement in anemia of CKD patients compared with ESA. However, further trials are needed to establish the efficacies.
- Musredo (molidustat) / Bayer
[VIRTUAL] MOLIDUSTAT FOR ANAEMIA IN JAPANESE PATIENTS UNDERGOING PERITONEAL DIALYSIS: A SINGLE ARM, OPEN-LABEL, PHASE 3 STUDY (Mini-Orals Hall) - Mar 19, 2021 - Abstract #ERAEDTA2021ERA_EDTA_471;
Molidustat maintained Hb in the prespecified range (≥ 11.0 g/dL to < 13.0 g/dL) and was well-tolerated over the 36 weeks of treatment. Molidustat offers a potential alternative to ESAs in patients with renal anaemia undergoing PD.
- | Journal: UPLC-MS-Based Procedures to Detect Prolyl-hydroxylase Inhibitors of HIF in Urine. (Pubmed Central) - Mar 9, 2021
The applicability of the newly developed methods was verified by the analysis of urine samples containing molidustat, roxadustat or daprodustat. The developed procedures enabled to detect the compounds under investigation and their main metabolites.
- | Preclinical, Journal: Hypoxia-inducible factor (HIF) prolyl hydroxylase inhibitors induce autophagy and have a protective effect in an in-vitro ischaemia model. (Pubmed Central) - Nov 19, 2020
The new class of PHD inhibitors (FG4592, FG2216, GSK1278863, Bay85-3934) have the higher potency than DMOG. The interplay between autophagy, HIF stabilisation and neuroprotection in ischaemic stroke merits further investigation.