Delving into the Latest Updates on Enarodustat with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Enarodustat (JAN), 恩那度司他

+ [5]

Target

HIF-PHs

Action

inhibitors

Mechanism

HIF-PHs inhibitors(Hypoxia-inducible factor prolyl hydroxylase inhibitors)

Therapeutic Areas

Hemic and Lymphatic DiseasesUrogenital DiseasesRespiratory Diseases

Active Indication

chronic renal failure anemiaAnemia of renal diseaseChronic Kidney Diseases+ [1]

Inactive Indication-

Originator Organization

Japan Tobacco, Inc.

Active Organization

Shenzhen Salubris Pharmaceuticals Co., Ltd.

JW PHARMACEUTICAL Corp.

Japan Tobacco, Inc.

Inactive Organization

Akros Pharma, Inc.

Drug Highest PhaseApproved

First Approval Date

Japan (25 Sep 2020),

Anemia of renal disease

Regulation-

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Structure/Sequence

Molecular FormulaC17H16N4O4

InChIKeyNALAUGMPMIVAOW-UHFFFAOYSA-N

CAS Registry1262132-81-9

View All Structures (2)

The CANNON trial is a prospective, open-label, randomized, multicenter study designed to investigate rational hemoglobin target value in patients with anemia of non-dialysis chronic kidney disease treated with enarodustat. Eligible patients are randomly assigned 1:1 to the high-hemoglobin target group （hemoglobin of 13 g/dl）and low-hemoglobin target group （hemoglobin of 11 g/dl）and administered with enarodustat to achieve and maintain target hemoglobin over 96 weeks. The first primary endpoint was the difference of mean change in 36-Item Short Form Health Survey at week 24. The second primary endpoint was safety endpoints included time to major adverse cardiovascular + event (MACE+; all-cause mortality, myocardial infarction, stroke, and congestive heart failure requiring hospitalization) during 96 weeks.

Start Date01 Dec 2024

Sponsor / Collaborator

Zhongshan Hospital Fudan University

[+1]

NCT06737081

/ RecruitingPhase 2

A Parallel, Open-label Phase II Clinical Study of Enarodustat (SAL-0951) Tablets in the Treatment of Chemotherapy-induced Anemia in Patients With Non-myeloid Malignancies

The purpose of this study is to evaluate the safety and efficacy of SAL-0951 in the treatment of chemotherapy-induced anemia (CIA) in patients with non-myeloid malignancies

Start Date14 Sep 2024

Sponsor / Collaborator

Shenzhen Salubris Pharmaceuticals Co., Ltd.

CTR20243024

/ RecruitingPhase 2

恩那度司他（SAL-0951）片在非髓系恶性肿瘤患者中治疗化疗引起贫血的平行、开放Ⅱ期临床研究

[Translation] A parallel, open-label phase II clinical study of Enadostat (SAL-0951) tablets in the treatment of chemotherapy-induced anemia in patients with non-myeloid malignancies

主要目的：评估恩那度司他（SAL-0951）片在非髓系恶性肿瘤患者中治疗化疗引起贫血的安全性。次要目的：评估恩那度司他（SAL-0951）片在非髓系恶性肿瘤患者中治疗化疗引起贫血的疗效。探索性目的：探索恩那度司他（SAL-0951）片在非髓系恶性肿瘤患者中治疗化疗引起贫血的红细胞相关检查值、铁代谢相关检查值的影响、药代动力学特征

[Translation]

Primary objective: To evaluate the safety of Enadostat (SAL-0951) tablets in the treatment of chemotherapy-induced anemia in patients with non-myeloid malignancies. Secondary objective: To evaluate the efficacy of Enadostat (SAL-0951) tablets in the treatment of chemotherapy-induced anemia in patients with non-myeloid malignancies. Exploratory objective: To explore the effects of Enadostat (SAL-0951) tablets on red blood cell-related examination values, iron metabolism-related examination values, and pharmacokinetic characteristics in the treatment of chemotherapy-induced anemia in patients with non-myeloid malignancies.

Start Date08 Sep 2024

Sponsor / Collaborator

Shenzhen Salubris Pharmaceuticals Co., Ltd.

100 Clinical Results associated with Enarodustat

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100 Translational Medicine associated with Enarodustat

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100 Patents (Medical) associated with Enarodustat

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61

Literatures (Medical) associated with Enarodustat

01 Feb 2025·Kidney Medicine

EPO-Mimetic Peptide Pegmolesatide Therapy for Pure Red Cell Aplasia in a Patient with Non-dialysis-dependent Type 1 Diabetic Nephropathy: A Case Report

Article

Author: Yang, Man ; Fan, Qiu-Ling ; Chen, Qiong ; Liu, Xuan ; Wang, Juan

Pure red cell aplasia (PRCA) is a rare complication of erythropoietin (EPO) therapy, characterized by a severe deficiency in red blood cell production. There is no guideline on the treatment for PRCA because there have been too few cases to perform prospective cohort studies. The main treatments for PRCA include immediate cessation of EPO, restrictive transfusion, and immunosuppressive therapies. A 35-year-old male patient with type 1 diabetic nephropathy was diagnosed with PRCA. Enarodustat and roxadustat were administered successively after discontinuation of EPO, but anemia did not improve, and the patient was maintained with weekly blood transfusions. Subsequently, the EPO-mimetic peptide pegmolesatide was administered, and the patient's hemoglobin started to increase after 1 week and increased from 50 g/L to 92 g/L over approximately 3 months. Based on these findings, we speculate that pegmolesatide can provide a safe, effective, and convenient therapeutic strategy for PRCA in Chinese patients with chronic kidney disease.

01 Feb 2025·Analytical and Bioanalytical Chemistry

LC-HRMS screening procedure for the detection of 11 different classes of prohibited substances in dried urine spots for doping control purposes

Article

Author: Tsivou, Maria ; Pizzolato, Francesca ; Honesová, Lenka ; Gmeiner, Günter ; Mazzarino, Monica ; Van Eenoo, Peter

Dried urine spots have recently been proposed as an alternative matrix in the anti-doping field. Drying urine may open the opportunity to limit microbial and thermal degradation of the prohibited substances during transportation to the anti-doping laboratories without the need for refrigeration or freezing. In this study, a multi-targeted initial testing procedure was developed for the determination of 237 prohibited drugs/metabolites from 11 different classes in dried urine spots. The comparability between two different microsampling techniques (i.e., Whatman^® FTA DMPK-C cards and Mitra^® tips) was evaluated. The developed method was then used to evaluate the stability of the target compounds in urine for 7 days under different environmental conditions to simulate the transportation of the urine samples from the collection sites to anti-doping laboratories. Sample preparation consists of (i) extraction of the analytes from the collection device using a mixture of acetonitrile/methanol (1/1) for 30 min at 40 °C, (ii) enzymatic hydrolysis, and (iii) sample concentration by solid-phase extraction. Analysis was performed using liquid chromatography coupled to high-resolution mass spectrometry. The entire workflow was validated in terms of specificity (analytes were distinguishable from the matrix interferences), sensitivity (only with the Mitra^® tips the limits of detection comply with the World Anti-Doping Agency's requirements for the majority of the target compounds), carry-over (no signals in the negative urine injected after the positive urine), matrix effect (16-28% for Mitra^® tips and 22-35% for DMPK-C cards), and extraction yield (Mitra^® tips: 51-88%; DMPK-C cards: 40-76%). As proof of concept, authentic urine samples were analyzed: results obtained in dried urine were compared with those of fluid urine, providing good agreement. Stability studies showed that the target compounds were stable for the whole duration of the study (7 days) at -20 and 4 °C in both fluid and dried urine. At 50 °C or at 20-25 °C, several thiazide-based compounds were completely degraded to their degradation product in the first 24 h or after 3-4 days in fluid urine, whereas in dried urine the compounds were detectable for the entire duration of the study.

16 Dec 2024·ChemMedChem

Crystallographic and Selectivity Studies on the Approved HIF Prolyl Hydroxylase Inhibitors Desidustat and Enarodustat

Article

Author: Kaur, Samanpreet ; Tumber, Anthony ; Corner, Thomas P. ; Nakashima, Yu ; Allen, Mark D. ; Schnaubelt, Lara I. ; Fiorini, Giorgia ; Schofield, Christopher J. ; Salah, Eidarus ; Brewitz, Lennart

AbstractProlyl hydroxylase domain‐containing proteins 1–3 (PHD1–3) are 2‐oxoglutarate (2OG)‐dependent oxygenases catalysing C‐4 hydroxylation of prolyl residues in α‐subunits of the heterodimeric transcription factor hypoxia‐inducible factor (HIF), modifications that promote HIF‐α degradation via the ubiquitin‐proteasome pathway. Pharmacological inhibition of the PHDs induces HIF‐α stabilisation, so promoting HIF target gene transcription. PHD inhibitors are used to treat anaemia caused by chronic kidney disease (CKD) due to their ability to stimulate erythropoietin (EPO) production. We report studies on the effects of the approved PHD inhibitors Desidustat and Enarodustat, and the clinical candidate TP0463518, on activities of a representative set of isolated recombinant human 2OG oxygenases. The three molecules manifest selectivity for PHD inhibition over that of the other 2OG oxygenases evaluated. We obtained crystal structures of Desidustat and Enarodustat in complex with the human 2OG oxygenase factor inhibiting hypoxia‐inducible factor‐α (FIH), which, together with modelling studies, inform on the binding modes of Desidustat and Enarodustat to active site Fe(II) in 2OG oxygenases, including PHD1–3. The results will help in the design of selective inhibitors of both the PHDs and other 2OG oxygenases, which are of medicinal interest due to their involvement inter alia in metabolic regulation, epigenetic signalling, DNA‐damage repair, and agrochemical resistance.

100 Deals associated with Enarodustat

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External Link

KEGG	Wiki	ATC	Drug Bank
D11523	Enarodustat	B03A	DB14985

R&D Status

Approved

10 top approved records.

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Indication	Country/Location	Organization	Date
chronic renal failure anemia	South Korea	JW PHARMACEUTICAL Corp.	17 Nov 2022
Anemia of renal disease	Japan	Japan Tobacco, Inc.	25 Sep 2020

Developing

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
chronic renal failure anemia	Phase 3	China	Shenzhen Salubris Pharmaceuticals Co., Ltd.	09 Dec 2020
Chronic Kidney Diseases	Phase 3	China	Shenzhen Salubris Pharmaceuticals Co., Ltd.	22 Feb 2002
Anemia in chronic kidney disease	Phase 2	China	Shenzhen Salubris Pharmaceuticals Co., Ltd.	08 Dec 2020
Kidney Failure, Chronic	Phase 2	United States	Akros Pharma, Inc.	01 May 2013
Altitude Sickness	IND Approval	China	Shenzhen Salubris Pharmaceuticals Co., Ltd.	11 Mar 2025

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Clinical Result

Indication

Phase

Evaluation

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


ASN2018	Phase 3	Anemia \| Chronic Kidney Diseases Maintenance	-	Enarodustat 2 mg	nhmraqwvbq(rqhrwniwnf) = gyfjzbctes dqtdftutzz (cgfreubcih )	Positive	23 Oct 2018
				Enarodustat 4 mg	nhmraqwvbq(rqhrwniwnf) = drakndpozp dqtdftutzz (cgfreubcih )
FO019 (ERA2015)	Not Applicable	Anemia \| Chronic Kidney Diseases Maintenance hemoglobin \| Erythropoiesis Stimulating Agents (ESAs) \| iv iron ... View more	40	JTZ-951 1 mg	(pwlwhpmkeg) = The results of reticulocyte count, hematocrit level and red blood cells in terms of changes from baseline at week 8 were similar to that in hemoglobin jrjqvjddbn (bclacckolg ) View more	Positive	21 May 2015
				JTZ-951 3 mg
FP380 (ERA2015)	Not Applicable	Anemia in chronic kidney disease hemoglobin \| erythropoietin	22	JTZ-951 1 mg	(gapsruawio) = The results of reticulocyte count, hematocrit level and red blood cells in terms of changes from baseline at Week 6 were similar to that in hemoglobin ysfjldmtle (jbadjipziy ) View more	Positive	21 May 2015