Desidustat: First Approval

Dhillon, Sohita

doi:10.1007/s40265-022-01744-w

Cited by 18 publications

(12 citation statements)

References 11 publications

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“…Therefore, large, high-quality multinational studies with long-term evaluations are needed to further examine different dosing strategies. In addition to roxadustat, other HIF-PHIs have been used clinically or are undergoing clinical trials for the treatment of CKD-related anemia ( Beuck et al, 2012 ; Dhillon, 2020 ; Markham, 2020 ; Figg et al, 2021 ; Markham, 2021 ; Dhillon, 2022 ). Although all HIF-PHIs have similar mechanisms of action, their specific effects on cells and preferred targets may differ.…”

Section: Effect Of Roxadustat On Anemiamentioning

confidence: 99%

Roxadustat: Not just for anemia

Zhu

Jiang²,

Wei³

et al. 2022

Front. Pharmacol.

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Roxadustat is a recently approved hypoxia-inducible factor prolyl hydroxylase inhibitor that has demonstrated favorable safety and efficacy in the treatment of renal anemia. Recent studies found it also has potential for the treatment of other hypoxia-related diseases. Although clinical studies have not yet found significant adverse or off-target effects of roxadustat, clinicians must be vigilant about these possible effects. Hypoxia-inducible factor regulates the expression of many genes and physiological processes in response to a decreased level of oxygen, but its role in the pathogenesis of different diseases is complex and controversial. In addition to increasing the expression of hypoxia-inducible factor, roxadustat also has some effects that may be HIF-independent, indicating some potential off-target effects. This article reviews the pharmacological characteristics of roxadustat, its current status in the treatment of renal anemia, and its possible effects on other pathological mechanisms.

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Section: Effect Of Roxadustat On Anemiamentioning

confidence: 99%

Roxadustat: Not just for anemia

Zhu

Jiang²,

Wei³

et al. 2022

Front. Pharmacol.

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“…To date, many PHD2 inhibitors have been reported, − and among them, six have been approved, including Roxadustat, Vadadustat, Daprodustat, Enarodustat, Molidustat, and Desidustat (Table S1). On December 18, 2018, the first-in-class PHD inhibitor Roxadustat ( 1a ) (Figure A), developed by FibroGen, was approved by the National Medical Products Administration (NMPA) in China .…”

Section: Introductionmentioning

confidence: 99%

Preferred Conformation-Guided Discovery of Potent and Orally Active HIF Prolyl Hydroxylase 2 Inhibitors for the Treatment of Anemia

Zhang

Sun

et al. 2023

J. Med. Chem.

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In this work, we discovered a novel series of prolyl hydroxylase 2 (PHD2) inhibitors with improved metabolic properties based on a preferred conformation-guided drug design strategy. Piperidinyl-containing linkers with preferred metabolic stability were designed to match the dihedral angle of the desired docking conformation in the PHD2 binding site with the lowest energy conformation. Based on the piperidinyl-containing linkers, a series of PHD2 inhibitors with high PHD2 affinity and favorable druggability were obtained. Remarkably, compound 22, with an IC 50 of 22.53 nM toward PHD2, significantly stabilized hypoxia-inducible factor α (HIFα) and upregulated the expression of erythropoietin (EPO). Furthermore, oral administration of 22 dose-dependently stimulated erythropoiesis in vivo. Preliminary preclinical studies showed that 22 has good pharmacokinetic properties and an excellent safety profile, even at 10 times the efficacious dose (200 mg/kg). Taken together, these results indicate that 22 is a promising candidate for anemia treatment.

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“…A depth literature review reveals that not a single method is available for the determination of newer Desidustat antianemic agents till date [7][8][9][10][11][12][13]. So though of interest for qualitative and quantitative estimation of Desidustat in bulk and tablet dosage form by beneficial highperformance thin-layer chromatography (HPTLC) method came as it is less time-and mobile phase-consuming, costeffective, environmental pollution problem controlling…”

Section: Introduction [1-7]mentioning

confidence: 99%

A sensitive, precise, accurate, and economic planar chromatographic method developed and validated for quantification of Desidustat as per guideline

Pandya¹,

Kachhiya²,

Solanki³

et al. 2023

Separation Science Plus

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Anemia with chronic kidney disease treating newer hope is recently approved Desidustat. By following International Conference on Harmonization Quality guideline Q2 (R1), an economic high‐performance thin‐layer chromatography method has been developed for the estimation of Desidustat. Pre‐coated silica gel 60 F254 plates as stationary phase along with mobile phase toluene:methanol:glacial acetic acid (7.5:2.5:0.3 v/v/v), and 230 nm detection wavelength was selected as optimized. Developed method was found linear in quantity per band range of 100 ng/band to 600 ng/band for Desidustat with 0.9979 regression coefficient. Standard spiking method showed method accuracy with a mean percentage recovery of 99.21%–101.63%. Limit of detection and limit of quantitation were found to be 3.94 and 11.94 ng/band, respectively. The method was found to be linear, precise, accurate, robust, rugged, selective, sensitive, and specific for the quantification of Desidustat in bulk and tablet dosage form and successfully can be applied for the qualitative and quantitative determination of Desidustat in bulk and marketed tablet formulation.

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Desidustat: First Approval

Cited by 18 publications

References 11 publications

Roxadustat: Not just for anemia

Roxadustat: Not just for anemia

Preferred Conformation-Guided Discovery of Potent and Orally Active HIF Prolyl Hydroxylase 2 Inhibitors for the Treatment of Anemia

A sensitive, precise, accurate, and economic planar chromatographic method developed and validated for quantification of Desidustat as per guideline

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