Desidustat is a small molecule inhibitor of hypoxia-inducible factor-prolyl hydroxylase (HIF-PH) discovered and developed by Zydus Lifesciences for the treatment of anemia associated with chronic kidney disease (CKD). This review summarizes the preclinical and clinical profile of desidustat which led to its approval and clinical use in India.
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| http://dx.doi.org/10.3389/fneph.2024.1459425 | DOI Listing |
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Desidustat: a novel PHD inhibitor for the treatment of CKD-induced anemia.
Front Nephrol
October 2024
Zydus Research Centre, Zydus Lifesciences Limited, Ahmedabad, Gujarat, India.
Desidustat is a small molecule inhibitor of hypoxia-inducible factor-prolyl hydroxylase (HIF-PH) discovered and developed by Zydus Lifesciences for the treatment of anemia associated with chronic kidney disease (CKD). This review summarizes the preclinical and clinical profile of desidustat which led to its approval and clinical use in India.
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Drug Metab Dispos
February 2024
Pharmacokinetics Dynamics and Metabolism, Pfizer Inc, United States
Article Synopsis
- OATP1B is crucial for the liver's ability to remove high molecular weight acids and zwitterions; this study investigates its role in the uptake of low molecular weight hypoxia-inducible factor prolyl hydroxylase inhibitors, known as "Dustats."
- Five specific acid dustats were shown to be transported by OATP1B1/1B3 in lab cells, while a neutral compound (molidustat) was not transported by these transporters.
- The use of rifampin, an OATP1B inhibitor, significantly affected the uptake and clearance of these acids in both human liver cells and in monkey studies, highlighting the importance of OATP1B in their pharmacokinetics.
A Novel Spectrophotometric Method Development for Quantification of Desidustat in Bulk and Pharmaceutical Dosage Form.
Drug Metab Bioanal Lett
November 2023
Shobhaben Pratapbhai Patel School of Pharmacy & Technology Management, SVKM's NMIMS, Deemed to be University, Vile Parle West, Mumbai, Maharashtra, 400056, India.
Background: Desidustat (DES) belongs to a new category of drugs, i.e., Hypoxia-Inducible Factor (HIF) propyl hydroxylase inhibitor, and is used for the treatment of anemia in chronic kidney disease.
View Article and Find Full Text PDFNonclinical Pharmacokinetic Evaluation of Desidustat: a Novel Prolyl Hydroxylase Inhibitor for the Treatment of Anemia.
Eur J Drug Metab Pharmacokinet
September 2022
Department of Drug Metabolism and Pharmacokinetics, Zydus Research Centre, Zydus Lifesciences Limited, Sarkhej-Bavla N.H. No. 8A, Moraiya. Tal: Sanand, Ahmedabad, Gujarat, 382213, India.
Background And Objectives: Desidustat is a novel prolyl hydroxylase domain (PHD) inhibitor for the treatment of anemia. The objective of this study was to investigate the pharmacokinetics and drug-drug interaction properties of desidustat using in vitro and in vivo nonclinical models.
Methods: In vitro, Caco2 cell permeability, plasma protein binding, metabolism, cytochrome P450 (CYP) inhibition, and CYP induction were examined.
Prolyl hydroxylase inhibitor desidustat improves anemia in erythropoietin hyporesponsive state.
Curr Res Pharmacol Drug Discov
April 2022
Department of Pharmacology and Toxicology, Zydus Research Centre, Cadila Healthcare Limited, Sarkhej Bavla NH 8A, Moraiya, Ahmedabad, Gujarat, India.
Article Synopsis
- Many patients with chronic kidney disease experience anemia that is resistant to erythropoietin (EPO) due to factors like inflammation and improper iron usage.
- The study tested desidustat, a drug that inhibits certain enzymes, in rats to see if it could help manage anemia in cases where EPO was ineffective.
- Results showed that desidustat reduced resistance to EPO, lowered inflammation markers, and maintained healthy hemoglobin levels, suggesting it could be a new treatment option for EPO-resistant renal anemia.
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