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Front Cover: Discovery of Molidustat (BAY 85‐3934): A Small‐Molecule Oral HIF‐Prolyl Hydroxylase (HIF‐PH) Inhibitor for the Treatment of Renal Anemia (ChemMedChem 10/2018)
Author(s) -
Beck Hartmut,
Jeske Mario,
Thede Kai,
Stoll Friederike,
Flamme Ingo,
Akbaba Metin,
Ergüden JensKerim,
Karig Gunter,
Keldenich Jörg,
Oehme Felix,
Militzer HansChristian,
Hartung Ingo V.,
Thuss Uwe
Publication year - 2018
Publication title -
chemmedchem
Language(s) - English
Resource type - Reports
SCImago Journal Rank - 0.817
H-Index - 100
eISSN - 1860-7187
pISSN - 1860-7179
DOI - 10.1002/cmdc.201800275
Subject(s) - erythropoietin , kidney disease , hypoxia (environmental) , anemia , hypoxia inducible factors , pharmacology , kidney , medicine , chemistry , biochemistry , oxygen , gene , organic chemistry
The Front Cover shows key elements of the pharmacological action of molidustat, a novel small‐molecule inhibitor of the hypoxia‐inducible factor prolyl hydroxylase (HIF‐PH). Inhibition of HIF‐PH leads to a restoration of erythropoietin (EPO) production in the kidney by mimicking hypoxia and subsequently to an increased formation of oxygen‐carrying red blood cells in the bone marrow. This novel pharmacological concept has the potential to lead to a more physiological treatment of anemia than by parenteral administration of recombinant human erythropoietin (rhEPO), which is the current standard of care. Molidustat was identified at Bayer AG in the course of a multiparameter lead optimization starting from a high‐throughput screening hit, and is currently being investigated in phase 3 clinical studies for the treatment of anemia in patient with chronic kidney disease (CKD). More information can be found in the Full Paper by Hartmut Beck, Mario Jeske et al. on page 988 in Issue 10, 2018 (DOI: 10.1002/cmdc.201700783).