DS-1093 / Daiichi Sankyo - LARVOL DELTA

Discovery of DS79540454 via fragment-based drug discovery strategy: New scaffolds of hypoxia-inducible factor prolyl hydroxylase inhibitor. (PubMed, Bioorg Med Chem Lett) - "We discovered brand-new amino succinic acid scaffolds by combining the structural information on the crystal structure complexed with 6-acetamide nicotinic acid. DS79540454 exhibits high enzyme inhibitory activity equivalent to that of DS-1093a, which has advanced to clinical trials."

Journal • Hematological Disorders

Discovery of DS-1093a: An oral hypoxia-inducible factor prolyl hydroxylase inhibitor for the treatment of renal anemia. (PubMed, Bioorg Med Chem Lett) - "Furthermore, through the optimization of pyrimidine derivatives, we discovered DS-1093a, which has a wide safety margin with potent in vitro activity and an optimal pharmacokinetic profile. DS-1093a achieved an increase in hemoglobin levels in an adenine-induced rat model of chronic kidney disease after its continuous administration for 4 days."

Journal • Anemia • Chronic Kidney Disease • Hematological Disorders • Nephrology • Renal Disease

Pilot PK/PD Study of DS-1093a in Patients With Chronic Kidney Disease (clinicaltrials.gov) - P1; N=30; Recruiting; Sponsor: Daiichi Sankyo Inc.

New P1 trial • Biosimilar • Chronic Kidney Disease • Renal Disease