Chemical synthesis route and research and development background of Daprodustat drug

Daprodustat is an oral small molecule erythropoietin receptor agonist (HIF-PHI drug), mainly used to treat anemia caused by chronic kidney disease. In terms of research and development background, the development goal of daprostat is to provide patients with chronic kidney disease with a safe, efficient, orally available anemia treatment option to replace traditional injectable recombinant human erythropoietin (rHuEPO) therapy. Its research and development focuses on increasing endogenous erythropoietin levels by regulating the hypoxia-inducible factor (HIF) signaling pathway, thereby promoting red blood cell production and improving anemia symptoms while minimizing injection-related inconvenience and cardiovascular risks.

In terms of chemical synthesis, daporostat is a small molecule organic compound. Its core structure contains aromatic heterocycles and amide linking groups, ensuring that it has a highly selective inhibitory effect on HIF prolyl hydroxylase in the body. Synthetic routes are usually based on multi-step organic reactions, including key heterocycle construction, amidation reactions, and functional group protection and deprotection steps. By carefully controlling reaction conditions and stereochemistry, the R&D team is able to obtain high-purity target molecules while ensuring molecular activity and pharmacokinetic properties.

The design of the synthesis route of dapocestat not only focuses on product purity, but also on reaction economy and industrial production. During the research and development process, researchers optimized the reaction conditions of each step, including solvent selection, catalyst dosage and temperature control, to increase the yield and reduce the formation of by-products. This systematic optimization provides feasibility for mass production of drugs, reduces production costs and environmental burdens, and lays the foundation for subsequent marketing.

In addition, the research and development background of daprostat also includes the support of preclinical pharmacological research. Its ability to selectively regulate the HIF pathway and its effectiveness in red blood cell production have been verified through in vitro and animal experiments, providing a scientific basis for subsequent human trials. The chemical synthesis route and pharmacological verification complement each other, forming a complete research and development chain from molecular design, synthesis to clinical application of daprostat, which embodies the systematic strategy of modern small molecule drugs from chemical research and development to precision treatment.

Keyword tags: dapoprimostat, chemical synthesis, research and development background, HIF-PHI, renal anemia, oral drugs, hypoxia-inducible factor, chronic kidney disease.

Reference materials:https://go.drugbank.com/drugs/DB13973