Clausen, FDA-approved small-molecule kinase inhibitors. Trends Pharmacol Sci, 2015. 36(7): p. 422-39.Wu P, Nielsen TE, Clausen MH (2015) FDA-approved small-molecule kinase inhibitors. Trends Pharmacol Sci 36: 422-39.Wu P, Nielsen TE and Clausen MH. FDA-approved small-molecule kinase ...
To date, the US FDA has approved 28 small-molecule kinase inhibitors, half of which were approved in the past 3 years. While the clinical data of these approved molecules are widely presented and structure–activity relationship (SAR) has been reported for individual molecules, an updated review...
Accordingly, as additional research on the pathogenesis of various diseases is performed, it is quite likely that there will be a notable increase in the number of protein kinase therapeutic targets. The FDA has approved 80 small molecule therapeutic protein kinase inhibitors as of 1 January 2024 ...
Of the 34 FDA approved oral small-molecule kinase inhibitors (KI), 23 (68%) have warnings for hepatotoxicity in product labeling. To better understand the mechanisms of KI hepatotoxicity and whether such effects can be predicted, we examined 34 KIs for cytotoxicity in primary rat and human ...
In this study, by taking a high-throughput approach with a GFP-reporter system for the SaeRS TCS, we screened small molecule libraries for Sae-inhibitors and found that two anti-cancer drugs have excellentin vivoefficacy in a murine model of staphylococcal infection. To understand theirin vivoef...
Small molecule inhibitors of EphA4 with different scaffolds, e.g., 2,5-dimethylpyrrolyl benzene14 and rhynchophylline6, have been identified. Nonetheless, a major challenge for further drug development is the toxicity of lead compounds15. Repurposing of already-approved drugs for other indications ...
Gohlke H, Klebe G (2002) Approaches to the description and prediction of the binding affinity of small‐molecule ligands to macromolecular receptors. Angew Chem Int Ed 41(15):2644–2676 Article CAS Google Scholar Genheden S, Ryde U (2015) The MM/PBSA and MM/GBSA methods to estimate liga...
Small molecule drugs are organic compounds with low molecular weight. For a long time, they have been the backbone of the pharmaceutical industry. There are several benefits that make small molecules important drugs in therapy, such as the possibility of oral administration and cell membrane ...
Pexidartinib is a small chemical molecule, orally accessible tyrosine kinase inhibitor with selective activity against the KIT proto-oncogene, receptor tyrosine kinase (KIT), CSF1 receptor, and FMS-like tyrosine kinase 3 with an internal tandem replication mutation (FLT3-ITD) used to treat tenosyn...
However, small molecule oral HIF-PHi compounds have been approved for some years in both China and Japan. In clinical trials, both vadadustat and daprodustat have displayed efficacy and safety comparable to darbepoietin (Sarnak et al., 2023; Singh et al., 2022). There are important ...