Article
Discovery of BLU-945, a Reversible, Potent, and Wild-Type-Sparing Next-Generation EGFR Mutant Inhibitor for Treatment-Resistant Non-Small-Cell Lung Cancer.
Journal of medicinal chemistry - 28 Jul 2022
Eno Meredith S, Brubaker Jason D, Campbell John E, De Savi Chris, Guzi Timothy J, Williams Brett D, Wilson Douglas, Wilson Kevin, Brooijmans Natasja, Kim Joseph, Özen Ayşegül, Perola Emanuele, Hsieh John, Brown Victoria, Fetalvero Kristina, Garner Andrew, Zhang Zhuo, Stevison Faith, Woessner Rich, Singh Jatinder, Timsit Yoav, Kinkema Caitlin, Medendorp Clare, Lee Christopher, Albayya Faris, Zalutskaya Alena, Schalm Stefanie, Dineen Thomas A
Abstract excerpt
While epidermal growth factor receptor (EGFR) tyrosine kinase inhibitors (TKIs) have changed the treatment landscape for EGFR mutant (L858R and ex19del)-driven non-small-cell lung cancer (NSCLC), most patients will eventually develop resistance to TKIs. In the case of first- and second-generation TKIs, up to 60% of patients will develop an EGFR T790M mutation, while third-generation irreversible TKIs, like...
Topics
- Carcinoma, Non-Small-Cell Lung
- Drug Resistance, Neoplasm
- ErbB Receptors
- Humans
- Lung Neoplasms
- Mutation
- Protein Kinase Inhibitors