Research at Beijing Scitech-Mq Pharmaceuticals Ltd. has led to the identification of inhibitors of epidermal growth factor receptor (EGFR; HER1; erbB1) and its mutants which are reported to be useful for the treatment of cancer and autoimmune diseases.
Suzhou Puhe Biopharma Co. Ltd. presented promising preclinical profile data on PH009-1, a novel fourth-generation epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor (TKI). Besides ex19del (D), L858R (L) and T790M (T) as the more prevalent EGFR mutations, a segment of patients further acquire C797S (C)-resistant mutation. Current therapies address some single, double or triple mutation-expressing cancers. However, multiple-mutant positive cancers where T790M and/or C797S are involved pose a treatment challenge. The development of pan mutant EGFR TKIs is thus a much-desired research goal.
Researchers from Therapex Co. Ltd. recently reported the discovery and preclinical evaluation of a novel fourth-generation epidermal growth factor receptor (EGFR) inhibitor for overcoming C797S mutation-mediated acquired resistance in non-small-cell lung cancer (NSCLC), which has been reported as the most common acquired resistance mechanism in NSCLC.
Scorpion Therapeutics Inc. has named STX-241 as its next development candidate. STX-241 is an orally bioavailable, highly selective, central nervous system (CNS)-penetrant, fourth-generation EGFR tyrosine kinase inhibitor (TKI) designed to inhibit C797S mutations with a co-occurring EGFR exon 19 deletion or exon 21 mutation (double mutant) in non-small-cell lung cancer (NSCLC).
Whether as primary tumors or metastases, brain tumors remain stubbornly intractable to the progress that has occurred in many other tumor types. As Igor Vivanco, who is a senior lecturer in the Institute of Pharmaceutical Science at King’s College London, noted in his talk at the European Society for Medical Oncology Targeted Anticancer Therapies (ESMO TAT) meeting in Paris this week, the last win in glioblastoma was the addition of temozolomide to the radiotherapy standard of care in 2005. And temozolomide’s benefit is measured in months, not years.
Medshine Discovery Inc. has divulged amide compounds acting as epidermal growth factor receptor (EGFR) mutant inhibitors reported to be useful for the treatment of cancer.
Blueprint Medicines Corp. has disclosed EGFR (L858R/T790M/C797S triple mutant) and/or EGFR (exon 19 deletion mutant) inhibitors reported to be useful for the treatment of cancer.
Researchers from Nalo Therapeutics Inc. presented the discovery and preclinical evaluation of a novel orally bioavailable and brain-penetrant epidermal growth factor receptor (EGFR) inhibitor, NX-019, being developed as a potential therapeutic agent to treat EGFR-mutant solid tumors.
