AZ7550

Description: AZ7550 is a novel and active metabolite of AZD-9291 (Osimertinib) which inhibits the activity of IGF1R with an IC50 of 1.6 uM. AZD9291 is an irreversible inhibitor of both EGFR sensitizing (EGFRm+) and T790M resistance mutations with selectivity over the wild type form of the receptor. Following observations of significant tumor inhibition in preclinical models, the clinical candidate was administered clinically to patients with T790M positive EGFR-TKI resistant NSCLC and early efficacy has been observed, accompanied by an encouraging safety profile. Epidermal growth factor receptor (EGFR) inhibitors have been used clinically in the treatment of non-small-cell lung cancer (NSCLC) patients harboring sensitizing (or activating) mutations for a number of years. Despite encouraging clinical efficacy with these agents, in many patients resistance develops leading to disease progression. In most cases, this resistance is in the form of the T790M mutation. In addition, EGFR wild type receptor inhibition inherent with these agents can lead to dose limiting toxicities of rash and diarrhea.

References: J Med Chem. 2014 Oct 23; 57(20):8249-67.

Related Products?AZ7550 Mesylate; AZ7550 hydrochloride