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Ref Type Journal Article
PMID (27573423)
Authors Xu X, Mao L, Xu W, Tang W, Zhang X, Xi B, Xu R, Fang X, Liu J, Fang C, Zhao L, Wang X, Jiang J, Hu P, Zhao H, Zhang L
Title AC0010, an Irreversible EGFR Inhibitor Selectively Targeting Mutated EGFR and Overcoming T790M-Induced Resistance in Animal Models and Lung Cancer Patients.
Journal Vol Issue Date Pages Journal Short Title
Molecular cancer therapeutics 15 11 2016 Nov 2586-2597 Mol Cancer Ther
URL
Abstract Text AC0010 is a pyrrolopyrimidine-based irreversible EGFR inhibitor, structurally distinct from previously reported pyrimidine-based irreversible EGFR inhibitors, such as osimertinib and rociletinib. AC0010 selectively inhibits EGFR-active and T790M mutations with up to 298-fold increase in potency compared with wild-type EGFR. In a xenograft model, oral administration of AC0010 at a daily dose of 500 mg/kg resulted in complete remission of tumors with EGFR-active and T790M mutations for over 143 days with no weight loss. Three major metabolites of AC0010 were tested and showed no wild-type EGFR inhibition or off-target effects, such as inhibition of IGF-1R. AC0010 is safe in non-small cell lung cancer (NSCLC) patients at a dose range between 50 and 550 mg once per day, and no hyperglycemia or other severe adverse effects were detected, such as grade 3 QT prolongation. The objective responses were observed in NSCLC patients with EGFR T790M mutation. Mol Cancer Ther; 15(11); 2586-97. ©2016 AACR.

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Molecular Profile Treatment Approach
Gene Name Source Synonyms Protein Domains Gene Description Gene Role
Therapy Name Drugs Efficacy Evidence Clinical Trials
Abivertinib Abivertinib 1 1
Drug Name Trade Name Synonyms Drug Classes Drug Description
Abivertinib Avitinib|AC0010|AC0010MA BTK inhibitor 36 EGFR Inhibitor 3rd gen 26 Abivertinib (AC0010) is a BTK inhibitor and a third-generation EGFR inhibitor that blocks the activity of mutant forms of EGFR while sparing wild-type EGFR, which potentially results in increased apoptosis and cell cycle arrest, and decreased viability and colony formation, and inhibits tumor growth (PMID: 27573423, PMID: 31310800).
Gene Variant Impact Protein Effect Variant Description Associated with drug Resistance
Molecular Profile Indication/Tumor Type Response Type Therapy Name Approval Status Evidence Type Efficacy Evidence References