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| Authors | ST. Durant, KG. Pike, N Colclough, L Riches, A Garcia-Trinidad, T Hunt, S Ling, J Stott, I Barrett, L Zheng, Y Wang, K Chen, T Zhang, VP Reddy, A Sykes, P Johnstrom, G Jones, A Pierce, J Karlin, J Kahn, J Allen, K Valerie, R Illingworth and M Pass | ||||||||||||
| Title | AZD1390, a potent and selective orally bioavailable blood-brain barrier-penetrant ATM inhibitor, radiosensitizes and improves survival of orthotopic glioma and metastatic brain tumor models | ||||||||||||
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| URL | http://mct.aacrjournals.org/content/17/1_Supplement/A104 | ||||||||||||
| Abstract Text | Mol Cancer Ther 2018;17(1 Suppl):Abstract nr A104 | ||||||||||||
| Molecular Profile | Treatment Approach |
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| Gene Name | Source | Synonyms | Protein Domains | Gene Description | Gene Role |
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| Drug Name | Trade Name | Synonyms | Drug Classes | Drug Description |
|---|---|---|---|---|
| AZD1390 | AZD 1390|AZD-1390 | ATM Inhibitor 13 | AZD1390 is a selective inhibitor of ATM that is optimized for blood-brain barrier penetration, thus may preferentially sensitize CNS tumors for radiotherapy (Mol Cancer Ther 2018;17(1 Suppl):Abstract nr A104, PMID: 29938225, PMID: 31299316). |
| Gene | Variant | Impact | Protein Effect | Variant Description | Associated with drug Resistance |
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| Molecular Profile | Indication/Tumor Type | Response Type | Therapy Name | Approval Status | Evidence Type | Efficacy Evidence | References |
|---|---|---|---|---|---|---|---|
| ATM positive | lung cancer | sensitive | AZD1390 | Preclinical - Cell line xenograft | Actionable | In a preclinical study, AZD1390 inhibited Atm activity, sensitized lung cancer cells to radiotherapy in culture, and demonstrated efficacy in cell line xenograft models (Mol Cancer Ther 2018;17(1 Suppl):Abstract nr A104). | detail... |
| TP53 mutant | glioblastoma | sensitive | AZD1390 | Preclinical - Cell culture | Actionable | In a preclinical study, TP53 mutant glioblastoma cells demonstrated increased sensitivity to radiosensitization by AZD1390 treatment compared to TP53 wild-type cells in culture (Mol Cancer Ther 2018;17(1 Suppl):Abstract nr A104). | detail... |
| ATM positive | glioblastoma | sensitive | AZD1390 | Preclinical - Cell line xenograft | Actionable | In a preclinical study, AZD1390 inhibited Atm activity, sensitized glioblastoma cell lines to radiotherapy in culture, and demonstrated efficacy in mouse models of glioblastoma (Mol Cancer Ther 2018;17(1 Suppl):Abstract nr A104). | detail... |