bibw-2992 and Brain-Neoplasms

bibw-2992 has been researched along with Brain-Neoplasms* in 1 studies

Other Studies

1 other study(ies) available for bibw-2992 and Brain-Neoplasms

Article	Year
Discovery and Evaluation of Clinical Candidate AZD3759, a Potent, Oral Active, Central Nervous System-Penetrant, Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitor. Journal of medicinal chemistry, 2015, Oct-22, Volume: 58, Issue:20 Recent reports suggest that an increasing number of patients with lung cancer, especially those with activating mutations of the epidermal growth factor receptor (EGFR), also present with brain metastases and leptomeningeal metastases. These patients have poor prognosis as there are no approved drugs for these indications. Available agents have poor efficacy for these patients even at well above their standard dose. Herein, we report the discovery of (4-[(3-chloro-2-fluorophenyl)amino]-7-methoxyquinazolin-6-yl (2R)-2,4-dimethylpiperazine-1-carboxylate 1m (AZD3759), an investigational drug currently in Phase 1 clinical trial, which has excellent central nervous system penetration and which induces profound regression of brain metastases in a mouse model. Topics: Animals; Brain; Brain Neoplasms; Central Nervous System; Clinical Trials, Phase I as Topic; Dogs; Drug Discovery; ErbB Receptors; Macaca fascicularis; Male; Mice; Piperazines; Positron-Emission Tomography; Protein Kinase Inhibitors; Protein-Tyrosine Kinases; Quinazolines; Rats; Rats, Wistar; Xenograft Model Antitumor Assays	2015

Article

Year

Discovery and Evaluation of Clinical Candidate AZD3759, a Potent, Oral Active, Central Nervous System-Penetrant, Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitor.

Journal of medicinal chemistry, 2015, Oct-22, Volume: 58, Issue:20

Recent reports suggest that an increasing number of patients with lung cancer, especially those with activating mutations of the epidermal growth factor receptor (EGFR), also present with brain metastases and leptomeningeal metastases. These patients have poor prognosis as there are no approved drugs for these indications. Available agents have poor efficacy for these patients even at well above their standard dose. Herein, we report the discovery of (4-[(3-chloro-2-fluorophenyl)amino]-7-methoxyquinazolin-6-yl (2R)-2,4-dimethylpiperazine-1-carboxylate 1m (AZD3759), an investigational drug currently in Phase 1 clinical trial, which has excellent central nervous system penetration and which induces profound regression of brain metastases in a mouse model.

Topics: Animals; Brain; Brain Neoplasms; Central Nervous System; Clinical Trials, Phase I as Topic; Dogs; Drug Discovery; ErbB Receptors; Macaca fascicularis; Male; Mice; Piperazines; Positron-Emission Tomography; Protein Kinase Inhibitors; Protein-Tyrosine Kinases; Quinazolines; Rats; Rats, Wistar; Xenograft Model Antitumor Assays

2015