The use of azepane as a scaffold for drug discovery remains of interest. The azepane linker is the key to efficient activity. A number of seven-membered ring derivatives have been prepared or investigated for their potential or actual pharmacological properties. Examples include azaalkane derivatives as PKB (protein kinase B) inhibitors.
Puma Biotechnology announced the initiation of its ALISertib in CAncer (ALISCA-Lung1) Phase II trial of alisertib monotherapy for the treatment of patients with extensive stage small cell lung cancer. The ALISCA-Lung1 trial will enroll up to 60 patients with extensive stage small cell lung cancer who have progressed on or after first-line platinum-based chemotherapy and immunotherapy. The primary endpoint of the trial is objective response rate, with secondary endpoints of duration of response, disease control rate, progression-free survival and overall survival. Based upon the outcomes of the study, Puma anticipates meeting with the FDA to explore the potential for an accelerated approval pathway for alisertib in small cell lung cancer. Alisertib is an orally active and selective Aurora A kinase inhibitor, which binds to Aurora A kinase resulting in mitotic spindle abnormalities, mitotic accumulation. Chemenu has been working to develop more compounds for drug discovery. Here are the building blocks we can provide.
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