A first-in-human phase I study to determine the maximum tolerated dose of the oral Src/ABL inhibitor AZD0424.

ABSTRACT:

Background

Src is involved in cancer invasion and metastasis. AZD0424, an oral inhibitor of Src and ABL1, has shown evidence of anti-tumour activity in pre-clinical studies.

Methods

A phase Ia, dose escalation study was performed to assess the safety of continuous oral dosing with AZD0424 in advanced solid tumours. Secondary objectives included investigation of AZD0424 pharmacokinetics, effect on Src activity using markers of bone turnover, and anti-tumour activity.

Results

41 patients were treated; 34 received AZD0424 once-daily at doses ranging from 5 mg to 150 mg, and 7 received 40 mg bi-daily 41.5% of patients experienced at least one AZD0424-related adverse event that was Grade 3-5 in severity, with patients treated at doses above 60 mg per day experiencing multi

SUBMITTER: Woodcock VK 

PROVIDER: S-EPMC5877436 | biostudies-literature | 2018 Mar

REPOSITORIES: biostudies-literature