The trial is being carried out at the University of Texas MD Anderson Cancer Center, Houston, Oncology Partners, Houston, and at UT Southwestern Medical Center, Dallas, Texas, US.
University of Texas MD Anderson Cancer Center Thoracic/Head & Neck Medical Oncology professor and chair John Heymach said: "Acquired resistance to erlotinib curtails the clinical utility of this drug in the treatment of NSCLC.
"BGB324’s novel mechanism holds tremendous potential for improving the treatment outcomes in this setting and I am excited to be able to offer my patients the drug in this clinical trial and look forward to reporting the outcomes in due course."
A total of 66 patients will be enrolled in the multi-centre trial, which is designed to determine the maximum dose of BGB324 that can be safely administered in combination with erlotinib.
The trial will also identify the recommended Phase II dose of BGB324 as well as evaluate the safety, pharmacokinetics and clinical activity of BGB324 in combination with erlotinib.
BerGenBio CEO Richard Godfrey said: "The initiation of the NSCLC trial demonstrates our continuing clinical progress with BGB324, our first-in-class selective Axl inhibitor.
"This is our second Phase Ib trial following the initiation of the acute myeloid leukaemia trial in November 2014 and we look forward to reporting results from these studies later in 2015."
BGB324 is a first-in-class, highly selective small molecule inhibitor of the Axl receptor tyrosine kinase and it blocks the epithelial-mesenchymal transition (EMT), a major driver in drug-resistance and metastasis.