BerGenBio Presents Positive Phase Ia Data on BGB324 at AACR

BERGEN, Norway, April 9, 2014 /PRNewswire/ --



or the "Company"), an oncology biopharmaceutical company, announces that results from its successful Phase Ia clinical study for lead compound, BGB324, was presented at the American Association of Cancer Research annual conference, which took place on April 5-9, 2014.

BGB324 is a first-in-class, highly selective small molecule inhibitor of the Axl receptor tyrosine kinase. It blocks the epithelial-mesenchymal transition (EMT), which is a key driver in drug-resistance and metastasis.

The poster entitled "BGB324, a selective small molecule Axl kinase inhibitor to overcome EMT-associated drug resistance in carcinomas: Therapeutic rationale and early clinical studies", detailed the results of a single ascending dose study, which evaluated the safety and tolerability, and pharmacokinetics of BGB324 in 32 healthy volunteers. BGB324 was shown to be safe and well tolerated in doses up to 1.5 g/daily with a predictable PK profile and long plasma half-life, allowing for different dosing options. Reported adverse events in doses up to 1 gm were no more than grade 1 in severity and were fully reversible. The most common adverse event reported was gastrointestinal in nature and occurred more frequently at higher doses (above 1 gm).

The poster also included results from preclinical in vivo studies in animal models of triple negative breast cancer (TNBC), pancreatic cancer and non-small cell lung cancer (NSCLC). Data from these studies demonstrated that BGB324, in combination with targeted chemotherapeutic agents, effectively delays or blocks acquired drug resistance, leading to a significant prolonged survival in these disease models. BGB324 was also shown to block the ability of TNBC cells to initiate tumour formation, a characteristic of cancer stem cells.

Richard Godfrey, Chief Executive Officer of BerGenBio, commented: "There is an urgent unmet medical need for new therapies that are able to overcome drug resistance. The encouraging results from the Phase Ia trial combined with strong preclinical data support our view that blocking Axl with BGB324 is a promising new treatment option for drug resistant cancers. BGB324 is the only selective Axl inhibitor in clinical development and has the potential to significantly enhance the efficiency of targeted and chemotherapeutic agents. Following the results of these studies, we will initiate multi-centre Phase Ib trials in NSCLC and AML patients starting in the near future."

About the Axl kinase receptor 

Axl is a member of the Tyro3, Axl, Mer receptor (TAMR) tyrosine kinase family and is a fundamental receptor to cancer biology. It plays a crucial role in the epithelial-mesenchymal transition (EMT) which is a key driver of metastasis (cancer spread) and a mechanism of drug-resistance. The Axl receptor is regarded as one of the most promising new therapeutic targets for cancer drug development.

About Non-Small Cell Lung Cancer  

Non-small cell lung cancer (NSCLC) is an aggressive form of cancer, classified as any type of epithelial lung cancer other than small cell lung carcinoma. About 85% to 90% of lung cancers are NSCLC. There are 3 primary types of NSCLC: adenocarcinoma, squamous cell carcinoma and large cell carcinoma. The American Cancer Society estimates that 228,190 new cases of NSCLC will be diagnosed in 2013.

About BerGenBio AS 

BerGenBio AS is a biopharmaceutical company located in Bergen, Norway. The company is committed to developing first in class therapeutics that inhibit EMT, preventing the formation of cancer stem cells and disrupting the important mechanisms of acquired cancer drug resistance. The company is founded on proprietary platform technology called CellSelect™, which uses information from RNAi screening studies to identify and validate novel drug targets and biomarkers. BGB324 is the first compound in BerGenBio's pipeline to enter clinical trials, with additional compounds and drug targets at different stages of preclinical development.

SOURCE BerGenBio