BGB324 Enhances Immune Checkpoint Inhibitor Efficacy in Preclinical Cancer Models

BERGEN, Norway, September 21, 2015 /PRNewswire/ --

BerGenBio AS ("BerGenBio" or the "Company"), an oncology biopharmaceutical company, has announced new preclinical data on lead compound, BGB324, in combination with immune checkpoint inhibitors, has been presented as a poster at CRI-CIMT-EATI-AACR - The Inaugural International Cancer Immunotherapy Conference: Translating Science into Survival, in New York.

This preclinical data highlights that BGB324, a first-in-class, highly selective small molecule inhibitor of the Axl receptor tyrosine kinase, used in combination with immune checkpoint inhibitors (anti-CTLA-4 and anti-PD-1) in mouse carcinoma models showed enhanced tumour clearance, survival and tumour infiltration of cytotoxic T lymphocytes compared with checkpoint inhibition alone.

The poster entitled "BGB324, a selective small molecule inhibitor of the receptor tyrosine kinase Axl, enhances immune checkpoint inhibitor efficacy", was presented on Friday, September 18. The studies were conducted in an aggressive mammary adenocarcinoma (4T1) syngeneic mouse model. BGB324 (50 mg/kg bid) significantly enhanced responsiveness to anti-CTLA-4/anti-PD-1 treatment (10 mg/kg of each, 4 doses) in Balb/C mice bearing established 4T1 tumours. The well-tolerated combination of BGB324 + anti-CTLA-4/anti-PD-1 resulted in durable primary tumour clearance in 23% of treated mice versus 5.6% obtained with anti-CTLA-4/anti-PD-1 alone (p=0.0157). In a separate study, BGB324 + anti-CTLA-4 treated resulted in 22% long-term primary tumour clearance while no response was observed with anti-CTLA4 treatment alone. The extensive metastasis to the lung, liver and spleen characteristic of this model were concomitantly abrogated in the animals responding to the combination treatment. In addition, BGB324 + anti-CTLA-4/anti-PD-1 treated tumours displayed enhanced infiltration of cytotoxic T lymphocytes. Importantly, responding animals rejected orthotopic 4T1 tumor cell re-challenge, demonstrating sustained tumour immunity.

BGB324 is the only selective Axl inhibitor currently in clinical development. Phase Ib clinical trials are underway as single agent and in combination with standard of care drug (cytarabine) in acute myeloid leukaemia (AML), and in combination with erlotinib in non-small cell lung cancer (NSCLC).

Richard Godfrey, Chief Executive Officer of BerGenBio, commented:

"This promising new preclinical data demonstrates the rationale for combining BGB324 with immune checkpoint inhibitors to treat aggressive cancer. In addition to the ongoing development of BGB324 in AML and NSCLC, this data suggests that BGB324 could also be used in combination with cancer immunotherapeutic agents to enhance their efficiency."

About BGB324 

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 immune evasion, drug-resistance and metastasis.

About BerGenBio AS 

BerGenBio AS is a clinical stage biopharmaceutical company focused on developing first-in-class drugs for aggressive cancers. The company is a world leader in understanding the biology of epithelial-mesenchymal transition (EMT), a widely recognised key pathway in immune evasion, acquired cancer drug-resistance and metastasis. BerGenBio AS is founded on proprietary platform technology, CellSelect™, to identify and validate novel drug targets and biomarkers. The company has progressed its lead drug candidate BGB324, an EMT inhibitor, into clinical trials in AML and NSCLC, while pursuing the pre-clinical development of additional compounds and proprietary EMT drug targets. http://www.bergenbio.com

SOURCE BerGenBio