New BGB324 study points to novel mechanism to enhance immunotherapy efficacy

Presented at CRI-CIMT-EATI-AACR – The 2nd International Cancer Immunotherapy Conference
Bergen, Norway, September 25, 2016 – Leading oncology biopharmaceutical company BerGenBio AS, today released important new preclinical study data on its first-in-class AXL inhibitor, BGB324. The study showed AXL to be a key factor in tumour resistance to the emerging class of new immune checkpoint inhibitors that can be targeted through combination therapy with BGB324. The study data was presented in a poster today at CRI-CIMT-EATI-AACR – The 2nd International Cancer Immunotherapy Conference, in New York.
The new study evaluated whether BGB324 used in combination with immune checkpoint inhibitors (anti-CTLA-4 and anti-PD-1) in mouse carcinoma models enhanced the effect of immune checkpoint blockade in aggressive adenocarcinomas displaying limited immunogenicity. BGB324 is a highly selective small molecule inhibitor of the AXL receptor tyrosine kinase. An important regulator of the tumour cell plasticity related to EMT (Epithelial-to-Mesenchymal Transition), AXL signalling is also a key suppressor of the innate anti-tumour immune response. Thus AXL contributes uniquely to both tumour intrinsic and extrinsic mechanisms that suppress anti-tumour immunity. The new study shows that AXL was induced in tumours by immune checkpoint inhibitor treatment and postulated that this could limit their efficacy.
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:
“We believe this strong new preclinical data clearly demonstrates the rationale for combining BGB324 with immune checkpoint inhibitors to treat aggressive cancers. This study shows that these inhibitors actually increase AXL expression that supports immune evasion. Treatment with BGB2324 counters this, increasing tumor immunogenicity and promoting the anti-tumour response. 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.”
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BerGenBio AS
+47 917 86 304
Richard Godfrey, CEO
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RHA
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Richard Hayhurst

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. www.bergenbio.com