Bayer begins inhibitor study treating advanced KRAS-mutated tumours

Trial explores potential of therapy in treating multiple cancer types

Bayer has begun a phase 1 clinical trial for BAY3498264, an investigational oral selective SOS1 inhibitor, to assess its safety and efficacy in patients with advanced KRAS G12C-mutated solid tumours.

This study represents a significant advancement in targeting a variety of KRAS-mutated cancers, including non-small cell lung cancer (NSCLC), pancreatic cancer, and colorectal cancer.

“The start of the trial with our novel SOS1 small molecule inhibitor marks a significant step in our commitment to targeting key drivers of tumour cell survival and growth,” said Dominik Ruettinger, MD, PhD, Global Head of Research and Early Development for Oncology at Bayer’s Pharmaceuticals Division. “This innovative approach has the potential to enhance the treatment options available for patients, offering the possibility to reduce or potentially stop tumour progression.”

Developed in-house, BAY3498264 targets the mitogen-activated protein kinase (MAPK) signalling pathway, which is crucial for cell proliferation and tumour growth.

KRAS mutations are common in many cancers, driving tumour growth and survival. The study will evaluate the dose escalation and combination therapy potential of BAY3498264.

BAY3498264, when combined with a KRAS targeting agent, could slow or inhibit cancer cell growth by enhancing the effectiveness of KRAS inhibition. This dual approach aims to improve treatment responses in various cancers reliant on the KRAS/MAPK pathway.

“Lung cancer remains the leading cause of cancer-related deaths, and new treatments are urgently needed,” added Ruettinger. The International Agency for Research on Cancer predicts significant increases in lung cancer incidence and mortality by 2040, highlighting the importance of developing new therapies.

Bayer’s initiative reflects a broader effort to address the high unmet medical need in oncology. The trial’s success could pave the way for improved outcomes in patients with KRAS-mutated cancers, providing hope for those with limited treatment options.

The open-label, first-in-human dose escalation study (NCT06659341) will evaluate the safety, tolerability, and preliminary efficacy of BAY3498264 as a combination therapy in patients with advanced KRAS G12C-mutated solid tumours.

With the potential to treat a variety of KRAS-mutated cancers, BAY3498264 represents a significant advancement in Bayer’s precision oncology development portfolio.