Reading, UK, 12 December 2024 – Bayer announced today initiation of a Phase I clinical trial with BAY3498264, an investigational oral selective Son of Sevenless Homologue 1 (SOS1) inhibitor. 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.3 Kirsten rat sarcoma (KRAS) is one of the most commonly mutated oncogenes in human cancer, found in up to 85% of cancers driven by RAS alterations.1
Developed in-house, BAY3498264 is being evaluated for the potential to address the unmet medical need of improving efficacy of treatment targeting the mitogen-activated protein kinase (MAPK) signaling pathway, which regulates cell proliferation and plays a critical role in tumour growth and carcinogenesis2. “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. This innovative approach has the potential to enhance the treatment options available for patients, offering the possibility to reduce or potentially stop tumour progression,” said Dominik Ruettinger, M.D., Ph.D., Global Head of Research and Early Development for Oncology at Bayer’s Pharmaceuticals Division. “We look forward to advancing the programme through clinical development, strengthening Bayer’s innovative oncology treatments by broadening the range of druggable targets”.
BAY3498264 is a selective SOS1 inhibitor which, when combined with a KRAS targeting agent, shows potential as a therapeutic agent for KRAS-mutant cancers, such as non-small cell lung cancer (NSCLC), pancreatic cancer and colorectal cancer. SOS1 facilitates KRAS activation and influences downstream signaling pathways. Co-inhibiting SOS1 with KRAS may help to slow or inhibit the growth of cancer cells reliant on this pathway, by enhancing the effectiveness of KRAS inhibition and contributing to deeper and/or longer-lasting treatment responses in various cancers.
KRAS mutations are common drivers of several types of cancer such as lung cancer, especially in NSCLC. Lung cancer was the most diagnosed cancer in 2022 worldwide, accounting for nearly 2.5 million new cases globally.4 Lung cancer remains the leading cause of cancer-related deaths, with the International Agency for Research on Cancer (IARC) predicting significant increases in both incidence (55.8%) and mortality (60.3%) by 2040.5 KRAS mutations activate pathways that promote tumour growth and survival, making the KRAS/MAPK pathway a key therapeutic target for addressing the needs of patients with these mutations.
ENDS
Bayer Media Contact:
Veronica Yao, +44 (0) 7870 485 926
Email: veronica.yao@bayer.com
Notes to Editors
About Oncology at Bayer
Bayer is committed to delivering science for a better life by advancing a portfolio of innovative treatments. The company has the passion and determination to develop new medicines that help improve and extend the lives of people living with cancer. The oncology franchise at Bayer includes several marketed products across diverse indications and multiple compounds in different stages of clinical development. We have a wealth of expertise in areas including Tumour Cell Intrinsic Pathways, Targeted Radionuclide Therapies, and Next-Generation Immuno-Oncology. With our portfolio we are advancing cancer treatments from early to metastatic stage, with the goal of extending survival while limiting side effects for the cancer patients we serve.
About Bayer
Bayer is a global enterprise with core competencies in the life science fields of health care and nutrition. In line with its mission, “Health for all, Hunger for none,” the company’s products and services are designed to help people and the planet thrive by supporting efforts to master the major challenges presented by a growing and aging global population. Bayer is committed to driving sustainable development and generating a positive impact with its businesses. At the same time, the Group aims to increase its earning power and create value through innovation and growth. The Bayer brand stands for trust, reliability and quality throughout the world. In fiscal 2023, the Group employed around 100,000 people and had sales of 47.6 billion euros. R&D expenses before special items amounted to 5.8 billion euros. For more information, go to www.bayer.co.uk.
Forward-Looking Statements
This release may contain forward-looking statements based on current assumptions and forecasts made by Bayer management. Various known and unknown risks, uncertainties and other factors could lead to material differences between the actual future results, financial situation, development or performance of the company and the estimates given here. These factors include those discussed in Bayer’s public reports which are available on the Bayer website at www.bayer.co.uk. The company assumes no liability whatsoever to update these forward-looking statements or to conform them to future events or developments.
References:
1. Simanshu et al. 2017 Cell. 2017 June 29; 170(1): 17–33.
2. Braicu C et al. A comprehensive review on MAPK: A promising therapeutic target in cancer. Cancers 2019, 11, 1618; doi:10.3390/cancers11101618
3. A Phase I Study of BAY3498264 Given Together With Sotorasib in Participants Who Have Advanced Solid Cancers With Specific Genetic Changes Called KRASG12C Mutation. Clinicaltrials.gov. Available at: https://clinicaltrials.gov/study/NCT06659341. Last access: November 2024.
4. Global cancer statistics 2022, GLOBOCAN estimates of incidence and mortality worldwide for 36 cancers in 185 countries, Freddie Bray BSc, MSc, PhD, Mathieu Laversanne MSc, Hyuna Sung PhD, Jacques Ferlay ME, Rebecca L. Siegel MPH, Isabelle Soerjomataram MD, MSc, PhD, Ahmedin Jemal DVM, PhD
5. International Agency for Research on Cancer, Cancer Tomorrow, Predictions of the future cancer incidence and mortality burden worldwide up until 2050.
RP-PF-ONC-GB-0163 / December 2024