Building a Pipeline with Purpose

As the most commonly diagnosed cancer affecting women globally, the impact of breast cancer on patients, families, and healthcare systems is profound. Despite medical advances of the past few decades, breast cancer remains the fourth leading cause of cancer mortality worldwide and the number one cause of cancer death in women, responsible for over 650,000 deaths in 2022^1,2. This is a disease that touches almost everyone on the planet, and unfortunately many patients worldwide do not have access to the latest therapies. BeOne’s mission is to make innovative oncology medicines that are more affordable and accessible globally, and we are turning our attention to breast cancer because we think we can develop therapies that are more effective and better tolerated than today’s medicines and make them available to more patients around the world.

Historically, in solid tumors BeOne has been most visible for its activity in lung and gastrointestinal cancers where we have established a deep immuno-oncology and targeted therapy portfolio centered around our backbone PD-1 inhibitor. And while those programs remain key areas of focus for us, our commitment to generating clinically impactful medicines that are accessible to more patients globally has driven us to expand our solid tumor pipeline and apply our innovation to address the world’s most deadly cancers including breast cancer.

In the face of sobering statistics and even more compelling patient stories, we are building a robust pipeline of differentiated investigational medicines for breast cancer to develop new therapies that may both effectively combat the disease and improve the quality of life for patients receiving treatment. In just the last year we have advanced three new molecules into clinical development for breast cancer – two cyclin dependent kinase (CDK) inhibitors and an antibody-drug conjugate (ADC) – and this week we are convening with clinical and industry peers at the annual San Antonio Breast Cancer Symposium. We are pleased to be sharing the first clinical data for our selective CDK4 inhibitor, as well as discussing our deep and broad commitment in this important disease area.

Our breast cancer pipeline features cell cycle dependent kinase inhibitors designed to deliver potentially better efficacy and reduced toxicity relative to currently available options. CDK inhibitors work by targeting checkpoint proteins that control cell division, effectively aiming to halt the growth of cancer cells. CDK4/6 inhibitors are already a crucial part of breast cancer therapy for certain patients, but they come with limitations—particularly dose-dependent toxicities and resistance mutations that can limit their effectiveness. Our CDK4 inhibitor is uniquely designed to be highly selective for CDK4 over CDK6, which we hope will allow it to deliver the same or better efficacy as current treatments but with fewer side effects. The results of our ongoing Phase 1 study support continued development, demonstrating that the molecule has been generally well tolerated across a range of doses with encouraging early signs of clinical activity emerging. We’re hopeful that as we advance development, our CDK4 inhibitor will further differentiate itself as an effective and better tolerated option for people with breast cancer.

Complementing our CDK4 inhibitor, we’re also in Phase 1 testing a novel CDK2 inhibitor which is designed to address CDK2 and cyclin E-driven resistance mechanisms that often limit the effectiveness of CDK4/6 inhibitors. We think this mechanism has the potential to increase the effectiveness of CDK4 inhibition and provide an option for CDK4/6 resistant disease.

In addition to our two CDK inhibitors, our pipeline targets breast cancer with novel ADCs and other molecularly targeted agents and modalities. In Phase 1 development we have an ADC targeting the B7H4 protein, which is broadly expressed in breast and gynecologic cancers. This molecule is an investigational targeted therapy designed to deliver a potent cancer-killing drug directly to the cancer cells. And our preclinical pipeline includes a diverse collection of novel molecules — multispecific antibodies, targeted protein degraders, and more small molecules and ADCs — with potential complementary or synergistic applications in breast cancer.

The science that supports our portfolio is compelling, but the critical step is translating the science into clinical results that have a meaningful impact for patients. We never lose sight of that responsibility, and as we continue to advance our breast cancer pipeline, we do so for the patients and families who may be able to experience more, better days as a result of medicines we make. The fight against breast cancer is ongoing, and we’re committed to being a force for progress.