Drug Discovery

Our challenge: pioneering innovative drug development to overcome cancer. For the genuine smiles of patients and their families. We strive to deliver disease-free lives, “Today and Every Day”, and to liberate patients from the anxiety of illness.

Taiho Pharmaceutical continues to take on the challenge of discovering new drugs, leveraging proprietary drug-discovery platform technologies and innovative research approaches to bring hope to all the people worldwide awaiting new treatments.

Our Research Vision at Taiho Pharmaceutical

The drug discovery research centers in Tsukuba and Zurich are the core bases for drug discovery in Taiho Pharmaceutical. They play a pivotal role in achieving our high in-house drug discovery rate of approximately 70%. Their mission is to address unmet medical needs and discover breakthrough drugs that have not been applied in clinical practice, thereby helping to support cures for serious diseases. To deliver novel drugs developed in-house to patients, we leverage our proprietary drug-discovery platform technologies to continuously expand our pipeline of clinical candidates. The drug discovery landscape today is changing rapidly, and the pharmaceutical companies are facing an era of discontinuity and uncertainty. To foster innovation in contexts where optimal solutions are hard to predict, we are constantly striving to strengthen the capabilities of our research team and upgrade our research infrastructure. We are promoting the development of a world-class research organization, both in terms of human talent and physical resources. About 70% of our drug discovery efforts focus on the oncology field —research on the causes and treatment of tumors. Taiho Pharmaceutical has mainly focused on discovering oncology drugs that expand the lifespan of patients while reducing side effects and developing symptomatic treatments for other disease areas. However, this approach alone cannot truly relieve patients from anxiety about their illness. That’s why we have shifted our research toward drug discovery to overcome cancer. Developing new drugs that can be classified as drugs to overcome cancer is an extremely challenging endeavor. Nevertheless, we embrace this lofty goal and continue to take on the challenge by leveraging synergies between our proprietary drug-discovery platform technologies and the innovative ideas.

Unmet medical needs: Medical needs related to diseases that currently have no effective treatments or indicated drugs, or in more broadly speaking, “unanswered medical challenges.”

Unique Strengths of Taiho Drug Discovery

Taiho Pharmaceutical’s drug discovery platform serves as a drug discovery engine for identifying the most promising targets, based on experimental data from a diverse range of biological mechanisms, thereby facilitating the identification of new drug candidate compounds. At our Tsukuba Research Institute, through collaborating with companies and academic institutions worldwide, we have established our own drug-discovery platform technologies. Taiho Pharmaceutical’s strength in drug discovery lies in our comprehensive research approach driven by the sophisticated integration of proprietary drug-discovery platforms. At the core of our approach is Cysteinomix, an innovative platform for the discovery of drugs designed to form covalent bonds with a specific amino acid (cysteine) in target proteins. We recognized the potential of Cysteinomix early on and have been building a compound library for over 10 years to identify hit compounds. Currently, we are actively leveraging Cysteinomix in our drug discovery effort to tackle the challenges of refractory cancers with low treatment satisfaction, and to explore new modalities (drug discovery technologies and methods). While developing new covalent inhibitors, we are also advancing fundamental research to further enhance Cysteinomix and broaden the scope of potential drug discovery targets. Translational Research, which bridges drug discovery and clinical trials, also plays an important role. We are advancing our unique translational research by analyzing a wide range of clinical trial data generated from the extensive clinical pipeline we have built.

Cysteinomix: Taiho Pharmaceutical’s unique drug-discovery platform technology, which achieves high potency and selectivity by covalently binding drugs to the specific cysteine residues of therapeutic target proteins. This technology promises potential clinical benefits such as reduced toxicity.

In March 2025, Taiho Pharmaceutical acquired Araris Biotech AG’s next-generation Antibody-Drug Conjugates (ADCs) drug-discovery platform, AraLinQTM.
Special Features of Next-Generation ADCs Enabled by AraLinQTM

  • Precisely binds to a specific site, ensuring extremely high uniformity.
  • Enhanced physicochemical properties and improved stability in the bloodstream.
  • Capable of carrying multiple payloads with different mechanisms of action (MoAs).

AraLinQTM Technology

These features are expected to enhance cancer selectivity and therapeutic efficacy, delivering a groundbreaking solution to the current challenges of toxicity and limited efficacy in ADCs.

By leveraging this new drug discovery platform, AraLinQTM, we will develop innovative new drugs for various types of cancer.

Prospects and Challenges in Drug Discovery Research

Under the communication slogan “Today and Every Day,” Taiho Pharmaceutical strives through our drug discovery to help patients living with illnesses enjoy their invaluable daily lives, Today and Every Day. We are currently conducting drug discovery research in developing new treatments for refractory cancers such as pancreatic cancer and metastatic brain tumors. However, even in non-refractory cancers, while anticancer drugs can shrink tumors, achieving complete recovery remains challenging. Patients living with cancer often experience deep anxiety and uncertainty, falling short of our vision to support people’s “Today and Every Day.” We strive to be a force that liberates patients from this anxiety. Our unwavering goal is to continuously explore the potential of drug discovery that leads to complete recovery, a vision we are determined to pursue.
Two drug discovery platforms, Cysteinomix and AraLinQTM, drive this challenge forward. By leveraging these platforms, we strive to identify innovative new drugs. At the same time, we are continuously evolving our drug discovery platforms to address the growing diversity and complexity of drug development. We believe that integrating the platforms we have established and maximizing their value is essential. Taiho Pharmaceutical remains committed to taking on the challenge of addressing unmet medical needs.

Product Pipeline