On December 12, 2019, another class 1.1 targeted anti-cancer new drug TY-302 capsule developed by TYK Medicines was granted IND approval for the treatment of hormone receptor-positive and epidermal growth factor receptor-2-negative (HR+/HER2-) locally advanced or metastatic breast cancer and other advanced solid tumors or hematologic tumors.

Breast cancer is the most common type of cancer among women, with 2 million breast cancer patients diagnosed worldwide in 2018, 75% of whom are HR-positive. Breast Cancer in China shows that by 2021, there will be 2.5 million breast cancer patients in China. Patients with advanced breast cancer have a lower survival rate compared to those with early-stage breast cancer, with a 5-year survival rate of 85% for locally advanced patients and only 27% for patients with metastatic breast cancer [1].

TY-302 is a compound with completely independent intellectual property rights independently developed by TYK Medicines and is a potent and highly selective oral cyclin-dependent kinase 4/6 (CDK4/6) inhibitor. As a new targeted therapy, CDK4/6 inhibitors have a unique anti-tumor mechanism of action and are the hotspot of tumor treatment research in recent years. There are currently three CDK4/6 inhibitors approved worldwide – Pfizer’s Palbociclib (trade name: Ibrance), Novartis’ Ribociclib (trade name: Kisqali) and Eli Lilly’s Abemaciclib (trade name: Verzenio), of which Ibrance, as the first CDK4/6 inhibitor on the market, sales revenue exceeded $4 billion in 2018.

CDK4/6 is a key regulator of the cell cycle from the G1 phase to the S phase, catalyzing the phosphorylation of the retinocytoma gene (Rb), resulting in the dissociation of the transcription factor E2F bound by the Rb protein, thereby initiating the transcription of downstream molecules. At present, CDK4/6 is found to be overactive in most malignant tumors, showing significant activity, and resulting in uncontrolled proliferation. Therefore, inhibiting the function of cyclin can inhibit the growth of tumor cells in a targeted manner without much harm to normal cells. CDK4/6 may also be the most promising treatment direction for endocrine-resistant breast cancer patients.

“We are very pleased to learn that TY-302 capsules have obtained IND approval, which marks that the second 1.1 Class new drug obtained by TYK Medicines this year is about to enter clinical research. In follow-up clinical studies, we will propose as a monotherapy or in combination with hormone therapy mainly for the first- and second-line treatment of HR+/HER2- patients with postmenopausal locally advanced or metastatic breast cancer, and will also explore the use of TY-302 alone or in combination for the treatment of other tumors with abnormal regulation of the CDK4/6 pathway, such as acute myeloid leukemia, ovarian cancer, melanoma, lung cancer, triple-negative breast cancer, and head and neck tumors, etc.” Dr. Yusheng Wu, the founder, chairman and CEO of TYK Medicines, said, “TYK Medicines has been committed to the research and development of innovative drugs, and all departments of the company have worked together to complete preclinical research from mechanism research to compound screening to pharmacology, pharmacodynamics, pharmacokinetics, safety assessment, and other preclinical research with the fastest speed and high quality, and successfully submitted all IND application materials. The company currently has a first-class R&D and management team, including National Thousand Talents Program expert, Zhejiang Thousand Talents Program expert, overseas returnee doctoral experts, and clinical experts, has rich experience in new drug research and development of well-known multinational pharmaceutical companies, will aim at ‘best-in-class & first-in-class’, develop more and better innovative drugs accessible to Chinese patients, so that ordinary Chinese patients can access and afford the best medicine.” “The Company is currently focused on the anti-tumor small molecule, with a pipeline of not only world-leading First-in-Class new drugs, but also high-success mature target Best-in-Class new drugs that balance unmet clinical needs and commercial viability.” Dr. Jun Li, the company’s Chief Scientific Officer, said, “TY-302 is a typical representative of the mature targets in the TYK Medicines’ pipeline, with Best-in-Class potential.”

Reference

1. Fan L, Strasser-Weippl K, Li JJ, St Louis J, Finkelstein DM, Yu KD, Chen WQ, Shao ZM, Goss PE. Breast cancer in China. Lancet Oncol. 2014 Jun;15(7):e279-89. doi: 10.1016/S1470-2045(13)70567-9. PMID: 24872111.