Recently, Keythera (Suzhou) Biopharmaceuticals Co., Ltd. (“Keythera”) has received approval from the National Medical Products Administration (NMPA) for the clinical trial of their internally developed product, KF-0210 tablets. The KF-0210 tablets meet the relevant requirements for drug registration and have been granted permission to proceed with clinical trials for osteoarthritis. Thus, the KF-0210 tablets will enter the Phase II clinical development stage.

KF-0210 tablets are small molecule oral formulations developed by Keythera Biopharmaceuticals. They are highly selective and potent antagonists of the E-type prostaglandin receptor 4 (EP4), with a selectivity 500 times greater than other tested prostaglandin receptors. Prostaglandins are metabolites of arachidonic acid catalyzed by cyclooxygenase (COX). Among them, prostaglandin E2 (PGE2) is the main mediator of inflammatory pain and inflammation. Antagonists of the PGE2 receptor EP4 can achieve anti-inflammatory and analgesic effects by blocking downstream signaling pathways of PGE2 without affecting prostaglandins, especially PGI2, thereby avoiding adverse effects on the kidneys and cardiovascular system caused by COX-2 inhibitors. Results from animal models of arthritis have demonstrated that KF-0210 tablets have the efficacy to alleviate pain and inflammation without affecting clotting-related signaling pathways. Phase I clinical trial results of KF-0210 tablets indicate good safety and pharmacokinetic characteristics.

Osteoarthritis (OA) is the most common joint disease primarily characterized by damage to joint cartilage and involvement of the entire joint tissue. It eventually leads to cartilage degeneration, fibrosis, rupture, ulceration, and damage to the entire joint surface. OA is a degenerative joint disease that severely impacts the quality of life for patients, manifested by joint pain, stiffness, swelling, and limited mobility. It is a major cause of disability in the elderly. According to literature reports, there are currently over 300 million OA patients worldwide, and the overall incidence of primary OA in the Chinese population over the age of 40 has reached 46.3%. Moreover, with the acceleration of population aging and the increasing prevalence of obesity, the incidence of OA is gradually rising. Drug therapy is one of the important approaches for pain management in OA. The Chinese Guideline for the Diagnosis and Treatment of Osteoarthritis (2021 edition) recommends oral nonsteroidal anti-inflammatory drugs (NSAIDs), including non-selective NSAIDs and selective cyclooxygenase-2 (COX-2) inhibitors, for OA patients with persistent or moderate to severe pain. However, caution is needed regarding gastrointestinal and cardiovascular adverse events. EP4 receptor antagonists can provide anti-inflammatory and analgesic effects while avoiding potential prothrombotic tendencies and the associated cardiovascular side effects caused by COX-2 inhibitors. They are expected to become a safer new generation of anti-inflammatory and analgesic drugs.

About Keythera Biopharmaceuticals

Keythera Pharmaceuticals is a clinical-stage biotechnology company that focuses on the clinical development of small molecule new drugs for oncology and autoimmune diseases. The company's founder and management team have extensive experience in preclinical and clinical development, as well as world-class innovation capabilities. Through a comprehensive strategy with the product pipeline as the core and technology platforms as support, the company has achieved effective acceleration of new drug development, reduced the risks associated with drug development, and achieved differentiation in its product pipeline. The company currently has six product pipelines covering the fields of oncology and autoimmune diseases. Since its establishment, the company has received numerous honors and awards, including being recognized as a leading company in the Suzhou Industrial Park and Suzhou area, winning the First Prize of the 10th Innovation and Entrepreneurship National Competition (Start-up Group) in 2021, and being selected as a “ Unicorn Cultivation Enterprise” in Suzhou in 2022.

Back to List