On 21 March, according to the CDE's official website, Kangpu Biopharmaceuticals, Ltd. (hereinafter referred to as "Kangpu") was granted an implied licence to conduct clinical trials for KPG-818 capsule, a Class 1 chemotherapy, with the indication of systemic lupus erythematosus.
Immunomodulators are a class of drugs that regulate the body's immune system and activate or inhibit the immune response, and can be used clinically to treat various immune system-related diseases. In recent years, with the in-depth study of immune system-related diseases, a new generation of immunomodulatory compounds with more significant effects and higher safety have been discovered.
KPG-818, designed and developed by Kangpu, is a new generation of oral molecular gel immunomodulatory drugs belonging to the E3 ubiquitin ligase complex CRL4-CRBN modulator. According to public information, KPG-818 exhibits a high affinity for target CRBN binding, and is able to efficiently degrade the zinc-finger transcription factors Aiolos (IKZF3) and Ikaros (IKZF1), which are closely related to the development and proliferation of B-lymphocytes, and to effectively regulate the expression levels of cytokines, such as TNF-alpha, IL-6, IL-2, IL-10, and so on.
Currently, KPG-818 is undergoing a number of clinical trials overseas, including Phase I clinical trials for haematological tumours and Phase Ib/IIa clinical trials for systemic lupus erythematosus. In February this year, Kangpu presented a poster on the efficacy data of KPG-818 in animal models for the treatment of Crohn's disease at the 19th ECCO Congress, and announced that it will be submitted to the US Phase II clinical trial.
The approved indication for KPG-818 in China is systemic lupus erythematosus, and Kangpu may conduct additional clinical trials for KPG-818 in the future.
Focusing on the development of innovative drugs for cancer, autoimmune diseases, inflammation and other therapeutic areas, Kangpu owns the world's leading proprietary patents on the new generation of molecular gel-protein ubiquitination and its degradation technologies, such as NeoMIDES®, SelPDEiS®, X-SYNERGY®, and so on. At present, based on the above technologies, Kangpu has successfully built up a rich pipeline in research and development.
Among them, KPG-121 is a new generation CRBN E3 ubiquitin ligase complex CRL4CRBN regulator, which has inhibitory cell proliferation activity as well as anti-angiogenic activity, and at the same time is able to enhance the body's immunomodulatory function. In November 2023, Kangpu presented a case report on KPG-121 at the 2023 Society for Immunotherapy of Cancer Annual Meeting and announced that it will initiate a global, multi-centre Phase II/III registrational clinical trial of KPG-121 for the treatment of metastatic desmoplasia-resistant prostate cancer.
KPG-712 is a new-generation small molecule PDE4 inhibitor with strong affinity for PDE4 targets, which can reverse specific signals in the immune system by inhibiting cyclic adenosine monophosphate (cAMP) hydrolysis in immune cells, thus achieving the purpose of treating self-immune and other related diseases. According to the official website, KPG-712 is currently in the IND-Enabling stage of dual-reporting in China and the US.
In addition, Kangpu has three other drugs in its pipeline related to CRBN E3 ubiquitin ligase complex CRL4CRBN in preclinical studies to be developed for the treatment of haematological tumours, solid tumours and other diseases.
By accelerating the clinical progress of the projects under development and fully laying out the subsequent pipeline, Kangpu is expected to harvest more innovative new-generation molecular gel-protein ubiquitination degradation small molecule drugs.
