Tumor

 
Chipscreen Biosciences focuses on cancer therapies. Chidamide, the first original innovative drug discovered and developed by Chipscreen, was the first oral subtype-selective histone deacetylase (HDAC) inhibitor with a novel epigenetic modulating mechanism.
 
Over the last decade, a large body of scientific studies has found that epigenetics plays critical roles in the escape from host immune surveillance, differentiation of cancer stem cells associated with tumor recurrence, epithelial-to-mesenchymal transition (EMT) associated with tumor metastasis, and elimination of drug-resistant cells from heterogeneous tumors. Epigenetic drugs have thus become a key focus of drug research and development, and Chipscreen Biosciences has been working in this area over 20 years.

• In December 2014, Chidamide was approved by the CFDA for relapsed and refractory peripheral T-cell lymphoma (PTCL), its first approved indication;
• In November 2019, Chidamide was approved by the NMPA in combination with an aromatase inhibitor for the treatment of post-menopausal patients with hormone receptor-positive, HER2-negative, recurrent or progressive locally advanced or metastatic breast cancer previously treated with endocrine therapy. This approval made Chidamide the first epigenetic drug approved for solid tumor therapy in the world, following groundbreaking evidence that Chidamide can effectively prevent tumor resistance in combination with other targeted drugs;
• In June 2021, chidamide monotherapy to treat relapsed/refractory (R/R) adult T-cell leukemia (ATL) was approved for marketing in Japan;
• In December 2021, chidamide monotherapy to treat relapsed/refractory (R/R) peripheral T-cell lymphoma (PTCL) was approved for marketing in Japan;
• In March 2023, chidamide was approved for the indication of breast cancer in Taiwan, China.
• In April 30, 2024, Chidamide was approved to use in combination with R-CHOP (rituximab, cyclophosphamide, doxorubicin, vincristine, and prednisone) for previously untreated diffuse large B-cell lymphoma (DLBCL) patients with positive MYC and BCL2 expression in China.

Chiauranib is a new molecular entity independently designed and developed by Chipscreen Biosciences, with global patent protection. It is a multi-target multi-pathway selective kinase inhibitor, a novel small molecule anti-tumor drug that can selectively inhibit multiple kinase targets such as Aurora B, CSF1R, and VEGFR/PDGFR/DDR. In September 2023, the enrollment in the phase III clinical trial of chiauranib monotherapy of small cell lung cancer was completed. The trial is ongoing globally.

CS23546 is a small molecule PD-L1 inhibitor independently developed by Chipscreen Biosciences. In June 2023, CS23546 has been approved for clinical trials in advanced malignant tumors in China, and the phase I clinical trial is currently ongoing in China.

  
Metabolic Diseases

 
Metabolic diseases are the most common chronic conditions, these conditions typically cause health problems often related to damage to blood cerebral vessels and vital organs, such as heart, liver and kidney, etc. Short-term efficacy from the medicine and lack of efficacious treatment are the main contributors to the waste of medical resources and poor prognosis, thus there is a strong ongoing demand for treatment for metabolic disorders. 
 
Chiglitazar, our first product targeting metabolic diseases, is a configuration-restricted pan-PPAR agonist with a chemical structure completely different from thiazolidinedione compounds. As an innovative drug with a brand-new mechanism of action, no lessons could be drawn from the success of predecessors, and the lack of existing clinical studies on pan-PPAR agonists worldwide posed major difficulties to the research and development process. Chiglitazar eventually overcame these obstacles to achieve good results for both efficacy and safety, and is now the world’s first pan-PPAR agonist to complete phase III clinical trials. In Oct. 2021, Chiglitazar was approved for marketing by the National Medical Products Administration (NMPA) to treat Type 2 Diabetes. The unique pharmacodynamic molecular mechanism of Chiglitazar makes it an exciting prospect for both diabetes and its related complications, and clinical exploration for a range of conditions is currently underway.

The company is also in the early stages of developing candidate compounds targeting other metabolic diseases, such as hyperlipidemia, non-alcoholic steatohepatitis, and chronic kidney disease.

Autoimmune disorders

 
Autoimmune disorders is a general category for a large group of conditions featuring over 100 pathological types, including common diseases such as rheumatoid arthritis, psoriasis, and systemic lupus erythematosus, as well as various types of rare diseases. These conditions range in severity from minor impacts on quality of life to life-threatening. Due to the significant heterogeneity of pathological characteristics in different patients, clinical treatment tends to be ineffective, and in some cases no treatment exists. Therefore, new treatments are urgently demanded in the clinic.

CS12192, Chipscreen Biosciences's first variety in this field and a JAK3/JAK1/TBK1 selective kinase inhibitor with a novel mechanism of action, is significantly different from existing clinical drugs in target selection and molecular mechanism. Compared with JAK kinase inhibitors on the market, CS12192 not only effectively suppresses the inflammation mediated by over-activation of immune cells, but also reduces tissue infiltration of immune cells by inhibiting TBK1, resulting in better efficacy and safety. CS12192 is therefore expected to provide a new differentiated treatment option for autoimmune diseases. The phase I clinical study of CS12192 has been completed in China.

CS32582 is a highly selective small molecule allosteric inhibitor of tyrosine kinase 2 (TYK2) independently developed by Chipscreen Biosciences. It specifically binds to the regulatory pseudokinase JH2 domain of TYK2, ensuring selective inhibition of TYK2 without inhibiting other family members like JAK1, JAK2, and JAK3 at therapeutic doses. This unique feature ensures both therapeutic efficacy and safety. The inhibition of TYK2 by CS32582 can effectively block downstream signaling pathways mediated by cytokines such as interleukin (IL)-23, IL-12, and type I interferon (IFN), thereby exerting therapeutic effects on autoimmune diseases such as psoriasis. In preclinical studies, CS32582 showed significant therapeutic effects in mouse models of psoriasis. In October 2023, an application for clinical trials of CS32582 capsules in the treatment of psoriasis in China has been approved, and the phase I clinical trial is currently ongoing in China.

Field of viral Diseases

With the advancement of globalization, public health security is being endangered seriously by known and unknown viral infections, and viral infectious diseases will become one of the most threatening diseases to human beings in the future. The most significant difficulties for current antiviral therapies lie in insufficient treatment, easy drug resistance, and easy rebound after discontinuation. Developing high-efficacy and low-resistance specific or broad-spectrum antiviral drugs helps to deal with existing known viral infectious diseases actively, and such drugs can serve as a technical reserve of the antiviral treatment system to resist unknown virus risks.

With regard to hepatitis B virus (HBV), we have started the R&D of drugs with different mechanisms of action, so as to address existing unmet clinical needs and achieve the long-term goal of functional cure in the future. 

Field of Central Nervous System Diseases

Central nervous system diseases refer to a large category of cognitive and motor dysfunction diseases that directly affect the quality of life and mental health of humans, which mainly include neurodegenerative disorders represented by Alzheimer's disease, psychiatric diseases represented by major depressive disorder, and other sensory and motor disorders such as epilepsy, pain, and spinal nerve damage. Along with global economic development and the advent of an aging society, increasing attention has been paid to the unmet clinical needs of central nervous system diseases. Considering the complex mechanism of central nervous system diseases, the slow preclinical pathological process, and the difficulty in timely intervention and treatment, such diseases have become a key and pressing area of global drug R&D. By 2020, there had been more than 40 million patients with Alzheimer's disease worldwide and about 10 million in China. The efficacy of existing drugs has been limited due to a lack of breakthroughs in the drugs with new mechanisms of action in the past decade.

We have long been committed to the R&D of innovative new drugs, with the mission of overcoming challenging diseases. With regard to Alzheimer's disease, in addition to the mainstream mechanisms and targets around the β-amyloid plaque, Tau protein phosphorylation, and acetylcholinesterase, we have carried out the R&D of new drugs against differentiated targets based on the epidemiology and real-world objective evidence of Alzheimer's disease, as well as human genetic associations. It is our expectation that these efforts will contribute to this therapeutic area.

Also, we have been focusing on and actively participating in the R&D of new drugs related to other central nervous system diseases like neuralgia.