What's so great about Shengliptin, the new glucose-lowering drug that's expected to be the best in class?

  • Categories:Media
  • Author:Arterial Network Wang Shiwei
  • Origin:
  • Time of issue:2019-08-23
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(Summary description) CGeneTech (Suzhou, China) Co., Ltd.  announced the completion of its Pre-A round of financing last month, stating that its flagship product, Centigliptin, is expected to be the best-in-class product.

What's so great about Shengliptin, the new glucose-lowering drug that's expected to be the best in class?

(Summary description) CGeneTech (Suzhou, China) Co., Ltd.  announced the completion of its Pre-A round of financing last month, stating that its flagship product, Centigliptin, is expected to be the best-in-class product.

  • Categories:Media
  • Author:Arterial Network Wang Shiwei
  • Origin:
  • Time of issue:2019-08-23
  • Views:0

  CGeneTech (Suzhou, China) Co., Ltd.  announced the completion of its Pre-A round of financing last month, stating that its flagship product, Centigliptin, is expected to be the best-in-class product.
  Centagliptin is a new glucose-lowering drug that is an enterostatin-based DPP-4 inhibitor. Since the launch of the world's first DPP-4 inhibitor, selegiline, in the US market in 2006, DPP-4 has become the most popular target in the development of new drugs for diabetes, and several Top 10 pharmaceutical companies have developed a number of new drugs in the category of selegiline in a few years from different perspectives, including efficacy, dosage form and side effects.
  In China, although there are already five imported listerin drugs on the market and included in the medical insurance, DPP-4 is still the most lively battlefield for the strongest pharmaceutical companies in the country. According to incomplete statistics from, more than 10 pharmaceutical companies, including Hengrui, Xinlitai, Shengshi Tai Ke, Hesco and others, have advanced 12 new domestic listerine drugs to clinical trials, so the battle is not anxious.
  However, Dr. Yu Qiang, the founder of CGeneTech , emphasized that the phrase "expected to be the bestinclass" was a statement he decided to use in the press release after much deliberation. Recently, interviewed Dr. Yu, who told us his entrepreneurial story and the origin of his confidence in Shengliptin.

  A chemist who doesn't want to make new drugs is not a good boss

  Like most entrepreneurs active in the new drug industry today, Dr. Yu Qiang is a returnee, highly educated and experienced in the field. The difference is that the first thing Dr. Yu did when he returned to China was not to look for a business direction or demand angel investment, but to file a patent for the invention of the molecular formula of the Shengliptin drug precursor he brought back.
  In 2009, Yu returned to China with the capital and his team, and in 2010, he landed his new company, CGeneTech , in the Suzhou Industrial Park (SIP) BioBay. At that time, the young BioBAY was just starting out. Yu Qiang was impressed by the professionalism and enthusiasm of the team, and he described his first feeling of security when he moved into BioBAY as, "We looked at many parks in China and felt that BioBAY would be a place where we could realise our ideas."
  During his nine years at BioBAY, Dr Yu has had his darkest moments of running out of money to invest in new drug development, and the joy of driving Shengliptin from a drug precursor molecule with a molecular weight of less than 400 to a novel hypoglycemic drug that completed a phase I clinical trial with a very large sample of 194 cases.
  Today, CGeneTech has become a well-known small molecule drug developer in China, building a development pipeline from Class 1 new drug development, Class 2 flash release formulation platform to Class 3 first-in-class generic drugs, including a product line for various indications such as cancer, diabetes, psychiatric diseases and rare diseases.
  Qiang Yu graduated from Peking University with a Bachelor's degree in Chemistry and holds a PhD in Chemistry from the University of Kansas, where he completed his post-doctoral research with Professor Ronald Borchardt, President of the American Association of Pharmaceutical Sciences (AAPS), and developed a unique knowledge of drug bioefficacy evaluation.
  Prior to returning to China, Dr Yu founded a new drug fragment molecule company in the US, providing pre-development services for drug molecules to major pharmaceutical and biotechnology companies in the US.
  In late 2006, selegiline (generic name: Genovel) was approved for marketing by the US FDA. For type 2 diabetes, for which there is no proven cure, the launch of sitagliptin, with its targeted properties, was undoubtedly a major event. Selegiline became one of the fastest growing new drugs in terms of sales after its launch and the fastest in history to exceed US$1 billion in annual sales, capturing over 15% of the diabetes drug market in the US. Since then, Novartis, Bristol-Myers Squibb, Eli Lilly and Takeda Pharmaceuticals have launched DPP-4 inhibitors with the same mechanism of action, such as vildagliptin, saxagliptin, alogliptin and ligliptin.
  At that time, Yu Qiang, who was engaged in the development of drug precursors, also began to focus on DPP-4 (dipeptidyl peptidase IV) inhibitors. When the body eats, the small intestine secretes glucagon-like peptide-1 (GLP-1), glucose-dependent insulinotropic polypeptide (GIP) and other enteroglucagon to promote insulin secretion by beta cells, thus lowering blood sugar. DPP-4 inhibitors can inhibit the action of DPP-4, maintain the effect of enteroglucagon and prevent the rise of blood glucose after meals in type 2 diabetic patients.
  After research, Yu Qiang found that the DPP-4 inhibitory effect of selegiline was more pronounced when the right side of the molecular formula was adjusted in the combined structure of the two molecular formulae. He then used the company's platform to design and sell more than 20 adjusted DPP-4 inhibitor precursor compounds to the public. These precursor compounds, which provided front-line researchers in the US with "ammunition" for the development of DPP-4 inhibitors, sold well and brought Yu Qiang considerable income.
  However, making money is not his goal in selling these precursor compounds. Yu Qiang wanted to use feedback from the professional market to identify the most promising DPP-4 inhibitor precursor compound structures, and two months later, he found the most structurally optimal DPP-4 inhibitor precursor compound under the prevailing conditions, the precursor to Shengliptin.
  It is probably true that there is a pharmacologist living in every chemist's heart. Yu Qiang quickly ended his career in the United States and devoted all his energy to the development of the druggability of this precursor compound. However, as a lot of work was needed to develop the precursor compound to the lead compound and then to pre-clinical and clinical studies, Yu Qiang approached Mr. Ding Torping, who had done dozens of national drug development and filings on his own, to join the venture. Mr. Ding, who also holds a Bachelor's degree in chemistry from Peking University and a Master's degree in medicinal chemistry from China Union Medical College, brought Shengliptin's pre-clinical research into the fast lane.

  Making the best Me-Too new drug

  "It'sveryeasytobedifferentbutverydifficulttobebetter (differentiation is easy, optimisation is hard)." To be the Bestinclass is what Dr. Yu Qiang has been asking of Centigliptin since the beginning.
  In 2016, CGeneTech completed a preclinical study comparing head-to-head with selegiline in terms of efficacy, safety, half-life, toxicology and pathology, and obtained significantly better data than selegiline, and initiated a Phase I clinical trial in early 2018.
  In July 2019, the phase I clinical trial of head-to-head comparison of selegiline and selegiline was completed. Dr. Yu Qiang told that it was actually very risky to do a head-to-head comparison study with a star DPP-4 inhibitor like selegiline in a Phase I clinical trial, as it would be tantamount to declaring selegiline out of the new drug development arena if no data on the efficacy and safety of selegiline could be obtained.
  But Dr Yu had enough confidence in Selegiline, "Our goal is to be the best in class, so we can only PK the best drug down." In 2016, sales of selegiline accounted for half of the sales of DPP-4 inhibitors in key hospitals in China, and the head-to-head comparison data with selegiline will be quite convincing in the market. At his insistence, the phase I clinical trial of selegiline enrolled 194 patients and completed comparative study programs on safety, efficacy and drug relevance.
  Data from the Phase I clinical trial showed that the DPP-4 inhibitory capacity equivalent to 100 mg of selegiline intake was already achieved at 50 mg of selegiline intake. Centagliptin is administered once a day, peaks 1 to 2 hours after dosing, and has a longer drug half-life than selegiline, allowing for longer-term maintenance of steady-state glucose reduction.
  In safety studies, the data showed that there were virtually undetectable adverse effects of selegiline intake on the patient's body, lower than in the blank and selegiline groups. Diabetes requires long-term medication and safety is the first factor that doctors consider when prescribing medication. In addition, despite the long half-life of selegiline, no residual drug accumulation in the body was observed in the Phase I clinical trial.
  In a drug association study with metformin, the most widely used non-insulin glucose-lowering drug in China, no drug interactions with the latter were observed.
  Dr. Yu Qiang pointed out that although domestic pharmaceutical companies have been conducting research on new domestic DPP-4 inhibitors for a short period of time, few breakthroughs have been made and drug safety control has become the biggest bottleneck in the advancement of clinical research. "Among them, rash is a type of side effect that is widely present in domestic DPP-4 inhibitors and has remained unresolved." Then, of the nearly 200 patients in the Phase I clinical trial completed with Shengliptin, not one developed rash. It was the beautiful Phase I clinical trial data that allowed CGeneTech to proceed with initiating a late-stage clinical trial of Centagliptin. CGeneTech will be the fastest clinical developer of new DPP-4 inhibitors among its peers in China.
  Diabetes is one of the most prevalent epidemic diseases in the world, and China has the highest number of diabetics in the world. According to statistics, by 2017, the number of people with diabetes in China had reached 114 million, and a large stock of patients has accumulated while the prevalence rate has entered a stable phase from an explosive period. However, the domestic diabetes drug market is very special, with less than 1/4 of the total number of patients suffering from the disease being compliant with their medication, while drugs with extremely high side effects such as insulin and biguanides are still the mainstream of the drug market. According to some data, the use rate of new hypoglycemic drugs, including DPP-4 inhibitors, GLP-1 agonists and SGLT-2 inhibitors, is less than 10% in the prescription of diabetes drugs in key kilometre hospitals in China.
  As new drugs such as DPP-4 inhibitors continue to enter the basic medical insurance and various treatment guidelines, their market demand will gradually be unleashed.

  The "self-blooded" model of combining generic and innovative drugs

  Unlike new drug companies founded by biologists and pharmacologists who focus on specific therapeutic areas and do vertical research, chemist Dr. Qiang Yu's company has a more extensive drug development pipeline.
  "Survival, for innovative drug companies, is the most important thing." New drug development requires massive capital investment and lasts for a long time. Relying solely on external financing would easily lead to drug development being put on hold under the immense pressure of cash flow. In Dr Yu's view, abandoning the pipeline in development would not only be a fatal blow to the company itself, but also irresponsible to investors.
  Looking back years later, the choice of generic drug development and sales with high technical barriers not only brought cash flow to the company and helped it carry through the difficult period from 2014 to 2016 when the amount of R&D investment was at its highest, but also served to improve the team's R&D capabilities.
  CGeneTech's technical staff has the basic ability to develop a number of drugs after the generic development force, "Instead of training the team with the most highly sophisticated technology, we should rely on relatively mature drugs and technology." Currently, a number of first generic drugs for rare diseases from Centurion have been transferred to the public or entered clinical trials.
  Dr. Yu Qiang pointed out that subsequently, the company will also strengthen the research and development of new anti-tumour drugs and form a research and development strength close to that of diabetes drugs.


The world's first SGLT-2/DPP-4 dual target inhibitor with complementary advantages has been approved for clinical use

Recently, Shengshi Taike's Class 1 innovative drug SGLT-2/DPP-4 dual target inhibitor CGT-2201 has been granted implicit permission for clinical trials by the National Drug Administration. CGT-2201, which targets SGLT-2 and DPP-4, two important targets related to glucose metabolism, can be better used for the treatment of diabetes and its derivatives, including diabetes nephropathy and non-alcoholic fatty liver disease. In 2021, the number of diabetes patients in China will reach 141 million, ranking first in the world. Among the numerous patients with diabetes in China, 20-40% may suffer from complications of diabetes nephropathy. Among the existing hypoglycemic drugs, only sodium glucose cotransporter 2 (SGLT-2) inhibitor has significant renal protection effect in clinical verification, but its inherent reproductive and urinary system infection risks limit its use. Based on SGLT-2 inhibitors and combined with the characteristics of dipeptidyl peptidase 4 (DPP-4) inhibitors, we design and develop a drug that can improve blood sugar, reduce side effects of urinary and reproductive system infections, is not limited by renal function, and has kidney benefits. It is expected to fill the market gap and meet the needs of patients. Based on this market background and target characteristics, Shengshi Taike utilizes its own small molecule chimera drug technology platform to develop multi head multifunctional new drug products with synergistic mechanisms, with CGT-2201 being one of its representative works. It fuses the respective mechanism characteristics of SGLT-2 and DPP-4. On the basis of inhibiting the activity of SGLT-2 to reduce the reabsorption of glucose in the kidney, it also slows down the inactivation of DPP-4 on GLP-1, playing a dual role mechanism to play a superposition effect; While achieving considerable hypoglycemic effect, it can reduce the side effects of existing SGLT-2 drug urinary system infection; At the same time, without kidney excretion, it can reduce the burden of the kidney and reduce the contraindication of diabetes patients with renal insufficiency. Therefore, this drug will have the advantage of better controlling blood sugar and protecting patient kidney function. Shengshi Tyco was founded in Suzhou Industrial Park in 2010. Its core team has decades of experience in the whole life cycle of international drugs, and is committed to the R&D and industrialization of high-quality and differentiated small molecule innovative drugs. The company has built a product pipeline covering multiple disease fields such as hypoglycemic, anticancer, and autoimmune diseases with an integrated drug research and development technology platform and a diversified business perspective. In the field of hypoglycemic drugs, Shenggliptin, the core product independently developed by the company, has submitted an NDA (product launch application) to the National Drug Administration and has been accepted. The results of the Phase 3 clinical trial showed that low doses can reach the predetermined trial endpoint, while the high-dose group can also demonstrate the safety of the drug well. The therapeutic effect of "half the dose" is twice as effective, making it expected to become the best hypoglycemic drug in the class. At the same time, the company has also carried out a comprehensive layout around oral drugs and derivative diseases of various targets related to diabetes. CGT-2201, which was approved for clinical use this time, is one of its pipeline matrix members.

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