Huateng Pharma Develops Sitagliptin & Linagliptin Anti-diabetic Intermediates

Sitagliptin (MK-0431) is an orally available, highly selective DPP-4 inhibitor with an IC50 of 18 nM. It is used for the treatment of type 2 diabetes. Sitagliptin is a new FDA-approved anti-type 2 diabetes drug and is the first dipeptidyl peptidase-IV inhibitor for the treatment of type 2 diabetes.


Sitagliptin's mechanism of action differs from previous oral hypoglycemic agents in that it controls blood glucose levels in diabetic patients by increasing the ability of their own pancreatic beta cells to produce insulin and increasing insulin secretion when blood glucose rises. Sitagliptin is an orally effective drug with good market prospect. It has significant hypoglycemic effect alone or in combination with metformin and pioglitazone, and is safe to take, well tolerated and has few adverse effects.


Sitagliptin is often administered as a phosphate to prevent and treat type 2 diabetes, hyperglycemia, insulin resistance, obesity and hypertension, as well as certain complications. Sitagliptin phosphate was developed by Merck and launched in Mexico and the United States in 2006 and approved for the treatment of type 2 diabetes in the European Union in 2007. Sitagliptin phosphate tablets are now the second most popular oral diabetes drug in the United States.


“Sitagliptin is a promising drug for the treatment of type 2 diabetes. In response to this trend, our management decides to introduce a new product line, providing Sitagliptin and Linagliptin intermediates with high purity and the most reasonable price,” says the Marketing Chief of Huateng Pharma. ”Previously, we have already been a trust-wothy CDMO for pharmaceutical intermediates, offering custom synthesis and scale-up services for many years. We believe our relationship with our partners will be further strengthened after the launch of these popular pharmaceutical intermediates.”


Sitagliptin is the first oral DPP-4 inhibitor in the world. It was first approved by FDA in October 2006. According to the global drug Research and development database of Rongyun, sitagliptin sales have been stable at around $3.5 billion to $4 billion in recent years.


In 2009, sitagliptin phosphate tablets were approved to land in China, and entered the national Medical insurance (Class B) in 2017. With the help of medical insurance, the volume of sitagliptin phosphate tablets was rapidly expanded. The sales volume of sitagliptin phosphate tablets in hospitals nationwide rose by 112% in the next year, and exceeded 1 billion yuan in 2020. This year, the growth rate is also rapid, with the hospital sales exceeding 1.5 billion, a year-on-year growth of 17.57%.


In addition to Sitagliptin, Linagliptin (BI-1356) is a highly potent and selective DPP-4 inhibitor with an IC50 of 1 nM. Selectivity for DPP-4 was more than 10,000 times higher than for other dipeptidyl peptidases such as DPP-2, DPP-8, and DPP9. Linagliptin, developed by Boehringer Ingelheim, was approved by the FDA on May 2, 2011, for use in combination with diet and exercise to improve glycemic level control in type 2 diabetes. Linagliptin improves glycemic control by inhibiting dipeptidyl peptidase-4 (DPP-4).


Huateng Pharma is a full-service Contract Development Manufacturing Organizations (CDMO) for pharmaceutical intermediates, including Sitagliptin, Linagliptin and Alogliptin intermediates, offering our customers innovative solutions to their bespoke projects, from the early clinical phase through to the commercial stage.



About Huateng Pharma

Huateng Pharma is a global provider in contract development and manufacturing for intermediates.  With our focus on operational excellence, and the integration of manufacturing operations with EHS, quality assurance, quality control, regulatory, supply chain management and project management, we can manufacture, scale-up and supply high-quality intermediates and APIs from our China facility.


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Address: Lugu Business Plaza E1, Yuelu District, Changsha City, Hunan Province, China

Manufacturing Base: Tongguan Kiln, Wangcheng district, Changsha, Hunan, China



Zip code: 410205

Telephone: +86 731 89916275

Fax: +86 0731-82251112-818