Huateng Pharma Develops SGLT-2 inhibitors Against Diabetes

CHANGSHA, China - April 20, 2023 - PRLog -- SGLT-2 inhibitor is a new type of oral hypoglycemic drug that has received great attention in recent years. SGLT-2 inhibitors, such as dapagliflozin, canagliflozin and empagliflozin were launched in the United States in 2012 and launched in Europe in 2014, and they were approved in China in 2017-2018 for clinical use. Its hypoglycemic mechanism is different from the previous hypoglycemic drugs. It inhibits the reabsorption of glucose by the kidneys and lowers the renal glucose threshold, thereby promoting the excretion of urinary sugar and lowering blood sugar.

At present, in many areas, although metformin is firmly in the first-line hypoglycemic drug position due to its reliable hypoglycemic effect, good safety, low risk of hypoglycemia, and low price, there is no convincing evidence of cardiovascular benefits for metformin. Based on the principles of evidence-based medicine, SGLT-2 inhibitors and GLP-1 receptor agonists with sufficient evidence of clinical benefits have already met the basic conditions to become first-line hypoglycemic drugs.

In May 2022, the Harvard Medical School research team published a paper entitled Cardiovascular Outcomes in Patients Initiating First-Line Treatment of Type 2 Diabetes With Sodium-Glucose Cotransporter-2 Inhibitors Versus Metformin : A Cohort Study in the Annals of Internal Medicine, a leading medical journal, showing that:

1.Compared with metformin, SGLT-2 inhibitors as first-line treatment can significantly reduce the risk of hospitalization for heart failure by 22%.
2.For patients with previous cardiovascular disease, the risk of myocardial infarction was also significantly reduced.
3.However, SGLT-2 inhibitors failed to reduce stroke or all-cause mortality.

As a professional pharmaceutical intermediates and API supplier, Huateng Pharma has three SGLT-2 inhibitors in development (https://us.huatengsci.com/product/175.html): Dapagliflozin, Canagliflozin, Empagliflozin and their intermediates(as below). Looking ahead, sales of SGLT-2 inhibitors are expected to grow further, and Huateng Pharma will focus on reducing the cost of manufacturing these drugs and improving the quality of intermediates and drugs.

Canagliflozin Intermediates

(5-Bromo-2-methylphenyl)[5-(4-fluorophenyl)-2-thienyl]methanone
CAS NO.1132832-75-7

2-(4-Fluorophenyl)-5-[(5-iodo-2-methylphenyl)methyl]thiophene
CAS NO.:898566-17-1

2-[(5-bromo-2-methylphenyl)methyl]-5-(4-fluorophenyl)thiophene
CAS NO.1030825-20-7

2-(4-Fluorophenyl)thiophene
CAS NO.58861-48-6

Dapagliflozin Intermediates

4-Iodo-1-chloro-2-(4-ethoxybenzyl)benzene
CAS NO.1103738-29-9

Benzene, 4-bromo-1-chloro-2-[(4-ethoxyphenyl)methyl]-
CAS NO.461432-23-5

Empagliflozin Intermediates

(3S)-3-[4-[(5-bromo-2-chlorophenyl)methyl]phenoxy]oxolane
CAS NO.915095-89-5

(S)-4-iodo-1-chloro-2-(4-tetrahydrofuran-3-yloxy-benzyl)-benzene
CAS NO.915095-94-2