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Biocatalyzed Synthesis of Antidiabetic Drugs
Published in Peter Grunwald, Pharmaceutical Biocatalysis, 2019
Sitagliptin (Fig. 11.24, 41) (sold under the trade name Januvia™ by Merck Sharp & Dhome) was the first marketed oral antihyperglycemic drug belonging to the gliptin family (Aroda et al., 2012). Sitagliptin can be used either alone or combined with metformin or thiazolidinedione, other oral antihyperglycemic agents in the treatment of Type 2 DM, already discussed before (Kim et al., 2005). Sitagliptin is the most widely sold DPP-4 inhibitors in the US and worldwide, reaching sales of 6,358 million USD in 2014 with an expected rise to 7,525 in 2020. Sitagliptin was the second leading antidiabetic product in 2014, after insulin glargine, and is predicted to be the leading product by 2020 (Cahn et al., 2016; Fernandes et al., 2016).
Recent Advances in Nanostructured Enzyme Catalysis for Chemical Synthesis in Organic Solvents
Published in Grunwald Peter, Biocatalysis and Nanotechnology, 2017
Zheng Liu, Jun Ge, Diannan Lu, Guoqiang Jiang, Jianzhong Wu
Enzymes have unique capabilities to catalyze chemical reactions with high chemo-, regio-, and stereo-selectivity, high turnover rate and mild solution conditions. Utilizing enzymes for chemical synthesis would enable high-yield production of complex molecules and circumvention of intermediate separation, leading to a shortened synthetic route with reduced energy consumption and minimized waste discharge (Liese et al., 2006; Pollard and Kosjek, 2008; Patel, 2011; Torrelo et al., 2015). Such efficiency is illustrated with the industrial synthesis of Sitagliptin, an antidiabetic drug that inhibits dipeptidyl peptidase and therefore decreases the blood glucose level in human body. The conventional route for chemical synthesis of Sitagliptin involves a rhodium- catalyzed asymmetric amine hydrogenation at high pressure. A transaminase is able to convert prositagliptin ketone to sitagliptin with enzyme efficiency over 99.95% and a yield of 92%. In comparison with the rhodium-catalyzed process, the enzymatic process increases the overall yield by 10–13%, reduces the total waste by 19%, and excludes the use of hazardous heavy metals (Savile et al., 2010).
Becoming less noxious
Published in Michael R. Greenberg, Siting Noxious Facilities, 2018
Fast forward a quarter of a century when Merck receives the 2016 Energy Star Sustained Excellence award from the EPA for its efforts to reduce energy use at various sites. It received the same award in 2017.49Newsweek ranked Merck number 150 out of 500 global companies in greening and number 82 in the U.S. Merck had also received prominent awards that directly relate to pollution prevention and ISD. In 2010, it received the Presidential Green Chemistry challenge award from the U.S. EPA for developing a biocatalyst would increase the yield of sitagliptin and reduce byproduct wastes.50 (Sitagliptin treats people with type 2 diabetes).
Sodium-glucose transporter (SGLT2) inhibition: A potential target for treatment of type-2 Diabetes Mellitus with Natural and Synthetic compounds
Published in Egyptian Journal of Basic and Applied Sciences, 2023
Shubham Batra, Prabhjeet Kaur Bamrah, Manjusha Choudhary
Ertugliflozin, a novel family of selective SGLT2 inhibitors newly approved by the FDA for the treatment of T2DM in 2017. Similar to other SGLT2 inhibitors, ertugliflozin very selectively inhibits SGLT2 to decrease renal glucose sensitivity and filtered glucose reabsorption in the kidney, increasing urine glucose excretion. Ertugliflozin does not affect insulin secretion or sensitivity, unlike other SGLT2 inhibitors. Additionally, it can be taken in combination with some medications, such as metformin, sitagliptin, and sulfonylureas, in addition to insulin [28].