A review of phenformin, metformin, and imeglimin
| Autor: | Sushma Ramsinghani, Subin S Kim, Raghunandan Yendapally, Donald Sikazwe, Amy P. Witte, Rheaclare Fraser-Spears, Brittany La-Viola |
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| Rok vydání: | 2020 |
| Předmět: |
Blood Glucose
Imeglimin endocrine system diseases medicine.drug_class Type 2 diabetes Phenformin Pharmacology 03 medical and health sciences chemistry.chemical_compound 0302 clinical medicine Pharmacokinetics Diabetes mellitus Drug Discovery Animals Humans Hypoglycemic Agents Medicine Triazines business.industry Biguanide nutritional and metabolic diseases medicine.disease Metformin Diabetes Mellitus Type 2 chemistry 030220 oncology & carcinogenesis Lactic acidosis Acidosis Lactic business 030217 neurology & neurosurgery medicine.drug |
| Zdroj: | Drug Development Research. 81:390-401 |
| ISSN: | 1098-2299 0272-4391 |
| DOI: | 10.1002/ddr.21636 |
| Popis: | Diabetes mellitus is a serious metabolic disorder affecting millions of people worldwide. Phenformin and metformin are biguanide antidiabetic agents that are conveniently synthesized in a single-step chemical reaction. Phenformin was once used to lower blood glucose levels, but later withdrawn from the market in several countries because it was frequently associated with lactic acidosis. Metformin is still a widely prescribed medication for the treatment of type 2 diabetes despite the introduction of several newer antidiabetic agents. Metformin is administered orally and has desirable pharmacokinetics. Incidence of metformin-induced lactic acidosis is serious but very rare. Imeglimin, a novel molecule being investigated by Poxel and Sumitomo Dainippon Pharma in Japan, is currently in clinical trials for the treatment of type 2 diabetes. Unlike metformin, imeglimin is a cyclic molecule containing a triazine ring. However, like metformin, imeglimin is also a basic small molecule. Imeglimin is synthesized from metformin as a precursor via a single step chemical reaction. Recent mechanism of action studies suggests that imeglimin improves mitochondria function, when given in combination with metformin it helps achieve better glycemic control in patients with type 2 diabetes. We herein describe and compare the current status, synthesis, physicochemical properties, pharmacokinetic parameters, mechanism of action, and preclinical/clinical studies of metformin and imeglimin. |
| Databáze: | OpenAIRE |
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