Luseogliflozin

Last updated
Luseogliflozin
Luseogliflozin structure.svg
Clinical data
Trade names Lusefi
Other namesTS-071
ATC code
Legal status
Legal status
  • Rx-only in Japan
Identifiers
CAS Number
PubChem CID
DrugBank
UNII
CompTox Dashboard (EPA)
Chemical and physical data
Formula C23H30O6S
Molar mass 434.55 g·mol−1
3D model (JSmol)
  • CCOC1=CC=C(C=C1)CC2=C(C=C(C(=C2)[C@H]3[C@@H]([C@H]([C@@H]([C@H](S3)CO)O)O)O)OC)C

Luseogliflozin (trade name Lusefi) is a pharmaceutical drug (an SGLT2 inhibitor) used for the treatment of type 2 diabetes mellitus. [1] [2] It was approved for use in Japan in 2014. [1] In a meta-analysis involving data from 10 randomized controlled trials (1304 patients), Dutta et. al. demonstrated the good glycaemic efficacy (mean glycated hemoglobin reduction of -0.76% and mean fasting glucose reduction of -26.69mg/dl) and safety of luseogliflozin 2.5mg/day as compared to placebo. Additional benefits include significant reduction in systolic blood pressure (-4.19 mm Hg), serum triglycerides (-12.60mg/dl), uric acid (-0.48mg/dl) and alanine aminotransferase (-4.11 IU/L) as compared to placebo, highlighting the beneficial impact on the different aspects of metabolic syndrome. [3]

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Remogliflozin etabonate (INN/USAN) is a drug of the gliflozin class for the treatment of non-alcoholic steatohepatitis ("NASH") and type 2 diabetes. Remogliflozin was discovered by the Japanese company Kissei Pharmaceutical and is currently being developed by BHV Pharma, a wholly owned subsidiary of North Carolina, US-based Avolynt, and Glenmark Pharmaceuticals through a collaboration with BHV. In 2002, GlaxoSmithKline (GSK) received a license to use it. From 2002 to 2009, GSK carried out a significant clinical development program for the treatment of type-2 diabetes mellitus in various nations across the world and obesity in the UK. Remogliflozin etabonate's pharmacokinetics, pharmacodynamics, and clinical dose regimens were characterized in 18 Phase I and 2 Phase II investigations. Due to financial concerns, GSK stopped working on remogliflozin and sergliflozin, two further SGLT2 inhibitors that were licensed to the company, in 2009. Remogliflozin was commercially launched first in India by Glenmark in May 2019.

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Gliflozins are a class of drugs in the treatment of type 2 diabetes (T2D). They act by inhibiting sodium/glucose cotransporter 2 (SGLT-2), and are therefore also called SGLT-2 inhibitors. The efficacy of the drug is dependent on renal excretion and prevents glucose from going into blood circulation by promoting glucosuria. The mechanism of action is insulin independent.

SGLT2 inhibitors, also called gliflozins or flozins, are a class of medications that modulate sodium-glucose transport proteins in the nephron, unlike SGLT1 inhibitors that perform a similar function in the intestinal mucosa. The foremost metabolic effect of this is to inhibit reabsorption of glucose in the kidney and therefore lower blood sugar. They act by inhibiting sodium-glucose transport protein 2 (SGLT2). SGLT2 inhibitors are used in the treatment of type 2 diabetes. Apart from blood sugar control, gliflozins have been shown to provide significant cardiovascular benefit in people with type 2 diabetes). Several medications of this class have been approved or are currently under development. In studies on canagliflozin, a member of this class, the medication was found to enhance blood sugar control as well as reduce body weight and systolic and diastolic blood pressure.

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References

  1. 1 2 Markham A, Elkinson S (June 2014). "Luseogliflozin: first global approval". Drugs. 74 (8): 945–50. doi:10.1007/s40265-014-0230-8. PMID   24848756. S2CID   1770988.
  2. Samukawa Y, Sata M, Furihata K, Ito T, Ueda N, Ochiai H, et al. (September 2017). "Luseogliflozin, an SGLT2 Inhibitor, in Japanese Patients With Mild/Moderate Hepatic Impairment: A Pharmacokinetic Study". Clinical Pharmacology in Drug Development. 6 (5): 439–447. doi: 10.1002/cpdd.364 . PMID   28783873.
  3. Dutta D, Kadian J, Mahajan K, Dhall A, Sharma M (Mar 2023). "Efficacy and safety of luseogliflozin in improving glycaemic and non-glycaemic outcomes in type-2 diabetes: A meta-analysis". Diabetes Metab Syndr. 17 (3): 102742. doi:10.1016/j.dsx.2023.102742. PMID   36933330.