Canagliflozin
From Proteopedia
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Canagliflozin is an inhibitor of subtype 2 sodium-glucose transport proteins (SGLT2), which is responsible for at least 90% of renal glucose reabsorption (the remaining 10% is done by SGLT1). Blocking this transporter causes up to 119 grams of blood glucose per day to be eliminated through the urine,<ref name="a34">[https://clarivate.com/products/biopharma/ "Integrity - Clarivate"]</ref> corresponding to 476 kilocalories. Additional water is eliminated by osmotic diuresis, resulting in a lowering of blood pressure. | Canagliflozin is an inhibitor of subtype 2 sodium-glucose transport proteins (SGLT2), which is responsible for at least 90% of renal glucose reabsorption (the remaining 10% is done by SGLT1). Blocking this transporter causes up to 119 grams of blood glucose per day to be eliminated through the urine,<ref name="a34">[https://clarivate.com/products/biopharma/ "Integrity - Clarivate"]</ref> corresponding to 476 kilocalories. Additional water is eliminated by osmotic diuresis, resulting in a lowering of blood pressure. | ||
| - | Canagliflozin also inhibits renal SGLT1, contributing to about 10% of daily urinary glucose excretion. | + | Canagliflozin also inhibits renal SGLT1, contributing to about 10% of daily urinary glucose excretion.<ref name="a35">PMID:32064793</ref><ref name="a36">PMID:34232488</ref> |
This mechanism is associated with a low risk of hypoglycaemia (too low blood glucose) compared to other types of anti-diabetic drugs such as sulfonylurea derivatives and insulin.[37] | This mechanism is associated with a low risk of hypoglycaemia (too low blood glucose) compared to other types of anti-diabetic drugs such as sulfonylurea derivatives and insulin.[37] | ||
Revision as of 08:26, 24 January 2024
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References
- ↑ "Canagliflozin Monograph for Professionals". Drugs.com. American Society of Health-System Pharmacists. Retrieved 6 April 2019.
- ↑ "Integrity - Clarivate"
- ↑ Sokolov V, Yakovleva T, Chu L, Tang W, Greasley PJ, Johansson S, Peskov K, Helmlinger G, Boulton DW, Penland RC. Differentiating the Sodium-Glucose Cotransporter 1 Inhibition Capacity of Canagliflozin vs. Dapagliflozin and Empagliflozin Using Quantitative Systems Pharmacology Modeling. CPT Pharmacometrics Syst Pharmacol. 2020 Apr;9(4):222-229. PMID:32064793 doi:10.1002/psp4.12498
- ↑ Koufakis T, Mustafa OG, Tsimihodimos V, Ajjan RA, Kotsa K. Insights Into the Results of Sotagliflozin Cardiovascular Outcome Trials: Is Dual Inhibition the Cherry on the Cake of Cardiorenal Protection? Drugs. 2021 Aug;81(12):1365-1371. PMID:34232488 doi:10.1007/s40265-021-01559-1
