W4 ICS Integrated CVS Flashcards
The patient has found out on Google that SGLT2 inhibitors ‘gliflozins’ have a structural
component which is similar to glucose structure, and they are now worried that this could cause to them diabetes. Explain to the patient why this is not possible and what is the function of this structural component in gliflozins?
The Glycone part is essential for their activity. It reproduces the glucose bind with Thr156/Lys157 of SGLT2, allowing the drug to bind the SGLT2 blocking glucose binding.
Other sugar moiety/substitutions affect the potency/sometimes resulting in loss of activity. Although the Glycone moiety is structurally related to glucose, it won’t effect in any mean the glucose levels of the patient. On the contrary, blocking the activity of SGLT2 will increase the excretion with urine of glucose, reducing its blood level.
