Dapagliflozin

408.875

408.87

1592732-453-0

1ULL0QJ8UC

C78126

A10BD|A10BK01|A - Alimentary tract and metabolism

99.4

2.3

1.349

65

609°C

322.1±31.5 °C

1.614

P201, P202, P260, P263, P264, P270, P280, P281, P301+P312, P305+P351+P338, P308+P313, P310, P314, P330, P337+P313, P405, P501

H302

|Danger|H302 (100%): Harmful if swallowed [Warning Acute toxicity, oral]|P201, P202, P260, P263, P264, P270, P273, P280, P281, P301+P312, P305+P351+P338, P308+P313, P310, P314, P330, P337+P313, P405, and P501|Aggregated GHS information provided by 9 companies from 6 notifications to the ECHA C&L Inventory. Each notification may be associated with multiple companies.

Age, gender, race, and body weight do not affect dapagliflozin dosing requirements. Although age does not affect dosing requirements, safety has not been established in pediatric populations and patients at an especially advanced age may be more susceptible to adverse effects. Animal studies in pregnancy showed no fetal toxicity in the first trimester but exposure later in pregnancy was associated with renal pelvic dilatation and maternal toxicity at much higher doses than the maximum recommended human dose. Due to this data, dapagliflozin is not recommended in the second and third trimester of pregnancy. Dapagliflozin is excreted in milk from rats, though this may not necessarily be the case in humans. Children under 2 years old who are exposed to dapagliflozin may be at risk of improper kidney development. Dapagliflozin is not recommended in patients with a creatinine clearance below 45mL/min and is contraindicated in patients with creatinine clearance below 30mL/min. Dose adjustments are not necessary in patients with hepatic impairment at any stage, although the risk and benefit to the patient must be assessed as there is limited data on dapagliflozin use in this population.

91%.

Dapagliflozin is indicated to improve glycemic control in adult patients with type 2 diabetes mellitus along with diet and exercise.|FDA Label|Qtrilmet is indicated in adults aged 18 years and older with type 2 diabetes mellitus:to improve glycaemic control when metformin with or without sulphonylurea (SU) and either saxagliptin or dapagliflozin does not provide adequate glycaemic control.when already being treated with metformin and saxagliptin and dapagliflozin.|Type 2 diabetes mellitusForxiga is indicated in adults for the treatment of insufficiently controlled type 2 diabetes mellitus as an adjunct to diet and exercise- as monotherapy when metformin is considered inappropriate due to intolerance.-- in addition to other medicinal products for the treatment of type 2 diabetes.For study results with respect to combination of therapies, effects on glycaemic control, cardiovascular and renal events, and the populations studied, see sections 4.4, 4.5 and 5.1.Type 1 diabetes mellitusForxiga is indicated in adults for the treatment of insufficiently controlled type 1 diabetes mellitus as an adjunct to insulin in patients with BMI ≥ 27 kg/m2, when insulin alone does not provide adequate glycaemic control despite optimal insulin therapy.Heart failureForxiga is indicated in adults for the treatment of symptomatic chronic heart failure with reduced ejection fraction.Chronic kidney diseaseForxiga is indicated in adults for the treatment of chronic kidney disease.|Type 2 diabetes mellitusEdistride is indicated in adults for the treatment of insufficiently controlled type 2 diabetes mellitus as an adjunct to diet and exercise- as monotherapy when metformin is considered inappropriate due to intolerance.- in addition to other medicinal products for the treatment of type 2 diabetes.For study results with respect to combination of therapies, effects on glycaemic control, cardiovascular and renal events, and the populations studied, see sections 4.4, 4.5 and 5.1.Heart failureEdistride is indicated in adults for the treatment of symptomatic chronic heart failure with reduced ejection fraction.Chronic kidney diseaseEdistride is indicated in adults for the treatment of chronic kidney disease |Treatment of chronic kidney disease|Prevention of cardiovascular events in patients with chronic heart failure|Treatment of type II diabetes mellitus|Treatment of type I diabetes mellitus|Treatment of ischaemic heart disease|Treatment of Coronavirus disease 2019 (COVID-19)

Dapagliflozin inhibits the sodium-glucose contransporter 2(SGLT2) which is primarily located in the proximal tubule of the nephron. SGLT2 facilitates 90% of glucose resorption in the kidneys and so its inhibition allows for glucose to be excreted in the urine. This excretion allows for better glycemic control and potentially weight loss in patients with type 2 diabetes mellitus.

Compounds that inhibit SODIUM-GLUCOSE TRANSPORTER 2. They lower blood sugar by preventing the reabsorption of glucose by the kidney, and are used in the treatment of TYPE 2 DIABETES MELLITUS. (See all compounds classified as Sodium-Glucose Transporter 2 Inhibitors.)

Oral dapagliflozin reaches a maximum concentration within 1 hour of administration when patients have been fasting. When patients have consumed a high fat meal, the time to maximum concentration increases to 2 hours and the maximum concentration decreases by half though a dose adjustment is not necessary. Oral dapagliflozin is 78% bioavailable.|75.2% of dapagliflozin is recovered in the urine with 1.6% of the dose unchanged by metabolism. 21% of the dose is excreted in the feces with 15% of the dose unchanged by metabolism.|118L.|Oral plasma clearance was 4.9 mL/min/kg, and renal clearance was 5.6 mL/min.

Dapagliflozin is primarily glucuronidated to become the inactive 3-O-glucuronide metabolite(60.7%). Dapagliflozin also produces another minor glucuronidated metabolite(5.4%), a de-ethylated metabolite(<5%), and a hydroxylated metabolite(<5%). Metabolism of dapagliflozin is mediated by cytochrome p-450(CYP)1A1, CYP1A2, CYP2A6, CYP2C9, CYP2D6, CYP3A4, uridine diphosphate glucuronyltransferase(UGT)1A9, UGT2B4, and UGT2B7. Glucuronidation to the major metabolite is mediated by UGT1A9.

13.8h.

Dapagliflozin inhibits the sodium-glucose contransporter 2(SGLT2) which is primarily located in the proximal tubule of the nephron. SGLT2 facilitates 90% of glucose resorption in the kidneys and so its inhibition allows for glucose to be excreted in the urine. This excretion allows for better glycemic control and potentially weight loss in patients with type 2 diabetes mellitus.

(2S,3R,4R,5S,6R)-2-(4-chloro-3-(4-ethoxybenzyl)phenyl)-6- (hydroxymethyl)tetrahydro-2H-pyran-3,4,5-triol

Human drugs -> Qtrilmet -> EMA Drug Category|Drugs used in diabetes -> Human pharmacotherapeutic group|Human drugs -> Forxiga -> EMA Drug Category|Human drugs -> Edistride -> EMA Drug Category|Human Drugs -> EU pediatric investigation plans|Human Drugs -> FDA Approved Drug Products with Therapeutic Equivalence Evaluations (Orange Book) -> Active Ingredients