farxiga

Report
Farxiga™ - Dapagliflozin
Manufacturer: Bristol-Meyer Squibb
FDA Approval Date: January 8, 2014
Farxiga™ - Dapagliflozin
Clinical Application
• Indications:
• Adjunct to diet and exercise to improve
glycemic control in Type 2 Diabetes
• Place in therapy:
• Alternative to existing add-on therapies by
improving glycemic control without
associated weight gain or hypoglycemic
risk
Farxiga™ - Dapagliflozin
Clinical Application
• Contraindications:
• History of serous hypersensitivity reaction
• Severe renal impairment, ESRD, dialysis
• Warnings and Precautions
• May cause symptomatic hypotension
• Impairment in renal function may occur
• Risk of hypoglycemia when used with insulin or
insulin secretagogues
• Increased risk of genital mycotic infections
• May cause increased LDL-C elevation
Farxiga™ - Dapagliflozin
Clinical Application
• Pregnancy:
• Category C
• Adverse events observed in animal studies
• Lactation:
• Excretion in breast milk unknown; use is
not recommended
Farxiga™ - Dapagliflozin
Drug Facts
• Pharmacology:
• Selectively inhibits sodium-glucose
cotransporter 2 (SGLT-2) in the proximal
renal tubules, reduces absorption of filtered
glucose from the tubular lumen, increases
urinary excretion of glucose
Farxiga™ - Dapagliflozin
Drug Facts
Pharmacokinetics
A
Tmax 2 hrs; absorption not affected by food
D
91% protein bound
M
Extensive, primarily mediated by UGT1A9; CYPmediated (minor)
E
Primarily via urine (75%) and feces (21%)
Farxiga™ - Dapagliflozin
Drug Interactions
• Drug Interactions – Object Drugs:
• Duloxetine 
• Hypoglycemic agents 
Farxiga™ - Dapagliflozin
Drug Interactions
• Drug Interactions – Precipitant Drugs:
•
•
•
•
•
•
Corticosteroids 
Loop diuretics 
MAO Inhibitors 
Salicylates 
SSRIs 
Thiazide diuretics 
Farxiga™ - Dapagliflozin
Adverse Effects
Female genital mycotic infections
(6.9%) [1.5%]
UTI (4.3%) [3.7%]
Male genital mycotic infections
(2.7%)[0.3%]
Back pain (4.2%) [3.2%]
Nasopharyngitis (6.3%) [6.2%]
Dyslipidemia (2.5%) [1.5%]
Increased urination (3.8%) [1.7%]
Dysuria (2.1%) [0.7%]
Pain in extremity (1.7%) [1.4%]
Constipation (1.9%) [1.5%]
Farxiga™ - Dapagliflozin
Monitoring Parameters
• Efficacy Monitoring:
• Blood glucose, Hgb A1c
• Toxicity Monitoring:
• Renal function, LDL-C
Farxiga™ - Dapagliflozin
Prescription Information
• Dosing: 5-10 mg once daily
• Cost: $347 for 30-day supply
• Source: Medi-Span (via Lexi-comp online)
• Accessed 3/13/2014
Farxiga™ - Dapagliflozin
Literature Review
• A multicenter, double-blind,
randomized, active-controlled,
noninferiority, phase 3 study
• [Dapagliflozin + metformin] vs.
[Glipizide + metformin]
• Primary endpoint
• Absolute change in HbA1c from baseline
to week 52
Nauck, et al. Diabetes Care 2011; 34:2015-22.
Farxiga™ - Dapagliflozin
Literature Review
• Secondary Endpoints
• Absolute change in total body weight (TBW)
• Proportion of patients reporting at least one
episode of hypoglycemia
• Proportion of patients achieving a TBW
decrease ≥5%
Nauck, et al. Diabetes Care 2011; 34:2015-22.
Farxiga™ - Dapagliflozin
Literature Review
•
•
•
•
N = 801
Age ≥ 18 yrs (mean age 59)
6.5% < HbA1c ≤ 10% (mean 7.7%)
57% receiving metformin monotherapy
≥ 1500 mg/day
• Median metformin dose at
randomization 2000 mg/day
Nauck, et al. Diabetes Care 2011; 34:2015-22.
Farxiga™ - Dapagliflozin
Literature Review
Nauck, et al. Diabetes Care 2011; 34:2015-22.
Farxiga™ - Dapagliflozin
Literature Review
Nauck, et al. Diabetes Care 2011; 34:2015-22.
Farxiga™ - Dapagliflozin
Literature Review
Nauck, et al. Diabetes Care 2011; 34:2015-22.
Farxiga™ - Dapagliflozin
Literature Review
• Conclusions
• Comparable long-term efficacy of
dapagliflozin with glipizide with fewer
hypoglycemic episodes along with
sustained weight loss
• Dapagliflozin is a potential valuable
alternative to sulfonylureas as add-on
therapy when metformin monotherapy fails
to maintain adequate glycemic control
Nauck, et al. Diabetes Care 2011; 34:2015-22.
Farxiga™ - Dapagliflozin
Summary
• Farxiga, dapagliflozin, is the second in class agent that
selectively inhibits SGLT2 receptor which modulates
reabsorption of glucose in the kidney, resulting in
excretion of glucose in the urine
• Indicated as an adjunct to diet and exercise to improve
glycemic control in adults with Type 2 Diabetes
• Initially dosed 5 mg once daily in the morning
• Most common side effects include genital infections,
urinary tract infections, and nasopharyngitis
• Alternative to existing add-on therapies by improving
glycemic control without associated weight gain or
hypoglycemic risk
Farxiga™ - Dapagliflozin
References
1.
2.
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5.
http://www.farxiga.com
Farxiga package insert. Bristol-Meyers Squibb.
January 2014.
Farxiga. Lexicomp Drug Information. Accessed
through UpToDate. Accessed on March 13, 2014.
Nauck MA, et al. Dapagliflozin versus glipizide as
add-on therapy in patients with Type 2 Diabetes
who have inadequate glycemic control with
metformin. Diabetes Care 2011; 34:2015-2022.
Bailey CJ, et al. Effect of dapagliflozin in patients
with type 2 diabetes who have inadequate glycemic
control with metformin: a randomized, double-blind,
placebo-controlled trial. Lancet 2010; 375:2223-33.

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