Sodium-Glucose Cotransporter 2 Inhibitor

Sodium-Glucose Transporter 2 Inhibitors

Type 2 Diabetes Mellitus

<section class="Section" data-sectioncode="34089-3"><a name="ID_fd36fb00-7c31-4b1a-ad48-5d227ed82c01"></a><a name="section-10"></a><h1>11 DESCRIPTION</h1>Dapagliflozin, an inhibitor of SGLT2, is described chemically as D-glucitol, 1,5-anhydro-1-C-[4-chloro-3-[(4-ethoxyphenyl)methyl]phenyl]-, (1S)-, compounded with (2S)-1,2-propanediol, hydrate (1:1:1). The empirical formula is C21H25ClO6•C3H8O2•H2O and the molecular weight is 502.98. The structural formula is:<div class="Figure"><a name="id6857421"></a><img alt="Dapagliflozin Chemical Structure" src="dapagliflozin-struct.jpg"/></div>FARXIGA is available as a film-coated tablet for oral administration containing the equivalent of 5 mg dapagliflozin as dapagliflozin propanediol or the equivalent of 10 mg dapagliflozin as dapagliflozin propanediol, and the following inactive ingredients: microcrystalline cellulose, anhydrous lactose, crospovidone, silicon dioxide, and magnesium stearate. In addition, the film coating contains the following inactive ingredients: polyvinyl alcohol, titanium dioxide, polyethylene glycol, talc, and yellow iron oxide.</section>

FARXIGA

Farxiga

dapagliflozin

dapagliflozin 10 MG Oral Tablet

dapagliflozin 10 MG Oral Tablet [Farxiga]

dapagliflozin 5 MG Oral Tablet

dapagliflozin 5 MG Oral Tablet [Farxiga]

Biguanide

Dipeptidyl Peptidase 4 Inhibitor

Dipeptidyl Peptidase 4 Inhibitors

<section class="Section" data-sectioncode="34089-3"><a name="S11"></a><a name="section-10"></a><h1>11 DESCRIPTION</h1>TRIJARDY XR tablets for oral use contain: empagliflozin, linagliptin, and metformin hydrochloride.<div class="Section" data-sectioncode="42229-5"><a name="section-10.1"></a>EmpagliflozinEmpagliflozin is an inhibitor of the sodium-glucose co-transporter 2 (SGLT2).The chemical name of empagliflozin is D-Glucitol,1,5-anhydro-1-C-[4-chloro-3-[[4-[[(3S)-tetrahydro-3-furanyl]oxy]phenyl]methyl]phenyl]-, (1S).The molecular formula is C23H27ClO7 and the molecular weight is 450.91. The structural formula is:<img alt="Chemical Structure" src="trijardy-01.jpg"/>Empagliflozin is a white to yellowish, non-hygroscopic powder. It is very slightly soluble in water, sparingly soluble in methanol, slightly soluble in ethanol and acetonitrile, soluble in 50% acetonitrile/water, and practically insoluble in toluene.</div><div class="Section" data-sectioncode="42229-5"><a name="section-10.2"></a>LinagliptinLinagliptin is an inhibitor of the dipeptidyl peptidase-4 (DPP-4) enzyme.The chemical name of linagliptin is 1H-Purine-2,6-dione, 8-[(3R)-3-amino-1-piperidinyl]-7-(2-butyn-1-yl)-3,7-dihydro-3-methyl-1-[(4-methyl-2-quinazolinyl)methyl]-The molecular formula is C25H28N8O2 and the molecular weight is 472.54. The structural formula is:<img alt="Chemical Structure" src="trijardy-02.jpg"/>Linagliptin is a white to yellowish, not or only slightly hygroscopic solid substance. It is very slightly soluble in water. Linagliptin is soluble in methanol, sparingly soluble in ethanol, very slightly soluble in isopropanol, and very slightly soluble in acetone.</div><div class="Section" data-sectioncode="42229-5"><a name="section-10.3"></a>Metformin hydrochlorideMetformin hydrochloride (N,N-dimethylimidodicarbonimidic diamide hydrochloride) is a biguanide. Metformin hydrochloride is a white to off-white crystalline compound with a molecular formula of C4H11N5∙HCl and a molecular weight of 165.63. Metformin hydrochloride is freely soluble in water and is practically insoluble in acetone, ether, and chloroform. The pKa of metformin is 12.4. The pH of a 1% aqueous solution of metformin hydrochloride is 6.68. The structural formula is:<img alt="Chemical Structure" src="trijardy-03.jpg"/></div><div class="Section" data-sectioncode="42229-5"><a name="section-10.4"></a>TRIJARDY XREach film coated tablet of TRIJARDY XR consists of an extended-release metformin hydrochloride core tablet that is coated with the immediate-release drug substances: empagliflozin and linagliptin.TRIJARDY XR tablets for oral administration are available in four strengths containing:<ul class="Disc"><li>5 mg empagliflozin/2.5 mg linagliptin/1000 mg metformin hydrochloride extended-release</li><li>10 mg empagliflozin/5 mg linagliptin/1000 mg metformin hydrochloride extended-release</li><li>12.5 mg empagliflozin/2.5 mg linagliptin/1000 mg metformin hydrochloride extended-release</li><li>25 mg empagliflozin/5 mg linagliptin/1000 mg metformin hydrochloride extended-release</li></ul>Each film-coated tablet of TRIJARDY XR contains the following inactive ingredients: Tablet Core: polyethylene oxide, hypromellose, and magnesium stearate. Film Coatings and Printing Ink: hydroxypropyl cellulose, hypromellose, talc, titanium dioxide, arginine, polyethylene glycol, carnauba wax, purified water, shellac glaze, n-butyl alcohol, propylene glycol, ammonium hydroxide, isopropyl alcohol, ferrosoferric oxide and ferric oxide yellow (5 mg/2.5 mg/1000 mg and 25 mg/5 mg/1000 mg), ferric oxide yellow and ferric oxide red (10 mg/5 mg/1000 mg), and ferrosoferric oxide and ferric oxide red (12.5 mg/2.5 mg /1000 mg).</div></section>

Trijardy XR

24 HR empagliflozin 10 MG / linagliptin 5 MG / metformin hydrochloride 1000 MG Extended Release Oral Tablet

24 HR empagliflozin 10 MG / linagliptin 5 MG / metformin hydrochloride 1000 MG Extended Release Oral Tablet [Trijardy]

24 HR empagliflozin 12.5 MG / linagliptin 2.5 MG / metformin hydrochloride 1000 MG Extended Release Oral Tablet

24 HR empagliflozin 12.5 MG / linagliptin 2.5 MG / metformin hydrochloride 1000 MG Extended Release Oral Tablet [Trijardy]

24 HR empagliflozin 25 MG / linagliptin 5 MG / metformin hydrochloride 1000 MG Extended Release Oral Tablet

24 HR empagliflozin 25 MG / linagliptin 5 MG / metformin hydrochloride 1000 MG Extended Release Oral Tablet [Trijardy]

24 HR empagliflozin 5 MG / linagliptin 2.5 MG / metformin hydrochloride 1000 MG Extended Release Oral Tablet

24 HR empagliflozin 5 MG / linagliptin 2.5 MG / metformin hydrochloride 1000 MG Extended Release Oral Tablet [Trijardy]

Trijardy

empagliflozin

empagliflozin / linagliptin / metformin

linagliptin

metformin

Farxiga (dapagliflozin) is an oral medication prescribed for individuals with diabetes, heart disease, or kidney disease to enhance their health outcomes. Here's how Farxiga is utilized:

Farxiga is employed in adults with type 2 diabetes mellitus, complementing dietary and exercise measures to regulate blood sugar levels.

It helps lower the likelihood of hospitalization due to heart failure in adults with type 2 diabetes who have either cardiovascular disease or multiple cardiovascular risk factors.

Farxiga reduces the risk of cardiovascular death, hospitalization for heart failure, and urgent heart failure visits in adults already dealing with heart failure.

It also diminishes the risk of further deterioration in kidney function, progression to end-stage kidney disease (ESKD), cardiovascular-related deaths, and hospitalization due to heart failure in adults with chronic kidney disease who are at risk. 

Farxiga operates by inhibiting the sodium-glucose cotransporter 2 (SGLT2) found in the kidneys' proximal renal tubules. This inhibition prevents the reabsorption of glucose, causing it to be excreted in the urine. Additionally, Farxiga reduces sodium reabsorption in the kidneys, affecting various physiological functions. These include reducing the heart's preload and afterload, regulating sympathetic activity, and decreasing renal pressure.

Farxiga received FDA approval on January 8, 2014, and belongs to the class of medications known as selective sodium-glucose cotransporter-2 inhibitors.

Report Adverse Event 

Prescribing Information

Medication Guide 

Submit MSL Request

Pharmacy List 

Online Sample Form 

Coverage Authorization Request 

Coverage Authorization Appeals 

Enroll in Patient Savings Program 

Farxiga Support 

Other HCP Resources: Video

Other HCP Resources 

Wallet Card 

Farxiga Newly Diagnosed CKD Patient Tear Sheet 

What is CKD & How Farxiga May Help - Brochure 

What is CKD & How Farxiga May Help - Brochure (Spanish)

Side Effects 

FAQs: Diabete, CKD & Heart Failure 

Instructions For Use: Diabetes

Instructions For Use: CKD

Trijardy XR tablets combine empagliflozin, linagliptin, and metformin, which are all oral medications for managing blood sugar levels.

This prescription medication, Trijardy XR, is employed in conjunction with dietary and exercise measures to enhance blood sugar regulation in adults diagnosed with type 2 diabetes mellitus. Additionally, it is utilized to reduce the risk of mortality resulting from heart attack, stroke, or heart failure in adults who have both type 2 diabetes and heart disease.

It's important to note that Trijardy XR is not intended for the treatment of type 1 diabetes.

Farxiga®(dapagliflozin)	Trijardy®(empagliflozin / linagliptin / metformin)

Prescription Only Farxiga (dapagliflozin) is an oral medication prescribed for individuals with diabetes, heart disease, or kidney disease to enhance their health outcomes. Here's how Farxiga is...	Prescription Only Trijardy XR tablets combine empagliflozin, linagliptin, and metformin, which are all oral medications for managing blood sugar levels. This prescription medication, Trijardy XR,...
Dosage & Administration
Administration
Oral . Learn more.	Oral . Learn more.
Dosing
Recommended starting dose is 5 mg orally once daily. Dose can be increased to 10 mg orally once daily for additional glycemic control. . Learn more.	The maximum recommended dose of TRIJARDY XR is 25 mg empagliflozin, 5 mg linagliptin and 2000 mg metformin HCl. Take once daily with a meal in the morning. Swallow whole; do not split, crush, dissolve, or chew.. Learn more.
Latin Shorthand
Starting Dose: 5mg PO qd. Can be increased to 10mg PO qd for additional glycemic control.. Learn more.	Max dose TRIJARDY XR: 25 mg empagliflozin, 5 mg linagliptin, 2000 mg metformin HCl. Take 1x daily with AM meal. Swallow whole; no splitting, crushing, dissolving, or chewing.. Learn more.
Financial Assistance
Out-Of-Pocket Costs With Copay Card
$0. Learn more.	$10. Learn more.
Annual Cap
$175 per month. Learn more.	$175 per month. Learn more.
Assistance Expiration
Learn more.	12/31/23. Learn more.
Generics
No lower-cost generic available	No lower-cost generic available
Physician Advisory
Adverse Reactions
Most common adverse reactions (5% or greater incidence) were female genital mycotic infections, nasopharyngitis, and urinary tract infections. . Learn more.	Most common adverse reactions (5% or greater incidence) were upper respiratory tract infection, urinary tract infection, nasopharyngitis, diarrhea, constipation, headache, and gastroenteritis. . Learn more.
Mechanism of Actions (MoA)
SGLT2 Inhibitors. Learn more.	SGLT2 Inhibitors. Learn more.
Special Populations

Farxiga® Alternatives