Sodium-Glucose Transporter 2 Inhibitors

Sodium-Glucose Cotransporter 2 Inhibitor

Diabetes Mellitus, Type 2

<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: anhydrous lactose, crospovidone, magnesium stearate, microcrystalline cellulose, and silicon dioxide. In addition, the film coating contains the following inactive ingredients: polyethylene glycol, polyvinyl alcohol, talc, titanium dioxide, and yellow iron oxide.</section>

FARXIGA

Farxiga

dapagliflozin 10 MG Oral Tablet [Farxiga]

dapagliflozin 5 MG Oral Tablet [Farxiga]

dapagliflozin

dapagliflozin 10 MG Oral Tablet

dapagliflozin 5 MG Oral Tablet

Dipeptidyl Peptidase 4 Inhibitors

Dipeptidyl Peptidase 4 Inhibitor

<section class="Section" data-sectioncode="34089-3"><a name="S11"></a><a name="section-10"></a><h1>11 DESCRIPTION</h1>STEGLUJAN (ertugliflozin and sitagliptin) tablet for oral use contains ertugliflozin L-pyroglutamic acid, a SGLT2 inhibitor, and sitagliptin phosphate, a DPP-4 inhibitor.ErtugliflozinThe chemical name of ertugliflozin L-pyroglutamic acid is (1S,2S,3S,4R,5S)-5-(4-chloro-3-(4-ethoxybenzyl)phenyl)-1-(hydroxymethyl)-6,8-dioxabicyclo[3.2.1]octane-2,3,4-triol, compound with (2S)-5-oxopyrrolidine-2-carboxylic acid. The molecular formula is C27H32ClNO10 and the molecular weight is 566.00.The chemical structure is:<img alt="Chemical Structure" src="steglujan-01.jpg"/>Ertugliflozin L-pyroglutamic acid is a white to off-white powder that is soluble in ethyl alcohol and acetone, slightly soluble in ethyl acetate and acetonitrile and very slightly soluble in water.SitagliptinSitagliptin phosphate monohydrate is described chemically as 7-[(3R)-3-amino-1-oxo-4-(2,4,5-trifluorophenyl)butyl]-5,6,7,8-tetrahydro-3-(trifluoromethyl)-1,2,4-triazolo[4,3-a]pyrazine phosphate (1:1) monohydrate.The empirical formula is C16H15F6N5O∙H3PO4∙H2O and the molecular weight is 523.32. The structural formula is:<div class="Figure"><img alt="Chemical Structure" src="steglujan-02.jpg"/></div>Sitagliptin phosphate monohydrate is a white to off-white, crystalline, non-hygroscopic powder. It is soluble in water and N,N-dimethyl formamide; slightly soluble in methanol; very slightly soluble in ethanol, acetone, and acetonitrile; and insoluble in isopropanol and isopropyl acetate.STEGLUJAN is available for oral use as film-coated tablets containing:<ul class="Disc"><li>6.48 mg ertugliflozin L-pyroglutamic acid equivalent to 5 mg of ertugliflozin and 128.5 mg sitagliptin phosphate monohydrate equivalent to 100 mg sitagliptin (STEGLUJAN 5/100)</li><li>19.43 mg ertugliflozin L-pyroglutamic acid equivalent to 15 mg of ertugliflozin and 128.5 mg sitagliptin phosphate monohydrate equivalent to 100 mg sitagliptin (STEGLUJAN 15/100)</li></ul>Inactive ingredients are microcrystalline cellulose, dibasic calcium phosphate anhydrous, croscarmellose sodium, sodium stearyl fumarate, magnesium stearate, and propyl gallate.The film coating contains: hypromellose, hydroxypropyl cellulose, titanium dioxide, iron oxide red, iron oxide yellow, ferrosoferric oxide/black iron oxide, and carnauba wax.</section>

STEGLUJAN

ertugliflozin

ertugliflozin / sitagliptin

ertugliflozin 15 MG / sitagliptin 100 MG Oral Tablet

Steglujan

ertugliflozin 15 MG / sitagliptin 100 MG Oral Tablet [Steglujan]

ertugliflozin 5 MG / sitagliptin 100 MG Oral Tablet

ertugliflozin 5 MG / sitagliptin 100 MG Oral Tablet [Steglujan]

sitagliptin

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.

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FAQs: Diabete, CKD & Heart Failure 

Instructions For Use: Diabetes

Instructions For Use: CKD

Steglujan is a medication that combines ertugliflozin and sitagliptin. These two components work together to manage blood sugar levels. Ertugliflozin helps the kidneys remove glucose from the bloodstream, while sitagliptin regulates insulin production in response to meals.

Steglujan is prescribed alongside diet and exercise to enhance blood sugar control in adults diagnosed with type 2 diabetes mellitus. It is important to note that Steglujan is not intended for the treatment of type 1 diabetes.

Farxiga®(dapagliflozin)	Steglujan®(ertugliflozin / sitagliptin)

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 Steglujan is a medication that combines ertugliflozin and sitagliptin. These two components work together to manage blood sugar levels. Ertugliflozin helps the kidneys remove...
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.	Recommended starting dose is 5 mg ertugliflozin/100 mg sitagliptin once daily, taken in the morning, with or without food. Increase dose to 15 mg ertugliflozin/100 mg sitagliptin once daily in those tolerating STEGLUJAN for additional glycemic control. . Learn more.
Latin Shorthand
Starting Dose: 5mg PO qd. Can be increased to 10mg PO qd for additional glycemic control.. Learn more.	5 mg ertugliflozin/100 mg sitagliptin qd in AM, with or without food. Increase to 15 mg ertugliflozin/100 mg sitagliptin qd for those tolerating STEGLUJAN and needing additional glycemic control.. Learn more.
Financial Assistance
Out-Of-Pocket Costs With Copay Card
$0. Learn more.	$0. Learn more.
Annual Cap
$175 per month. Learn more.	$583 per fill . Learn more.
Assistance Expiration
Learn more.	12 uses. 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 associated with ertugliflozin (incidence ≥5%): female genital mycotic infections. Most common adverse reactions associated with sitagliptin (incidence ≥5%): upper respiratory tract infection, nasopharyngitis and headache. In the add-on to sulfonylurea and add-on to insulin studies, hypoglycemia was also more commonly reported in patients treated with sitagliptin compared to placebo.. Learn more.
Mechanism of Actions (MoA)
SGLT2 Inhibitors. Learn more.	SGLT2 Inhibitors. Learn more.
Special Populations

Farxiga® Alternatives