Alogliptin 12.5 mg Tablet, Film Coated, 9,000-count
🆔 Identity & classification
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🏷️ RxNorm drug class
This medicine belongs to the Dipeptidyl Peptidase 4 Inhibitor class.
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🏭 Manufacturer & labeler
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🩺 Clinical
Alogliptin is used along with diet and exercise to lower blood sugar levels in patients with type 2 diabetes (condition in which blood sugar is too high because the body does not produce or use insulin normally). Alogliptin is in a class of medications called dipeptidyl peptidase-4 (DPP-4) inhibitors. It works by increasing the amount of insulin in the body to control blood sugar. Alogliptin is not used to treat type 1 diabetes (condition in which the body does not produce insulin and, therefore, cannot control the amount of sugar in the blood) or diabetic ketoacidosis (a serious condition tha...
Read the full MedlinePlus article ↗- After you eat, your gut releases natural hormones that signal your pancreas to release insulin. An enzyme in your body called DPP-4 normally destroys those hormones within minutes....
- What exactly does alogliptin do — how does it lower my blood sugar?
- It depends on how well your kidneys are working. Since alogliptin is mostly cleared through the kidneys, your prescriber will likely lower your dose if your kidney function is redu...
- Can I take alogliptin if I have kidney problems?
Patient education
Supplement & herbal interactions
Some supplements/herbs that may interact with Alogliptin — tap one for details:
Alogliptin may be associated with lower levels of 1 nutrient — worth a chat with your pharmacist, not a cause for alarm.
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Ask a licensed pharmacist directly — free, answered by our team.
💊 What it looks like
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🧪 Inactive Ingredients / Excipients
Inactive ingredients, also called excipients, are components of the drug product other than the active ingredient. They may include fillers, dyes, coatings, preservatives, flavors, or other formulation ingredients.
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UNII 3K9958V90M
A liquid solvent derived from fermentation or chemical synthesis. In medicines, alcohol dissolves active ingredients, helps preserve the product, and improves how the body absorbs certain drugs.
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Butyl alcohol is a clear liquid organic solvent derived from petroleum or natural sources. In medicines, it helps dissolve active ingredients and serves as a solvent in liquid formulations and some topical products.
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Croscarmellose sodium is a plant-based substance derived from cellulose. It acts as a disintegrant, helping tablets and capsules break down quickly in the digestive system so the medicine can be absorbed.
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UNII EX438O2MRT
Ferric oxide yellow is a naturally occurring iron compound used as a colorant in medications. It gives tablets, capsules, and other forms a yellow or golden hue for identification and appearance.
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UNII XM0M87F357
A dark iron oxide compound that gives medicines their black or dark color. It's used as a colorant in tablets and capsules to help identify the product and make it visually distinctive.
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UNII UKE75GEA7F
Hydroxypropyl cellulose is a plant-based polymer used as a binder and thickener. It helps hold tablet ingredients together, controls how fast the medicine dissolves, and improves the texture of liquid formulations.
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UNII 0WZ8WG20P6
Hypromellose 2910 is a plant-based cellulose derivative that acts as a thickener, binder, and film-coating agent. It helps control how quickly the medicine dissolves and protects the tablet or capsule from moisture and light.
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UNII 70097M6I30
Magnesium stearate is a salt made from magnesium and stearic acid, a fatty substance. It's used in tablets and capsules as a lubricant and glidant to help ingredients flow smoothly during manufacturing and prevent sticking.
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UNII 3OWL53L36A
A natural sugar alcohol derived from seaweed or synthesized in the lab. It's used as a filler to add bulk, a sweetener in sugar-free formulas, and a disintegrant to help tablets break apart in the stomach.
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UNII OP1R32D61U
Microcrystalline cellulose is a purified form of cellulose, a natural fiber from plant sources. It acts as a binder and filler in tablets and capsules, helping hold ingredients together and give the medicine its shape and size.
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UNII Q662QK8M3B
Polyethylene glycol 8000 is a synthetic polymer made from ethylene oxide. It acts as a binder and filler in tablets and capsules, helping hold ingredients together and add bulk to the medicine.
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UNII 46N107B71O
Shellac is a natural resin secreted by the lac beetle. It's used as a coating on tablets and capsules to control how quickly the medicine dissolves and to improve appearance and stability.
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UNII 15FIX9V2JP
Titanium dioxide is a bright white mineral powder commonly used as a colorant and opacifying agent. It makes pills and tablets white or lighter in color and helps make coatings non-transparent.
13 inactive ingredients listed in the exact product block matched to this NDC.
Where does this data come from?
ingredient classCode="IACT" elements from the exact product block matched by this NDC. Label-section narrative from DailyMed / the openFDA label index is shown separately when available.Inactive ingredient FAQ
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💲 Pricing
A drug doesn't have one price. Each row is a different public payment system, and none is what you'd pay at the counter — that depends on your insurance. The ⓘ on each row explains what it measures.
| Price system | Per each | Per package |
|---|---|---|
| Retail pharmacies payNADAC · weekly | Not in the retail survey — common for institutional, discontinued, or low-volume packs. | |
| Medicaid paysCMS SDUD · 12 mo | No recent Medicaid claims on file for this NDC — rare and low-volume NDCs are suppressed in the public data. | |
| Medicare drug plans payPart D · Q2 2026 | $6.22 | $55,985.40 / 9000 tablets |
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🔁 Therapeutic equivalents
| Product | Labeler | Pack | NADAC/unit | TE | Status | Price vs. this |
|---|---|---|---|---|---|---|
| Alogliptin 12.5 mg 45802-0103-65 | Padagis | 30 tablets | $5.054 | — | Availability likely | — |
| Nesina 12.5 mg 64764-0125-02 | Takeda | 7 tablets | — | — | FDA listed | — |
| Alogliptin 12.5 mgthis 71610-0661-09 | Aphena | 9000 tablets | — | — | FDA listed | — |
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⏳ Availability & generic status
We did not find an FDA-approved generic match for this exact strength, form and route. Patent/protection dates below may affect future generic timing.
Why the date isn’t exact: Generic timing can change because patents may be challenged, settled, licensed, added, removed, or worked around with a narrower label — and FDA approval does not always mean a pharmacy can get the generic today.
🛈 What do these terms mean?
- Patent
- Legal protection listed in the Orange Book that may delay generic approval or launch. Issued by the U.S. Patent & Trademark Office.
- Substance patent
- Covers the active drug molecule itself — the hardest to design around. A generic generally can’t launch until it expires.
- Formulation (product) patent
- Covers a specific formulation or dosage form. A generic can sometimes work around it with a different formulation.
- Method-of-use patent
- A patent covering one specific approved use of the drug — not necessarily the whole molecule. A generic can sometimes launch with a “skinny label” that carves out the protected use and keeps the others.
- Skinny label
- A generic label that omits a still-patented use when the FDA allows it — letting a generic reach the market for the unprotected uses.
- Exclusivity
- FDA-granted marketing protection, separate from patents — e.g. 5-yr new chemical entity, 7-yr orphan drug, or a +6-month pediatric extension.
- Paragraph IV
- A generic applicant’s formal challenge to a listed patent. It can potentially lead to earlier generic entry, but often involves litigation or a settlement.
- RLD / RS
- Reference Listed Drug — the brand product the FDA uses as the reference for generic applications. Reference Standard — the product the FDA expects generics to compare against in bioequivalence testing.
- TE / AB rating
- FDA therapeutic-equivalence rating. An AB rating generally means the FDA considers a generic therapeutically equivalent to — and substitutable for — the brand.
- LOE (loss of exclusivity)
- The latest patent or exclusivity currently listed — the loss-of-exclusivity / latest-listed-protection date shown on this page. Paragraph-IV challenges and settlements can move the real date earlier; FDA approval and a manufacturer’s decision to market can move it later.
Built from the FDA Orange Book. The bars above are scaled to each protection’s expiry; the red LOE marker is the last one to lapse.
| Patent | Type | Use code | Expires |
|---|---|---|---|
| US 7807689 ↗ | Drug substance | U-1337 | Jun 27, 2028 |
| US 7807689 ↗ | Drug substance | U-1337 | Jun 27, 2028 |
| US 7807689 ↗ | Drug substance | U-1337 | Jun 27, 2028 |
| US 8697125 ↗ | Drug product | — | Jun 16, 2029 |
| US 8697125 ↗ | Drug product | — | Jun 16, 2029 |
| US 8697125 ↗ | Drug product | — | Jun 16, 2029 |
| Code | What it grants | Expires |
|---|---|---|
| M-300 | New indication / labeling change (3-year) | Jul 27, 2026 |
| M-300 | New indication / labeling change (3-year) | Jul 27, 2026 |
| M-300 | New indication / labeling change (3-year) | Jul 27, 2026 |
Is there a generic version of ALOGLIPTIN 12.5 MG TABLET?
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📊 Medicare Part D spend CMS · PART D · 2026 (Q1)
🔬 Reported adverse events (FAERS)
Top reported reactions
Reporter sex
Serious outcomes
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📦 Packaging — all sizes for this product
| Package NDC | Description | Marketing start | Status |
|---|---|---|---|
| 71610-0661-09 You're viewing this | 9000 TABLET, FILM COATED in 1 BOTTLE (71610-661-09) | 2022-09-08 | Active |
| 71610-0661-18 | 3000 TABLET, FILM COATED in 1 BOTTLE (71610-661-18) | 2022-10-17 | Active |
You're viewing the largest of 2 pack sizes for this product.
Pack size FAQ
What quantity is in NDC 71610-0661-09?
What is the difference between NDC 71610-0661-09 and NDC 71610-0661-18?
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🧭 About this NDC listing & data coverage
What data is (and isn’t) available for this NDC — tap to expand
| NDC identity (package / product / labeler codes) | ✓ Available |
| Labeler | ✓ Available |
| Product & package description | ✓ Available |
| Marketing category & status | ✓ Available |
| Active ingredient / dosage form / route | ✓ Available |
| FDA label (SPL via DailyMed) | ✓ Available |
| Package photos | ✓ Available |
| Inactive ingredients (structured) | ✓ Available |
| NADAC pharmacy acquisition price (CMS) | — Not published for this NDC CMS publishes NADAC only for NDCs reported in its retail-pharmacy survey. |
| Orange Book / therapeutic-equivalence data | ✓ Available |
| HCPCS J-code billing crosswalk | — Not published for this NDC Most self-administered / retail products have no J-code — that is normal. |
| Medicaid utilization (CMS SDUD) | — Not published for this NDC CMS reports utilization only for NDCs with Medicaid claims above its privacy threshold. |
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📄 Full prescribing information FDA SPL
🎯 Indications and Usage ▾
1 INDICATIONS AND USAGE Alogliptin tablets are a dipeptidyl peptidase-4 (DPP-4) inhibitor indicated as an adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes mellitus. ( 1.1 , 14 ) Important Limitations of Use: Not for treatment of type 1 diabetes or diabetic ketoacidosis. ( 1.1 )
1.1Monotherapy and Combination Therapy Alogliptin tablets are indicated as an adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes mellitus [see Clinical Studies (14) ]. Important Limitations of Use Alogliptin tablets are not indicated for the treatment of type 1 diabetes mellitus or diabetic ketoacidosis, as it would not be effective in these settings.
⏱️ Dosage and Administration ▾
2 DOSAGE AND ADMINISTRATION The recommended dose in patients with normal renal function or mild renal impairment is 25 mg once daily. ( 2.1 ) Can be taken with or without food. ( 2.1 ) Adjust dose if moderate or severe renal impairment or end-stage renal disease (ESRD). ( 2.2 ) Degree of Renal Impairment Creatinine Clearance (mL/min) Recommended Dosing Moderate ≥30 to <60 12.5 mg once daily Severe/ESRD <30 6.25 mg once daily
2.1Recommended Dosing The recommended dose of alogliptin tablets is 25 mg once daily. Alogliptin tablets may be taken with or without food.
2.2Patients with Renal Impairment No dose adjustment of alogliptin tablets is necessary for patients with mild renal impairment (creatinine clearance [CrCl] ≥60 mL/min). The dose of alogliptin tablets is 12.5 mg once daily for patients with moderate renal impairment (CrCl ≥30 to <60 mL/min). The dose of alogliptin tablets is 6.25 mg once daily for patients with severe renal impairment (CrCl ≥15 to <30 mL/min) or with end-stage renal disease (ESRD) (CrCl <15 mL/min or requiring hemodialysis).
Alogliptin tablets may be administered without regard to the timing of dialysis. Alogliptin tablets have not been studied in patients undergoing peritoneal dialysis [see Use in Specific Populations (8.6) , Clinical Pharmacology (12.3) ]. Because there is a need for dose adjustment based upon renal function, assessment of renal function is recommended prior to initiation of alogliptin tablets therapy and periodically thereafter.
💊 Dosage Forms and Strengths ▾
3 DOSAGE FORMS AND STRENGTHS 25 mg tablets are light red, oval, biconvex, film-coated, with "TAK ALG-25" printed on one side. 12.5 mg tablets are yellow, oval, biconvex, film-coated, with "TAK ALG-12.5" printed on one side. 6.25 mg tablets are light pink, oval, biconvex, film-coated, with "TAK ALG-6.25" printed on one side. Tablets: 25 mg, 12.5 mg and 6.25 mg ( 3 )
⛔ Contraindications ▾
4 CONTRAINDICATIONS History of a serious hypersensitivity reaction to alogliptin-containing products, such as anaphylaxis, angioedema or severe cutaneous adverse reactions. History of a serious hypersensitivity reaction to alogliptin-containing products, such as anaphylaxis, angioedema or severe cutaneous adverse reactions. ( 4 )
⚠️ Warnings and Cautions ▾
5 WARNINGS AND PRECAUTIONS Acute pancreatitis: There have been postmarketing reports of acute pancreatitis. If pancreatitis is suspected, promptly discontinue alogliptin tablets. ( 5.1 ) Heart failure: Consider the risks and benefits of alogliptin tablets prior to initiating treatment in patients at risk for heart failure.
If heart failure develops, evaluate and manage according to current standards of care and consider discontinuation of alogliptin tablets ( 5.2 ). Hypersensitivity: There have been postmarketing reports of serious hypersensitivity reactions in patients treated with alogliptin tablets such as anaphylaxis, angioedema and severe cutaneous adverse reactions, including Stevens-Johnson syndrome. In such cases, promptly discontinue alogliptin tablets, assess for other potential causes, institute appropriate monitoring and treatment and initiate alternative treatment for diabetes.
( 5.3 ) Hepatic effects: Postmarketing reports of hepatic failure, sometimes fatal. Causality cannot be excluded. If liver injury is detected, promptly interrupt alogliptin tablets and assess patient for probable cause, then treat cause if possible, to resolution or stabilization.
Do not restart alogliptin tablets if liver injury is confirmed and no alternative etiology can be found. ( 5.4 ) Hypoglycemia: When an insulin secretagogue (e.g., sulfonylurea) or insulin is used in combination with alogliptin tablets, a lower dose of the insulin secretagogue or insulin may be required to minimize the risk of hypoglycemia. ( 5.5 ) Arthralgia: Severe and disabling arthralgia has been reported in patients taking DPP-4 inhibitors.
Consider as a possible cause for severe joint pain and discontinue drug if appropriate. ( 5.6 ) Bullous pemphigoid: There have been postmarketing reports of bullous pemphigoid requiring hospitalization in patients taking DPP-4 inhibitors. Tell patients to report development of blisters or erosions.
If bullous pemphigoid is suspected, discontinue alogliptin tablets. ( 5.7 ) Macrovascular outcomes: There have been no clinical studies establishing conclusive evidence of macrovascular risk reduction with alogliptin tablets or any other antidiabetic drug. ( 5.8 )
5.1Pancreatitis Acute pancreatitis has been reported in the postmarketing setting and in randomized clinical trials. In glycemic control trials in patients with type 2 diabetes, acute pancreatitis was reported in 6 (0.2%) patients treated with alogliptin tablets 25 mg and 2 (<0.1%) patients treated with active comparators or placebo. In the EXAMINE trial (a cardiovascular outcomes trial of patients with type 2 diabetes and high cardiovascular (CV) risk), acute pancreatitis was reported in 10 (0.4%) of patients treated with alogliptin tablets and in 7 (0.3%) of patients treated with placebo.
It is unknown whether patients with a history of pancreatitis are at increased risk for pancreatitis while using alogliptin tablets . After initiation of alogliptin tablets, patients should be observed for signs and symptoms of pancreatitis. If pancreatitis is suspected, alogliptin tablets should promptly be discontinued and appropriate management should be initiated.
5.2Heart Failure In the EXAMINE trial which enrolled patients with type 2 diabetes and recent acute coronary syndrome, 106 (3.9%) of patients treated with alogliptin tablets and 89 (3.3%) of patients treated with placebo were hospitalized for congestive heart failure. Consider the risks and benefits of alogliptin tablets prior to initiating treatment in patients at risk for heart failure, such as those with a prior history of heart failure and a history of renal impairment, and observe these patients for signs and symptoms of heart failure during therapy.
Patients should be advised of the characteristic symptoms of heart failure and should be instructed to immediately report such symptoms. If heart failure develops, evaluate and manage according to current standards of care and consider discontinuation of alogliptin t…
🤒 Adverse Reactions ▾
6 ADVERSE REACTIONS The following serious adverse reactions are described below or elsewhere in the prescribing information: Pancreatitis [see Warnings and Precautions (5.1) ] Heart Failure [see Warnings and Precautions (5.2) ] Hypersensitivity Reactions [see Warnings and Precautions (5.3) ] Hepatic Effects [see Warnings and Precautions (5.4) ] Severe and Disabling Arthralgia [see Warnings and Precautions (5.6) ] Bullous Pemphigoid [see Warnings and Precautions (5.7) ] The most common adverse reactions (4% or greater incidence) are nasopharyngitis, headache and upper respiratory tract infection.
( 6.1 ) To report SUSPECTED ADVERSE REACTIONS, contact Takeda Pharmaceuticals at 1-877-TAKEDA-7 (1-877-825-3327) or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch.
6.1Clinical Trials Experience Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in practice. A total of 14,778 patients with type 2 diabetes participated in 14 randomized, double-blind, controlled clinical trials of whom 9052 subjects were treated with alogliptin tablets, 3469 subjects were treated with placebo and 2257 were treated with an active comparator.
The mean duration of diabetes was seven years, the mean body mass index (BMI) was 31 kg/m 2 (49% of patients had a BMI ≥30 kg/m 2 ), and the mean age was 58 years (26% of patients ≥65 years of age). The mean exposure to alogliptin tablets was 49 weeks with 3348 subjects treated for more than one year. In a pooled analysis of these 14 controlled clinical trials, the overall incidence of adverse reactions was 73% in patients treated with alogliptin tablets 25 mg compared to 75% with placebo and 70% with active comparator.
Overall discontinuation of therapy due to adverse reactions was 6.8% with alogliptin tablets 25 mg compared to 8.4% with placebo or 6.2% with active comparator. Adverse reactions reported in ≥4% of patients treated with alogliptin tablets 25 mg and more frequently than in patients who received placebo are summarized in Table 1 . Table 1.
Adverse Reactions Reported in ≥4% Patients Treated with Alogliptin Tablets 25 mg and More Frequently Than in Patients Given Placebo in Pooled Studies Number of Patients (%) Alogliptin Tablets 25 mg Placebo Active Comparator N=6447 N=3469 N=2257 Nasopharyngitis 309 (4.8) 152 (4.4) 113 (5.0) Upper Respiratory Tract Infection 287 (4.5) 121 (3.5) 113 (5.0) Headache 278 (4.3) 101 (2.9) 121 (5.4) Hypoglycemia Hypoglycemic events were documented based upon a blood glucose value and/or clinical signs and symptoms of hypoglycemia.
In the monotherapy study, the incidence of hypoglycemia was 1.5% in patients treated with alogliptin tablets compared to 1.6% with placebo. The use of alogliptin tablets as add-on therapy to glyburide or insulin did not increase the incidence of hypoglycemia compared to placebo. In a monotherapy study comparing alogliptin tablets to a sulfonylurea in elderly patients, the incidence of hypoglycemia was 5.4% with alogliptin tablets compared to 26% with glipizide (Table 2) .
Table 2. Incidence and Rate of Hypoglycemia Adverse reactions of hypoglycemia were based on all reports of symptomatic and asymptomatic hypoglycemia; a concurrent glucose measurement was not required; intent-to-treat population. in Placebo and Active-Controlled Studies when Alogliptin Tablets Were Used as Add-On Therapy to Glyburide, Insulin, Metformin, Pioglitazone or Compared to Glipizide or Metformin Add-On to Glyburide (26 Weeks) Alogliptin Tablets 25 mg Placebo N=198 N=99 Overall (%) 19 (9.6) 11 (11.1) Severe (%) Severe events of hypoglycemia were defined as those events requiring medical assistance or exhibiting depressed level or loss of consciousness or seizure.
0 1 (1) Add-On to Insulin (± Metformin) (26 Weeks) Alogliptin Tablets 25 mg Placebo N=129 N=129 Overall (%) 35 (27) 31 (…
🔄 Drug Interactions ▾
7 DRUG INTERACTIONS Alogliptin tablets are primarily renally excreted. Cytochrome (CYP) P450-related metabolism is negligible. No significant drug-drug interactions were observed with the CYP-substrates or inhibitors tested or with renally excreted drugs [see Clinical Pharmacology (12.3) ].
👥 Use in Specific Populations ▾
8 USE IN SPECIFIC POPULATIONS
8.1Pregnancy Risk Summary Limited data with alogliptin in pregnant women are not sufficient to determine a drug-associated risk for major birth defects or miscarriage. There are risks to the mother and fetus associated with poorly controlled diabetes in pregnancy [see Clinical Considerations ]. No adverse developmental effects were observed when alogliptin was administered to pregnant rats and rabbits during organogenesis at exposures 180 and 149 times the 25 mg clinical dose, respectively, based on plasma drug exposure (AUC) [see Data ] .
The estimated background risk of major birth defects is 6-10% in women with pre-gestational diabetes with a HbA1c >7 and has been reported to be as high as 20-25% in women with HbA1c >10. The estimated background risk of miscarriage for the indicated population is unknown. In the U.S. general population, the estimated background risk of major birth defects and miscarriage in clinically recognized pregnancies is 2-4% and 15-20%, respectively.
Clinical Considerations Disease-associated maternal and/or embryo/fetal risk Poorly controlled diabetes in pregnancy increases the maternal risk for diabetic ketoacidosis, pre-eclampsia, spontaneous abortions, preterm delivery, still birth and delivery complications. Poorly controlled diabetes increases the fetal risk for major birth defects, still birth, and macrosomia related morbidity. Data Animal Data Alogliptin administered to pregnant rabbits and rats during the period of organogenesis did not cause adverse developmental effects at doses of up to 200 mg/kg and 500 mg/kg, or 149 times and 180 times, the 25 mg clinical dose, respectively, based on plasma drug exposure (AUC).Placental transfer of alogliptin into the fetus was observed following oral dosing to pregnant rats.
No adverse developmental outcomes were observed in offspring when alogliptin was administered to pregnant rats during gestation and lactation at doses up to 250 mg/kg (~ 95 times the 25 mg clinical dose, based on AUC).
8.2Lactation Risk Summary There is no information regarding the presence of alogliptin in human milk, the effects on the breastfed infant, or the effects on milk production. Alogliptin is present in rat milk: however, due to species specific differences in lactation physiology, animal lactation data may not reliably predict levels in human milk . The developmental and health benefits of breastfeeding should be considered along with the mother's clinical need for alogliptin tablets and any potential adverse effects on the breastfed infant from alogliptin tablets or from the underlying maternal condition.
8.4Pediatric Use Safety and effectiveness of alogliptin tablets in pediatric patients have not been established.
8.5Geriatric Use Of the total number of patients (N=9052) in clinical safety and efficacy studies treated with alogliptin tablets, 2257 (24.9%) patients were 65 years and older and 386 (4.3%) patients were 75 years and older. No overall differences in safety or effectiveness were observed between patients 65 years and over and younger patients. While this clinical experience has not identified differences in responses between the elderly and younger patients, greater sensitivity of some older individuals cannot be ruled out.
8.6Renal Impairment A total of 602 patients with moderate renal impairment (eGFR ≥30 and <60 mL/min/1.73 m 2 ) and 4 patients with severe renal impairment/end-stage renal disease (eGFR <30 mL/min/1.73 m 2 or <15 mL/min/1.73 m 2 , respectively) at baseline were treated with alogliptin tablets in clinical trials in patients with type 2 diabetes. Reductions in HbA1c were generally similar in this subgroup of patients. The overall incidence of adverse reactions was generally balanced between alogliptin tablets and placebo treatments in this subgroup of patients.
In the EXAMINE trial of high CV risk type 2 diabetes patients, 694 patients had moderate renal impairment and 78 patients had severe renal impairm…
🤰 Pregnancy ▾
8.1Pregnancy Risk Summary Limited data with alogliptin in pregnant women are not sufficient to determine a drug-associated risk for major birth defects or miscarriage. There are risks to the mother and fetus associated with poorly controlled diabetes in pregnancy [see Clinical Considerations ]. No adverse developmental effects were observed when alogliptin was administered to pregnant rats and rabbits during organogenesis at exposures 180 and 149 times the 25 mg clinical dose, respectively, based on plasma drug exposure (AUC) [see Data ] .
The estimated background risk of major birth defects is 6-10% in women with pre-gestational diabetes with a HbA1c >7 and has been reported to be as high as 20-25% in women with HbA1c >10. The estimated background risk of miscarriage for the indicated population is unknown. In the U.S. general population, the estimated background risk of major birth defects and miscarriage in clinically recognized pregnancies is 2-4% and 15-20%, respectively.
Clinical Considerations Disease-associated maternal and/or embryo/fetal risk Poorly controlled diabetes in pregnancy increases the maternal risk for diabetic ketoacidosis, pre-eclampsia, spontaneous abortions, preterm delivery, still birth and delivery complications. Poorly controlled diabetes increases the fetal risk for major birth defects, still birth, and macrosomia related morbidity. Data Animal Data Alogliptin administered to pregnant rabbits and rats during the period of organogenesis did not cause adverse developmental effects at doses of up to 200 mg/kg and 500 mg/kg, or 149 times and 180 times, the 25 mg clinical dose, respectively, based on plasma drug exposure (AUC).Placental transfer of alogliptin into the fetus was observed following oral dosing to pregnant rats.
No adverse developmental outcomes were observed in offspring when alogliptin was administered to pregnant rats during gestation and lactation at doses up to 250 mg/kg (~ 95 times the 25 mg clinical dose, based on AUC).
🧒 Pediatric Use ▾
8.4Pediatric Use Safety and effectiveness of alogliptin tablets in pediatric patients have not been established.
🧓 Geriatric Use ▾
8.5Geriatric Use Of the total number of patients (N=9052) in clinical safety and efficacy studies treated with alogliptin tablets, 2257 (24.9%) patients were 65 years and older and 386 (4.3%) patients were 75 years and older. No overall differences in safety or effectiveness were observed between patients 65 years and over and younger patients. While this clinical experience has not identified differences in responses between the elderly and younger patients, greater sensitivity of some older individuals cannot be ruled out.
🆘 Overdosage ▾
10 OVERDOSAGE The highest doses of alogliptin tablets administered in clinical trials were single doses of 800 mg to healthy subjects and doses of 400 mg once daily for 14 days to patients with type 2 diabetes (equivalent to 32 times and 16 times the maximum recommended clinical dose of 25 mg, respectively). No serious adverse reactions were observed at these doses. In the event of an overdose, it is reasonable to institute the necessary clinical monitoring and supportive therapy as dictated by the patient's clinical status.
Per clinical judgment, it may be reasonable to initiate removal of unabsorbed material from the gastrointestinal tract. Alogliptin is minimally dialyzable; over a three-hour hemodialysis session, approximately 7% of the drug was removed. Therefore, hemodialysis is unlikely to be beneficial in an overdose situation.
It is not known if alogliptin tablets are dialyzable by peritoneal dialysis.
🧬 Clinical Pharmacology ▾
12 CLINICAL PHARMACOLOGY
12.1Mechanism of Action Increased concentrations of the incretin hormones such as glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic polypeptide (GIP) are released into the bloodstream from the small intestine in response to meals. These hormones cause insulin release from the pancreatic beta cells in a glucose-dependent manner but are inactivated by the dipeptidyl peptidase-4 (DPP-4) enzyme within minutes. GLP-1 also lowers glucagon secretion from pancreatic alpha cells, reducing hepatic glucose production.
In patients with type 2 diabetes, concentrations of GLP-1 are reduced but the insulin response to GLP-1 is preserved. Alogliptin is a DPP-4 inhibitor that slows the inactivation of the incretin hormones, thereby increasing their bloodstream concentrations and reducing fasting and postprandial glucose concentrations in a glucose-dependent manner in patients with type 2 diabetes mellitus. Alogliptin selectively binds to and inhibits DPP-4 but not DPP-8 or DPP-9 activity in vitro at concentrations approximating therapeutic exposures.
12.2Pharmacodynamics Single-dose administration of alogliptin tablets to healthy subjects resulted in a peak inhibition of DPP-4 within two to three hours after dosing. The peak inhibition of DPP-4 exceeded 93% across doses of 12.5 mg to 800 mg. Inhibition of DPP-4 remained above 80% at 24 hours for doses greater than or equal to 25 mg.
Peak and total exposure over 24 hours to active GLP-1 were three to four fold greater with alogliptin tablets (at doses of 25 to 200 mg) than placebo. In a 16 week, double-blind, placebo-controlled study, alogliptin tablets 25 mg demonstrated decreases in postprandial glucagon while increasing postprandial active GLP-1 levels compared to placebo over an eight hour period following a standardized meal. It is unclear how these findings relate to changes in overall glycemic control in patients with type 2 diabetes mellitus.
In this study, alogliptin tablets 25 mg demonstrated decreases in two hour postprandial glucose compared to placebo (-30 mg/dL versus 17 mg/dL, respectively). Multiple-dose administration of alogliptin to patients with type 2 diabetes also resulted in a peak inhibition of DPP-4 within one to two hours and exceeded 93% across all doses (25 mg, 100 mg and 400 mg) after a single dose and after 14 days of once-daily dosing. At these doses of alogliptin tablets, inhibition of DPP-4 remained above 81% at 24 hours after 14 days of dosing.
Cardiac Electrophysiology In a randomized, placebo-controlled, four-arm, parallel-group study, 257 subjects were administered either alogliptin 50 mg, alogliptin 400 mg, moxifloxacin 400 mg or placebo once daily for a total of seven days. No increase in corrected QT (QTc) was observed with either dose of alogliptin. At the 400 mg dose, peak alogliptin plasma concentrations were 19 fold higher than the peak concentrations following the maximum recommended clinical dose of 25 mg.
12.3Pharmacokinetics The pharmacokinetics of alogliptin tablets has been studied in healthy subjects and in patients with type 2 diabetes. After administration of single, oral doses up to 800 mg in healthy subjects, the peak plasma alogliptin concentration (median T max ) occurred one to two hours after dosing. At the maximum recommended clinical dose of 25 mg, alogliptin tablets were eliminated with a mean terminal half-life (T 1/2 ) of approximately 21 hours.
After multiple-dose administration up to 400 mg for 14 days in patients with type 2 diabetes, accumulation of alogliptin was minimal with an increase in total [e.g., area under the plasma concentration curve (AUC)] and peak (i.e., C max ) alogliptin exposures of 34% and 9%, respectively. Total and peak exposure to alogliptin increased proportionally across single doses and multiple doses of alogliptin ranging from 25 mg to 400 mg. The intersubject coefficient of variation for alogliptin AUC was 17%.
The pharmacokinetics of alogliptin tablets we…
🧬 Mechanism of Action ▾
12.1Mechanism of Action Increased concentrations of the incretin hormones such as glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic polypeptide (GIP) are released into the bloodstream from the small intestine in response to meals. These hormones cause insulin release from the pancreatic beta cells in a glucose-dependent manner but are inactivated by the dipeptidyl peptidase-4 (DPP-4) enzyme within minutes. GLP-1 also lowers glucagon secretion from pancreatic alpha cells, reducing hepatic glucose production.
In patients with type 2 diabetes, concentrations of GLP-1 are reduced but the insulin response to GLP-1 is preserved. Alogliptin is a DPP-4 inhibitor that slows the inactivation of the incretin hormones, thereby increasing their bloodstream concentrations and reducing fasting and postprandial glucose concentrations in a glucose-dependent manner in patients with type 2 diabetes mellitus. Alogliptin selectively binds to and inhibits DPP-4 but not DPP-8 or DPP-9 activity in vitro at concentrations approximating therapeutic exposures.
📦 How Supplied / Storage and Handling ▾
16 HOW SUPPLIED/STORAGE AND HANDLING Alogliptin tablets are available as film-coated tablets containing 25 mg, 12.5 mg or 6.25 mg of alogliptin as follows: 25 mg tablet: light red, oval, biconvex, film-coated, with "TAK ALG-25" printed on one side, available in: NDC 45802-150-65 Bottles of 30 tablets 12.5 mg tablet: yellow, oval, biconvex, film-coated, with "TAK ALG-12.5" printed on one side, available in: NDC 45802-103-65 Bottles of 30 tablets 6.25 mg tablet: light pink, oval, biconvex, film-coated, with "TAK ALG-6.25" printed on one side, available in: NDC 45802-087-65 Bottles of 30 tablets Storage Store at 25°C (77°F); excursions permitted to 15° to 30°C (59° to 86°F) [see USP Controlled Room Temperature].
📦 Storage and Handling ▾
Storage Store at 25°C (77°F); excursions permitted to 15° to 30°C (59° to 86°F) [see USP Controlled Room Temperature].
📋 Description ▾
11 DESCRIPTION Alogliptin tablets contain the active ingredient alogliptin, which is a selective, orally bioavailable inhibitor of the enzymatic activity of dipeptidyl peptidase-4 (DPP-4). Chemically, alogliptin is prepared as a benzoate salt, which is identified as 2-({6-[(3 R )-3-aminopiperidin-1-yl]-3-methyl-2,4-dioxo-3,4-dihydropyrimidin-1(2 H )-yl}methyl)benzonitrile monobenzoate. It has a molecular formula of C 18 H 21 N 5 O 2 ∙C 7 H 6 O 2 and a molecular weight of 461.51 daltons.
The structural formula is: Alogliptin benzoate is a white to off-white crystalline powder containing one asymmetric carbon in the aminopiperidine moiety. It is soluble in dimethylsulfoxide, sparingly soluble in water and methanol, slightly soluble in ethanol and very slightly soluble in octanol and isopropyl acetate. Each alogliptin tablet contains 34 mg, 17 mg or 8.5 mg alogliptin benzoate, which is equivalent to 25 mg, 12.5 mg or 6.25 mg, respectively, of alogliptin and the following inactive ingredients: mannitol, microcrystalline cellulose, hydroxypropyl cellulose, croscarmellose sodium and magnesium stearate.
In addition, the film coating contains the following inactive ingredients: hypromellose, titanium dioxide, ferric oxide (red or yellow) and polyethylene glycol, and is marked with printing ink (Gray F1). Chemical Structure
💬 Information for Patients ▾
17 PATIENT COUNSELING INFORMATION Advise the patient to read the FDA-approved patient labeling (Medication Guide). Inform patients of the potential risks and benefits of alogliptin tablets. Patients should be informed that acute pancreatitis has been reported during use of alogliptin tablets.
Patients should be informed that persistent, severe abdominal pain, sometimes radiating to the back, which may or may not be accompanied by vomiting, is the hallmark symptom of acute pancreatitis. Patients should be instructed to promptly discontinue alogliptin tablets and contact their physician if persistent severe abdominal pain occurs. Patients should be informed of the signs and symptoms of heart failure.
Before initiating alogliptin tablets, patients should be asked about a history of heart failure or other risk factors for heart failure including moderate to severe renal impairment. Patients should be instructed to contact their healthcare providers as soon as possible if they experience symptoms of heart failure, including increasing shortness of breath, rapid increase in weight, or swelling of the feet. Patients should be informed that allergic reactions have been reported during use of alogliptin tablets.
If symptoms of allergic reactions (including skin rash, hives and swelling of the face, lips, tongue and throat that may cause difficulty in breathing or swallowing) occur, patients should be instructed to discontinue alogliptin tablets and seek medical advice promptly. Patients should be informed that postmarketing reports of liver injury, sometimes fatal, have been reported during use of alogliptin tablets. If signs or symptoms of liver injury occur, patients should be instructed to discontinue alogliptin tablets and seek medical advice promptly.
Inform patients that hypoglycemia can occur, particularly when an insulin secretagogue or insulin is used in combination with alogliptin tablets. Explain the risks, symptoms and appropriate management of hypoglycemia. Inform patients that severe and disabling joint pain may occur with this class of drugs.
The time to onset of symptoms can range from one day to years. Instruct patients to seek medical advice if severe joint pain occurs. Inform patients that bullous pemphigoid may occur with this class of drugs.
Instruct patients to seek medical advice if blisters or erosions occur [see Warnings and Precautions (5.7) ] . Instruct patients to take alogliptin tablets only as prescribed. If a dose is missed, advise patients not to double their next dose.
Instruct patients to read the Medication Guide before starting alogliptin tablets therapy and to reread each time the prescription is refilled. Instruct patients to inform their healthcare provider if an unusual symptom develops or if a symptom persists or worsens. ALO332 R5
💬 Medication Guide ▾
MEDICATION GUIDE Alogliptin Tablets Read this Medication Guide carefully before you start taking alogliptin tablets and each time you get a refill. There may be new information. This information does not take the place of talking with your doctor about your medical condition or treatment.
If you have any questions about alogliptin tablets, ask your doctor or pharmacist. What is the most important information I should know about alogliptin tablets? Serious side effects can happen to people taking alogliptin tablets, including: Inflammation of the pancreas (pancreatitis) : Alogliptin tablets may cause pancreatitis which may be severe.
Certain medical conditions make you more likely to get pancreatitis. Before you start taking alogliptin tablets: Tell your doctor if you have ever had: pancreatitis kidney problems liver problems Stop taking alogliptin tablets and call your doctor right away if you have pain in your stomach area (abdomen) that is severe and will not go away. The pain may be felt going from your abdomen through to your back.
The pain may happen with or without vomiting. These may be symptoms of pancreatitis. Heart failure: Before you start taking alogliptin tablets: Tell your healthcare provider if you have ever had heart failure or have problems with your kidneys.
Contact your healthcare provider right away if you have any of the following symptoms: increasing shortness of breath or trouble breathing especially when lying down an unusually fast increase in weight swelling of feet, ankles, or legs These may be symptoms of heart failure. What is alogliptin tablets? Alogliptin tablets is a prescription medicine used along with diet and exercise to improve blood sugar (glucose) control in adults with type 2 diabetes.
Alogliptin tablets are unlikely by themselves to cause your blood sugar to be lowered to a dangerous level (hypoglycemia). However, hypoglycemia may still occur with alogliptin tablets. Alogliptin tablets are not for people with type 1 diabetes.
Alogliptin tablets are not for people with diabetic ketoacidosis (increased ketones in blood or urine). It is not known if alogliptin tablets are safe and effective in children under the age of 18. Who should not take alogliptin tablets?
Do not take alogliptin tablets if you: Are allergic to any ingredients in alogliptin tablets or have had a serious allergic (hypersensitivity) reaction to alogliptin tablets. See the end of this Medication Guide for a complete list of the ingredients in alogliptin tablets. Symptoms of a serious allergic reaction to alogliptin tablets may include: swelling of your face, lips, throat and other areas on your skin raised, red areas on your skin (hives) difficulty with swallowing or breathing skin rash, itching, flaking or peeling If you have any of these symptoms, stop taking alogliptin tablets and contact your doctor or go to the nearest hospital emergency room right away.
What should I tell my doctor before and during treatment with alogliptin tablets? Before you take alogliptin tablets, tell your doctor if you: have or have had inflammation of your pancreas (pancreatitis) have kidney or liver problems have other medical conditions are pregnant or plan to become pregnant. It is not known if alogliptin tablets can harm your unborn baby.
Talk with your doctor about the best way to control your blood sugar while you are pregnant or if you plan to become pregnant are breastfeeding or plan to breastfeed. It is not known whether alogliptin passes into your breast milk. Talk with your doctor about the best way to feed your baby if you are taking alogliptin tablets Tell your doctor about all the medicines you take, including prescription and over-the-counter medicines, vitamins and herbal supplements.
Know the medicines you take. Keep a list of them and show it to your doctor and pharmacist before you start any new medicine. Alogliptin tablets may affect the way other medicines work, and other medicines may affect how alogliptin tablets work…