Alogliptin 12.5 mg Tablet, Film Coated, 30-count — NDC 45802-103-65 (Billing 45802-0103-65)
This is a package of 30 tablets of Alogliptin 12.5 mg Tablet, Film Coated from Padagis Israel Pharmaceuticals Ltd, marketed since Apr 2016 and currently FDA-listed; retail pharmacies pay about $4.96 per tablet (NADAC). It is this product's only package size.
Identity & classification
Regulatory identifiers FDA, NLM and CMS codes for this package
Drug-database identifiers Medi-Span GPI and First Databank GCN / HICL / AHFS classification
- GSN (GCN sequence number): 070524
- GCN: 34085
- GPI-14 (Medi-Span): 27550010100320
- HICL (First Databank): 039968
- AHFS class code: 68:20.05.00
- RxCUI (RxNorm): 1368006
Where does this data come from?
- FDA openFDA NDC Directory · synced Oct 1, 2026
- FDA label on DailyMed · label index refreshed Oct 1, 2026
- RxNorm (NLM RxNav) · catalog refreshed Oct 1, 2026
- Medi-Span GPI (licensed)
- First Databank (licensed) · refreshed Oct 1, 2026
RxNorm drug class
This medicine belongs to the Dipeptidyl Peptidase 4 Inhibitor class.
Where does this data come from?
- RxClass (NLM) · catalog refreshed Oct 1, 2026
Clinical
- It helps lower blood sugar in adults with type 2 diabetes, alongside healthy eating and exercise. It is not for type 1 diabetes or diabetic ketoacidosis.
- You take it by mouth, usually once a day, with or without food. If you have kidney problems, your dose may be adjusted. Follow your prescriber's directions and the pharmacy label.
- The most common ones are cold-like symptoms such as a stuffy nose or sore throat, and headache. These are usually mild. Tell us if they bother you.
- Call for severe stomach pain, swelling of your face or throat, a severe rash, yellow skin or eyes, swelling or shortness of breath, severe joint pain, or blisters. Some of these ma...
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.
Where does this data come from?
- MedlinePlus (NLM) · refreshed Oct 1, 2026
- FDA label on DailyMed · label index refreshed Oct 1, 2026
Ask a licensed pharmacist directly — free, answered by our team.
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 ea | Per package |
|---|---|---|
| Retail pharmacies payNADAC · weekly | $4.957 | $148.70 / 30 tablets |
| Medicaid paysCMS SDUD · 12 mo | $5.22 | $156.74 / 30 tablets |
| Medicare drug plans payPart D · Q2 2026 | $5.85 | $175.61 / 30 tablets |
Where does this data come from?
- CMS NADAC weekly file · file of Sep 30, 2026
- CMS ASP pricing files · refreshed Sep 20, 2026
- CMS Medicaid State Drug Utilization Data · through Q1 2026
- CMS Part D plan pricing files · refreshed Sep 24, 2026
- VA National Acquisition Center price file
Packaging — all sizes for this product
| Package NDC | Description | Marketing start | Marketing end | Status |
|---|---|---|---|---|
| 45802-0103-65 You're viewing this Main listing | 30 TABLET, FILM COATED in 1 BOTTLE | 2016-04-08 | — | Active |
Therapeutic equivalents
| Product | Labeler | Pack | NADAC/unit | TE | Status | Price vs. this |
|---|---|---|---|---|---|---|
| Alogliptin 12.5 mgthis 45802-0103-65 | Padagis | 30 tablets | $4.957 | — | Availability likely | — |
| Nesina 12.5 mg 64764-0125-02 | Takeda | 7 tablets | — | — | FDA listed | — |
| Alogliptin 12.5 mg 71610-0661-09 | Aphena | 9000 tablets | — | — | FDA listed | — |
Where does this data come from?
- FDA openFDA NDC Directory · synced Oct 1, 2026
- FDA Orange Book · refreshed Sep 3, 2026
- CMS NADAC weekly file · file of Sep 30, 2026
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?
The FDA approved a generic — why can’t I get it at my pharmacy yet?
Why do different websites show different generic release dates?
What does “FDA listed” mean?
What does a patent or protection date mean here?
What does “current Orange Book estimate” mean?
Can a generic come out before the last patent expires?
Can a generic come out after the listed dates?
What is the difference between patents and exclusivity?
Why are there multiple patent dates?
Where does this data come from?
- FDA Orange Book · refreshed Sep 3, 2026
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.
Where does this data come from?
IACT rows and label-wide narrative are kept separate; availability and product-level specificity depend on the submitted label.- FDA label on DailyMed · label index refreshed Oct 1, 2026
- FDA openFDA NDC Directory · synced Oct 1, 2026
Inactive ingredient FAQ
Are inactive ingredients the same for every manufacturer?
Why might an inactive ingredient be missing?
Can inactive ingredients matter?
Manufacturer & labeler
Where does this data come from?
- FDA openFDA NDC Directory · synced Oct 1, 2026
- Drugs@FDA
Full prescribing information FDA SPL
🎯 Indications and Usage ▾
1 INDICATIONS AND USAGE Alogliptin tablets are indicated as an adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes mellitus. 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 ) Limitations of Use: Should not be used in patients with type 1 diabetes mellitus.
( 1 ) Limitations of Use Alogliptin tablet is not recommended for use in patients with type 1 diabetes mellitus.
⏱️ Dosage and Administration ▾
2 DOSAGE AND ADMINISTRATION The recommended dosage in patients with normal renal function or mild renal impairment is 25 mg orally once daily. ( 2.1 ) Can be taken with or without food. ( 2.1 ) Adjust dosage if moderate or severe renal impairment or end-stage renal disease (ESRD). ( 2.2 ) Degree of Renal Impairment Creatinine Clearance (mL/min) Recommended Dosage Moderate ≥30 to <60 12.5 mg once daily Severe/ESRD <30 6.25 mg once daily
2.1Recommended Dosage The recommended dosage of alogliptin tablets is 25 mg taken orally once daily. Do not spilt tablet. Alogliptin tablets may be taken with or without food. [see Clinical Pharmacology (12.3) ] Instruct patients if a dose is missed, not to double their next dose.
2.2Patients with Renal Impairment Assess renal function prior to initiation of alogliptin tablets and periodically thereafter [see Use in Specific Populations (8.6) ] . 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) ].
💊 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 Alogliptin tablets is contraindicated in patients with a history of serious hypersensitivity to alogliptin or any of the excipients in Alogliptin tablets. Reactions such as anaphylaxis, angioedema and severe cutaneous adverse reactions have been reported [see Warnings and Precautions (5.3) , Adverse Reactions (6.2) ] . History of serious hypersensitivity to alogliptin or any of the excipients in Alogliptin tablets. ( 4 )
⚠️ Warnings and Cautions ▾
5 WARNINGS AND PRECAUTIONS 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. If hypersensitivity reactions occur, discontinue alogliptin tablets, treat promptly and monitor until signs and symptoms resolve.
( 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: Consider lowering the dosage of insulin secretagogue or insulin to reduce the risk of hypoglycemia when initiating Alogliptin tablets. ( 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 )
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 mellitus, 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 mellitus 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 mellitus 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 tablets.
5.3Hypersensitivity Reactions There have been postmarketing reports of serious hypersensitivity reactions in patients treated with alogliptin tablets [see Adverse Reactions (6.2) ] . These reactions include anaphylaxis, angioedema, and severe cutaneous adverse reactions, including Stevens-Johnso… [Excerpted — this section continues on DailyMed.]
🤒 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) ] Most common adverse reactions (incidence >4%) 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 mellitus participated in 14 randomized, double-blind, controlled clinical trials of whom 9,052 subjects were treated with alogliptin tablets, 3,469 subjects were treated with placebo and 2,257 were treated with an active comparator.
The racial distribution of patients exposed to trial medication was 71% White, 17% Asian, 6% Black or African American, 2% American Indian or Alaska Native, 0% Native Hawaiian/Other Pacific Islander and 5% Multiracial or other racial groups. The ethnic distribution was 30% Hispanic or Latino and 70% was not Hispanic or Latino. The mean duration of diabetes mellitus 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 3,348 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 adult 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% of Adult Patients with Type 2 Diabetes Mellitus Treated with Alogliptin Tablets 25 mg and More Frequently Than in Patients Given Placebo in Pooled Trials Number of Patients (%) Alogliptin Tablets 25 mg Placebo Active Comparator N=6447 N=3469 N=2257 Nasopharyngitis 309 (5) 152 (4) 113 (5) Upper Respiratory Tract Infection 287 (4) 121 (4) 113 (5) Headache 278 (4) 101 (3) 121 (5) Hypoglycemia Hypoglycemic events were documented based upon a blood glucose value and/or clinical signs and symptoms of hypoglycemia.
In the monotherapy trial, 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 trial 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 Trials in Adults with Type 2 Diabetes Mellitus when Alogliptin Tablets Were Used as Add-On Therapy to Glyburide, Insulin, Metformin, Pioglitazone or Compared to Glipizide or… [Excerpted — this section continues on DailyMed.]
🔄 Drug Interactions ▾
7 DRUG INTERACTIONS
7.1Insulin Secretagogues and Insulin Insulin and insulin secretagogues are known to cause hypoglycemia. Coadministration of alogliptin tablets with an insulin secretagogue (e.g., sulfonylurea) or insulin may require lower dosages of the insulin secretagogue and insulin to reduce the risk of hypoglycemia [see Warnings and Precautions (5.5) ] .
👥 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 mellitus 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 mellitus 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 mellitus in pregnancy increases the maternal risk for diabetic ketoacidosis, pre-eclampsia, spontaneous abortions, preterm delivery and delivery complications. Poorly controlled diabetes mellitus 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 The safety and effectiveness of alogliptin tablets have not been established in pediatric patients. Effectiveness of alogliptin tablets was not demonstrated in a 52 week, randomized, double-blind, placebo-controlled trial (NCT02856113) in 151 pediatric patients aged 10 to 17 years with inadequately controlled type 2 diabetes mellitus.
8.5Geriatric Use Of the total number of patients (N=9052) in clinical safety and efficacy trials treated with alogliptin tablets, 2,257 (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.
8.6Renal Impairment A total of 602 adult 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 mellitus. In the EXAMINE trial of high CV risk type 2 diabetes mellitus patients, 694 patients had moderate renal impairment and 78 patients had severe renal impairment or end-stage renal disease at baseline.
The recommended dose is 12.5 mg once daily in patients with moderate… [Excerpted — this section continues on DailyMed.]
🤰 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 mellitus 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 mellitus 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 mellitus in pregnancy increases the maternal risk for diabetic ketoacidosis, pre-eclampsia, spontaneous abortions, preterm delivery and delivery complications. Poorly controlled diabetes mellitus 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 The safety and effectiveness of alogliptin tablets have not been established in pediatric patients. Effectiveness of alogliptin tablets was not demonstrated in a 52 week, randomized, double-blind, placebo-controlled trial (NCT02856113) in 151 pediatric patients aged 10 to 17 years with inadequately controlled type 2 diabetes mellitus.
🧓 Geriatric Use ▾
8.5Geriatric Use Of the total number of patients (N=9052) in clinical safety and efficacy trials treated with alogliptin tablets, 2,257 (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.
🆘 Overdosage ▾
10 OVERDOSAGE 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. In the event of an overdose, contact the Poison Help Line (1-800-222-1222) or a medical toxicologist for additional overdosage management recommendations.
🧬 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 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 mellitus, 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 Dose-Response Relationships 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 mellitus 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 mellitus. The pharmacokinetics of alogliptin tablets were similar in healthy subjects and in patients with type 2 diabetes mellitus. After multiple-dose administration up to 400 mg for 14 days in patients with type 2 diabetes mellitus, 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%. Absorption 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.
The absolute bioavailabi… [Excerpted — this section continues on DailyMed.]
🧬 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 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 mellitus, 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 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 ▾
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 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: croscarmellose sodium, hydroxypropyl cellulose, magnesium stearate, mannitol, and microcrystalline cellulose.
In addition, the film coating contains the following inactive ingredients: ferric oxide (red or yellow), hypromellose, polyethylene glycol, and titanium dioxide 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). Pancreatitis Inform patients that acute pancreatitis has been reported during use of alogliptin tablets. Educate patients 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.
Instruct patients to promptly discontinue alogliptin tablets and contact their physician if persistent severe abdominal pain occurs [see Warnings and Precautions (5.1) ] . Heart Failure Inform patients 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.
Instruct patients 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 [see Warnings and Precautions (5.2) ] . Hypersensitivity Reactions Inform patients that allergic reactions have been reported during use of alogliptin tablets. Instruct patients 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 discontinue alogliptin tablets and seek medical advice promptly [see Warnings and Precautions (5.3) ] .
Hepatic Effects Inform patients that postmarketing reports of liver injury, sometimes fatal, have been reported during use of alogliptin tablets. Instruct patients if signs or symptoms of liver injury occur, patients should discontinue alogliptin tablets and seek medical advice promptly [see Warnings and Precautions (5.4) ] . Hypoglycemia with Concomitant Use with Insulin or Insulin Secretagogues Inform patients that hypoglycemia can occur, particularly when an insulin secretagogue or insulin is used in combination with alogliptin tablets.
Educate patients about the risks, symptoms and appropriate management of hypoglycemia [see Warnings and Precautions (5.5) ] . Severe and Disabling Arthralgia 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 [see Warnings and Precautions (5.6) ] . Bullous Pemphigoid 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) ] .
Dosage Instruct patients to take alogliptin tablets only as prescribed. Instruct patients if a dose is missed, not to double their next dose.
💬 Medication Guide ▾
This Medication Guide has been approved by the U.S. Food and Drug Administration. ALO332 R9 April 2025 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: 1. 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 high blood triglyceride levels kidney problems stones in your gallbladder (gall stones) liver problems a history of alcoholism 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. 2.
Heart failure: Heart failure means your heart does not pump blood well enough. Before you start taking alogliptin tablets: Tell your doctor if you have ever had heart failure or have problems with your kidneys. Contact your doctor 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 unusual tiredness These may be symptoms of heart failure.
What are alogliptin tablets? Alogliptin tablets are a prescription medicine used along with diet and exercise to improve blood sugar (glucose) control in adults with type 2 diabetes mellitus. Alogliptin tablets are not for people with type 1 diabetes mellitus.
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 heart failure 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 if alogliptin tablets 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… [Excerpted — this section continues on DailyMed.]
🧬 Pharmacokinetics ▾
12.3Pharmacokinetics The pharmacokinetics of alogliptin tablets has been studied in healthy subjects and in patients with type 2 diabetes mellitus. The pharmacokinetics of alogliptin tablets were similar in healthy subjects and in patients with type 2 diabetes mellitus. After multiple-dose administration up to 400 mg for 14 days in patients with type 2 diabetes mellitus, 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%. Absorption 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.
The absolute bioavailability of alogliptin tablets is approximately 100%. Effect of Food Administration of alogliptin tablets with a high-fat meal results in no significant change in total and peak exposure to alogliptin. Distribution Following a single, 12.5 mg intravenous infusion of alogliptin to healthy subjects, the volume of distribution during the terminal phase was 417 L, indicating that the drug is well distributed into tissues.
Alogliptin is 20% bound to plasma proteins. Elimination Alogliptin tablets was eliminated with a mean terminal half-life (t 1/2 ) of approximately 21 hours. The renal clearance of alogliptin (9.6 L/hr) indicates some active renal tubular secretion and systemic clearance was
14.0L/hr. Metabolism Alogliptin does not undergo extensive metabolism and 60% to 71% of the dose is excreted as unchanged drug in the urine. Two minor metabolites were detected following administration of an oral dose of [ 14 C] alogliptin, N -demethylated, M-I (less than 1% of the parent compound), and N -acetylated alogliptin, M-II (less than 6% of the parent compound).
M-I is an active metabolite and is an inhibitor of DPP-4 similar to the parent molecule; M-II does not display any inhibitory activity toward DPP-4 or other DPP-related enzymes. In vitro data indicate that CYP2D6 and CYP3A4 contribute to the limited metabolism of alogliptin. Alogliptin exists predominantly as the ( R )-enantiomer (more than 99%) and undergoes little or no chiral conversion in vivo to the ( S )-enantiomer.
The ( S )-enantiomer is not detectable at the 25 mg dose. Excretion The primary route of elimination of [ 14 C] alogliptin-derived radioactivity occurs via renal excretion (76%) with 13% recovered in the feces, achieving a total recovery of 89% of the administered radioactive dose. Specific Populations Geriatric Patients Age (18 to 80 years old) did not have any clinically meaningful effect on the pharmacokinetics of alogliptin.
Male and Female Patients Gender did not have any clinically meaningful effect on the pharmacokinetics of alogliptin. Racial or Ethnic Groups Race (White, Black or African American and Asian) did not have any clinically meaningful effect on the pharmacokinetics of alogliptin. Patients with Renal Impairment A single-dose, open-label study was conducted to evaluate the pharmacokinetics of alogliptin 50 mg in patients with chronic renal impairment compared with healthy subjects.
In patients with mild renal impairment (creatinine clearance [CrCl] ≥60 to <90 mL/min), an approximate 1.2-fold increase in plasma AUC of alogliptin was observed. In patients with moderate renal impairment (CrCl ≥30 to <60 mL/min), an approximate two-fold increase in plasma AUC of alogliptin was observed. In patients with severe renal impairment (CrCl ≥15 to <30 mL/min) and end-stage renal disease (ESRD) (CrCl <15 mL/min or requiring dialysis), an approximate three- and four-fold increase in plasma AUC of alogliptin were observed, respectively.
Dialysis removed approximately 7% of the drug… [Excerpted — this section continues on DailyMed.]
🧬 Pharmacodynamics ▾
12.2Pharmacodynamics Dose-Response Relationships 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 mellitus 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.
🔬 Clinical Studies ▾
14 CLINICAL STUDIES
14.1Overview of Clinical Trials in Adults with Type 2 Diabetes Mellitus Alogliptin tablets have been studied as monotherapy and in combination with metformin, a sulfonylurea, a thiazolidinedione (either alone or in combination with metformin or a sulfonylurea) and insulin (either alone or in combination with metformin). A total of 14,053 patients with type 2 diabetes mellitus were randomized in 11 double-blind, placebo- or active-controlled clinical safety and efficacy trials conducted to evaluate the effects of alogliptin tablets on glycemic control.
The racial distribution of patients exposed to trials medication was 70% White, 17% Asian, 6% Black or African American, 2% American Indian or Alaska Native, 0% Native Hawaiian/Other Pacific Islander and 5% Multiracial or other racial groups. The ethnic distribution was 30% Hispanic or Latino. Patients had an overall mean age of 57 years (range 21 to 91 years).
In patients with type 2 diabetes mellitus, treatment with alogliptin tablets produced clinically meaningful and statistically significant improvements in hemoglobin A1c (A1C) compared to placebo. As is typical for trials of agents to treat type 2 diabetes mellitus, the mean reduction in A1C with alogliptin tablets appears to be related to the degree of A1C elevation at baseline. Alogliptin tablets had similar changes from baseline in serum lipids compared to placebo.
14.2Patients with Inadequate Glycemic Control on Diet and Exercise A total of 1,768 patients with type 2 diabetes mellitus participated in three double-blind trials to evaluate the efficacy and safety of alogliptin tablets in patients with inadequate glycemic control on diet and exercise. All three trials had a four week, single-blind, placebo run-in period followed by a 26 week randomized treatment period. Patients who failed to meet prespecified hyperglycemic goals during the 26 week treatment periods received glycemic rescue therapy.
In a 26 week, double-blind, placebo-controlled trial, a total of 329 patients (mean baseline A1C = 8%) were randomized to receive alogliptin tablets 12.5 mg, alogliptin tablets 25 mg or placebo once daily. Treatment with alogliptin tablets 25 mg resulted in statistically significant improvements from baseline in A1C and fasting plasma glucose (FPG) compared to placebo at Week 26 (Table 3) . A total of 8% of patients receiving alogliptin tablets 25 mg and 30% of those receiving placebo required glycemic rescue therapy.
Improvements in A1C were not affected by gender, age or baseline body mass index (BMI). The mean change in body weight with alogliptin tablets was similar to placebo. Table 3.
Glycemic Parameters at Week 26 in a Placebo-Controlled Monotherapy Trial of Alogliptin Tablets Intent-to-treat population using last observation in the trial Alogliptin Tablets 25 mg Placebo A1C (%) N=128 N=63 Baseline (mean) 7.9
8.0Change from baseline (adjusted mean Least squares means adjusted for treatment, baseline value, geographic region and duration of diabetes mellitus ) -0.6 0 Difference from placebo (adjusted mean with 95% confidence interval) -0.6 p<0.01 compared to placebo (-0.8, -0.3) ˗ % of patients (n/N) achieving A1C ≤7% 44% (58/131) 23% (15/64) FPG (mg/dL) N=129 N=64 Baseline (mean) 172 173 Change from baseline (adjusted mean ) -16 11 Difference from placebo (adjusted mean with 95% confidence interval) -28 (-40, -15) ˗ In a 26 week, double-blind, active-controlled trial, a total of 655 patients (mean baseline A1C = 8.8%) were randomized to receive alogliptin tablets 25 mg alone, pioglitazone 30 mg alone, alogliptin tablets 12.5 mg with pioglitazone 30 mg or alogliptin tablets 25 mg with pioglitazone 30 mg once daily.
Coadministration of alogliptin tablets 25 mg with pioglitazone 30 mg resulted in statistically significant improvements from baseline in A1C and FPG compared to alogliptin tablets 25 mg alone and to pioglitazone 30 mg alone (Table 4) . A total of 3% of patients receiving alogliptin tablet… [Excerpted — this section continues on DailyMed.]
🧪 Nonclinical Toxicology ▾
13 NONCLINICAL TOXICOLOGY
13.1Carcinogenesis, Mutagenesis, Impairment of Fertility Carcinogenesis Rats were administered oral doses of 75, 400 and 800 mg/kg alogliptin for two years. No drug-related tumors were observed up to 75 mg/kg or approximately 32 times the maximum recommended clinical dose of 25 mg, based on area under the plasma concentration curve (AUC) exposure. At higher doses (approximately 308 times the maximum recommended clinical dose of 25 mg), a combination of thyroid C-cell adenomas and carcinomas increased in male but not female rats.
No drug-related tumors were observed in mice after administration of 50, 150 or 300 mg/kg alogliptin for two years, or up to approximately 51 times the maximum recommended clinical dose of 25 mg, based on AUC exposure. Mutagenesis Alogliptin was not mutagenic or clastogenic, with and without metabolic activation, in the Ames test with S. typhimurium and E. coli or the cytogenetic assay in mouse lymphoma cells. Alogliptin was negative in the in vivo mouse micronucleus study.
Impairment of Fertility In a fertility study in rats, alogliptin had no adverse effects on early embryonic development, mating or fertility at doses up to 500 mg/kg, or approximately 172 times the clinical dose based on plasma drug exposure (AUC).
📄 Carcinogenesis, Mutagenesis, Impairment of Fertility ▾
13.1Carcinogenesis, Mutagenesis, Impairment of Fertility Carcinogenesis Rats were administered oral doses of 75, 400 and 800 mg/kg alogliptin for two years. No drug-related tumors were observed up to 75 mg/kg or approximately 32 times the maximum recommended clinical dose of 25 mg, based on area under the plasma concentration curve (AUC) exposure. At higher doses (approximately 308 times the maximum recommended clinical dose of 25 mg), a combination of thyroid C-cell adenomas and carcinomas increased in male but not female rats.
No drug-related tumors were observed in mice after administration of 50, 150 or 300 mg/kg alogliptin for two years, or up to approximately 51 times the maximum recommended clinical dose of 25 mg, based on AUC exposure. Mutagenesis Alogliptin was not mutagenic or clastogenic, with and without metabolic activation, in the Ames test with S. typhimurium and E. coli or the cytogenetic assay in mouse lymphoma cells. Alogliptin was negative in the in vivo mouse micronucleus study.
Impairment of Fertility In a fertility study in rats, alogliptin had no adverse effects on early embryonic development, mating or fertility at doses up to 500 mg/kg, or approximately 172 times the clinical dose based on plasma drug exposure (AUC).
📄 Package Label / Principal Display Panel ▾
PRINCIPAL DISPLAY PANEL - 6.25 mg Tablet Bottle Label NDC 45802- 087 -65 Rx Only Alogliptin Tablets 6.25 mg DISPENSE WITH MEDICATION GUIDE 30 Tablets Padagis ® PRINCIPAL DISPLAY PANEL - 6.25 mg Tablet Bottle Label
PRINCIPAL DISPLAY PANEL - 12.5 mg Tablet Bottle Label NDC 45802- 103 -65 Rx Only Alogliptin Tablets 12.5 mg DISPENSE WITH MEDICATION GUIDE 30 Tablets Padagis ® PRINCIPAL DISPLAY PANEL - 12.5 mg Tablet Bottle Label
PRINCIPAL DISPLAY PANEL - 25 mg Tablet Bottle Label NDC 45802- 150 -65 Rx Only Alogliptin Tablets 25 mg DISPENSE WITH MEDICATION GUIDE 30 Tablets Padagis ® PRINCIPAL DISPLAY PANEL - 25 mg Tablet Bottle Label