Linagliptin API Manufacturers & Suppliers
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Linagliptin | CAS No: 668270-12-0 | GMP-certified suppliers
A medication that supports improved glycemic control in adults with type 2 diabetes when used alongside diet and exercise, including use within combination treatment regimens.
Therapeutic categories
Primary indications
- Linagliptin is indicated for the treatment of type II diabetes in addition to diet and exercise
- It should not be used to treat type I diabetes or in diabetic ketoacidosis
- An extended-release combination product containing empagliflozin, linagliptin, and metformin was approved by the FDA in January 2020 for the improvement of glycemic control in adults with type 2 diabetes mellitus when used adjunctively with diet and exercise
Product Snapshot
- Linagliptin is an oral small‑molecule API supplied mainly as film‑coated or extended‑release tablets
- It is used for glycemic control in adults with type 2 diabetes as an adjunct to diet and exercise, including use in approved combination products
- The drug is approved in major regulated markets including the US, Canada, and the EU
Clinical Overview
Linagliptin is a competitive, reversible DPP‑4 inhibitor that slows enzymatic degradation of glucagon‑like peptide 1 and glucose‑dependent insulinotropic polypeptide. Increased concentrations of these incretin hormones enhance glucose‑dependent insulin secretion and suppress glucagon release, reducing hepatic glycogenolysis and improving postprandial and fasting glycemia. A single 5 mg oral dose produces greater than 80 percent DPP‑4 inhibition for at least 24 hours, supporting once‑daily dosing.
The compound exhibits a non‑linear pharmacokinetic profile with concentration‑dependent protein binding. Absorption is oral, and unlike several other DPP‑4 inhibitors, clearance is not primarily renal, an important consideration for patients with impaired kidney function. Linagliptin is a substrate and inhibitor of CYP3A and P‑glycoprotein transport pathways, so potential interactions should be evaluated when coadministered with agents affecting these systems. It also interacts with organic cation transporters. Elimination occurs mainly via biliary and intestinal routes.
Safety considerations include reports of hypersensitivity reactions, angioedema, pancreatitis, and joint pain within the class. Hypoglycemia risk increases when combined with insulin or insulin secretagogues. Linagliptin is generally weight neutral and has not demonstrated a dose‑dependent effect on QT intervals in available clinical data.
Commercially, linagliptin is marketed in various regions under products such as Tradjenta or as part of combination regimens, though brand names vary globally.
For API procurement, sourcing should prioritize suppliers with demonstrated control of stereochemistry, impurity profiles, and particle size distribution, along with full regulatory documentation to support global registration and finished product manufacturing.
Identification & chemistry
| Generic name | Linagliptin |
|---|---|
| Molecule type | Small molecule |
| CAS | 668270-12-0 |
| UNII | 3X29ZEJ4R2 |
| DrugBank ID | DB08882 |
Pharmacology
| Summary | Linagliptin is a competitive, reversible DPP‑4 inhibitor that slows degradation of the incretin hormones GLP‑1 and GIP. By preserving these peptides, it enhances glucose‑dependent insulin secretion and suppresses glucagon release, supporting reduced hepatic glucose output. Its sustained DPP‑4 inhibition leads to increased incretin activity and corresponding improvements in key glycemic biomarkers. |
|---|---|
| Mechanism of action | Linagliptin is a competitive, reversible DPP-4 inhibitor. Inhibition of this enzyme slows the breakdown of GLP-1 and glucose-dependant insulinotropic polypeptide (GIP). GLP-1 and GIP stimulate the release of insulin from beta cells in the pancreas while inhibiting release of glucagon from pancreatic beta cells. These effects together reduce the breakdown of glycogen in the liver and increase insulin release in response to glucose. |
| Pharmacodynamics | A 5mg oral dose of linagliptin results in >80% inhibition of dipeptidyl peptidase 4 (DPP-4) for ≥24 hours. Inhibition of DPP-4 increases the concentration of glucagon-like peptide 1 (GLP-1), leading to decreased glycosylated hemoglobin and fasting plasma glucose. |
Targets
| Target | Organism | Actions |
|---|---|---|
| Dipeptidyl peptidase 4 | Humans | inhibitor |
ADME / PK
| Absorption | Oral bioavailability of linagliptin is 30%. |
|---|---|
| Half-life | The terminal half life of linagliptin is 155 hours. |
| Protein binding | Linagliptin is 99% protein bound at a concentration of 1nmol/L and 75-89% protein bound at a concentration of >30nmol/L. |
| Metabolism | An oral dose of linagliptin is excreted primarily in the feces. 90% of an oral dose is excreted unchanged in the urine and feces. The predominant metabolite in the plasma is CD1790 and the predominant metabolite recovered after excretion was M489(1). Other metabolites are produced through oxidation, oxidative degradation, N-acetylation, glucuronidation, and cysteine adduct formation. Other metabolites have been identified through mass spectrometry though no structures were determined. Metabolism of linagliptin is mediated by cytochrome P450 3A4, aldo-keto reductases, and carbonyl reductases. |
| Route of elimination | 84.7% of linagliptin is eliminated in the feces and 5.4% is eliminated in the urine. |
| Volume of distribution | A single intravenous dose of 5mg results in a volume of distribution of 1110L. However an intravenous infusion of 0.5-10mg results in a volume of distribution of 380-1540L. |
| Clearance | Total clearance of linagliptin is 374mL/min. |
Formulation & handling
- Oral small‑molecule xanthine derivative with low aqueous solubility, favoring solid oral tablet formulations and potentially requiring solubility‑enhancing excipients.
- Stable for conventional solid‑dose processing; not a peptide or biologic and does not require special handling beyond standard small‑molecule controls.
- Food effects are minimal, though high‑fat meals alter absorption parameters without clinically meaningful impact, allowing flexible administration.
Regulatory status
| Lifecycle | Most Canadian and several U.S. patents have already expired, with one remaining U.S. patent scheduled to lapse in late 2025. With products marketed in the US, Canada, and the EU, the API is transitioning toward a mature, largely post‑patent market. |
|---|
| Markets | US, Canada, EU |
|---|
Supply Chain
| Supply chain summary | Linagliptin is supplied by a single originator manufacturer, with branded combination products such as those marketed in the US, Canada, and the EU. Commercial presence is well established across these major markets. Multiple patents have already expired in the US and Canada, and the remaining US protection ends in late 2025, indicating that generic manufacturing pathways are already open in some regions and likely to broaden as remaining exclusivities lapse. |
|---|
Safety
| Toxicity | No dosage adjustment is necessary based on race, age, weight, sex, renal impairment, or hepatic impairment. Studies of efficacy and safety in pediatric populations were not included in the original drug approvalbut recent clinical trials show linagliptin to be well tolerated in patients 10 to 18 years old. Animal studies showed an increased risk of lymphoma in female rats at over 200 times the clinical dose. Aside from this effect, linagliptin was not shown to be mutagenic, clastogenic, or have an effect on fertility. |
|---|
- No clinically relevant toxicity differences were observed across demographic or organ‑function subgroups
- Pediatric safety data remain limited despite recent tolerability findings in adolescents
- High‑dose animal studies identified lymphoma incidence in female rats at exposures ›200× human levels
Linagliptin is a type of DPP4-Inhibitors
DPP4-Inhibitors, or dipeptidyl peptidase-4 inhibitors, belong to the subcategory of pharmaceutical active ingredients known for their therapeutic role in managing type 2 diabetes mellitus. These inhibitors work by targeting and inhibiting the action of the enzyme dipeptidyl peptidase-4 (DPP4) in the body.
DPP4 is responsible for breaking down incretin hormones, such as glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic polypeptide (GIP). By inhibiting DPP4, DPP4-Inhibitors enhance the levels and activity of these hormones. GLP-1 and GIP play crucial roles in regulating blood sugar levels by stimulating insulin release, inhibiting glucagon secretion, and slowing down gastric emptying.
The main advantage of DPP4-Inhibitors is their ability to improve glycemic control without the risk of hypoglycemia, which is a common side effect of some other diabetes medications. They are typically used as an adjunct therapy in combination with other antidiabetic agents, such as metformin, to achieve optimal glucose management.
Commonly prescribed DPP4-Inhibitors include sitagliptin, saxagliptin, linagliptin, and alogliptin. These drugs are available in oral tablet formulations, allowing for convenient administration. They have shown efficacy in lowering HbA1c levels and have a favorable safety profile.
It is important to note that DPP4-Inhibitors are not suitable for individuals with type 1 diabetes or those with a history of pancreatitis. As with any medication, there may be potential side effects, such as upper respiratory tract infections, headache, and gastrointestinal discomfort, which should be discussed with a healthcare professional.
In conclusion, DPP4-Inhibitors are a subcategory of pharmaceutical APIs that act by inhibiting the enzyme DPP4, thereby enhancing the effects of incretin hormones involved in glucose regulation. They are widely used in the management of type 2 diabetes mellitus, offering glycemic control benefits with a reduced risk of hypoglycemia.
Linagliptin (DPP4-Inhibitors), classified under Anti-diabetics
Anti-diabetics, belonging to the pharmaceutical API (Active Pharmaceutical Ingredient) category, are a group of compounds designed to manage and treat diabetes mellitus, a chronic metabolic disorder characterized by high blood sugar levels. These medications play a vital role in controlling diabetes and preventing complications associated with the disease.
Anti-diabetics encompass a wide range of drug classes, including biguanides, sulfonylureas, thiazolidinediones, dipeptidyl peptidase-4 (DPP-4) inhibitors, sodium-glucose cotransporter-2 (SGLT2) inhibitors, and glucagon-like peptide-1 (GLP-1) receptor agonists. Each class works through different mechanisms to regulate blood sugar levels and improve insulin sensitivity.
Biguanides, such as metformin, reduce glucose production by the liver and enhance insulin sensitivity in peripheral tissues. Sulfonylureas, like glipizide, stimulate insulin secretion from pancreatic beta cells. Thiazolidinediones, including pioglitazone, improve insulin sensitivity in muscle and adipose tissues. DPP-4 inhibitors, such as sitagliptin, increase insulin release and inhibit glucagon secretion. SGLT2 inhibitors, like dapagliflozin, decrease renal glucose reabsorption, leading to increased urinary glucose excretion. GLP-1 receptor agonists, such as exenatide, enhance insulin secretion, suppress glucagon release, slow gastric emptying, and promote satiety.
These anti-diabetic APIs serve as the foundational ingredients for the formulation of various oral tablets, capsules, and injectable medications used in the treatment of diabetes. By targeting different aspects of glucose regulation, they help patients achieve and maintain optimal blood sugar levels, thus reducing the risk of diabetic complications, such as cardiovascular disease, neuropathy, and nephropathy.
It is crucial for healthcare professionals to prescribe and administer these anti-diabetic medications appropriately, considering factors like the patient's medical history, co-existing conditions, and potential drug interactions. Regular monitoring of blood glucose levels and close medical supervision are necessary to ensure effective diabetes management.
In conclusion, anti-diabetics form a critical category of pharmaceutical APIs used for the treatment of diabetes. These compounds, encompassing various drug classes, work through distinct mechanisms to regulate blood sugar levels and improve insulin sensitivity. By facilitating glucose control, anti-diabetic APIs help mitigate the risk of complications associated with diabetes mellitus, ultimately promoting better health outcomes for patients.
Linagliptin API manufacturers & distributors
Compare qualified Linagliptin API suppliers worldwide. We currently have 28 companies offering Linagliptin API, with manufacturing taking place in 10 different countries. Use the table below to review supplier type, countries of origin, certifications, product portfolio and GMP audit availability.
| Supplier | Type | Country | Product origin | Certifications | Portfolio |
|---|---|---|---|---|---|
| ACE Japan | Producer | Japan | Japan | CoA | 76 products |
| AXXO GmbH | Distributor | Germany | World | CoA, GMP, GDP, MSDS, USDMF | 243 products |
| Bakul Pharma Private Limi... | Producer | India | India | BSE/TSE, CoA, FDA, GMP, MSDS | 52 products |
| Beijing Huikang Boyuan | Producer | China | China | CoA, USDMF | 10 products |
| Bidachem | Producer | Italy | Italy | CoA, GMP | 14 products |
| Boehringer Ingelheim | Producer | Germany | Germany | CoA, GMP | 35 products |
| Chengdu Firster Pharmaceu... | Producer | China | China | CoA | 2 products |
| Dr. Reddy's | Producer | India | India | BSE/TSE, CoA, EDMF/ASMF, FDA, GMP, KDMF, MSDS, USDMF, WC | 170 products |
| Emeishan Hongsen Biopharm... | Producer | China | China | CoA, MSDS | 107 products |
| Fuxing Long Rui Pharma | Producer | China | China | CoA, USDMF | 10 products |
| Global Pharma Tek | Distributor | India | India | BSE/TSE, CoA, FDA, GMP, ISO9001, MSDS | 484 products |
| HEC Pharm | Producer | Germany | Unknown | CoA, USDMF | 31 products |
| Honour Lab | Producer | India | India | CoA, GMP, USDMF, WC | 30 products |
| Morepen Laboratories Ltd. | Producer | India | India | BSE/TSE, CoA, EDMF/ASMF, FDA, GMP, ISO9001, MSDS, USDMF, WC | 22 products |
| MSN Pharma | Producer | India | India | CoA, GMP, USDMF, WC | 31 products |
| Mylan | Producer | India | India | CoA, GMP, USDMF, WC | 201 products |
| Polpharma | Producer | Poland | Poland | BSE/TSE, CoA, EDMF/ASMF, FDA, GMP, KDMF, MSDS, USDMF | 64 products |
| Rochem International, Inc... | Distributor | United States | United States | BSE/TSE, CoA, GMP, ISO9001, MSDS | 144 products |
| SETV Global | Producer | India | India | CoA, FDA, GMP | 515 products |
| Shanghai Wonder Pharma | Producer | China | China | CoA, USDMF | 5 products |
| Shaoxing Hantai Pharma | Distributor | China | China | CoA | 162 products |
| Sinoway industrial Co.,Lt... | Distributor | China | China | CoA, GMP, ISO9001, MSDS, USDMF | 757 products |
| Solfyn International LLP | Distributor | India | China | BSE/TSE, CoA, GMP, ISO9001, USDMF, WHO-GMP | 24 products |
| Sun Pharma | Producer | India | India | CoA, USDMF | 219 products |
| Tenatra Exports Private L... | Distributor | India | India | BSE/TSE, CoA, FDA, GMP, MSDS | 263 products |
| Vonage Pharma (Former Plu... | Producer | Turkey | Turkey | CoA, GMP, MSDS, USDMF, WC | 28 products |
| Wisdom Pharma | Producer | China | China | CoA, USDMF | 12 products |
| Yangtze River Pharmaceuti... | Producer | China | China | CoA, FDA, GMP, ISO14001 | 34 products |
When sending a request, specify which Linagliptin API quality you need: for example EP (Ph. Eur.), USP, JP, BP, or another pharmacopoeial standard, as well as the required grade (base, salt, micronised, specific purity, etc.).
Use the list above to find high-quality Linagliptin API suppliers. For example, you can select GMP, FDA or ISO certified suppliers. Visit our help page to learn more about sourcing APIs via Pharmaoffer.
