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Ertugliflozin | CAS No: 1210344-57-2 | GMP-certified suppliers
A medication that supports improved glycemic control in adults with type 2 diabetes, serving as an adjunct to lifestyle measures across major regulated markets.
Therapeutic categories
Primary indications
- Ertugliflozin is indicated as an adjunct to diet and exercise to improve glycemic control in adult patients with type 2 diabetes mellitus (T2DM)
- It is also available in combination with either [metformin] or [sitagliptin]
- Ertugliflozin is not recommended for use to improve glycemic control in patients with type 1 diabetes mellitus
Product Snapshot
- Ertugliflozin is an oral small‑molecule API supplied as film‑coated tablets
- It is used as an adjunct therapy to support glycemic control in adults with type 2 diabetes
- It is approved in the US, EU, and Canada, with some investigational status noted for certain uses or combinations
Clinical Overview
The compound is a diphenylmethane derivative and exhibits selective inhibition of SGLT2 located in the proximal renal tubules. By blocking SGLT2, ertugliflozin reduces renal reabsorption of filtered glucose, lowers the renal threshold for glycosuria, and promotes urinary glucose excretion. These effects are dose dependent and are accompanied by increased urinary volume.
Pharmacodynamically, the glucose‑lowering response is independent of pancreatic beta‑cell function and does not directly induce insulin secretion. The renal mechanism remains active across a range of blood glucose concentrations, contributing to reductions in fasting and postprandial glucose.
Absorption and distribution parameters for ertugliflozin support once‑daily oral dosing. Metabolism occurs mainly via glucuronidation pathways involving UGT1A9 and UGT2B7, with additional contributions from UGT1A1 and UGT1A4. The molecule is also a substrate of P‑glycoprotein and BCRP transporters, which may influence disposition and drug–drug interaction potential. Elimination occurs through both renal and fecal pathways.
Safety considerations include risks associated with osmotic diuresis, volume depletion, and increased urinary glucose, which may predispose to genital mycotic infections. SGLT2 inhibitors have also been associated with rare events such as ketoacidosis and impaired renal function, and these risks require assessment in susceptible individuals.
In market practice, ertugliflozin is supplied as single‑agent tablets and as combination products. For API procurement, sourcing should prioritize manufacturers with validated control of stereochemistry, impurity profiles aligned with regulatory expectations, and reliable documentation to support global dossier submissions.
Identification & chemistry
| Generic name | Ertugliflozin |
|---|---|
| Molecule type | Small molecule |
| CAS | 1210344-57-2 |
| UNII | 6C282481IP |
| DrugBank ID | DB11827 |
Pharmacology
| Summary | Ertugliflozin inhibits the renal sodium‑glucose cotransporter 2, reducing glucose reabsorption in the proximal tubule and lowering the threshold for urinary glucose excretion. This action increases glucose elimination through urine and produces associated osmotic diuresis. Its therapeutic intent is to support glycemic control in adults with type 2 diabetes. |
|---|---|
| Mechanism of action | Kidneys play an integral role in glucose homeostasis. After being filtered into urine within the nephron, most of the plasma glucose is reabsorbed through two types of sodium-dependent glucose cotransporters (SGLTs), SGLT1 and SGLT2, expressed in proximal renal tubules.More specifically, SGLT2 is responsible for 80–90% of renal glucose reabsorption while SGLT1 is responsible for the remaining 10-20%.Under physiological conditions, less than one percent of glucose is excreted in urine.In the case of hyperglycemia, SGLTs become saturated and the renal threshold for urinary glucose excretion is increased. Kidneys respond to an elevated threshold for glycosuria by elevating glucose reabsorption and increasing maximum glucose reabsorptive capacity. Ertugliflozin is an inhibitor of SGLT2 that reduces renal reabsorption of filtered glucose and lowers the renal threshold for glucose, thereby increasing urinary glucose excretion. |
| Pharmacodynamics | Ertugliflozin causes a dose-dependent increase in urinary glucose excretion and an increase in urinary volume in patients with T2DM. |
Targets
| Target | Organism | Actions |
|---|---|---|
| Sodium/glucose cotransporter 2 | Humans | inhibitor |
ADME / PK
| Absorption | After administering single doses of 5 mg and 15 mg ertugliflozin under fasted conditions, the median T<sub>max</sub> was one hour. Plasma C<sub>max</sub> and AUC of ertugliflozin increase dose-proportionally.Following administration of a 15 mg dose, the C<sub>max</sub> was 268 ng/mL and the AUC was 1193 ng h/mL.The absolute oral bioavailability of ertugliflozin following administration of a 15 mg dose was approximately 100%,though it is reported to range from 70% to 90%. Administration of ertugliflozin with a high-fat and high-calorie meal decreases ertugliflozin C<sub>max</sub> by 29%. It prolongs T<sub>max</sub> by one hour but does not alter AUC compared to the fasted state. The observed effect of food on ertugliflozin pharmacokinetics is not considered clinically relevant, and ertugliflozin may be administered with or without food. |
|---|---|
| Half-life | The terminal elimination half-life of ertugliflozin ranges from 11 to 17 hours.The mean elimination half-life in T2DM patients with normal renal function was estimated to be 16.6 hours based on the population pharmacokinetic analysis. |
| Protein binding | Ertugliflozin is 93.6% bound to plasma proteins. Plasma protein binding is independent of ertugliflozin plasma concentrations and is not meaningfully altered in patients with renal or hepatic impairment. The blood-to-plasma concentration ratio of ertugliflozin is 0.66. |
| Metabolism | Ertugliflozin mainly undergoes O-glucuronidation mediated by UGT1A9 and UGT2B7 to form two pharmacologically inactive glucuronides. About 12% of the drug undergoes CYP-mediated oxidative metabolism.Several metabolites have been found in plasma, feces, and urine. In plasma, the unchanged form of ertugliflozin was found to be the major component of the administered dose. |
| Route of elimination | Following administration of an oral [<sup>14</sup>C]-ertugliflozin solution to healthy subjects, approximately 40.9% and 50.2% of the drug-related radioactivity was eliminated in feces and urine, respectively. Only 1.5% of the administered dose was excreted as unchanged ertugliflozin in urine and 33.8% as unchanged ertugliflozin in feces, which is likely due to biliary excretion of glucuronide metabolites and subsequent hydrolysis to form the parent compound. |
| Volume of distribution | The volume of distribution following oral administration was 215.3 L.The mean steady-state volume of distribution of ertugliflozin following an intravenous dose is 85.5 L. |
| Clearance | The apparent total plasma clearance rate after a single dose administration of 15 mg ertugliflozin is 178.7 mL/min.The mean systemic plasma clearance following an intravenous 100 µg dose was 11.2 L/hr. |
Formulation & handling
- Oral small‑molecule API typically formulated as film‑coated tablets, with low aqueous solubility requiring solubility‑enhancing excipients for consistent dissolution.
- Moderate lipophilicity and solid‑state stability support conventional oral solid‑dose manufacturing without special biologic handling requirements.
- Food has minimal impact on pharmacokinetics, allowing flexible administration timing from a formulation standpoint.
Regulatory status
| Lifecycle | The API is in a mature phase in the EU and Canada, with key U.S. patent protections largely expired except for one extending to 2027. Market dynamics reflect partial loss of exclusivity in the United States alongside established availability across major regulated markets. |
|---|
| Markets | EU, US, Canada |
|---|
Supply Chain
| Supply chain summary | Ertugliflozin is supplied by a single originator developer, with branded products marketed in the United States, European Union, and Canada. The molecule has an established global branded presence, primarily in fixed‑dose combinations. Multiple U.S. patents have already expired, with the final listed protection ending in 2027, indicating that generic entry is underway or expected in the near term. |
|---|
Safety
| Toxicity | The oral LD<sub>50</sub> is 500 mg/kg in rats.There are limited clinical experiences of ertugliflozin overdose. It is recommended to initiate supportive measures in the event of drug overdosage. Removal of ertugliflozin by hemodialysis has not been studied. |
|---|
- Oral LD50 in rats is approximately 500 mg/kg, indicating moderate acute toxicity in preclinical models
- Clinical data on ertugliflozin overdose are limited
- Pharmacokinetic behavior and elimination pathways under supratherapeutic exposure remain insufficiently characterized
Ertugliflozin is a type of SGLT2-inhibitors
SGLT2 inhibitors, short for Sodium-Glucose Co-Transporter 2 inhibitors, belong to the pharmaceutical API subcategory utilized in the treatment of type 2 diabetes mellitus (T2DM). These innovative drugs target the SGLT2 protein responsible for reabsorbing glucose in the kidneys, resulting in increased urinary glucose excretion.
By inhibiting SGLT2, these drugs effectively lower blood glucose levels and improve glycemic control in patients with T2DM. This mechanism of action is independent of insulin secretion or sensitivity, making SGLT2 inhibitors an attractive option for individuals who are resistant to or cannot tolerate other diabetes medications.
Some commonly prescribed SGLT2 inhibitors include canagliflozin, dapagliflozin, and empagliflozin. These pharmaceutical APIs are typically formulated into oral tablets, making them convenient for patient administration.
Clinical studies have demonstrated the effectiveness of SGLT2 inhibitors in reducing HbA1c levels, body weight, and blood pressure in patients with T2DM. Additionally, these medications have shown potential cardiovascular benefits, including a decreased risk of cardiovascular events.
However, it is important to note that SGLT2 inhibitors are not suitable for everyone, and their use should be carefully considered in patients with renal impairment or a history of ketoacidosis. Adverse effects may include genitourinary infections and increased risk of dehydration.
Overall, SGLT2 inhibitors are a promising class of pharmaceutical APIs that offer an innovative approach to managing T2DM by targeting renal glucose reabsorption. Ongoing research and development in this field aim to further optimize the therapeutic potential of SGLT2 inhibitors and improve patient outcomes.
Ertugliflozin (SGLT2-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.
Ertugliflozin API manufacturers & distributors
Compare qualified Ertugliflozin API suppliers worldwide. We currently have 2 companies offering Ertugliflozin API, with manufacturing taking place in 2 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 |
|---|---|---|---|---|---|
| Apino Pharma Co., Ltd. | Producer | China | China | BSE/TSE, CoA, GMP, MSDS | 229 products |
| Morepen Laboratories Ltd. | Producer | India | India | BSE/TSE, CoA, EDMF/ASMF, FDA, GMP, ISO9001, MSDS, USDMF | 22 products |
When sending a request, specify which Ertugliflozin 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 Ertugliflozin 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.
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