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Gliquidone | CAS No: 33342-05-1 | GMP-certified suppliers
A medication that supports glycemic control in type 2 diabetes patients by stimulating insulin secretion and enhancing peripheral insulin sensitivity.
Therapeutic categories
Primary indications
- Used in the treatment of diabetes mellitus type 2
Product Snapshot
- Gliquidone is an oral small molecule formulated as a tablet
- It is primarily used for the management of type 2 diabetes mellitus
- The API holds approved and investigational status in key regulatory markets
Clinical Overview
Pharmacodynamically, gliquidone lowers blood glucose levels by stimulating insulin release from the pancreatic beta cells. The drug binds to ATP-sensitive potassium (KATP) channels on the cell membrane, inhibiting potassium efflux. This inhibition leads to cellular depolarization, triggering the opening of voltage-dependent calcium channels. The resultant calcium influx promotes exocytosis of insulin-containing granules. Additionally, gliquidone may enhance peripheral tissue sensitivity to insulin, further facilitating glucose uptake.
Chemically, gliquidone belongs to the 1,3-isoquinolinedione class of compounds, characterized by an isoquinoline scaffold with carbonyl groups at positions 1 and 3. As a sulfonylurea derivative, it acts as an insulin secretagogue.
Key absorption, distribution, metabolism, and excretion (ADME) properties should be considered during drug development and clinical use. Gliquidone is extensively metabolized in the liver, primarily via cytochrome P450 enzymes including CYP2C9, which can affect its plasma levels and pharmacokinetics. The metabolites are excreted predominantly via the biliary route, minimizing renal clearance concerns compared to other agents in this class.
Safety and toxicity considerations include the potential for hypoglycemia, particularly in patients with hepatic or renal impairment. Caution is advised when gliquidone is co-administered with other CYP2C9 substrates or inhibitors, due to possible drug interactions. Monitoring for adverse effects such as gastrointestinal disturbances and allergic reactions is recommended.
Gliquidone has been marketed in several regions under various trade names, primarily for type 2 diabetes management. Regulatory approvals vary by country, reflecting regional clinical use patterns.
From an API sourcing and quality perspective, manufacturers should ensure compliance with international pharmacopeial standards, confirm purity, and control impurities specific to sulfonylurea synthesis. Stability and consistent potency are critical for therapeutic efficacy and safety. Due diligence on supplier certifications, batch-to-batch consistency, and regulatory compliance is essential for pharmaceutical formulation and manufacturing.
Identification & chemistry
| Generic name | Gliquidone |
|---|---|
| Molecule type | Small molecule |
| CAS | 33342-05-1 |
| UNII | C7C2QDD75P |
| DrugBank ID | DB01251 |
Pharmacology
| Summary | Gliquidone is a sulfonylurea-class antidiabetic agent indicated for type 2 diabetes mellitus. It lowers blood glucose by binding to ATP-sensitive potassium channels on pancreatic beta cells, causing membrane depolarization and subsequent insulin release. Additionally, it enhances peripheral tissue sensitivity to insulin, promoting glucose uptake. |
|---|---|
| Mechanism of action | The mechanism of action of gliquidone in lowering blood glucose appears to be dependent on stimulating the release of insulin from functioning pancreatic beta cells, and increasing sensitivity of peripheral tissues to insulin. Gliquidone likely binds to ATP-sensitive potassium channel receptors on the pancreatic cell surface, reducing potassium conductance and causing depolarization of the membrane. Membrane depolarization stimulates calcium ion influx through voltage-sensitive calcium channels. This increase in intracellular calcium ion concentration induces the secretion of insulin. |
| Pharmacodynamics | Gliquidone is an anti-diabetic drug in the sulfonylurea class. In patients with diabetes mellitus, there is a deficiency or absence of a hormone manufactured by the pancreas called insulin. Insulin is the main hormone responsible for the control of sugar in the blood. Gliquidone is an antidiabetic medication which is used in those patients with adult maturity onset or non-insulin dependent diabetes (NIDDM). It works by lowering blood sugar levels by stimulating the production and release of insulin from the pancreas. It also promotes the movement of sugar from the blood into the cells in the body which need it. |
Targets
| Target | Organism | Actions |
|---|---|---|
| ATP-binding cassette sub-family C member 8 | Humans | inhibitor |
| ATP-sensitive inward rectifier potassium channel 8 | Humans | inhibitor |
ADME / PK
| Half-life | The mean terminal half-life was approximately 8 hours (range 5.7-9.4 hours) |
|---|
Formulation & handling
- Gliquidone is an oral small molecule formulation primarily developed as a tablet.
- It has low water solubility, indicating potential challenges in formulation dissolution and bioavailability.
- Stability and handling considerations should address its moderately high lipophilicity (LogP 4.14) and solid state to maintain potency.
Regulatory status
Gliquidone is a type of Sulfonylureas
Sulfonylureas belong to a subcategory of pharmaceutical active ingredients known as antidiabetic agents. These compounds play a crucial role in managing type 2 diabetes, a metabolic disorder characterized by high blood sugar levels. Sulfonylureas work by stimulating the pancreas to produce more insulin, a hormone responsible for regulating blood glucose levels.
As pharmaceutical API, sulfonylureas are highly effective in lowering blood sugar levels by promoting insulin secretion and increasing the sensitivity of cells to insulin. This mechanism of action makes them valuable in the treatment of type 2 diabetes, especially when other measures such as diet and exercise have proven inadequate.
Sulfonylureas are widely prescribed due to their proven efficacy, oral administration convenience, and cost-effectiveness. They are available in various formulations, including tablets and extended-release formulations, allowing flexibility in dosing regimens. Additionally, their long-established presence in the market has resulted in a comprehensive understanding of their safety profile and potential side effects.
Some common sulfonylurea drugs include glipizide, glimepiride, and gliclazide. These compounds are often prescribed as part of a comprehensive treatment plan for type 2 diabetes, along with lifestyle modifications and other antidiabetic medications.
It is important to note that the use of sulfonylureas should be carefully monitored by healthcare professionals to ensure optimal blood sugar control and to minimize the risk of hypoglycemia, a potential side effect. Patients taking sulfonylureas should also be educated about the importance of regular blood glucose monitoring and adhering to prescribed dosages.
In conclusion, sulfonylureas represent an essential subcategory of pharmaceutical APIs used in the treatment of type 2 diabetes. Their mechanism of action, proven efficacy, and cost-effectiveness make them a valuable tool in managing this chronic metabolic condition. Healthcare professionals play a vital role in guiding the appropriate use of sulfonylureas to optimize patient outcomes and ensure safety.
Gliquidone (Sulfonylureas), 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.
Gliquidone API manufacturers & distributors
Compare qualified Gliquidone API suppliers worldwide. We currently have 2 companies offering Gliquidone 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 |
|---|---|---|---|---|---|
| AGC Pharma Chemicals | Distributor | Spain | Spain | CoA, GMP | 4 products |
| ICROM | Producer | Italy | Italy | CoA, GMP, USDMF | 19 products |
When sending a request, specify which Gliquidone 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.).
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