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Eprosartan | CAS No: 133040-01-4 | GMP-certified suppliers
A medication that supports effective management of hypertension and provides therapeutic options for diabetic nephropathy and ACE‑inhibitor‑intolerant congestive heart failure in clinical use.
Therapeutic categories
Primary indications
- For the management of hypertension alone or in combination with other classes of antihypertensive agents
- Also used as a first-line agent in the treatment of diabetic nephropathy, as well as a second-line agent in the treatment of congestive heart failure (only in those intolerant of ACE inhibitors)
Product Snapshot
- Oral small‑molecule API supplied primarily as tablet and film‑coated tablet formulations
- Used for hypertension management and for renal and cardiac comorbidity settings such as diabetic nephropathy and ACE‑inhibitor–intolerant congestive heart failure
- Approved in the US and Canada for relevant antihypertensive indications
Clinical Overview
Eprosartan is a benzoic acid derivative that acts within the renin–angiotensin system. Angiotensin II is a principal effector peptide responsible for vasoconstriction, aldosterone stimulation, sodium retention, and sympathetic activation. Eprosartan competitively and reversibly blocks binding of angiotensin II at AT1 receptors located in vascular smooth muscle and the adrenal cortex. This blockade reduces vasoconstriction, aldosterone secretion, and vasopressin release, collectively lowering systemic blood pressure.
The compound shows high selectivity for AT1 receptors, with affinity several orders of magnitude greater than for AT2 receptors. It has no intrinsic agonist activity at AT1. Eprosartan also binds to presynaptic AT1 receptors, inhibiting sympathetically mediated norepinephrine release, which contributes to additional blood pressure reduction. Because it does not inhibit bradykinin metabolism, it does not produce bradykinin‑related adverse effects associated with ACE inhibitors.
Absorption is variable and food may influence bioavailability, though the clinical impact is limited. Eprosartan is minimally metabolized and is eliminated largely unchanged via biliary and renal pathways. The elimination half-life is moderate and supports once‑ or twice‑daily dosing depending on formulation. Protein binding is high.
Safety considerations include the risk of hypotension, renal function changes, hyperkalemia, and rare angioedema. Use during pregnancy is contraindicated due to known risks associated with renin–angiotensin system blockade. Concomitant use with potassium-sparing agents or potassium supplements requires caution.
For API procurement, sourcing should prioritize compliance with pharmacopoeial specifications, validated impurity controls, and supply chain transparency to ensure consistent quality for formulation development and regulatory submissions.
Identification & chemistry
| Generic name | Eprosartan |
|---|---|
| Molecule type | Small molecule |
| CAS | 133040-01-4 |
| UNII | 2KH13Z0S0Y |
| DrugBank ID | DB00876 |
Pharmacology
| Summary | Eprosartan is an angiotensin II type‑1 (AT1) receptor antagonist that selectively and competitively blocks angiotensin II signaling in vascular and adrenal tissues. This inhibition reduces vasoconstriction, sympathetic noradrenaline release, and aldosterone-driven sodium retention. The resulting pharmacodynamic effect is decreased peripheral resistance and lowered blood pressure. |
|---|---|
| Mechanism of action | Eprosartan blocks the vasoconstrictor and aldosterone-secreting effects of angiotensin II by selectively blocking the binding of angiotensin II to the AT<sub>1</sub> receptor found in many tissues (e.g., vascular smooth muscle, adrenal gland). There is also an AT<sub>2</sub> receptor found in many tissues but it is not known to be associated with cardiovascular homeostasis. Eprosartan does not exhibit any partial agonist activity at the AT<sub>1</sub> receptor. Its affinity for the AT<sub>1</sub> receptor is 1,000 times greater than for the AT<sub>2</sub> receptor. In vitro binding studies indicate that eprosartan is a reversible, competitive inhibitor of the AT<sub>1</sub> receptor. Eprosartan has also been shown to bind to AT<sub>1</sub> receptors both presynaptically and synaptically. Its action on presynaptic AT<sub>1</sub> receptors results in the inhibition of sympathetically stimulated noradrenaline release. Unlike ACE inhibitors, eprosartan and other ARBs do not interfere with response to bradykinins and substance P, which allows for the absence of adverse effects that are present in ACE inhibitors (eg. dry cough). |
| Pharmacodynamics | Angiotensin II, the principal pressor agent of the renin-angiotensin system, is formed from angiotensin I in a reaction catalyzed by angiotensin-converting enzyme [kininase II]. It is responsible for effects such as vasoconstriction, stimulation of synthesis and release of aldosterone, cardiac stimulation, and renal reabsorption of sodium. Eprosartan selectively blocks the binding of angiotensin II to the AT<sub>1</sub> receptor, which in turn leads to multiple effects including vasodilation, a reduction in the secretion of vasopressin, and reduction in the production and secretion of aldosterone. The resulting effect is a decrease in blood pressure. |
Targets
| Target | Organism | Actions |
|---|---|---|
| Type-1 angiotensin II receptor | Humans | antagonist |
ADME / PK
| Absorption | Absolute bioavailability following a single 300 mg oral dose of eprosartan is approximately 13%. Administering eprosartan with food delays absorption. |
|---|---|
| Half-life | The terminal elimination half-life of eprosartan following oral administration is typically 5 to 9 hours. |
| Protein binding | Plasma protein binding of eprosartan is high (approximately 98%) and constant over the concentration range achieved with therapeutic doses. |
| Metabolism | Eprosartan is not metabolized by the cytochrome P450 system. It is mainly eliminated as unchanged drug. Less than 2% of an oral dose is excreted in the urine as a glucuronide. |
Formulation & handling
- Oral small‑molecule API with very low aqueous solubility, typically requiring solid‑state or solubility‑enhancing strategies for tablet formulation.
- Stable for standard solid‑dose processing; film coating may be used to aid manufacturability and handling rather than food‑related protection.
- Absorption not affected by food, allowing flexible administration without additional formulation controls for food effects.
Regulatory status
| Lifecycle | The active ingredient’s core patents in the United States and Canada expired between 2010 and 2017, indicating a fully mature lifecycle. With products marketed in both countries, the API is likely subject to established generic competition. |
|---|
| Markets | US, Canada |
|---|
Supply Chain
| Supply chain summary | Eprosartan appears to be supplied primarily by a small set of originator and affiliated companies, with Abbott and Solvay linked to both manufacturing and packaging activities. Branded products are established in the US and Canada, with no indication of broader global distribution in the provided data. All listed US and Canadian patents have expired, indicating that generic competition is already possible where regulatory pathways are available. |
|---|
Safety
| Toxicity | There was no mortality in rats and mice receiving oral doses of up to 3000 mg eprosartan/kg and in dogs receiving oral doses of up to 1000 mg eprosartan/kg. |
|---|
- High oral exposure margins observed in rodents (≤3000 mg/kg) and dogs (≤1000 mg/kg) without mortality, indicating low acute toxicity under test conditions
- Standard industrial handling should consider potential class‑related effects of angiotensin II receptor antagonists, including hemodynamic activity, when managing bulk material
- Controls for dust generation and ingestion pathways are recommended due to high-dose toxicology data being limited to controlled animal studies
Eprosartan is a type of Angiotensin Receptor Blockers
Angiotensin Receptor Blockers (ARBs) are a vital subcategory of pharmaceutical Active Pharmaceutical Ingredients (APIs) commonly used in the treatment of hypertension and various cardiovascular conditions. ARBs work by selectively blocking the angiotensin II type 1 receptors, which are responsible for causing vasoconstriction and promoting the release of aldosterone, a hormone that regulates blood pressure and fluid balance.
These APIs are highly effective in reducing blood pressure by preventing angiotensin II from binding to its receptors, thereby dilating blood vessels and reducing peripheral resistance. By inhibiting the angiotensin II signaling pathway, ARBs help relax and widen the blood vessels, which subsequently lowers blood pressure.
Some commonly prescribed ARBs include losartan, valsartan, and candesartan. These drugs offer several advantages over other antihypertensive medications, such as a lower risk of side effects and better tolerability. ARBs are also considered beneficial for patients with certain comorbidities, including heart failure and diabetic nephropathy.
Pharmaceutical companies play a crucial role in the development and manufacturing of high-quality ARB APIs. Stringent quality control measures and adherence to regulatory guidelines ensure the safety, efficacy, and reliability of these APIs. Moreover, the market demand for ARBs is consistently growing, presenting a significant opportunity for pharmaceutical companies to cater to the increasing medical needs of patients suffering from hypertension and related cardiovascular conditions.
In conclusion, Angiotensin Receptor Blockers (ARBs) are a valuable subcategory of pharmaceutical APIs that effectively manage hypertension and cardiovascular diseases. With their ability to target the angiotensin II receptors, ARBs provide a reliable therapeutic option for patients and contribute to improving overall cardiovascular health.
Eprosartan (Angiotensin Receptor Blockers), classified under Antihypertensive agents
Antihypertensive agents are a crucial category of pharmaceutical active pharmaceutical ingredients (APIs) used to treat high blood pressure, also known as hypertension. These medications are designed to lower blood pressure and reduce the risk of associated cardiovascular complications.
Antihypertensive agents function by targeting various mechanisms involved in blood pressure regulation. Some common classes of antihypertensive agents include angiotensin-converting enzyme (ACE) inhibitors, angiotensin II receptor blockers (ARBs), beta-blockers, calcium channel blockers (CCBs), and diuretics.
ACE inhibitors work by inhibiting the enzyme responsible for converting angiotensin I to angiotensin II, a hormone that constricts blood vessels. ARBs, on the other hand, block the receptors to which angiotensin II binds, thereby preventing its vasoconstrictive effects.
Beta-blockers reduce blood pressure by blocking the effects of adrenaline and noradrenaline, which are responsible for increasing heart rate and constricting blood vessels. CCBs inhibit calcium from entering the smooth muscles of blood vessels, resulting in relaxation and vasodilation. Diuretics promote the elimination of excess fluid and sodium from the body, reducing blood volume and thereby lowering blood pressure.
Antihypertensive agents are typically prescribed based on the individual patient's condition and specific needs. They can be used alone or in combination to achieve optimal blood pressure control. It is important to note that antihypertensive agents should be taken regularly as prescribed by a healthcare professional and may require periodic monitoring to ensure their effectiveness and manage any potential side effects.
In summary, antihypertensive agents play a vital role in the management of hypertension by targeting various mechanisms involved in blood pressure regulation. These medications offer significant benefits in reducing the risk of cardiovascular complications associated with high blood pressure.
Eprosartan API manufacturers & distributors
Compare qualified Eprosartan API suppliers worldwide. We currently have 5 companies offering Eprosartan API, with manufacturing taking place in 1 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 |
|---|---|---|---|---|---|
| Glochem | Producer | India | India | CoA, USDMF | 14 products |
| Hetero Drugs | Producer | India | India | CoA, GMP, USDMF, WC | 98 products |
| Mylan | Producer | India | India | CoA, GMP, WC | 201 products |
| SETV Global | Producer | India | India | CoA, FDA, GMP | 515 products |
| Unichem Labs. | Producer | India | India | CoA, GMP, USDMF, WC | 62 products |
When sending a request, specify which Eprosartan 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 Eprosartan 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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