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Fosinopril | CAS No: 98048-97-6 | GMP-certified suppliers
A medication that treats mild to moderate hypertension, supports congestive heart failure management, and may slow renal disease progression in hypertensive diabetic patients.
Therapeutic categories
Primary indications
- For treating mild to moderate hypertension, use as an adjunct in treating congestive heart failure, and may be used to slow the rate of progression of renal disease in hypertensive individuals with diabetes mellitus and microalbuminuria or overt nephropathy
Product Snapshot
- Fosinopril is available as an oral tablet formulation
- It is primarily indicated for hypertension management, adjunct treatment of congestive heart failure, and slowing renal disease progression in hypertensive diabetic patients
- The API is approved for use in the US and Canadian markets
Clinical Overview
The primary mechanism of action involves competitive inhibition of ACE, the enzyme responsible for converting angiotensin I to the potent vasoconstrictor angiotensin II. By decreasing angiotensin II levels, fosinoprilat reduces vasoconstriction, aldosterone secretion, and vasopressin release, thereby lowering blood pressure and mitigating sodium and water retention. Additionally, ACE inhibition elevates bradykinin levels by limiting its degradation, which may contribute to vasodilation. Fosinoprilat exhibits greater affinity for the C-domain of somatic ACE, which is mainly responsible for blood pressure regulation.
Pharmacodynamically, inhibition of ACE leads to decreased systemic vascular resistance and enhanced renal excretion of sodium and water. Increased plasma renin activity is observed as a consequence of interrupted feedback inhibition by angiotensin II. Fosinopril’s absorption and metabolism yield predictable exposure to fosinoprilat, facilitating its clinical use.
Safety considerations include risks associated with ACE inhibitors, such as hyperkalemia, angioedema, hypotension, and renal function impairment. Careful monitoring is necessary in patients with renal insufficiency, electrolyte disturbances, or concomitant diuretic therapy. Photosensitivity reactions have also been reported less frequently.
Fosinopril is marketed under several brand names globally, often combined with diuretics for enhanced antihypertensive effect. From an API procurement perspective, stringent quality control is essential to ensure the integrity of the phosphinic acid ester moiety and the absence of impurities that could affect prodrug activation or safety. Suppliers should comply with pharmacopeial standards and provide comprehensive analytical data to support consistent manufacturing and regulatory submissions.
Identification & chemistry
| Generic name | Fosinopril |
|---|---|
| Molecule type | Small molecule |
| CAS | 98048-97-6 |
| UNII | R43D2573WO |
| DrugBank ID | DB00492 |
Pharmacology
| Summary | Fosinoprilat, the active metabolite of fosinopril, competitively inhibits angiotensin-converting enzyme (ACE), primarily targeting the C-domain to reduce conversion of angiotensin I to angiotensin II. This inhibition attenuates vasoconstriction, aldosterone and vasopressin release, and sodium and water retention, thereby modulating blood pressure through disruption of the renin-angiotensin-aldosterone system (RAAS). Additionally, ACE inhibition increases bradykinin levels, contributing to vasodilation. |
|---|---|
| Mechanism of action | There are two isoforms of ACE: the somatic isoform, which exists as a glycoprotein comprised of a single polypeptide chain of 1277; and the testicular isoform, which has a lower molecular mass and is thought to play a role in sperm maturation and binding of sperm to the oviduct epithelium. Somatic ACE has two functionally active domains, N and C, which arise from tandem gene duplication. Although the two domains have high sequence similarity, they play distinct physiological roles. The C-domain is predominantly involved in blood pressure regulation while the N-domain plays a role in hematopoietic stem cell differentiation and proliferation. ACE inhibitors bind to and inhibit the activity of both domains, but have much greater affinity for and inhibitory activity against the C-domain. Fosinoprilat, the active metabolite of fosinopril, competes with ATI for binding to ACE and inhibits and enzymatic proteolysis of ATI to ATII. Decreasing ATII levels in the body decreases blood pressure by inhibiting the pressor effects of ATII as described in the Pharmacology section above. Fosinoprilat also causes an increase in plasma renin activity likely due to a loss of feedback inhibition mediated by ATII on the release of renin and/or stimulation of reflex mechanisms via baroreceptors. |
| Pharmacodynamics | Following oral administration, fosinopril is rapidly and completely hydrolyzed to its principle active metabolite, fosinoprilat. Hydrolysis is thought to occur in the gastrointestinal mucosa and liver. Fosinoprilat is a competitive inhibitor of ACE, a peptidyl dipeptidase that is part of the RAAS. The RAAS is a homeostatic mechanism for regulating hemodynamics, water and electrolyte balance. During sympathetic stimulation or when renal blood pressure or blood flow is reduced, renin is released from the granular cells of the juxtaglomerular apparatus in the kidneys. In the blood stream, renin cleaves circulating angiotensinogen to ATI, which is subsequently cleaved to ATII by ACE. ATII increases blood pressure using a number of mechanisms. First, it stimulates the secretion of aldosterone from the adrenal cortex. Aldosterone travels to the distal convoluted tubule (DCT) and collecting tubule of nephrons where it increases sodium and water reabsorption by increasing the number of sodium channels and sodium-potassium ATPases on cell membranes. Second, ATII stimulates the secretion of vasopressin (also known as antidiuretic hormone or ADH) from the posterior pituitary gland. ADH stimulates further water reabsorption from the kidneys via insertion of aquaporin-2 channels on the apical surface of cells of the DCT and collecting tubules. Third, ATII increases blood pressure through direct arterial vasoconstriction. Stimulation of the Type 1 ATII receptor on vascular smooth muscle cells leads to a cascade of events resulting in myocyte contraction and vasoconstriction. In addition to these major effects, ATII induces the thirst response via stimulation of hypothalamic neurons. ACE inhibitors inhibit the rapid conversion of ATI to ATII and antagonize RAAS-induced increases in blood pressure. ACE (also known as kininase II) is also involved in the enzymatic deactivation of bradykinin, a vasodilator. Inhibiting the deactivation of bradykinin increases bradykinin levels and may further sustain the effects of fosinoprilat by causing increased vasodilation and decreased blood pressure. |
Targets
| Target | Organism | Actions |
|---|---|---|
| Angiotensin-converting enzyme | Humans | inhibitor |
ADME / PK
| Absorption | Average absolute absorption is 36%. The primary site of absorption is the proximal small intestine (duodenum/jejunum). Food slows the rate of absorption with no effect on the extent of absorption. |
|---|---|
| Half-life | 12 hours |
| Protein binding | Fosinoprilat is ≥95% protein bound |
| Metabolism | Since fosinoprilat is not biotransformed after intravenous administration, fosinopril, not fosinoprilat, appears to be the precursor for the glucuronide and p-hydroxy metabolites. |
| Route of elimination | After oral administration of radiolabeled fosinopril, approximately half of the absorbed dose is excreted in the urine and the remainder is excreted in the feces. |
| Clearance | * 26 - 39 mL/min [healthy] |
Formulation & handling
- Fosinopril is a small molecule formulated exclusively for oral administration as tablets.
- Due to very low water solubility and high lipophilicity (LogP 5.62), formulation strategies should focus on enhancing bioavailability.
- Avoid co-administration with antacids and potassium-containing products to prevent reduced absorption and risk of hyperkalemia.
Regulatory status
| Lifecycle | The active pharmaceutical ingredient entered the market following patent expiry in the United States on January 10, 2010, with established availability in both the US and Canadian markets. The product is currently in a mature market phase. |
|---|
| Markets | Canada, US |
|---|
Supply Chain
| Supply chain summary | Fosinopril's manufacturing landscape includes multiple generic manufacturers and packagers, indicating a well-established supply chain primarily focused on generic production. The presence of branded products is mainly noted in the US and Canadian markets, with no recent patent protection suggesting that patent expiry has already allowed for generic competition. This supports a competitive environment with broad access to various generic formulations. |
|---|
Safety
| Toxicity | Human overdoses of fosinopril have not been reported, but the most common manifestation of human fosinopril overdosage is likely to be hypotension. Oral doses of fosinopril at 2600 mg/kg in rats were associated with significant lethality. The most common adverse effects include dizzines, cough, fatigue, and headache. |
|---|
- Overexposure may induce hypotension
- Appropriate measures should be in place to manage potential hemodynamic instability
- High oral doses in animal studies have demonstrated significant lethality
Fosinopril is a type of ACE inhibitors
ACE inhibitors, or angiotensin-converting enzyme inhibitors, are a subcategory of pharmaceutical APIs (active pharmaceutical ingredients) commonly used in the treatment of various cardiovascular conditions. These medications work by inhibiting the activity of the angiotensin-converting enzyme, which plays a crucial role in the regulation of blood pressure and fluid balance.
By blocking the action of this enzyme, ACE inhibitors help relax and widen the blood vessels, reducing peripheral resistance and ultimately lowering blood pressure. This mechanism of action makes ACE inhibitors highly effective in treating hypertension (high blood pressure) and congestive heart failure.
Additionally, ACE inhibitors have been found to be beneficial for patients with certain kidney disorders and diabetic nephropathy. By dilating the renal blood vessels, they can help improve renal function and reduce proteinuria.
Some commonly prescribed ACE inhibitors include lisinopril, enalapril, and ramipril. These medications are typically administered orally and are available in various dosage forms, including tablets and capsules.
It's worth noting that ACE inhibitors may have certain side effects, such as dry cough, dizziness, and hyperkalemia (high potassium levels). However, these side effects are generally mild and well-tolerated by most patients.
In summary, ACE inhibitors are a vital subcategory of pharmaceutical APIs used in the management of hypertension, heart failure, and certain renal disorders. Their ability to lower blood pressure and improve renal function makes them an essential tool in the treatment of cardiovascular diseases.
Fosinopril (ACE inhibitors), 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.
Fosinopril API manufacturers & distributors
Compare qualified Fosinopril API suppliers worldwide. We currently have 4 companies offering Fosinopril API, with manufacturing taking place in 4 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 |
|---|---|---|---|---|---|
| Amino Chemicals | Producer | Malta | Malta | CoA, USDMF | 20 products |
| Hetero Drugs | Producer | India | Unknown | CEP, CoA, FDA, GMP, USDMF, WC | 98 products |
| Sinoway industrial Co.,Lt... | Distributor | China | China | CEP, CoA, GMP, ISO9001, USDMF | 762 products |
| Sun Pharma | Producer | India | India | CoA, GMP, WC | 219 products |
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