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Azelnidipine | CAS No: 123524-52-7 | GMP-certified suppliers
A medication that treats hypertension by gradually lowering blood pressure without increasing heart rate, offering vasodilation and additional cardio-protective benefits.
Therapeutic categories
Primary indications
- For the treatment of hypertension
Product Snapshot
- Azelnidipine is an oral small molecule formulated as a calcium channel blocker
- It is primarily indicated for the treatment of hypertension
- The compound is currently in investigational status and not yet approved by major regulatory agencies
Clinical Overview
Pharmacodynamically, azelnidipine induces vasodilation by selectively inhibiting L-type voltage-dependent calcium channels on vascular smooth muscle cells. This blockade prevents calcium influx that would otherwise promote smooth muscle contraction, thereby causing vasorelaxation and lowering systemic blood pressure. Unlike some agents in its class, azelnidipine’s gradual reduction in blood pressure does not trigger reflex tachycardia. Additionally, it demonstrates a high affinity for vascular tissues and possesses antioxidative properties, contributing to anti-arteriosclerotic effects. Clinical investigations have reported cardio-protective, neuroprotective, and anti-atherosclerotic benefits, as well as a reduction in proteinuria and sympathetic nerve activity in hypertensive patients. It has also shown potential in preventing insulin resistance and is under study for post-ischemic stroke management.
Key pharmacokinetic data such as absorption, distribution, metabolism, and elimination parameters are limited in publicly available sources. However, azelnidipine is recognized as a substrate of cytochrome P450 enzymes, particularly CYP3A4, indicating potential metabolic interactions requiring consideration during co-administration with other CYP3A4 substrates or inhibitors.
Safety and toxicity profiles suggest a favorable tolerability with minimal incidence of reflex sympathetic activation, but detailed toxicological data should be reviewed during regulatory submissions. No major bradycardia issues have been reported, consistent with its gradual action profile.
Azelnidipine is marketed primarily by Daiichi-Sankyo Pharmaceuticals, Inc., mainly in Japan. It remains investigational or regionally approved in some markets. For API procurement, quality control should ensure compliance with established pharmacopeial standards and assessment of purity, polymorphism, and residual solvents. Given its metabolism via CYP3A4, sourcing must include data on impurity profiles relevant to enzyme interactions and rigorous batch-to-batch consistency to support clinical and regulatory demands.
Identification & chemistry
| Generic name | Azelnidipine |
|---|---|
| Molecule type | Small molecule |
| CAS | 123524-52-7 |
| UNII | PV23P19YUG |
| DrugBank ID | DB09230 |
Pharmacology
| Summary | Azelnidipine is a calcium channel blocker targeting voltage-dependent L-type calcium channels in vascular smooth muscle, inhibiting calcium influx and promoting vasodilation. This action leads to sustained blood pressure reduction without reflex tachycardia. Additionally, azelnidipine exhibits antioxidative properties and modulates sympathetic nerve activity, contributing to cardio-protective, anti-atherosclerotic, and metabolic effects. |
|---|---|
| Mechanism of action | Azelnidipine inhibits trans-membrane Ca2+ influx through the voltage-dependent channels of smooth muscles in vascular walls. Ca2+ channels are classified into various categories, including L-type, T-type, N-type, P/Q-type, and R-type Ca2+ channels. The L-type Ca2+ channels . Normally, calcium induces smooth muscle contraction, contributing to hypertension. When calcium channels are blocked, the vascular smooth muscle does not contract, resulting in relaxation of vascular smooth muscle walls and decreased blood pressure. |
| Pharmacodynamics | Azelnidipine is a vasodilator that induces a gradual decrease in blood pressure in hypertensive patients. Unlike other members of its drug class, azelnidipine does not induce reflex tachycardia due to vasodilation. This is likely due to the fact that it elicits a gradual fall in blood pressure It also exhibits a prolonged hypotensive effect and has been shown to have a strong anti-arteriosclerotic action in vessels due to its high affinity for vascular tissue and antioxidative activity . Clinical studies have demonstrated that azelnidipine markedly reduced heart rate and proteinuria in hypertensive patients by inhibiting sympathetic nerve activity. Azelnidipine has also been confirmed to have cardio-protective, neuroprotective, and anti-atherosclerotic properties, and has also been found to prevent insulin resistance . |
Targets
| Target | Organism | Actions |
|---|---|---|
| Voltage-dependent L-type calcium channel subunit beta-1 | Humans | agonist |
ADME / PK
| Absorption | Oral ingestion of azelnidipine demonstrates rapid and dose-dependent absorption . |
|---|---|
| Half-life | 16 –28 hours . |
| Protein binding | Azelnidipine is widely bound to human plasma proteins (90%–91%) . |
| Metabolism | Like most members of its class, azelnidipine primarily undergoes first-pass hepatic metabolism. Azelnidipine is metabolized by hepatic cytochrome P450 (CYP) 3A4 and has no active metabolite product. It may interact with other drugs or compounds that are substrates for this enzyme. Azelnidipine is lipophilic and has a potent affinity for membranes of vascular smooth muscle cells . |
| Route of elimination | In one study, following a single 4mg oral dose of 14C-labeled azelnidipine in humans, about 26% of the drug was thought to br excreted in the urine and 63% in the feces during the 1 week period post administration . |
| Volume of distribution | In a Chinese study examining the pharmacokinetics of the drug, the volume of distribution was found to be 1749 +/- 964 . |
Formulation & handling
- Azelnidipine is a lipophilic small molecule with low aqueous solubility, indicating challenges in oral formulation bioavailability.
- The compound is suitable for oral administration, with no indications for injectable formulation.
- High lipophilicity suggests potential sensitivity to formulation excipients and the need for proper handling to maintain stability.
Regulatory status
Safety
| Toxicity | As with any calcium channel blocker toxicity, bradycardia and hypotension may result from overdose. The treatment of patients with bradycardia and hypotension begins with supportive therapy and atropine, however, patients with severe toxicity do not have an adequate response and must be managed more aggressively. Calcium plays an imperative role in myocardial contractility, automaticity and vascular tone. Administration of exogenous calcium is of benefit in cases of toxicity . |
|---|
- Overdose may cause bradycardia and hypotension
- Monitor cardiovascular parameters closely during handling
- Severe toxicity cases may not respond to atropine, necessitating advanced supportive interventions
Azelnidipine is a type of Calcium Channel Blockers
Calcium channel blockers (CCBs) are a subcategory of pharmaceutical active pharmaceutical ingredients (APIs) widely used in the treatment of various cardiovascular conditions. CCBs work by blocking the influx of calcium ions into smooth muscle cells and cardiac muscle cells, leading to vasodilation and reduced cardiac contractility.
CCBs are commonly prescribed to manage hypertension (high blood pressure), angina (chest pain), and certain arrhythmias (irregular heart rhythms). They are also effective in treating Raynaud's disease and migraine headaches. These medications exert their therapeutic effects by selectively inhibiting L-type calcium channels in the heart and blood vessels.
By blocking calcium channels, CCBs help relax and widen blood vessels, reducing peripheral resistance and improving blood flow. This mechanism of action lowers blood pressure, relieves angina symptoms, and helps prevent certain types of abnormal heart rhythms.
Some well-known CCBs include amlodipine, nifedipine, diltiazem, and verapamil. These medications are available in various formulations, including immediate-release and extended-release tablets, as well as injectable solutions.
It's important to note that CCBs may cause certain side effects, such as dizziness, headache, flushing, and ankle swelling. They may also interact with other medications, so it's crucial to consult a healthcare professional before starting or changing any CCB therapy.
In summary, Calcium channel blockers are a subcategory of cardiovascular medications that inhibit calcium channels, resulting in vasodilation, decreased cardiac contractility, and overall therapeutic effects in conditions such as hypertension, angina, and arrhythmias. Proper medical supervision and individualized treatment plans are essential for optimizing the use of CCBs.
Azelnidipine (Calcium Channel 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.
Azelnidipine API manufacturers & distributors
Compare qualified Azelnidipine API suppliers worldwide. We currently have 4 companies offering Azelnidipine 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 |
|---|---|---|---|---|---|
| AXXO GmbH | Distributor | Germany | World | CoA, GMP, GDP, JDMF, KDMF, MSDS, USDMF | 243 products |
| Jeil Pharmaceutical | Producer | South Korea | South Korea | CoA, JDMF | 12 products |
| Mylan | Producer | India | India | CoA, GMP, WC | 201 products |
| Sinoway industrial Co.,Lt... | Distributor | China | China | CoA, GMP, ISO9001, USDMF | 762 products |
When sending a request, specify which Azelnidipine 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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