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Cilnidipine | CAS No: 132203-70-4 | GMP-certified suppliers
A medication that manages hypertension, supporting end-organ protection and offering utility in patients with diabetes, albuminuria, or chronic kidney disease.
Therapeutic categories
Primary indications
- Cilnidipine is indicated for the management of hypertension for end-organ protection
- It is reported to be useful in elderly patients and in those with diabetes and albuminuria
- Cilnidipine has been increasingly used in patients with chronic kidney disease
- Hypertension is the term used to describe the presence of high blood pressure
Product Snapshot
- Oral small‑molecule formulation supplied as film‑coated tablets
- Used for hypertension management, including use in patients with diabetes, albuminuria, and chronic kidney disease
- Classified as investigational with no major regulatory approvals such as FDA or EMA
Clinical Overview
Pharmacologically, cilnidipine produces antihypertensive effects through reduction of peripheral vascular resistance. It blocks L‑type calcium channels in vascular smooth muscle, limiting calcium influx and suppressing vasoconstriction. Concurrent inhibition of N‑type calcium channels at sympathetic nerve terminals reduces norepinephrine release and attenuates sympathetic drive. This dual mechanism contributes to an antisympathetic profile without inducing reflex tachycardia.
In pharmacodynamic studies, cilnidipine has demonstrated stable blood pressure reduction with a low incidence of excessive hypotension. Its activity on the sympathetic pathway differentiates it from L‑type–selective dihydropyridines and may support its use in patient groups where sympathetic overactivity is clinically relevant.
Cilnidipine is a substrate of CYP3A enzymes, including CYP3A4. While detailed absorption, distribution, metabolism, and excretion parameters are not provided here, its CYP3A‑mediated metabolism indicates potential interactions with inhibitors or inducers of this pathway. No specific organ impairment dosing data are provided. Safety considerations include the class‑associated risks of hypotension, dizziness, peripheral edema, and bradycardia. Effects on serum potassium have been reported within the broader class profiles referenced but are not specifically quantified for cilnidipine. Toxicity data beyond routine antihypertensive class effects are not detailed in the supplied information.
Cilnidipine is marketed in several Asian markets; specific brand names are region dependent and not listed in the provided data.
For API procurement, sourcing should prioritize manufacturers with established control of stereochemistry, impurity profiles, and CYP3A‑related metabolic impurities, supported by current GMP certification and region‑appropriate regulatory documentation.
Identification & chemistry
| Generic name | Cilnidipine |
|---|---|
| Molecule type | Small molecule |
| CAS | 132203-70-4 |
| UNII | 97T5AZ1JIP |
| DrugBank ID | DB09232 |
Pharmacology
| Summary | Cilnidipine is a dihydropyridine calcium channel blocker that inhibits L‑type channels in vascular smooth muscle, reducing calcium influx and lowering vascular tone. It also blocks N‑type calcium channels on sympathetic nerve terminals, limiting norepinephrine release and dampening sympathetic drive. These combined actions support blood pressure reduction in hypertension. |
|---|---|
| Mechanism of action | Cilnidipine acts on the L-type calcium channels of blood vessels by blocking the incoming calcium and suppressing the contraction of blood vessels, thereby reducing blood pressure. Cilnidipine also works on the N-type calcium channel located at the end of the sympathetic nerve, inhibiting the emission of norepinephrine and suppressing the increase in stress blood pressure. |
| Pharmacodynamics | Administration of cilnidipine has been shown to present an antisympathetic profile in vitro and in vivo. It decreases blood pressure safely and effectively without excessive blood pressure reduction or tachycardia. |
Targets
| Target | Organism | Actions |
|---|---|---|
| Voltage-dependent N-type calcium channel subunit alpha-1B | Humans | antagonist |
| Voltage-dependent L-type calcium channel | Humans | antagonist |
ADME / PK
| Absorption | Cilnidipine presents a very rapid absorption with a maximum peaked concentration after 2 hours. Its distribution tends to be higher in the liver as well as in kidneys, plasma and other tissues. Cilnidipine does not present a high accumulation in the tissue after repeated oral administration. Cilnidipine is reported to present very low bioavailability determined to be approximately 13%. This low bioavailability is suggested to be due to its low aqueous solubility and high permeability. Hence, efforts have been made in order to find an innovative formulation that can significantly improve the bioavailability of this drug. One of these formulations corresponds to the generation of polymeric nanoparticles which enhance the bioavailability by 2.5-3-fold. |
|---|---|
| Half-life | The half-life of the hypotensive effect for cilnidipine is of about 20.4 min. |
| Protein binding | Cilnidipine presents a very high protein binding that represents to even 98% of the administered dose. |
| Metabolism | Cilnidipine is metabolized by both liver and kidney. It is rapidly metabolized by liver microsomes by a dehydrogenation process. The major enzymatic isoform involved in cilnidipine dehydrogenation of the dihydropyridine ring is CYP3A. |
| Route of elimination | Cilnidipine gets eliminated through the urine in a proportion of 20% of the administered dose and 80% is eliminated by the feces. |
| Volume of distribution | Drugs on the group of dihydropyridines such as cilnidipine tend to have a large volume of distribution. |
Formulation & handling
- Low aqueous solubility and moderate lipophilicity favor solid oral formulations and may require solubility‑enhancing excipients for consistent dissolution.
- As a dihydropyridine, the API exhibits light sensitivity, so protection from UV exposure is needed during handling and formulation.
- Solid-state stability is generally good, but moisture control is recommended to prevent degradation and maintain tablet integrity.
Regulatory status
Safety
| Toxicity | The percentage of reports of cilnidipine that express drug toxicity reported as side effects are 5.26%. |
|---|
- Reported toxicity incidence is low but present, with approximately 5
- 26% of adverse event reports indicating cilnidipine‑related toxic effects
- Monitor for class‑consistent vasodilatory reactions (e
Cilnidipine 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.
Cilnidipine (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.
Cilnidipine API manufacturers & distributors
Compare qualified Cilnidipine API suppliers worldwide. We currently have 3 companies offering Cilnidipine 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 |
|---|---|---|---|---|---|
| Bengbu BBCA Tushan | Producer | China | China | CoA, JDMF | 2 products |
| Mahalaxmi Chemi Pharm | Producer | India | India | CoA | 13 products |
| Unique Chemicals | Producer | India | India | CoA, GMP, USDMF, WC | 8 products |
When sending a request, specify which Cilnidipine 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 Cilnidipine 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.
Frequently asked questions about Cilnidipine API
Sourcing
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Technical
What is Cilnidipine (CAS 132203-70-4) used for?
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