Clofezone (Rabeprazole) API Manufacturers & Suppliers
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Rabeprazole | CAS No: 117976-89-3 | GMP-certified suppliers
A medication that treats acid-reflux disorders, peptic ulcers, H. pylori infection, and prevents NSAID-induced gastrointestinal bleeding through effective gastric acid suppression.
Therapeutic categories
Primary indications
- For the treatment of acid-reflux disorders (GERD), peptic ulcer disease, H
- Pylori eradication, and prevention of gastroinetestinal bleeds with NSAID use
Product Snapshot
- Rabeprazole is an oral small molecule available in various delayed-release and extended-release tablet and capsule formulations, as well as granules and powder for suspension
- It is primarily indicated for acid-reflux disorders such as GERD, peptic ulcer disease, Helicobacter pylori eradication, and prevention of NSAID-induced gastrointestinal bleeding
- The product is approved in key regulatory markets including the United States and Canada, with both approved and investigational statuses
Clinical Overview
Chemically belonging to the class of sulfinylbenzimidazoles, rabeprazole is a substituted benzimidazole derivative containing a sulfinyl group at the 2-position of the benzimidazole moiety. It functions as a prodrug; upon reaching the acidic environment of gastric parietal cells, it is protonated and converted into an active sulfenamide metabolite that irreversibly inhibits the H+, K+-ATPase enzyme, the final proton pump responsible for acid secretion into the gastric lumen.
Pharmacodynamically, rabeprazole produces dose-dependent suppression of both basal and stimulated gastric acid secretion by selectively blocking the gastric proton pump. This mechanism prevents acid production, thereby reducing acid-related mucosal damage and associated symptoms. Unlike agents targeting histamine H2 receptors or exhibiting anticholinergic effects, rabeprazole directly inhibits the enzymatic activity of the proton pump.
Key absorption, distribution, metabolism, and excretion (ADME) characteristics include rapid conversion to the active form in acidic conditions. The metabolism primarily involves cytochrome P450 enzymes, notably CYP2C19 and CYP3A4, which may influence drug interactions and individual metabolic variability. Rabeprazole exhibits a relatively short chemical half-life in activation but achieves prolonged acid suppression due to irreversible enzyme binding.
Safety and toxicity considerations include monitoring for potential adverse effects associated with long-term acid suppression, such as increased risk of gastrointestinal infections and possible nutrient malabsorption. Caution is warranted in patients with hepatic impairment due to metabolic considerations. Rabeprazole has multiple global approvals and is marketed under various brand names worldwide, commonly utilized as part of combination regimens for H. pylori eradication.
For active pharmaceutical ingredient (API) procurement, attention should be given to the compound’s stereochemistry, purity profile, and polymorphic form due to their impact on bioavailability and stability. Suppliers should comply with Good Manufacturing Practice (GMP) standards and provide certificates of analysis to ensure consistency and regulatory compliance in pharmaceutical formulation development.
Identification & chemistry
| Generic name | Rabeprazole |
|---|---|
| Molecule type | Small molecule |
| CAS | 117976-89-3 |
| UNII | 32828355LL |
| DrugBank ID | DB01129 |
Pharmacology
| Summary | Rabeprazole is a proton-pump inhibitor that selectively and irreversibly inhibits the gastric H⁺/K⁺-ATPase enzyme on parietal cells, suppressing gastric acid secretion. Its primary therapeutic applications include the management of acid-related disorders such as gastroesophageal reflux disease, peptic ulcers, and Zollinger-Ellison syndrome. Rabeprazole’s acid suppression facilitates mucosal healing and supports adjunctive treatment in Helicobacter pylori eradication. |
|---|---|
| Mechanism of action | Rabeprazole belongs to a class of antisecretory compounds (substituted benzimidazole proton-pump inhibitors) that do not exhibit anticholinergic or histamine H2-receptor antagonist properties, but suppress gastric acid secretion by inhibiting the gastric H<sup>+</sup>/K<sup>+</sup>ATPase (hydrogen-potassium adenosine triphosphatase) at the secretory surface of the gastric parietal cell. Because this enzyme is regarded as the acid (proton) pump within the parietal cell, rabeprazole has been characterized as a gastric proton-pump inhibitor. Rabeprazole blocks the final step of gastric acid secretion. In gastric parietal cells, rabeprazole is protonated, accumulates, and is transformed to an active sulfenamide. When studied in vitro, rabeprazole is chemically activated at pH 1.2 with a half-life of 78 seconds. |
| Pharmacodynamics | Rabeprazole prevents the production of acid in the stomach. It reduces symptoms and prevents injury to the esophagus or stomach in patients with gastroesophageal reflux disease (GERD) or ulcers. Rabeprazole is also useful in conditions that produce too much stomach acid such as Zollinger-Ellison syndrome. Rabeprazole may also be used with antibiotics to get rid of bacteria that are associated with some ulcers. Rabeprazole is a selective and irreversible proton pump inhibitor, suppresses gastric acid secretion by specific inhibition of the H<sup>+</sup>, K<sup>+</sup> -ATPase, which is found at the secretory surface of parietal cells. In doing so, it inhibits the final transport of hydrogen ions (via exchange with potassium ions) into the gastric lumen. |
Targets
| Target | Organism | Actions |
|---|---|---|
| Potassium-transporting ATPase alpha chain 1 | Humans | inhibitor |
ADME / PK
| Absorption | Absolute bioavailability is approximately 52%. |
|---|---|
| Half-life | 1-2 hours (in plasma) |
| Protein binding | 96.3% (bound to human plasma proteins) |
| Metabolism | Hepatic |
| Route of elimination | Following a single 20 mg oral dose of 14C-labeled rabeprazole, approximately 90% of the drug was eliminated in the urine, primarily as thioether carboxylic acid; its glucuronide, and mercapturic acid metabolites. |
Formulation & handling
- Rabeprazole is formulated exclusively for oral administration, predominantly as delayed-release tablets, capsules, and granules to protect the active compound from gastric degradation.
- The API is a small molecule with moderate water solubility and LogP, suitable for solid oral forms with controlled-release properties.
- Food intake may delay absorption but does not significantly impact its bioavailability, indicating flexible dosing relative to meals.
Regulatory status
| Lifecycle | The active pharmaceutical ingredient (API) has reached or is approaching patent expiry dates in both the United States and Canada as of 2013, indicating a mature market with potential for generic competition in these regions. |
|---|
| Markets | Canada, US |
|---|
Supply Chain
| Supply chain summary | Rabeprazole is manufactured and supplied by multiple originator and generic companies, with branded products primarily present in the US and Canadian markets. The key originator brands have established global reach, notably in North America. Patent expirations between 2012 and 2013 indicate that generic competition is currently established or emerging within these markets. |
|---|
Rabeprazole is a type of Proton pump inhibitors
Proton pump inhibitors (PPIs) are a subcategory of pharmaceutical active pharmaceutical ingredients (APIs) commonly used for the treatment of gastroesophageal reflux disease (GERD), peptic ulcers, and other acid-related gastrointestinal conditions. PPIs work by inhibiting the gastric proton pump, which is responsible for the secretion of stomach acid.
The primary mechanism of PPIs involves blocking the final step in acid production, thereby reducing the amount of acid produced in the stomach. This inhibition occurs by binding irreversibly to the hydrogen-potassium ATPase enzyme system, also known as the proton pump, located on the parietal cells of the stomach lining. By reducing the acid levels, PPIs provide relief from the symptoms of acid reflux, such as heartburn and regurgitation, while promoting the healing of ulcers.
PPIs are available in various formulations, including delayed-release capsules, tablets, and oral suspensions. Some commonly prescribed PPIs include omeprazole, lansoprazole, pantoprazole, and esomeprazole. These medications are typically taken orally, with the dosage and duration of treatment determined by the severity of the condition and the individual patient's needs.
It is important to note that PPIs are intended for short-term use, generally ranging from four to eight weeks. Prolonged use of PPIs may lead to potential side effects, including an increased risk of gastrointestinal infections, vitamin and mineral deficiencies, and bone fractures.
In summary, proton pump inhibitors are a widely used subcategory of pharmaceutical APIs that effectively reduce stomach acid production. While they provide relief from acid-related conditions, careful consideration of their appropriate usage and potential side effects is necessary for optimal patient care.
Rabeprazole (Proton pump inhibitors), classified under Gastrointestinal Agents
Gastrointestinal Agents belong to the pharmaceutical API category that focuses on treating disorders and ailments related to the digestive system. These agents play a crucial role in addressing various gastrointestinal conditions, such as acid reflux, ulcers, irritable bowel syndrome (IBS), and inflammatory bowel disease (IBD).
One of the key types of gastrointestinal agents is proton pump inhibitors (PPIs), which work by reducing the production of stomach acid. PPIs help in treating conditions like gastroesophageal reflux disease (GERD) and peptic ulcers. Another essential class of agents is antacids, which neutralize excessive stomach acid, providing relief from heartburn and indigestion.
Gastrointestinal agents also include antispasmodics that alleviate abdominal cramps and spasms associated with conditions like IBS. These drugs work by relaxing the smooth muscles of the digestive tract. Additionally, there are drugs categorized as laxatives that aid in relieving constipation by promoting bowel movements.
Moreover, certain gastrointestinal agents act as antiemetics, effectively reducing nausea and vomiting. These drugs are particularly useful for patients undergoing chemotherapy or experiencing motion sickness.
Pharmaceutical companies develop and manufacture a wide range of gastrointestinal agents in various forms, including tablets, capsules, suspensions, and injections. These agents are typically formulated using active pharmaceutical ingredients (APIs) and other excipients to ensure their efficacy and safety.
In conclusion, gastrointestinal agents form a vital category of pharmaceutical APIs, providing relief from digestive disorders and improving overall gastrointestinal health. The availability of diverse agents catering to different conditions ensures that patients can receive targeted treatment for their specific gastrointestinal needs.
Rabeprazole API manufacturers & distributors
Compare qualified Rabeprazole API suppliers worldwide. We currently have 25 companies offering Rabeprazole API, with manufacturing taking place in 7 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 |
|---|---|---|---|---|---|
| Alkem Labs. | Producer | India | India | CoA, USDMF | 22 products |
| Chemo Iberica | Producer | Spain | Spain | CoA, USDMF | 12 products |
| Cipla | Producer | India | India | CoA, GMP, WC | 164 products |
| Daewoong Bio | Producer | South Korea | South Korea | CoA, JDMF | 12 products |
| Dr. Reddy's | Producer | India | India | BSE/TSE, CEP, CoA, EDMF/ASMF, FDA, GMP, MSDS, USDMF, WC | 170 products |
| Gonane Pharma | Producer | India | India | BSE/TSE, CoA, GMP, MSDS | 166 products |
| Hetero Drugs | Producer | India | India | CoA, GMP, JDMF, USDMF, WC | 98 products |
| Lee Pharma | Producer | India | India | CoA, GMP, WC | 21 products |
| Lupin | Producer | India | India | CoA, GMP, USDMF, WC | 155 products |
| Moehs | Producer | Spain | Spain | CEP, CoA, EDMF/ASMF, GMP, USDMF | 50 products |
| Mylan | Producer | India | India | CoA, GMP, USDMF, WC | 201 products |
| Quimica Sintetica | Producer | Spain | Unknown | CEP, CoA, JDMF | 51 products |
| Rajasthan Antibiotics | Producer | India | India | CoA, WC | 9 products |
| Raks Pharma | Producer | India | India | CoA, USDMF | 58 products |
| Ranbaxy Laboratories | Producer | India | India | CoA, JDMF | 7 products |
| Sandoz | Producer | Austria | Unknown | CoA, JDMF | 58 products |
| SEDANAH | Distributor | Jordan | World | CoA, GMP | 70 products |
| SETV Global | Producer | India | India | CoA, FDA, GMP | 515 products |
| Sinoway industrial Co.,Lt... | Distributor | China | China | CEP, CoA, GMP, ISO9001, MSDS, USDMF | 762 products |
| Sterile India | Producer | India | India | CoA, USDMF | 13 products |
| Sun Pharma | Producer | India | India | CoA, GMP, WC | 219 products |
| Syn-tech Chem | Producer | Taiwan | Taiwan | CoA, JDMF, USDMF | 22 products |
| Torrent Pharma | Producer | India | India | CoA, USDMF | 34 products |
| Tresinde Biotech | Producer | India | India | CoA, GMP | 50 products |
| Zhuhai Rundu | Producer | China | China | CoA, JDMF, WC | 11 products |
When sending a request, specify which Rabeprazole 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 Rabeprazole 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.
