Vonoprazan Fumarate is the fumarate salt form of vonoprazan, a potassium-competitive acid blocker (P-CAB) used as a gastric acid suppressant. It is a specialized pharmaceutical active ingredient that inhibits the gastric proton pump through a potassium-competitive mechanism. Vonoprazan Fumarate is an important API for pharmaceutical formulations used in acid-related gastrointestinal disorders and in combination regimens for Helicobacter pylori infection.
Vonoprazan is structurally different from conventional proton pump inhibitors because it does not require activation in an acidic environment. It directly and reversibly inhibits the gastric H+, K+-ATPase proton pump at the secretory surface of gastric parietal cells. This mechanism suppresses both basal and stimulated gastric acid secretion.
Vonoprazan Fumarate is chemically described as 1H-pyrrole-3-methanamine, 5-(2-fluorophenyl)-N-methyl-1-(3-pyridinylsulfonyl)-, (2E)-2-butenedioate (1:1). The empirical formula is C17H16FN3O2S·C4H4O4, corresponding to the molecular formula C21H20FN3O6S. Its molecular weight is 461.5 g/mol.
The fumarate salt is the pharmaceutical form used in marketed vonoprazan products. Vonoprazan Fumarate is also identified by development code TAK-438. The substance has been associated with CAS numbers 881681-01-2 and 1260141-27-2 in chemical and regulatory databases.
Vonoprazan acts as a potassium-competitive acid blocker. It inhibits the gastric H+, K+-ATPase enzyme system, which functions as the final proton pump responsible for gastric acid secretion.
The molecule competitively inhibits potassium binding at or near the potassium-binding site of the gastric proton pump. By preventing activation of the H+, K+-ATPase, vonoprazan suppresses gastric acid production.
Unlike traditional proton pump inhibitors, vonoprazan does not require conversion to an active form by gastric acid. Its direct action on the proton pump contributes to its pharmacological activity as a P-CAB.
Vonoprazan Fumarate API is relevant to pharmaceutical manufacturers and developers working on gastrointestinal medicines, acid-suppression therapies and combination treatments for H. pylori infection.
As a Vonoprazan Fumarate API manufacturer and supplier in India, the product can be positioned for pharmaceutical development and manufacturing applications requiring controlled-quality active pharmaceutical ingredient material.
Quality control of Vonoprazan Fumarate should include appropriate identity, assay, purity and related-substance testing. The applicable specification should be based on validated analytical procedures and the relevant regulatory or pharmacopoeial requirements.
Vonoprazan is used for the treatment of acid-related gastrointestinal conditions. Current FDA-approved uses include healing and maintenance of healed erosive esophagitis and relief of heartburn associated with non-erosive gastroesophageal reflux disease. Vonoprazan is also used in combination with antibiotics for treatment of H. pylori infection.
Its ability to provide sustained gastric acid suppression makes Vonoprazan Fumarate an important API for modern gastrointestinal pharmaceutical formulations.
The API is also relevant to fixed-combination products in which vonoprazan is administered together with antibacterial agents for eradication of H. pylori. Such products may contain vonoprazan together with amoxicillin and, depending on the regimen, clarithromycin.
Vonoprazan Fumarate is described by the FDA as a white to nearly white crystalline powder or crystals. It has a reported melting point of 194.8°C.
The substance has a distinctive solubility profile. According to FDA labeling, Vonoprazan Fumarate is soluble in dimethyl sulfoxide, sparingly soluble in N,N-dimethylacetamide, and slightly soluble in N,N-dimethylformamide, methanol and water. It is very slightly soluble in 99.5% ethanol and practically insoluble in 2-propanol, acetone, 1-octanol and acetonitrile.
These qualitative solubility descriptions are more appropriate than assigning an unsupported numerical aqueous-solubility value.
Quality control of Vonoprazan Fumarate requires suitable analytical procedures for confirming identity, potency and chemical purity. Chromatographic methods can be used to evaluate assay and related substances, while spectroscopic techniques can support identity testing.
Because Vonoprazan Fumarate is a defined crystalline salt, control of the salt form, purity profile and physical characteristics can be important during pharmaceutical manufacturing.
Potential quality attributes can include identification, assay, related substances, residual solvents, water content, elemental impurities and other parameters applicable to the manufacturing process and registered specification.
For pharmaceutical API documentation, numerical values should only be assigned to release specifications when supported by a recognized monograph, regulatory documentation or an applicable validated product specification.
Vonoprazan Fumarate is used as the active pharmaceutical ingredient in oral dosage forms. FDA labeling explains that marketed vonoprazan tablets contain vonoprazan as the fumarate salt. A 10 mg vonoprazan tablet corresponds to 13.36 mg of vonoprazan fumarate, while a 20 mg vonoprazan tablet corresponds to 26.72 mg of vonoprazan fumarate.
This distinction is important when calculating API quantities during formulation development because the labeled strength is expressed in terms of the vonoprazan active component rather than the complete fumarate salt mass.
Vonoprazan Fumarate should be stored and handled according to its applicable API specification, validated stability data, safety documentation and pharmaceutical manufacturing requirements.
Appropriate packaging and environmental controls should be used to maintain the chemical and physical quality of the API. Temperature, moisture, light exposure and container-closure requirements should be established from validated stability studies rather than applying unsupported universal conditions.
Manufacturing facilities should also use appropriate procedures for sampling, weighing and handling pharmaceutical API materials to minimize contamination and maintain product quality.
Vonoprazan Fumarate is a specialized gastrointestinal API with an established pharmacological mechanism based on potassium-competitive inhibition of the gastric proton pump. Its chemical structure, fumarate salt form and physical properties make accurate analytical characterization important during pharmaceutical development and manufacturing.
The API can be categorized as a P-CAB API, gastric acid suppressant API, gastrointestinal API and pharmaceutical active ingredient. It is particularly relevant to formulations designed for acid-related gastrointestinal conditions and H. pylori eradication regimens.
For pharmaceutical manufacturers and developers, control of identity, assay, related substances, residual solvents and other applicable quality attributes helps support consistent production of finished dosage forms.
Vonoprazan Fumarate is the fumarate salt of vonoprazan and belongs to the potassium-competitive acid blocker class. It has the molecular formula C21H20FN3O6S and a molecular weight of 461.5 g/mol. FDA labeling describes it as a white to nearly white crystalline powder or crystals with a melting point of 194.8°C.
Vonoprazan Fumarate is slightly soluble in water and has greater solubility in certain organic solvents, while being practically insoluble in several other solvents. It acts by inhibiting the gastric H+, K+-ATPase proton pump in a potassium-competitive manner.
With applications in acid-related gastrointestinal disorders and H. pylori treatment regimens, Vonoprazan Fumarate is an important gastrointestinal API, P-CAB API and pharmaceutical active ingredient for pharmaceutical development and manufacturing.
| Parameter | Specification |
|---|---|
| Appearance | white to off-white crystalline powder |
| Identification | IR & HPLC compliant |
| Assay (HPLC) | 98.0% – 102.0% |
| Melting Point | 194.8°C |
| Solubility | Slightly soluble in water |