Vorapaxar Sulfate is the sulfate salt of vorapaxar, a tricyclic himbacine-derived antiplatelet compound belonging to the protease-activated receptor-1 (PAR-1) antagonist class. It is an important cardiovascular active pharmaceutical ingredient used to reduce thrombotic cardiovascular events in specific patients with a history of myocardial infarction or peripheral arterial disease.
Vorapaxar Sulfate is the active pharmaceutical ingredient in the marketed product ZONTIVITY. It acts through a mechanism distinct from several commonly used antiplatelet agents by selectively inhibiting PAR-1, a receptor activated by thrombin on human platelets.
Vorapaxar Sulfate has the empirical formula C29H33FN2O4·H2SO4 and a molecular weight of 590.7 g/mol. PubChem also represents the corresponding salt formula as C29H35FN2O8S. The CAS Number of Vorapaxar Sulfate is 705260-08-8, while the free-base Vorapaxar has CAS Number 618385-01-6.
The development code associated with vorapaxar is SCH-530348, also written as SCH530348. Vorapaxar Sulfate is a chemically defined small-molecule API with a complex tricyclic structure derived from the himbacine scaffold.
The FDA describes Vorapaxar Sulfate as a white to off-white solid. The sulfate salt is used in pharmaceutical manufacturing and is incorporated into oral dosage forms.
Vorapaxar is a selective antagonist of protease-activated receptor-1 (PAR-1) expressed on platelets. PAR-1 is a major receptor through which thrombin activates human platelets.
By blocking PAR-1, Vorapaxar inhibits platelet activation and aggregation triggered by thrombin and thrombin receptor agonist peptide. This reduces thrombin-mediated platelet responses and contributes to the antiplatelet activity of the drug.
The FDA describes Vorapaxar as a reversible PAR-1 antagonist in terms of receptor interaction, although its long pharmacological half-life results in prolonged platelet inhibition.
Vorapaxar Sulfate API is relevant to pharmaceutical manufacturers and developers working on cardiovascular and antiplatelet medicines. As a Vorapaxar Sulfate API manufacturer and supplier in India, the product can be positioned for pharmaceutical development and manufacturing applications requiring controlled-quality cardiovascular API material.
Quality control is particularly important for Vorapaxar Sulfate because the product contains a defined sulfate salt form and a stereochemically complex molecular structure. Appropriate analytical procedures should confirm identity, assay, purity, related substances and other applicable quality attributes.
Vorapaxar Sulfate is an antiplatelet API associated with reduction of thrombotic cardiovascular events in patients with a history of myocardial infarction (MI) or peripheral arterial disease (PAD).
The FDA-approved product ZONTIVITY contains Vorapaxar Sulfate and is administered orally. Each tablet contains 2.08 mg of vorapaxar, equivalent to 2.5 mg of vorapaxar sulfate.
The active substance may be used in cardiovascular pharmaceutical development where inhibition of thrombin-mediated platelet activation through PAR-1 is the desired pharmacological mechanism.
Vorapaxar Sulfate is reported as a white to off-white solid. According to FDA labeling, it is freely soluble in methanol and slightly soluble in ethanol, acetone, 2-propanol and acetonitrile.
In aqueous solution, Vorapaxar Sulfate is slightly soluble at pH 1, with solubility decreasing as pH increases. This pH-dependent solubility behavior is an important characteristic of the sulfate salt and should be distinguished from the properties of the free-base form.
The FDA also notes that partial conversion from Vorapaxar Sulfate to the Vorapaxar free base can occur during manufacture and storage of the finished tablets. This characteristic highlights the importance of controlling the chemical form and related substances during pharmaceutical development and manufacturing.
Quality control of Vorapaxar Sulfate should include appropriate identification and purity testing. Chromatographic methods can be used to evaluate assay and related substances, while spectroscopic methods can support molecular identification.
Because Vorapaxar Sulfate contains multiple stereochemical centers, stereochemical integrity may also be an important quality attribute. The applicable API specification should define the appropriate analytical requirements based on the manufacturing process, regulatory documentation and validated methods.
Other potential quality attributes can include residual solvents, water content, elemental impurities, degradation products and process-related impurities, as applicable.
For CMS specifications, a numerical value should only be included when it is supported by an authoritative monograph, regulatory source or validated product specification. Unsupported values should not be presented as release specifications.
Vorapaxar Sulfate is a specialized cardiovascular API with a mechanism based on selective PAR-1 antagonism. Its tricyclic himbacine-derived structure distinguishes it from other classes of antiplatelet compounds.
During pharmaceutical development, control of API identity, assay, purity, stereochemical integrity and degradation profile is important for maintaining consistent product quality.
Vorapaxar Sulfate can be categorized as a PAR-1 antagonist API, antiplatelet API, cardiovascular API, thrombosis-related API and pharmaceutical active ingredient.
Vorapaxar Sulfate should be stored and handled according to the applicable API specification, validated stability data, safety documentation and pharmaceutical manufacturing requirements.
Appropriate environmental and packaging controls should be established from stability studies. Temperature, moisture, light exposure and container-closure requirements should not be assigned without supporting product-specific data.
Pharmaceutical facilities should also implement appropriate procedures for sampling, weighing and handling the API to maintain material integrity and prevent contamination.
Vorapaxar Sulfate is an important specialized API for cardiovascular pharmaceutical development. Its selective inhibition of platelet PAR-1 provides a pharmacological approach to reducing thrombin-mediated platelet activation.
The API is suitable for pharmaceutical development involving antiplatelet and cardiovascular products. Reliable analytical control of the sulfate salt, assay, purity and related substances supports consistent downstream manufacturing.
As a specialized pharmaceutical ingredient, Vorapaxar Sulfate can be positioned for applications involving antiplatelet medicines, PAR-1 antagonist formulations, cardiovascular pharmaceutical products and thrombotic cardiovascular disease therapies.
Vorapaxar Sulfate is the sulfate salt of Vorapaxar, a selective protease-activated receptor-1 antagonist with antiplatelet activity. It has the empirical formula C29H33FN2O4·H2SO4 and a molecular weight of 590.7 g/mol. Its CAS Number is 705260-08-8.
The API is described as a white to off-white solid. It is freely soluble in methanol, slightly soluble in several organic solvents, and slightly soluble in aqueous solution at pH 1, with decreasing solubility as pH increases.
Vorapaxar Sulfate can therefore be classified as a cardiovascular API, antiplatelet API, PAR-1 antagonist API and pharmaceutical active ingredient for pharmaceutical manufacturing and development.
| Parameter | Specification |
|---|---|
| Appearance | white to off-white crystalline powder |