Vorinostat is a synthetic antineoplastic active pharmaceutical ingredient belonging to the class of histone deacetylase (HDAC) inhibitors. It is also widely known as suberoylanilide hydroxamic acid (SAHA) and has the development code MK-0683. Vorinostat is marketed under the brand name ZOLINZA and is used in oncology for the treatment of certain forms of cutaneous T-cell lymphoma.
Vorinostat works by inhibiting histone deacetylase enzymes, which regulate the acetylation status of histones and other cellular proteins. Through inhibition of HDAC activity, Vorinostat can alter gene expression and cellular processes involved in proliferation, differentiation and apoptosis.
Vorinostat has the chemical name N-hydroxy-N'-phenyloctanediamide. Its molecular formula is C14H20N2O3, and its molecular weight is 264.32 g/mol. The CAS Number is 149647-78-9, and the FDA Global Substance Registration System identifies the substance with UNII 58IFB293JI.
The molecule contains a hydroxamic acid functional group and an anilide structure connected through an aliphatic chain. Vorinostat is a non-stereogenic small molecule, which simplifies stereochemical control compared with APIs containing multiple chiral centers.
The API is described as a white to light orange powder. Its physical and chemical properties are important considerations for pharmaceutical development, analytical characterization and finished-product manufacturing.
Vorinostat is a histone deacetylase inhibitor. HDAC enzymes remove acetyl groups from lysine residues on histones and other proteins. Inhibition of these enzymes increases acetylation of histones and can modify chromatin structure and gene transcription.
The resulting changes in cellular gene expression can influence cell-cycle regulation, differentiation and programmed cell death. Vorinostat therefore belongs to a specialized class of antineoplastic agents that act through epigenetic regulation rather than directly targeting DNA synthesis or microtubule assembly.
Its pharmacological classification is officially identified as a Histone Deacetylase Inhibitor.
Vorinostat API is relevant to pharmaceutical manufacturers and developers involved in oncology products and HDAC inhibitor formulations. As a Vorinostat API manufacturer and supplier in India, the product can be positioned for pharmaceutical development and manufacturing applications requiring controlled-quality oncology API material.
Quality control of Vorinostat should include suitable analytical procedures for identity, assay, purity and related substances. Because the molecule contains a hydroxamic acid group, control of chemical purity and degradation products is important during API manufacturing and storage.
The applicable release specification should be established using validated analytical methods and relevant regulatory or pharmacopoeial requirements.
Vorinostat is an established oncology API used for the treatment of cutaneous T-cell lymphoma (CTCL). FDA-approved ZOLINZA contains Vorinostat and is indicated for patients with progressive, persistent or recurrent disease after systemic therapies.
Vorinostat has also been investigated in other malignancies and disease areas because of its ability to modify gene expression through HDAC inhibition. However, approved indications should be distinguished from investigational applications.
For pharmaceutical manufacturing purposes, Vorinostat can be categorized as an oncology API, antineoplastic API, HDAC inhibitor API and hydroxamic acid pharmaceutical ingredient.
FDA chemistry documentation describes Vorinostat as a white to light orange powder with a molecular weight of approximately 264.3 g/mol. Differential scanning calorimetry showed an endothermic range of approximately 161.7–163.9°C, associated with melting of the material.
The FDA reports that Vorinostat is very slightly soluble in water and slightly soluble in ethanol. Another FDA pharmacology assessment reports aqueous solubility of approximately 0.1 mg/mL. Vorinostat is freely soluble in dimethyl sulfoxide (DMSO).
The pH of a saturated aqueous solution was reported as approximately 6.6 in FDA chemistry documentation. Because this is the pH of a saturated solution rather than a universal 1% API solution specification, it should be presented as a reference physical property rather than automatically treated as a release limit.
Quality control of Vorinostat API should include identity, assay, chromatographic purity and related-substance testing. Suitable spectroscopic and chromatographic methods can be used to confirm the molecular identity and evaluate chemical purity.
Important quality attributes may include residual solvents, water content, elemental impurities and degradation products, depending on the manufacturing process and applicable specification.
Because Vorinostat is a defined synthetic small molecule, conventional API characterization parameters such as melting behavior, solubility, pH of an aqueous solution and moisture content can be relevant. However, numerical values should only be entered into release specifications when supported by an applicable recognized standard or validated product specification.
Vorinostat is a specialized oncology API with an established mechanism based on inhibition of histone deacetylase enzymes. Its hydroxamic acid functionality is an important structural feature associated with its HDAC inhibitory activity.
During pharmaceutical development, control of API purity and stability is important because chemical degradation can affect the quality and performance of the finished dosage form. Analytical methods should therefore be capable of distinguishing Vorinostat from relevant degradation products and process-related impurities.
Vorinostat can be categorized as a histone deacetylase inhibitor API, antineoplastic API, oncology API, hydroxamic acid API and pharmaceutical active ingredient.
Vorinostat is commercially formulated as an oral pharmaceutical product. The FDA-approved ZOLINZA product contains 100 mg Vorinostat per capsule. The drug product is an immediate-release formulation.
For pharmaceutical manufacturing, the API must meet the applicable identity, purity and potency requirements before being incorporated into the finished dosage form. Appropriate controls for raw-material handling, weighing, blending and manufacturing should be implemented to maintain consistent product quality.
Vorinostat API should be stored and handled according to the applicable API specification, safety documentation and validated stability data.
Packaging and environmental conditions should protect the material from conditions that could affect its chemical quality. Temperature, humidity, light and container-closure requirements should be established using appropriate stability studies.
Pharmaceutical manufacturing facilities should use suitable procedures for sampling, handling and storage to minimize contamination and maintain API integrity.
Vorinostat is an established active pharmaceutical ingredient for oncology applications. Its HDAC inhibitory mechanism makes it part of a specialized class of epigenetic anticancer agents.
For pharmaceutical manufacturers and developers, accurate control of identity, assay, purity, related substances and physical properties is important for maintaining consistent API quality.
As a specialized pharmaceutical ingredient, Vorinostat can be positioned for applications involving HDAC inhibitor medicines, oncology formulations, antineoplastic products and pharmaceutical research and development.
Vorinostat is a synthetic histone deacetylase inhibitor and antineoplastic API also known as suberoylanilide hydroxamic acid (SAHA). It has the molecular formula C14H20N2O3, molecular weight 264.32 g/mol, and CAS Number 149647-78-9.
FDA chemistry documentation describes Vorinostat as a white to light orange powder, with a DSC melting range of approximately 161.7–163.9°C. Its aqueous solubility is low, with an FDA assessment reporting approximately 0.1 mg/mL, while the pH of a saturated aqueous solution is approximately 6.6.
With its established application in cutaneous T-cell lymphoma, Vorinostat is an important oncology API, HDAC inhibitor API, antineoplastic 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% |
| Loss on Drying | NMT 0.5% |
| Residue on Ignition | NMT 0.1% |
| Individual Impurity | NMT 0.5% |
| Total Impurities | NMT 1.0% |
| Water Content | NMT 0.5% |
| Melting Point | 161.7–163.9°C by DSC |