Venetoclax is a selective, orally bioavailable small-molecule inhibitor of B-cell lymphoma 2 (BCL-2), an anti-apoptotic protein involved in the survival of certain malignant cells. It is an important active pharmaceutical ingredient (API) used in the development and manufacture of medicines for hematological malignancies. Venetoclax is also known by the development codes ABT-199 and GDC-0199. Its CAS Number is 1257044-40-8, with the molecular formula C45H50ClN7O7S and molecular weight of approximately 868.4 g/mol.
Venetoclax belongs to a structurally complex class of pharmaceutical compounds and is characterized by multiple aromatic and heterocyclic functional groups. According to PubChem, the molecular formula of venetoclax is C45H50ClN7O7S and its molecular weight is 868.4 g/mol. The compound is registered under CAS Number 1257044-40-8.
As an active pharmaceutical ingredient, venetoclax requires controlled manufacturing, analytical testing and quality assurance throughout the production process. Commercial active-substance specifications may include identification, assay, related substances/impurities, residual solvents, water content, sulphated ash, crystal form and microbiological quality, depending on the applicable regulatory specification. The European Medicines Agency's assessment report for venetoclax describes these types of quality controls for the active substance.
Venetoclax works by selectively binding to the BCL-2 protein. BCL-2 is an anti-apoptotic protein that can contribute to the survival of cancer cells. By binding to BCL-2, venetoclax displaces pro-apoptotic proteins such as BIM, helping restore apoptotic signaling and promoting mitochondrial outer membrane permeabilization and activation of caspases. The current FDA prescribing information describes venetoclax as a selective and orally bioavailable BCL-2 inhibitor.
Venetoclax is used in pharmaceutical products intended for specific hematological malignancies. Current FDA labeling includes indications involving chronic lymphocytic leukemia (CLL) and small lymphocytic lymphoma (SLL). Venetoclax is also used in combination regimens for certain adults with newly diagnosed acute myeloid leukemia (AML). Exact approved indications, patient populations and combination regimens depend on the applicable regulatory jurisdiction and current product labeling.
Because venetoclax is a potent pharmaceutical compound, its API manufacturing and quality-control processes require appropriate controls for identity, purity, impurities, residual solvents and other critical quality attributes. Regulatory assessment of venetoclax has included commercial-scale batch data and stability testing of the active substance.
Venetoclax API quality is evaluated using appropriate analytical procedures designed to confirm identity, strength, purity and consistency. Identification may involve techniques such as infrared spectroscopy and chromatographic retention time, while assay and related-substance testing can be performed using validated chromatographic methods.
The public EMA assessment report identifies IR/HPLC identification, HPLC assay, HPLC impurities, residual-solvent testing, sulphated ash, water content, crystal-form testing and microbiological quality among the controls considered for venetoclax active substance.
For commercial API supply, individual acceptance criteria should be based on the applicable approved specification, customer requirements, pharmacopoeial requirements where applicable, and the manufacturer's validated analytical methods. Therefore, numerical limits should not be presented as universal values unless supported by the relevant specification or authoritative documentation.
Venetoclax has the chemical formula C45H50ClN7O7S and a molecular weight of approximately 868.4 g/mol. PubChem identifies the compound as a BCL-2 inhibitor and provides CAS Number 1257044-40-8 and other identifiers including UNII and ChEBI information.
Venetoclax has very low aqueous solubility, as noted in the current FDA prescribing information. This physicochemical characteristic is relevant to pharmaceutical formulation and product-development considerations.
Manufacturing of Venetoclax API requires controlled chemical processing, purification and analytical testing to achieve consistent quality. Critical quality attributes can include chemical identity, assay, related substances, residual solvents, water content and solid-state/crystal-form characteristics.
Analytical methods used for API quality control should be validated for their intended purpose. Regulatory assessment documentation indicates that venetoclax assay and impurity methods were evaluated for specificity and stability-indicating performance.
Quality documentation for pharmaceutical API supply may include a Certificate of Analysis (CoA), specification sheet, analytical test results, batch information and other documentation according to applicable customer and regulatory requirements.
Venetoclax API is relevant to pharmaceutical companies, formulation developers, research organizations and manufacturers working with oncology and hematology products. Its highly specific pharmacological activity and complex chemical structure make appropriate raw-material control and analytical characterization important during pharmaceutical development.
For API procurement and manufacturing applications, customers should evaluate the applicable grade, regulatory requirements, analytical specifications, documentation package, packaging configuration and storage conditions before commercial use.
Venetoclax is an important BCL-2 inhibitor API used in pharmaceutical products for selected hematological malignancies. With the chemical formula C45H50ClN7O7S, CAS Number 1257044-40-8 and molecular weight of approximately 868.4 g/mol, it represents a complex pharmaceutical active substance requiring rigorous quality control.
For pharmaceutical applications, Venetoclax API should be manufactured and tested according to applicable quality systems and product-specific specifications. Analytical controls covering identity, assay, impurities, residual solvents, water content, solid-state characteristics and other relevant quality attributes support consistent API quality.
| Parameter | Specification |
|---|---|
| Appearance | white to off-white crystalline powder |