Bevacizumab
[CAS# 216974-75-3]

Identification

• Classification: API >> Hormone and endocrine-regulating drugs >> Adrenal corticosteroids
• Name: Bevacizumab
• Synonyms: Avastatin; Avastin; Bevacituzumab
• Molecular Formula: C₆₆₃₈H₁₀₁₆₀N₁₇₂₀O₂₁₀₈S₄₄
• Molecular Weight: 149196.82
• CAS Registry Number: 216974-75-3
• EC Number: 692-134-7

Safety Data

• Hazard Symbols: GHS08 Warning
• Risk Statements: H361fd
• Safety Statements: P203-P280-P318-P405-P501

Discovery and Applications

Bevacizumab is a recombinant humanized monoclonal antibody designed to inhibit vascular endothelial growth factor A (VEGF-A), a key signaling protein involved in angiogenesis, the process by which new blood vessels form from pre-existing vessels. The discovery of bevacizumab emerged from extensive research into tumor biology and the critical role of VEGF-A in promoting tumor vascularization, which supports tumor growth and metastasis by supplying oxygen and nutrients.

Bevacizumab was developed through genetic engineering techniques that combined murine antibody variable regions with human antibody constant regions, creating a humanized antibody with reduced immunogenicity suitable for therapeutic use. It specifically binds to VEGF-A, preventing it from interacting with its receptors on the surface of endothelial cells. By blocking this interaction, bevacizumab inhibits the formation of new blood vessels, effectively starving tumors of their blood supply and inhibiting growth.

This antibody gained regulatory approval initially for the treatment of metastatic colorectal cancer and has since been approved for various other cancers including non-small cell lung cancer, glioblastoma, renal cell carcinoma, cervical cancer, and ovarian cancer. Its clinical applications have transformed cancer therapy by providing a targeted approach that complements conventional treatments such as chemotherapy and radiation therapy.

In addition to oncology, bevacizumab has found applications in ophthalmology, particularly in the treatment of neovascular age-related macular degeneration (AMD), diabetic retinopathy, and other conditions characterized by abnormal blood vessel growth in the eye. Its off-label use in ophthalmology has been widely adopted due to its effectiveness in reducing pathological angiogenesis and associated vision loss.

Bevacizumab is administered intravenously and dosing schedules vary depending on the disease being treated. Common side effects include hypertension, increased risk of bleeding, impaired wound healing, and proteinuria. Despite these potential adverse effects, bevacizumab remains a cornerstone in the management of several malignancies and angiogenesis-related diseases.

The development of bevacizumab represents a significant advancement in biotherapeutics by targeting a critical growth factor pathway in angiogenesis. Its success has paved the way for the development of other anti-angiogenic agents and highlighted the importance of targeted molecular therapies in medicine.

References

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