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Regorafenib: A comprehensive drug profile
Ahmed A Abdelgalil1, Hamad M Alkahtani2
1Central Laboratory, College of Pharmacy, King Saud University, Riyadh, Kingdom of Saudi Arabia.
Abstract:
Regorafenib is a small molecule tyrosine kinase inhibitor administered orally drug, act by inhibiting the activity of the VEGF receptors. It is used for the treatment of patients with metastatic colorectal cancer (CRC), advanced gastrointestinal stromal tumors, and hepatocellular carcinoma. This comprehensive profile on regorafenib includes an original data as well as data collected from the literature on Profiles of Methods of Drug Synthesis, different Physical Drug Profiles, Drug Analytical methods and Pharmacological profile (ADME). This chapter is divided into five main sections: General Description of the drug, Physical Characteristics, Methods of Preparation, Methods of Analysis, Pharmacology and List of References. These main sections are further divided to many sub-titles to cover most aspect of the drug in the light of the available literature. Among these sub-titles are the formulae, Elemental Analysis, physical characteristics which include constant of ionization, solubility, X-ray powder diffraction pattern, TGA, thermal conduct and spectroscopic and stability. Additionally, analytical techniques including Electrochemical, Spectrophotometric and chromatographic methods, ADME profiles and pharmacological effects were also discussed. Furthermore, methods and schemes are outlined for the preparation of the drug substance.
Insights
Regorafenib is an oral tyrosine kinase inhibitor targeting VEGF receptors, approved for metastatic colorectal cancer, advanced gastrointestinal stromal tumors, and hepatocellular carcinoma. This profile details its synthesis, physical and analytical characteristics, and pharmacological profile.
Area of Science:
- Pharmacology
- Medicinal Chemistry
- Drug Development
Background:
- Regorafenib is an oral small molecule tyrosine kinase inhibitor.
- It targets vascular endothelial growth factor (VEGF) receptors.
- Approved indications include metastatic colorectal cancer (CRC), advanced gastrointestinal stromal tumors (GIST), and hepatocellular carcinoma (HCC).
Purpose of the Study:
- To provide a comprehensive profile of regorafenib.
- To consolidate original and literature data on drug synthesis, physical characteristics, analytical methods, and pharmacology.
- To detail the drug's properties and preparation methods.
Main Methods:
- Literature review and data compilation.
- Analysis of drug synthesis pathways.
- Characterization of physical properties (e.g., solubility, stability, thermal analysis, spectroscopy).
- Evaluation of analytical techniques (e.g., chromatographic, spectrophotometric, electrochemical).
- Assessment of Absorption, Distribution, Metabolism, and Excretion (ADME) profiles.
Main Results:
- Detailed description of regorafenib's chemical and physical properties.
- Outlined methods and schemes for drug substance preparation.
- Comprehensive overview of analytical methodologies for quality control.
- Discussion of ADME profiles and pharmacological effects.
Conclusions:
- Regorafenib's multifaceted profile is crucial for understanding its therapeutic applications.
- This profile serves as a valuable resource for researchers and clinicians.
- Further research can build upon the synthesized data for drug optimization and application.
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