title: Quantitation of VEGFR2 (vascular endothelial growth factor receptor) inhibitors--review of assay methodologies and perspectives.
abstract: The introduction of small-molecule tyrosine kinase VEGFR2 (vascular endothelial growth factor receptor) inhibitors has added another dimension in the treatment of several oncology indications as they offer a unique mechanism. The VEGFR2 inhibitors have demonstrated superior benefits in treating certain types of cancer, such as renal cell carcinoma and hepatocellular carcinoma, as a monotherapy option. Many of the approved VEGFR2 inhibitors have also shown promise when used in combination with other anticancer agents. There are numerous bioanalytical methods published for the analysis of VEGFR2 inhibitors in preclinical and clinical samples. This review covers VEGFR2 inhibitors such as sunitinib, sorafenib, pazopanib and JI-101. In addition to providing a comprehensive review of the available methods for the above-mentioned VRGFR2 inhibitors, it also provides information on assays that can simultaneously measure multiple tyrosine kinase inhibitors, including VEGFR2 molecules. Based on the review, the published methodologies using LC/MS-MS or HPLC-UV are adequate for the quantification of the VEGFR2 inhibitors and can easily be established in a modern day bioanalytical laboratory. The availability of a plethora of assays for multiple tyrosine kinase inhibitors makes it easy to analyze a panel of compounds to support either therapeutic drug monitoring and/or clinical pharmacokinetics.
authors.affiliation: Jubilant Biosys, Second Stage, Industrial Suburb, Yeswanthpur, Bangalore-, 560 022, India.
authors.forename: Kuldeep
authors.initials: K
authors.lastname: Sharma
authors.affiliation: Jubilant Biosys, Second Stage, Industrial Suburb, Yeswanthpur, Bangalore-, 560 022, India.
authors.forename: P S
authors.initials: PS
authors.lastname: Suresh
authors.affiliation: Jubilant Biosys, Second Stage, Industrial Suburb, Yeswanthpur, Bangalore-, 560 022, India.
authors.forename: Ramesh
authors.initials: R
authors.lastname: Mullangi
authors.affiliation: Semler Research, VI Phase, J. P. Nagar, Bangalore-, 560 078, India.|CEO, Bioneeds India Private Lmited, Tumkur Road, Nelamangala Taluk, Bangalore Rural District, India.
authors.forename: N R
authors.initials: NR
authors.lastname: Srinivas
mesh_terms: D000818:Animals; D002853:Chromatography, Liquid / Q000379:methods*; D006801:Humans; D007211:Indoles / Q000032:analysis; D013058:Mass Spectrometry / Q000379:methods*; D051379:Mice; D009536:Niacinamide / Q000031:analogs & derivatives / Q000032:analysis; D010671:Phenylurea Compounds / Q000032:analysis; D047428:Protein Kinase Inhibitors / Q000032:analysis*; D011758:Pyrroles / Q000032:analysis; D000077157:Sorafenib; D000077210:Sunitinib; D040301:Vascular Endothelial Growth Factor Receptor-2 / Q000037:antagonists & inhibitors*
chemical_list: C561574:1-(1-(2-amino-pyridin-4-ylmethyl)-1H-indol-4-yl)-3-(5-bromo-2-methoxyphenyl)urea; D007211:Indoles; D010671:Phenylurea Compounds; D047428:Protein Kinase Inhibitors; D011758:Pyrroles; D009536:Niacinamide; D000077157:Sorafenib; D040301:Vascular Endothelial Growth Factor Receptor-2; D000077210:Sunitinib
keywords: HPLC; JI-101; LC-MS; VEGFR2 inhibitors; bioanalytical methods; review; sorafenib; sunitinib