Vandetanib and Lenvatinib for the Treatment of Thyroid Cancers
Hye-Hyun Kim
College of Pharmacy and Research Institute of Pharmaceutical Sciences, Gyeongsang National University, Jinju, Republic of Korea.
Sun-Young Han *
College of Pharmacy and Research Institute of Pharmaceutical Sciences, Gyeongsang National University, Jinju, Republic of Korea.
*Author to whom correspondence should be addressed.
Abstract
Several drugs with Rearranged during Transfection (RET) kinase-inhibitory activity were recently introduced for thyroid cancer patients. RET gene aberrations were found in differentiated thyroid cancers and medullary thyroid cancers, subsets of thyroid cancers. Rearrangement of RET gene was found in differentiated thyroid cancers and point mutations were observed in medullary thyroid cancers, and both types of RET gene change result in the ligand-independent activation of RET kinase activity. Given the relationship of RET activity and thyroid cancers, RET inhibitors were developed as anti-tumor agents for thyroid cancers. Vandetanib, sorafenib, cabozantinib, and lenvatinib was approved drugs for thyroid cancer patients, and discovery and development processes of vandetanib and lenvatinib were discussed in this review.
Keywords: RET, thyroid cancer, vandetanib, lenvatinib, kinase inhibitor, ZD6474, E7080