Radiolabelled tyrosine kinase inhibitors for the development of molecules of pharmacological interest

Objective of the project is the development of radiolabeled tyrosine kinase inhibitors that could be potentially used as radiopharmaceutical drugs for epidermal growth factor receptor family (Erb B) and specifically EGFR.

EGFR is overexpressed in a variety of tumors and involved in several signaling pathways regulating various cellular functions associated with carcinogenesis, metastasis, uncontrollable cell proliferation and resistance to some therapeutic methods. The EGFR inhibitors’ radiolabeling is among interesting issues of Radiopharmaceutical Chemistry, contributing to a valid diagnosis of tumors overexpressing EGFR and its metastases, used to monitor the patient’s response to the proposed treatment and to determine the appropriate treatment.

Following this perspective, the dissertation aims to develop radiolabeled EGFR inhibitors with radioisotopes used in Νuclear Μedicine for diagnosis and treatment. The inhibitors are either analogues of 4-anilinoquinazoline core or other structures used in Pharmaceutical Chemistry. The new analogues are evaluated as potential radiopharmaceuticals by in vitro studies, stability and lipophilicity studies as well as in vivo pharmacokinetic and / or imaging studies on experimental animals.

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