PT  - JOURNAL ARTICLE
AU  - JIRI JANOUSEK
AU  - PAVEL BARTA
AU  - ZBYNEK NOVY
AU  - KATERINA ZILKOVA
AU  - FRANTISEK TREJTNAR
TI  - Antiangiogenic Human Monoclonal Antibody Ramucirumab Radiolabelling: <em>In Vitro</em> Evaluation on VEGFR2-positive Cell Lines
AID  - 10.21873/anticanres.13170
DP  - 2019 Feb 01
TA  - Anticancer Research
PG  - 735--744
VI  - 39
IP  - 2
4099  - http://ar.iiarjournals.org/content/39/2/735.short
4100  - http://ar.iiarjournals.org/content/39/2/735.full
SO  - Anticancer Res2019 Feb 01; 39
AB  - Background/Aim: Radiolabelling of monoclonal antibodies (mAbs) could be beneficial in cancer diagnosis and therapy, however it may cause structural changes and consequently deteriorate their immunoreactivity. Materials and Methods: The therapeutic mAb ramucirumab (RAM) was technetium-99m labelled using either a direct or an indirect method with the use of two bifunctional chelating agents (HYNIC, DTPA). The radiochemical purity was assessed using instant thin-layer chromatography (ITLC) and high-performance liquid chromatography (HPLC) technique. The affinity of radiolabelled RAM was tested on human cancer cell lines. Results: The radiolabelling provided the following stable compounds: [99mTc]RAM, [99mTc]HYNIC-RAM and [99mTc]DTPA-RAM. Their radiochemical purity was over 95%. All prepared radiopharmaceuticals showed moderate affinity to the targeted receptor, in vitro. However, their affinity was one order lower compared to that of the natural mAb. Moreover, directly and DTPA-radiolabelled RAM demonstrated less favourable binding kinetics. Conclusion: Radiolabelling negatively affected the affinity of RAM to its targeted receptor.