Targeted Radiotheranostic For Diagnosis And Treatment Of Integrin Expressing Cancers
EBRGD
(177Lu-DOTA-EB-TATE and 225Ac-DOTA-EB-TATE)
EBRGD is a radiotherapeutic based on the EvaThera theranostic platform. EBRGD uses Evans blue dye to better target αvβ3-integrin expressing tumors in glioblastoma multiforme (GBM) and Non-Small-Cell Lung Cancer (NSCLC). Early studies investigating proof of concept demonstrated that tumor uptake was markedly improved over NOTA- or DOTA-RGD conjugates without Evans blue. Additionally, 64Cu-EBRGD proved effective for evaluating glioma grading and demarcation in preoperative patients with diverse glioma grades.
177Lu EBRGD has also been shown to synergistically extend survival and drecrease colorectal tumor volume when used in tandem with a PD-L1 checkpoint inhibit or immunotherapy.
EBRGD Benefits
Longer
Circulation
EBRGD demonstrated longer circulation half-life and enhanced tumor accumulation.
Precise Tumor Uptake
EBRGD accumulated in brain tumors that are rich in integrin αvβ3 and other neovasculature markers, but not in non-targeted structures.
Improved Targeting
Conversely, EBRGD did not accumulate in unrelated structures, including the brain parenchyma (excluding the choroid plexus).
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Data & Literature
EBRGD is a highly specific technology, targeting only αvβ3-integrin rich brain tumors, and has extended tumor exposure – it can still be seen circulating in the body at 24 hours post-injection.*
References –
*EBRGD Handout, data on file.
Photo courtesy of Jing jing Zhang and Zhaohui Zhu, private communication
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