Drug intelligence / Profile preview

yttrium-90 biotin

Development stage
Unknown
Modality
Small Molecules, Antibody-Radionuclide Conjugates → Antibody Conjugates → Antibody-Based Therapeutics
Administration
Intravenous
01

Overview

Yttrium-90 biotin is a radiopharmaceutical used as the therapeutic component of a pre-targeted three-step radioimmunotherapy (RIT) protocol. This approach, often referred to as the Milan protocol, involves the sequential administration of a biotinylated monoclonal antibody (such as anti-tenascin), followed by avidin and streptavidin to clear circulating antibody and provide high-affinity binding sites at the tumor, and finally yttrium-90 biotin. The biotin moiety binds to the pre-localized avidin/streptavidin complex with extremely high affinity (Kd ≈ 10^-15 M). Once localized, the yttrium-90 isotope delivers high-energy beta radiation to the tumor mass, inducing cell death primarily through DNA damage. This pre-targeting strategy is designed to maximize the radiation dose delivered to the tumor while minimizing systemic exposure and hematological toxicity, particularly to the red marrow, by allowing for rapid renal clearance of unbound radiolabeled biotin.

Other names
yttrium-90-labelled biotinyttrium90-labelled biotinyttrium 90-labelled biotinY-90 biotinY90 biotinY 90 biotin
02

Targets

DNA

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