Drug intelligence / Profile preview

yttrium-90 lintuzumab

Development stage
Phase 1
Lead developer
Actinium Pharmaceuticals
Modality
Antibody-Radionuclide Conjugates → Antibody Conjugates → Antibody-Based Therapeutics, Beta-minus Emitters → Radiopharmaceuticals, Monoclonal Antibodies → Antibody-Based Therapeutics
Administration
Intravenous
01

Overview

Yttrium-90 lintuzumab is a radioimmunoconjugate consisting of the humanized monoclonal antibody lintuzumab (HuM195) labeled with the beta-emitting radioisotope yttrium-90 ($^{90}$Y), typically via a chelator such as DOTA. Lintuzumab specifically targets the CD33 antigen, a 67-kDa transmembrane glycoprotein expressed on the surface of most myeloid leukemia cells and normal myeloid progenitors, but absent from non-hematopoietic tissues and pluripotent hematopoietic stem cells. Upon binding to CD33, the yttrium-90 isotope delivers localized high-energy beta radiation to the target cell and surrounding cells within the range of the beta particles (the "crossfire effect"). This radiation induces double-strand DNA breaks, leading to apoptosis. It has been primarily investigated for the treatment of acute myeloid leukemia (AML), particularly as a part of conditioning regimens or for the elimination of minimal residual disease.

Other names
yttrium Y 90 lintuzumabY-90 lintuzumabY90 lintuzumabY 90 lintuzumabHuM195-Y90HuM-195-Y90HuM 195-Y90
02

Targets

CD33 (Myeloid cell surface antigen CD33)DNA

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