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Invest Radiol. 2000 Jan;35(1):50-7.

Development of a tumor-targeting MR contrast agent using the high-affinity folate receptor: work in progress.

Author information

  • 1Biomedical Magnetic Resonance Laboratory, College of Medicine, and the Beckman Institute, University of Illinois, Urbana-Champaign, USA.

Abstract

RATIONALE AND OBJECTIVES:

Macromolecular contrast agents enhance tumors by means of active or passive targeting. Active targeting requires surface receptors. Many tumors of epithelial origin express the high-affinity folate receptor (hFR), including ovarian tumors. The objective of this research was to enhance tumors that express hFR using macromolecular contrast agents conjugated to folic acid.

METHODS:

The authors prepared a folate-conjugated dendrimer polychelate by attaching folic acid to a fourth-generation ammonia-core polyamidoamine dendrimer. The remaining amines were reacted with 2-(4-isothiocyanatobenzyl)-6-methyldiethylenetriamine pentaacetic acid. Relaxivity measurements (r1 and r2) and MRI were conducted at 4.7 T.

RESULTS:

The dendrimer r2 exceeded that of Gd-HP-DO3A by 8.2 times at 4.7 T. It increased the tumor percentage contrast enhancement, 24 hours after injection, of T2-weighted images by 33%.

CONCLUSIONS:

This new agent accumulates in tumors expressing hFR. These results do not differentiate between active and passive targeting mechanisms. Receptor-negative tumors suggest a mechanism other than a nonspecific blood pool effect.

PMID:
10639036
[PubMed - indexed for MEDLINE]
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