Molecular probes for multimodality imaging of anionic membrane surfaces

US9211349B2 · kind B2 · utility

Assignee

• Molecular Targeting Technologies, Inc. · US

Inventors

• Brian D. Gray · Exton, US
• Kai Chen · Rockville, US
• Koon Y. Pak · Malvern, US

Key dates

• Filing date: Jun 4, 2013
• Grant date: Dec 15, 2015
• Expiry date: Oct 4, 2033

Classification

• Technology area (CPC A): Human Necessities
• CPC primary: A61B6/037
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

Embodiments provide dual modality probes for imaging phosphatidylserine (PS) exposure and other anionic membrane surfaces. In various embodiments, the probes were constructed by utilizing a) the high selectivity of synthetic zinc (II) dipicolylamine coordination complexes (Zn-DPA) for targeting externalized PS which over-expresses in apoptotic and necrotic cells, b) a near-infrared (NIR) dye for optical imaging, and c) a widely used clinically approved radionuclide for PET (or SPECT) imaging. A variety of linking elements were incorporated into the probes between the Zn-DPA and radionuclide motif to modulate the pharmacokinetics. The in vitro and in vivo data of radiolabeled dipicolylamine probes demonstrated their utilities for imaging PS exposure with multiple imaging modalities.