Cathepsin B-Activated Prodrug for Precision Tumor Theranostics.

Area of Science:

• Biomedical Engineering
• Nanotechnology
• Oncology

Background:

• Chemotherapeutic agents cause systemic toxicity.
• Tumor microenvironments are diverse.
• Targeted drug delivery is needed.

Purpose of the Study:

• To develop an innovative theranostic prodrug system, NM-001.
• To achieve targeted drug delivery and release.
• To establish a dual-channel optical feedback mechanism for monitoring.

Main Methods:

• NM-001 targets integrin α_νβ₃ on tumor cells using cRGD peptide.
• Cathepsin B cleaves GFLG peptide, releasing chlorambucil (CLB) and generating NM-002.
• Fluorescence transitions from green to near-infrared (NIR) for monitoring.

Main Results:

• NM-001 demonstrated high selectivity for tumor cells.
• NM-001 showed substantial antitumor efficacy in vitro and in vivo.
• Dual-channel optical feedback enabled real-time monitoring of drug delivery and release.

Conclusions:

• NM-001 is a promising theranostic prodrug system.
• It offers a novel approach for personalized cancer diagnosis and therapy.
• The dual-channel feedback mechanism allows precise monitoring at the cellular level.