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Drug Distribution: Tissue Binding

Drug Distribution: Tissue Binding

Upon entering the systemic circulation, drugs can distribute into the interstitial and intracellular fluid of various tissue cells. This distribution is facilitated by the binding of drugs to different cellular components within tissues, which may lead to drug accumulation in specific areas. Drugs bound to tissue components serve as reservoirs that release free drugs back into the system, prolonging the drug's overall action. However, this accumulation can also result in local toxicity.
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Related Experiment Video

Updated: Mar 13, 2026

Automated Preparation of [68Ga]Ga-3BP-3940 on a Synthesis Module for PET Imaging of the Tumor Microenvironment

Automated Preparation of [⁶⁸Ga]Ga-3BP-3940 on a Synthesis Module for PET Imaging of the Tumor Microenvironment

Published on: April 25, 2025

Endoplasmic Reticulum Mediates Prolonged Tumor Retention of FAPI Radioconjugates and Enhanced Radiotherapeutic

Guoyu Wang¹, Fanglei Zhang¹, Daojia Liu¹

¹Department of Nuclear Medicine, Clinical Oncology School of Fujian Medical University affiliated with Fujian Cancer Hospital, Fuzhou, Fujian 350014, China.

Molecular Pharmaceutics

|March 11, 2026

Summary

This summary is machine-generated.

New radiotracers targeting fibroblast activation protein (FAP) and the endoplasmic reticulum (ER) show promise for radionuclide therapy. This dual-targeting approach significantly improves tumor retention and enhances radiotherapy efficacy.

Keywords:

endoplasmic reticulum fibroblast activation protein radioligand therapy retention time sequential targeting

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Pretargeted Radioimmunotherapy Based on the Inverse Electron Demand Diels-Alder Reaction

Pretargeted Radioimmunotherapy Based on the Inverse Electron Demand Diels-Alder Reaction

Published on: January 29, 2019

Area of Science:

Oncology
Radiochemistry
Molecular Imaging

Background:

Radiolabeled fibroblast activation protein inhibitors (FAPIs) are crucial for radionuclide therapy but suffer from limited tumor retention.
Existing methods to enhance FAPI retention often face challenges in clinical translation.

Purpose of the Study:

To develop a novel sequential targeting agent for enhanced tumor retention and radiotherapy efficacy.
To investigate the potential of endoplasmic reticulum (ER) targeting to prolong FAPI retention within tumors.

Main Methods:

Synthesis of a novel sequential targeting agent, FAPI-PEG3-K-PTSA, by conjugating an ER-targeting moiety (PTSA) to a FAPI core via a PEG3-K linker.
Radiolabeling of the compound with Lutetium-177 (177Lu) achieving high radiochemical yields (>95%).
Evaluation of cellular binding to FAP and ER localization, followed by in vivo studies to assess tumor uptake, retention, and therapeutic efficacy.

Main Results:

FAPI-PEG3-K-PTSA demonstrated specific binding to FAP and successful ER localization in cellular assays.
In vivo studies showed 3-5 fold higher tumor uptake and retention exceeding 72 hours compared to the FAPI-46 control.
The 177Lu-labeled compound achieved significant tumor suppression, highlighting its therapeutic potential.

Conclusions:

The developed sequential targeting strategy effectively prolongs intratumoral retention by utilizing FAP for initial tumor enrichment and ER-mediated internalization.
This approach overcomes rapid efflux, enhances radiotherapeutic outcomes, and offers a promising new direction for organelle-targeted radionuclide therapy.
The findings underscore the strong translational potential of organelle-targeted radionuclide therapy (TRT) for improved cancer treatment.