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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 29, 2026

Harnessing the Bioorthogonal Inverse Electron Demand Diels-Alder Cycloaddition for Pretargeted PET Imaging

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[¹⁶¹Tb]Tb-BPAMD as a High-Affinity Agent for Skeletal Targeting: Radiochemical and Biodistribution Insights.

Magdalena Radović¹, Pavle Sitarica¹, Dragana Stanković¹

¹"VINČA" Institute of Nuclear Sciences, National Institute of the Republic of Serbia, University of Belgrade, 11001 Belgrade, Serbia.

|March 28, 2026

Summary

The novel radiopharmaceutical [¹⁶¹Tb]Tb-BPAMD shows excellent bone targeting and stability for treating bone metastases. It offers improved selectivity over [¹⁷⁷Lu]Lu-BPAMD, making it a promising theranostic agent.

Keywords:

BPAMD DFT [161Tb]Tb-bisphosphonates biodistribution bone-targeting hydroxyapatite binding

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Published on: January 29, 2019

Area of Science:

Nuclear medicine
Radiopharmaceutical chemistry
Oncology

Background:

Bisphosphonate-based radiopharmaceuticals target skeletal metastases.
Terbium-161 (¹⁶¹Tb) offers Auger and conversion electron emission for enhanced dose delivery.
BPAMD is a DOTA-conjugated bisphosphonate suitable for bone targeting.

Purpose of the Study:

To evaluate [¹⁶¹Tb]Tb-BPAMD as a bone-targeted radiopharmaceutical.
To assess its theranostic and radiophysical advantages.
To compare its performance with [¹⁷⁷Lu]Lu-BPAMD.

Main Methods:

Radiolabeling of BPAMD with ¹⁶¹Tb and ¹⁷⁷Lu.
Assessment of radiochemical purity, physicochemical properties, and in vitro stability.
Hydroxyapatite (HAP) binding and in vivo biodistribution studies in rats.
Computational density functional theory (DFT) analyses.

Main Results:

[¹⁶¹Tb]Tb-BPAMD achieved >98% radiochemical yield with excellent stability (>97% at 48h) and strong HAP affinity (>98%).
Biodistribution showed high bone uptake (8.06% ID/g at 2h) and rapid blood clearance (<0.001% ID/g at 24h).
[¹⁶¹Tb]Tb-BPAMD demonstrated superior biodistribution selectivity compared to [¹⁷⁷Lu]Lu-BPAMD.

Conclusions:

[¹⁶¹Tb]Tb-BPAMD possesses excellent radiochemical and pharmacokinetic properties for bone targeting.
Its enhanced selectivity over [¹⁷⁷Lu]Lu-BPAMD highlights its potential.
This agent is a promising theranostic candidate for bone metastasis therapy.