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Drug Composition Matters: The Influence of Carrier Concentration on the Radiochemical Purity, Hydroxyapatite Affinity and In-Vivo Bone Accumulation of the Therapeutic Radiopharmaceutical 188Rhenium-HEDP

Drug Composition Matters: The Influence of Carrier Concentration on the Radiochemical Purity, Hydroxyapatite Affinity and In-Vivo Bone Accumulation of the Therapeutic Radiopharmaceutical 188Rhenium-HEDP

R Lange, J M H de Klerk, H J Bloemendal, R M Ramakers, F J Beekman, M M L van der Westerlaken, N H Hendrikse, R Ter Heine

Nucl Med Biol. 2015 May;42(5):465-469.

PMID: 25662844

Abstract:

Introduction:
(188)Rhenium-HEDP is an effective bone-targeting therapeutic radiopharmaceutical, for treatment of osteoblastic bone metastases. It is known that the presence of carrier (non-radioactive rhenium as ammonium perrhenate) in the reaction mixture during labeling is a prerequisite for adequate bone affinity, but little is known about the optimal carrier concentration.
Methods:
We investigated the influence of carrier concentration in the formulation on the radiochemical purity, in-vitro hydroxyapatite affinity and the in-vivo bone accumulation of (188)Rhenium-HEDP in mice.
Results:
The carrier concentration influenced hydroxyapatite binding in-vitro as well as bone accumulation in-vivo. Variation in hydroxyapatite binding with various carrier concentrations seemed to be mainly driven by variation in radiochemical purity. The in-vivo bone accumulation appeared to be more complex: satisfactory radiochemical purity and hydroxyapatite affinity did not necessarily predict acceptable bio-distribution of (188)Rhenium-HEDP.
Conclusions:
For development of new bisphosphonate-based radiopharmaceuticals for clinical use, human administration should not be performed without previous animal bio-distribution experiments. Furthermore, our clinical formulation of (188)Rhenium-HEDP, containing 10 μmol carrier, showed excellent bone accumulation that was comparable to other bisphosphonate-based radiopharmaceuticals, with no apparent uptake in other organs.
Advances in knowledge:
Radiochemical purity and in-vitro hydroxyapatite binding are not necessarily predictive of bone accumulation of (188)Rhenium-HEDP in-vivo.
Implications for patient care:
The formulation for (188)Rhenium-HEDP as developed by us for clinical use exhibits excellent bone uptake and variation in carrier concentration during preparation of this radiopharmaceutical should be avoided.

Chemicals Related in the Paper:

Catalog Number	Product Name	Structure	CAS Number	Price
AP13598657	Ammonium perrhenate		13598-65-7	Price

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