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Article

Sublingual Atropine Administration as a Tool to Decrease Salivary Glands’ PSMA-Ligand Uptake: A Preclinical Proof of Concept Study Using [68Ga]Ga-PSMA-11

1
Centre Européen de Recherche en Imagerie Médicale (CERIMED), Aix-Marseille University, CNRS, 13005 Marseille, France
2
Radiopharmacy Department, Assistance Publique-Hôpitaux de Marseille, CHU La Timone, CHU Nord, 13005 Marseille, France
3
Centre de Recherche en Cardiovasculaire et Nutrition (C2VN), Aix-Marseille University, INSERM, INRAE, 13005 Marseille, France
4
Nuclear Medicine Department, Assistance Publique-Hôpitaux de Marseille, CHU La Timone, CHU Nord, 13005 Marseille, France
*
Author to whom correspondence should be addressed.
Academic Editor: Hongjing Dou
Pharmaceutics 2022, 14(6), 1276; https://doi.org/10.3390/pharmaceutics14061276
Received: 25 April 2022 / Revised: 6 June 2022 / Accepted: 13 June 2022 / Published: 16 June 2022
Prostate Specific Membrane Antigen (PSMA)-directed radionuclide therapy has gained an important role in the management of advanced castration-resistant prostate cancer. Although extremely promising, the prolongation in survival and amelioration of disease-related symptoms must be balanced against the direct toxicities of the treatment. Xerostomia is amongst the most common and debilitating of these, particularly when using an alpha emitter. It is therefore of main importance to develop new preventive strategies. This preclinical study has evaluated the effect of α-adrenergic and anticholinergic drugs on [99mTc]TcO4 Single Photon Emission Computed Tomography/Computed Tomography (SPECT/CT) and [68Ga]Ga-PSMA-11 Positron Emission Tomography (PET/CT). Methods: The effects of phenylephrine, scopolamine, atropine, and ipratropium on salivary glands uptake were evaluated in non-tumor-bearing mice by [99mTc]TcO4 microSPECT/CT. The most efficient identified strategy was evaluated in non-tumor-bearing and xenografted mice by [68Ga]Ga-PSMA-11 PET/CT. Results: Scopolamine and atropine showed a significant decrease in the parotid glands’ uptake on SPECT/CT whereas phenylephrine and ipratropium failed. Atropine premedication (sublingual route), which was the most effective strategy, also showed a drastic decrease of [68Ga]Ga-PSMA-11 salivary glands’ uptake in both non-tumor-bearing mice (−51.6% for the parotids, p < 0.0001) and human prostate adenocarcinoma xenografted mice (−26.8% for the parotids, p < 0.0001). Conclusion: Premedication with a local administration of atropine could represent a simple, safe, and efficient approach for reducing salivary glands’ uptake. View Full-Text
Keywords: PSMA; prostate-specific membrane antigen; salivary glands; atropine PSMA; prostate-specific membrane antigen; salivary glands; atropine
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MDPI and ACS Style

Nail, V.; Louis, B.; Moyon, A.; Chabert, A.; Balasse, L.; Fernandez, S.; Hache, G.; Garrigue, P.; Taïeb, D.; Guillet, B. Sublingual Atropine Administration as a Tool to Decrease Salivary Glands’ PSMA-Ligand Uptake: A Preclinical Proof of Concept Study Using [68Ga]Ga-PSMA-11. Pharmaceutics 2022, 14, 1276. https://doi.org/10.3390/pharmaceutics14061276

AMA Style

Nail V, Louis B, Moyon A, Chabert A, Balasse L, Fernandez S, Hache G, Garrigue P, Taïeb D, Guillet B. Sublingual Atropine Administration as a Tool to Decrease Salivary Glands’ PSMA-Ligand Uptake: A Preclinical Proof of Concept Study Using [68Ga]Ga-PSMA-11. Pharmaceutics. 2022; 14(6):1276. https://doi.org/10.3390/pharmaceutics14061276

Chicago/Turabian Style

Nail, Vincent, Béatrice Louis, Anaïs Moyon, Adrien Chabert, Laure Balasse, Samantha Fernandez, Guillaume Hache, Philippe Garrigue, David Taïeb, and Benjamin Guillet. 2022. "Sublingual Atropine Administration as a Tool to Decrease Salivary Glands’ PSMA-Ligand Uptake: A Preclinical Proof of Concept Study Using [68Ga]Ga-PSMA-11" Pharmaceutics 14, no. 6: 1276. https://doi.org/10.3390/pharmaceutics14061276

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