Investigation of The Stability of 177LuPSMA-I&T Prostate-specific Membrane Antigen İnhibitor Used in The Treatment of Castration Resistant Prostate Cancer

Year 2021, Volume: 12 Issue: 2, 227 - 232, 20.08.2021

Ayşe Uğur Aziz Gültekin

Abstract

Objective: Internalization of the prostate-specific membrane antigen (PSMA) by ligand binding through clathrin-coated vesicle followed by endocytosis provides it an excellent target in prostate cancer imaging Gallium-68 (68Ga) and treatment Lutetium-177 (177Lu). The purpose of this research is to examine the in-vitro stability of the radiopharmaceutical (177LuPSMA-I&T) labeled with 177Lu of PSMA-I&T in saline.
Material-Method: Labeling of PSMA-I&T with 177Lu was carried out in the automated synthesis module. The labeled 200mCi (7.4 GBq) 177LuPSMA-I&T was incubated at 37oC for 72 hours. Samples taken at regular intervals up to 72 hours were analyzed by radio-high performance liquid chromatography (RP-HPLC). Results: The radiochemical efficiency of 177LuPSMA-I&T was > 99%. We determined that 177LuPSMA-I&T prepared with PSMA-I&T remained stable up to 6 hours, and deteriorated by 3.1% at the 24th hour. Conclusions: With the easy and fast labeled 177LuPSMA-I&T radiopharmaceutical is safe to use in treatment due to its stability in the first 6 hours.

Keywords

Prostate-specific membrane antigen, PSMA, 177LuPSMA-I&T, castration-resistant prostate cancer, radionuclide therapy

Kastrasyona Dirençli Prostat Kanseri Tedavisinde Kullanılan 177LuPSMA-I&T’nin İnvitro Stabilitesinin İncelenmesi

Abstract

Giriş: Prostat spesifik membran antijeni (PSMA), klatrin kaplı veziküller yoluyla hücreye bağlanır ve ardından endositoz yoluyla hücre içine girer. Bu özelliği nedeniyle, PSMA prostat kanseri görüntülemede Galyum-68 (68Ga) ve tedavide Lutesyum-177 (177Lu) ile işaretlenebilen mükemmel bir moleküldür. Çalışmanın amacı, PSMA-I&T'nin 177Lu ile işaretlenmiş radyofarmasötiğinin (177LuPSMA-I&T) serum fizyolojik içerisinde in-vitro stabilitesini incelemektir.
Materyal-Metod: PSMA-I&T'nin 177Lu ile işaretlemesi otomatik sentez modulünde gerçekleştirildi. İşaretlenmiş 200mCi (7,4 GBq) 177LuPSMA-I&T 37oC'de 72 saat inkübasyona bırakıldı. 72. saate kadar belirli aralıklarla alınan örnekler radyo-yüksek performanslı sıvı kromatografisi (RP-HPLC) ile analiz edildi.
Bulgular: 177LuPSMA-I&T'nin radyokimyasal verimi >% 99 bulundu. PSMA-I&T ile hazırlanan 177LuPSMA-I&T'nin ilk 6 saate kadar stabil kaldığı, 24. saatte ise stabilitesinde %3,3 oranında bozunumun başladığı, 48. saatten sonra ise kullanıma uygun olmadığı belirlendi.
Sonuç: 177LuPSMA-I&T ile tedavide radyofarmasötiğin ilk 6.saatteki stabilitesi nedeniyle görüntüleme ve tedavide kullanımının daha güvenli olduğu, gerektiğinde etiketlemeden sonraki 48 saate kadar kullanılabileceği sonucuna varılmıştır.

Keywords

Prostata spesifik membran antijeni, PSMA, 177LuPSMA-I&T, kastrasyona dirençli prostat kanseri, radyonüklid tedavisi

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