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

Yıl 2021, Cilt: 12 Sayı: 2, 227 - 232, 20.08.2021

Ayşe Uğur , Aziz Gültekin

Öz

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.

Anahtar Kelimeler

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

Öz

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.

Anahtar Kelimeler

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

Kaynakça

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