Preliminary evaluation of a novel PSMA-targeting radiopharmaceutical [68Ga]Ga/[177Lu]Lu–NYM032 for theranostic use in prostate cancer.
Purpose: A novel theranostic radiopharmaceutical targeting prostate-specific membrane antigen (PSMA), [68Ga]Ga/[177Lu]Lu–NYM032, was developed and its diagnostic and therapeutic potential in the treatment of prostate cancer (PCa) was preliminarily evaluated. Methods: The diagnostic efficacy of the P...
| Publicado en: | European Journal of Nuclear Medicine & Molecular Imaging Vol. 52; no. 5; pp. 1671 - 1685 |
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| Autores principales: | , , , , , , , , , |
| Formato: | Journal Article |
| Publicado: |
Springer Nature
Apr2025
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| Acceso en línea: | Ver este registro en EBSCOhost |
| fields | @attributes: recordID: 1 pdfLink: plink: https://search.ebscohost.com/login.aspx?direct=true&db=ccm&AN=183974330&site=ehost-live header: @attributes: shortDbName: ccm uiTerm: 183974330 longDbName: CINAHL Complete uiTag: AN controlInfo: bkinfo: dissinfo: jinfo: jid: 16197070 NPC jtl: European Journal of Nuclear Medicine & Molecular Imaging issn: 16197070 maglogo: N pubinfo: dt: Apr2025 vid: 52 iid: 5 pid: 237 pub: Springer Nature place: New York, New York artinfo: ui: 183974330 182036220 10.1007/s00259-024-07046-5 183974330 ppf: 1671 ppct: 14 formats: fmt: – @attributes: type: T – @attributes: type: P tig: atl: Preliminary evaluation of a novel PSMA-targeting radiopharmaceutical [68Ga]Ga/[177Lu]Lu–NYM032 for theranostic use in prostate cancer. aug: au: Fu, Haitian He, Huihui Wang, Yanjuan Li, Wenjin Luo, Yihui Chen, Liping Mi, Yuanyuan Sun, Chengwen Mao, Yong Yu, Chunjing affil: https://ror.org/02ar02c28 Department of Nuclear Medicine, Affiliated Hospital of Jiangnan University, No. 1000, Hefeng Road, 214000, Wuxi, Jiangsu Province, China sug: ab: Purpose: A novel theranostic radiopharmaceutical targeting prostate-specific membrane antigen (PSMA), [68Ga]Ga/[177Lu]Lu–NYM032, was developed and its diagnostic and therapeutic potential in the treatment of prostate cancer (PCa) was preliminarily evaluated. Methods: The diagnostic efficacy of the PET tracer [68Ga]Ga–NYM032 was first evaluated in PSMA-positive xenograft-bearing models (LNCaP models), followed by evaluation in 10 PCa patients using [68Ga]Ga–PSMA617 a comparator. Finally, the therapeutic potential of [177Lu]Lu–NYM032 was evaluated in LNCaP models. Results: [68Ga]Ga/[177Lu]Lu–NYM032 was well-tolerated, and no adverse events were observed in the preclinical and clinical studies. [68Ga]Ga–NYM032 demonstrated PSMA specificity and high radioactive uptake in LNCaP tumors. [68Ga]Ga–NYM032 uptake (SUVmax) did not differ from [68Ga]Ga–PSMA617 uptake in the same in situ lesions at the same p.i. time point (median 9.40 vs. 6.85, P = 0.123, n = 8). Compared with [68Ga]Ga–PSMA617 uptake, [68Ga]Ga–NYM032 uptake was significantly higher in osseous metastases (median 5.10 vs. 3.88, P < 0.001, n = 48), and higher in lymph node metastases (median 7.81 vs. 5.46, n = 2). [177Lu]Lu–NYM032 showed high aggregation in the lesions of LNCaP models and long retention times. [177Lu]Lu–NYM032 could inhibit tumor progression in LNCaP models, and its therapeutic efficiency strengthened with increasing radio-dosage (18.5–74 MBq/mouse). The tumor volume in the high radio-dosage treatment group (74 MBq/mouse) was significantly smaller than that in the blank control group at 21 days p.i. (107.14 ± 13.68 mm3 vs. 1351.86 ± 249.98 mm3, P < 0.001, n = 7). Conclusion: [68Ga]Ga/[177Lu]Lu-NYM032 has considerable potential as a novel and powerful theranostic radiopharmaceutical for PCa. Trial registration: The clinical evaluation of this study was registered at Clinicaltrial.gov (NCT06389695) on 29 Apr, 2024. pubtype: Academic Journal doctype: Journal Article ougenre: Article language: English refInfo: holdings: @attributes: islocal: N |
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