Phase I study of [68Ga]Ga-HX01 for targeting integrin αvβ3 and CD13 in healthy and malignancy subjects.
Purpose: Noninvasive angiogenesis visualization is essential for evaluating tumor proliferation, progression, invasion, and metastasis. This study aimed to translate the heterodimeric PET tracer [68Ga]Ga-HX01, which targets integrin αvβ3 and CD13 in neovascularization, into phase I clinical study. M...
| Publicado en: | European Journal of Nuclear Medicine & Molecular Imaging Vol. 52; no. 4; pp. 1293 - 1305 |
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| Autores principales: | , , , , , , , , , |
| Formato: | Journal Article |
| Publicado: |
Springer Nature
Mar2025
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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=183131171&site=ehost-live header: @attributes: shortDbName: ccm uiTerm: 183131171 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: Mar2025 vid: 52 iid: 4 pid: 237 pub: Springer Nature place: New York, New York artinfo: ui: 183131171 181182700 10.1007/s00259-024-07002-3 183131171 ppf: 1293 ppct: 12 formats: fmt: – @attributes: type: T – @attributes: type: P tig: atl: Phase I study of [68Ga]Ga-HX01 for targeting integrin αvβ3 and CD13 in healthy and malignancy subjects. aug: au: Zhang, Xiao Fang, Hanyi Yang, Biao Qin, Chunxia Hu, Fan Ruan, Weiwei Chen, Jing Zeng, Dexing Gai, Yongkang Lan, Xiaoli affil: https://ror.org/00p991c53 Department of Nuclear Medicine, Union Hospital, Tongji Medical College, Huazhong University of Science and Technology, No. 1277 Jiefang Ave, 430022, Wuhan, Hubei, China sug: ab: Purpose: Noninvasive angiogenesis visualization is essential for evaluating tumor proliferation, progression, invasion, and metastasis. This study aimed to translate the heterodimeric PET tracer [68Ga]Ga-HX01, which targets integrin αvβ3 and CD13 in neovascularization, into phase I clinical study. Methods: This study enrolled 12 healthy volunteers (phase Ia) and 10 patients with malignant tumors (phase Ib). The subjects in phase Ia were divided into low-dose (0.05 mCi/kg) and high-dose (0.1 mCi/kg) groups. For phase Ia subjects, PET/CT images, blood and urine samples were collected to analyze the biodistribution, pharmacokinetics, radiation dosimetry, and safety of [68Ga]Ga-HX01. For phase Ib patients, PET/MR scans were performed at 30 ± 5 and 60 ± 5 min after injection. The safety and preliminary diagnostic value of [68Ga]Ga-HX01 were assessed. Results: In phase Ia study, [68Ga]Ga-HX01 was distributed and metabolized similarly in two dosage groups as the highest accumulations in kidneys and urine. It possessed quick renal excretion and blood clearance with an elimination half-life (T1/2) of 28.92 ± 3.97 min. The total effective dose was 2.14 × 10− 2 mSv/MBq. In phase Ib study, [68Ga]Ga-HX01 clearly detected the lesions per patient, and found a total of 59 lesions with varying uptake levels. For safety evaluation, no serious adverse events were observed during the examination. Conclusion: [68Ga]Ga-HX01 has proved to be a translational radiopharmaceutical with reliable security, favorable pharmacokinetics, and the ability to visualize tumors. The preliminary results in malignancy patients warrant further investigation of [68Ga]Ga-HX01 in monitoring antiangiogenic therapy of patients with malignancies. Clinical trial registration: ClinicalTrials.gov, NCT06416774. Registered 11 May, 2024. pubtype: Academic Journal doctype: Journal Article ougenre: Article language: English refInfo: holdings: @attributes: islocal: N |
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