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Peer-reviewedCC BY-NC-ND 4.0ACS Omega

Synthesis and Preliminary Biological Evaluation of a Structurally Modified Niraparib-Based PARP-Targeted PET Tracer for Tumor Imaging

  • Jia Deng1,2,3
  • Die You1,2,3
  • Chunfang Zhang1,2,3
  • Chunmei Tian1,2,3
  • Xiangting Liu1,2,3
  • Xiaolu Dou1,2,3
  • Yan Zhao1,2,3
  • Yue Chen1,2,3
  1. 1Affiliated Hospital of Southwest Medical University , , No. 25, Taiping St. , , ,
  2. 2Nuclear Medicine and Theranostics Key Laboratory of Sichuan Province , No. 25, Taiping St. , , ,
  3. 3Southwest Medical University , , No. 25, Taiping St. , , ,
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Abstract

Poly(ADP-ribose) polymerase (PARP) is highly expressed in various malignancies and represents an important therapeutic target. Noninvasive evaluation of PARP expression is therefore of potential clinical significance for patient stratification. In this study, we developed and evaluated [68Ga]Ga-DOTA-MK-4827, a structurally modified PARP-targeted radiotracer derived from niraparib, featuring a two-carbon linker between the DOTA chelator and the pharmacophore. [68Ga]Ga-DOTA-MK-4827 demonstrated high uptake in MDA-MB-231 and OE-19 tumors with elevated PARP-1 expression, which was significantly reduced by blocking, supporting a PARP-related component of tumor accumulation. The tracer exhibited favorable pharmacokinetics, including high hydrophilicity and predominantly renal clearance, resulting in low abdominal background activity. Positron emission tomography (PET) imaging enabled clear tumor visualization with good contrast, supported by biodistribution findings. Preliminary clinical imaging further showed notable uptake in an esophageal cancer lesion, with immunohistochemical confirmation of PARP-1 expression in the biopsied tissue. These results suggest that [68Ga]Ga-DOTA-MK-4827 has potential as a PARP-targeted PET tracer for tumor imaging and merits further investigation in larger clinical cohorts.

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Cite

BibTeXRIS
BibTeX
@article{deng2026synthesis,
  title = {{Synthesis and Preliminary Biological Evaluation of a Structurally Modified Niraparib-Based PARP-Targeted PET Tracer for Tumor Imaging}},
  author = {Jia Deng and Die You and Chunfang Zhang and Chunmei Tian and Xiangting Liu and Xiaolu Dou and Yan Zhao and Yue Chen},
  journal = {ACS Omega},
  year = {2026},
  month = oct,
  doi = {10.1021/acsomega.6c08307},
  url = {https://pubs.acs.org/acsodf/article/11/41/63933/5447643/Synthesis-and-Preliminary-Biological-Evaluation-of},
  note = {CC BY-NC-ND 4.0},
}
RIS
TY  - JOUR
TI  - Synthesis and Preliminary Biological Evaluation of a Structurally Modified Niraparib-Based PARP-Targeted PET Tracer for Tumor Imaging
AU  - Jia Deng
AU  - Die You
AU  - Chunfang Zhang
AU  - Chunmei Tian
AU  - Xiangting Liu
AU  - Xiaolu Dou
AU  - Yan Zhao
AU  - Yue Chen
PY  - 2026
DA  - 2026/10/09
JO  - ACS Omega
DO  - 10.1021/acsomega.6c08307
UR  - https://pubs.acs.org/acsodf/article/11/41/63933/5447643/Synthesis-and-Preliminary-Biological-Evaluation-of
AB  - Poly(ADP-ribose) polymerase (PARP) is highly expressed in various malignancies and represents an important therapeutic target. Noninvasive evaluation of PARP expression is therefore of potential clinical significance for patient stratification. In this study, we developed and evaluated [68Ga]Ga-DOTA-MK-4827, a structurally modified PARP-targeted radiotracer derived from niraparib, featuring a two-carbon linker between the DOTA chelator and the pharmacophore. [68Ga]Ga-DOTA-MK-4827 demonstrated high uptake in MDA-MB-231 and OE-19 tumors with elevated PARP-1 expression, which was significantly reduced by blocking, supporting a PARP-related component of tumor accumulation. The tracer exhibited favorable pharmacokinetics, including high hydrophilicity and predominantly renal clearance, resulting in low abdominal background activity. Positron emission tomography (PET) imaging enabled clear tumor visualization with good contrast, supported by biodistribution findings. Preliminary clinical imaging further showed notable uptake in an esophageal cancer lesion, with immunohistochemical confirmation of PARP-1 expression in the biopsied tissue. These results suggest that [68Ga]Ga-DOTA-MK-4827 has potential as a PARP-targeted PET tracer for tumor imaging and merits further investigation in larger clinical cohorts.
SN  - 2470-1343
ER  -