SPECT and PET radiopharmaceuticals for molecular imaging of apoptosis: from bench to clinic

Xiaobo Wang, Han Feng, Shichao Zhao, Junling Xu, Xinyu Wu, Jing Cui, Ying Zhang, Yuhua Qin, Zhiguo Liu, Tang Gao, Yongju Gao and Wenbin Zeng _

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Oncotarget. 2017; 8:20476-20495. https://doi.org/10.18632/oncotarget.14730

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Xiaobo Wang1,2, Han Feng3, Shichao Zhao4, Junling Xu1, Xinyu Wu1, Jing Cui1, Ying Zhang1, Yuhua Qin3, Zhiguo Liu2,5, Tang Gao2, Yongju Gao1 and Wenbin Zeng2

1 Department of Nuclear Medicine, Henan Provincial People’s Hospital and People’s Hospital of Zhengzhou University, Zhengzhou, China

2 Xiangya School of Pharmaceutical Sciences and Molecular Imaging Research Center, Central South University, Changsha, China

3 Department of Pharmacy, Henan Provincial People’s Hospital and People’s Hospital of Zhengzhou University, Zhengzhou, China

4 Department of Cardiology, Henan Provincial People’s Hospital and People’s Hospital of Zhengzhou University, Zhengzhou, China

5 Department of Nuclear Medicine, Shandong Cancer Hospital and Institute, Shandong University, Jinan, China

Correspondence to:

Wenbin Zeng, email:

Yongju Gao, email:

Keywords: SPECT, PET, radiopharmaceuticals, apoptosis, clinical status

Received: November 02, 2016 Accepted: January 09, 2017 Published: January 18, 2017


Owing to the central role of apoptosis in many human diseases and the wide-spread application of apoptosis-based therapeutics, molecular imaging of apoptosis in clinical practice is of great interest for clinicians, and holds great promises. Based on the well-defined biochemical changes for apoptosis, a rich assortment of probes and approaches have been developed for molecular imaging of apoptosis with various imaging modalities. Among these imaging techniques, nuclear imaging (including single photon emission computed tomography and positron emission tomography) remains the premier clinical method owing to their high specificity and sensitivity. Therefore, the corresponding radiopharmaceuticals have been a major focus, and some of them like 99mTc-Annexin V, 18F-ML-10, 18F-CP18, and 18F-ICMT-11 are currently under clinical investigations in Phase I/II or Phase II/III clinical trials on a wide scope of diseases. In this review, we summarize these radiopharmaceuticals that have been widely used in clinical trials and elaborate them in terms of radiosynthesis, pharmacokinetics and dosimetry, and their applications in different clinical stages. We also explore the unique features required to qualify a desirable radiopharmaceutical for imaging apoptosis in clinical practice. Particularly, a perspective of the impact of these clinical efforts, namely, apoptosis imaging as predictive and prognostic markers, early-response indicators and surrogate endpoints, is also the highlight of this review.

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