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. 2021 Apr 8;22(8):3868. doi: 10.3390/ijms22083868

Table 1.

Summary of preclinical and clinical studies of radio-nanotargeted 188Re-(DXR)-liposome.

Preclinical Pharmacology, Therapeutic Effects and Safety Studies
No Animal Model Application Main Research Ref
1 C26 murine colon carcinoma Diagnosis Solid tumor, drug stability, imaging, PK, Bio-D [30]
2 HT-29 human colorectal adenocarcinoma Diagnosis Solid tumor, drug stability, imaging, PK, Bio-D, T/N ratio, autoradiogram [31]
3 C26 murine colon carcinoma Diagnosis Ascites meta, drug stability imaging, PK, Bio-D, autoradiogram [32]
4 F98 rat brain glioma Diagnosis Solid tumor, drug stability, imaging, PK, Bio-D, high T/N ratio, autoradiogram [33]
5 C26 murine colon carcinoma Therapy Solid tumor, PK, Bio-D, comparison 188Re-liposome/Lipo-DOX,
synergistic therapy effect of 188Re-DXR-liposome, histology		 [34]
6 C26 murine colon carcinoma Therapy Solid tumor, comparison 188Re-liposome/5-FU, safety, radiation effect [22]
7 C26 murine colon carcinoma Therapy Ascites meta, Imaging, PK, Bio-D, autoradiogram, comparison 188Re-liposome/Lipo-DOX, synergistic therapy effect of 188Re-DXR-liposome, histology [35]
8 C26 murine colon carcinoma Therapy Ascites meta, Imaging, PK, Bio-D, dosimetry, comparison 188Re-liposome/5-FU [36]
9 C26 murine colon carcinoma Therapy Lung meta, PK, Bio-D, dosimetry, excretion, comparison 188Re-liposome/5-FU [37]
10 LS-174T human colon adenocarcinoma Therapy Soild tumor, imaging, PK, Bio-D, dosimetry, comparison 188Re-liposome/5-FU [38]
11 4T1 murine breast cancer Therapy Orthotopic tumor, imaging, Bio-D, comparison 188Re-liposome/Lipo-DOX [39]
12 NCI-H292 non–small cell lung cancer Therapy Solid tumor, imaging, Bio-D, PK, comparison 188Re-liposome/188Re-BMEDA [40]
13 FaDu human hypopharyngeal carcinoma Therapy Orthotopic meta, imaging, Bio-D, PK, comparison 188Re-liposome/188Re-BMEDA [27]
14 ES-2-luc human ovarian cancer Therapy Ascites meta, imaging, comparison 188Re-liposome/188Re-BMEDA, radiation effect [23]
15 F98 rat brain glioma Therapy Solid tumor, dosimetry, histology, comparison 188Re-liposome/188Re-BMEDA [41]
16 C26 murine colon carcinoma Therapy Liver meta, imaging, combination of 188Re-liposome/Nexavar [42]
17 C26 murine colon carcinoma Therapy Solid tumor, Bio-D, PK, combination of 188Re-liposome/Lipo-Dox [43]
18 BE-3 human esophageal adenocarcinoma Therapy Solid tumor, imaging, Bio-D, safety, combination of 188Re-liposome/EBRT [44]
19 Acute toxicity of BMEDA in ICR mice Safety No Observed Adverse Effect Level (3 mg/kg) [45]
20 Acute toxicity of BMEDA in Beagle dog Safety No Observed Adverse Effect Level (2 mg/kg) [46]
21 Extended acute toxicity of 188Re-liposome in SD rat Safety No Observed Adverse Effect Level (185 MBq/kg) [47,48]
Clinical Safety and Therapeutic Effects Studies
1 Phase 0 eIND-metastatic tumors, 12 patients Safety Imaging, safety, dosimetry [29]
2 Low dose clinical trial for 2 ovarian cancer patients Therapy Safety, preliminary therapy evaluation, radiation effect [25]

Bio-D: Biodistribution; BMEDA: N,N-bis(2-mercaptoethyl)-N′,N′-diethyl-ethylenediamine; DXR: doxorubicin; EBRT: External beam radiotherapy; eIND: exploratory Investigational New Drug; ICR mice: Institute of Cancer Research mice; PK: Pharmacokinetics; SD rat: Sprague Dawley rat; T/N ratio:Tumor/Non-tumor ratio.