journal article·2026-07Open access

Gallium‐Containing Agents for Tumor Diagnosis and Therapy: Current Status and Future Prospects

Yue Han, Qi Li, Yufeng Zheng, Dandan Xia, Yongsheng Zhou

Small· Volume 22· Issue 39

Abstract

ABSTRACT Ga‐containing agents show great promise in tumor theranostics due to their unique physicochemical and biological features. Recent studies have extensively explored Ga‐containing radiopharmaceuticals, therapeutic compounds, and multifunctional formulations, clarifying their interactions with the tumor microenvironment and antitumor mechanisms. Clinically, Ga imaging agents, especially 68 Ga‐labeled probes, have become standard tools for precise diagnosis of prostate cancer, neuroendocrine tumors, and other malignancies, while Ga therapeutic agents act by interfering with DNA metabolism, regulating tumor immunity, and inhibiting angiogenesis. This review summarizes the current research status of Ga‐containing agents in tumor diagnosis and therapy, covering imaging/therapeutic mechanisms and clinical applications, and clarifies their advantages and limitations. To promote their clinical translation, future efforts should focus on AI‐assisted multimodal imaging, personalized theranostics, intelligent targeted delivery systems and standardized multicenter clinical promotion.
Source: crossref · Quality: baseline

Research context

OpenAlex topics: Nanoplatforms for cancer theranostics · Radiopharmaceutical Chemistry and Applications · Peptidase Inhibition and Analysis

SciVX discovery tags are terminology-based. OpenAlex topics are source-provided classifications.

Affiliations

Department of Prosthodontics Peking University School and Hospital of Stomatology & National Center for Stomatology & National Clinical Research Center for Oral Diseases & National Engineering Research Center of Oral Biomaterials and Digital Medical Devices & Beijing Key Laboratory of Digital Stomatology & Beijing Key Laboratory for Intelligent Biomanufacturing and Regeneration of Craniofacial Tissues & NHC Key Laboratory of Digital Stomatology Beijing China

School of Materials Science and Engineering Peking University Beijing China

Department of Dental Materials Peking University School and Hospital of Stomatology & National Center for Stomatology & National Clinical Research Center for Oral Diseases & National Engineering Research Center of Oral Biomaterials and Digital Medical Devices & Beijing Key Laboratory for Intelligent Biomanufacturing and Regeneration of Craniofacial Tissues & NHC Key Laboratory of Digital Stomatology & NMPA Key Laboratory for Dental Materials Beijing China

Funding

National Natural Science Foundation of China

References (100+)

Show source-provided references
1. 10.1186/s12943-023-01797-910.1186/s12943-023-01797-9 ↗
2. Synergism of Taxol and Gallium Nitrate in Human Breast Carcinoma Cells: Schedule Dependency
3. Lysosomal Accumulation of Gallium‐67 in Morris Hepatoma‐7316A and Shionogi Mammary Carcinoma‐115
4. 10.1097/RLU.000000000000201710.1097/RLU.0000000000002017 ↗
5. 10.1021/acsnano.2c0495610.1021/acsnano.2c04956 ↗
6. 10.1158/1535-7163.MCT-17-100910.1158/1535-7163.MCT-17-1009 ↗
7. 10.1038/s41467-024-51534-z10.1038/s41467-024-51534-z ↗
8. 10.1021/acs.jmedchem.2c0168410.1021/acs.jmedchem.2c01684 ↗
9. 10.3389/fonc.2023.127815710.3389/fonc.2023.1278157 ↗
10. 10.1038/s41580-023-00648-110.1038/s41580-023-00648-1 ↗
11. 10.3389/fimmu.2021.60769210.3389/fimmu.2021.607692 ↗
12. 10.1016/j.jinorgbio.2021.11141110.1016/j.jinorgbio.2021.111411 ↗
13. 10.1021/bi00271a01010.1021/bi00271a010 ↗
14. 10.1016/S0001-2998(78)80028-210.1016/S0001-2998(78)80028-2 ↗
15. Common Pathway for Tumor Cell Uptake of Gallium‐67 and Iron‐59 Via a Transferrin Receptor
16. 10.2147/IJN.S18112110.2147/IJN.S181121 ↗
17. 10.1039/D1NA00722J10.1039/D1NA00722J ↗
18. A Transferrin‐Mediated Uptake of Gallium‐67 By EMT‐6 Sarcoma. I. Studies in Tissue Culture
19. Inhibition of Gallium‐67 Uptake in Melanoma By an Anti‐Human Transferrin Receptor Monoclonal Antibody
20. 10.1378/chest.102.2.53010.1378/chest.102.2.530 ↗
21. 10.1158/1535-7163.MCT-06-028510.1158/1535-7163.MCT-06-0285 ↗
22. 10.1042/bj294087310.1042/bj2940873 ↗
23. 10.1038/nrm274510.1038/nrm2745 ↗
24. 10.1111/tra.1261310.1111/tra.12613 ↗
25. 10.1038/s41573-019-0036-110.1038/s41573-019-0036-1 ↗
26. 10.1021/acs.inorgchem.9b0056710.1021/acs.inorgchem.9b00567 ↗
27. 10.1016/j.jid.2023.01.03610.1016/j.jid.2023.01.036 ↗
28. 10.1158/0008-5472.CAN-18-160410.1158/0008-5472.CAN-18-1604 ↗
29. 10.3389/fimmu.2024.147277210.3389/fimmu.2024.1472772 ↗
30. 10.3390/ijms25181004710.3390/ijms251810047 ↗
31. 10.1093/clinchem/38.9.188310.1093/clinchem/38.9.1883 ↗
32. 10.1021/ic034009o10.1021/ic034009o ↗
33. 10.1159/00016360910.1159/000163609 ↗
34. A Comparative Study on Lysosomal Accumulation of Gallium‐67 and Indium‐111 in Morris Hepatoma 7316A
35. 10.1016/0047-0740(83)90079-710.1016/0047-0740(83)90079-7 ↗
36. 10.1021/acs.inorgchem.3c0039710.1021/acs.inorgchem.3c00397 ↗
37. 10.1007/s10534-024-00607-z10.1007/s10534-024-00607-z ↗
38. 10.1016/j.molmed.2020.11.00610.1016/j.molmed.2020.11.006 ↗
39. 10.20892/j.issn.2095-3941.2016.005510.20892/j.issn.2095-3941.2016.0055 ↗
40. Mechanism of Gallium‐67 Accumulation in Tumors
41. Comparison of Iron‐59, Indium‐111, and Gallium‐69 Transferrin as a Macromolecular Tracer of Vascular Permeability and the Transferrin Receptor
42. 10.3390/diagnostics801001610.3390/diagnostics8010016 ↗
43. 10.1097/MD.000000000001749110.1097/MD.0000000000017491 ↗
44. 10.1016/j.euf.2019.06.00810.1016/j.euf.2019.06.008 ↗
45. 10.1016/j.ijrobp.2024.07.13710.1016/j.ijrobp.2024.07.137 ↗
46. 10.1016/j.aace.2024.12.01110.1016/j.aace.2024.12.011 ↗
47. 10.5152/dir.2021.1942410.5152/dir.2021.19424 ↗
48. Gallium‐67‐Citrate Scanning for the Localization and Staging of Lymphomas
49. 10.1002/1097-0142(197601)37:1<250::AID-CNCR2820370134>3.0.CO;2-N10.1002/1097-0142(197601)37:1<250::AID-CNCR2820370134>3.0.CO;2-N ↗
50. 10.3816/CLM.2004.n.01110.3816/CLM.2004.n.011 ↗
51. 10.2214/ajr.145.4.67110.2214/ajr.145.4.671 ↗
52. 10.1016/j.ejrad.2007.03.00310.1016/j.ejrad.2007.03.003 ↗
53. 10.1016/S0022-5223(19)39617-510.1016/S0022-5223(19)39617-5 ↗
54. Accumulation and Localization of Gallium‐67 in Various Types of Primary Lung Carcinoma
55. 10.2214/ajr.147.5.91110.2214/ajr.147.5.911 ↗
56. Gallium‐67‐Citrate Scanning in Primary Cancer of the Liver: Diagnostic Value in the Presence of Cirrhosis and Relation to Alpha‐Fetoprotein
57. Correlation of Contrast Angiography and Histologic Pattern with Gallium Uptake in Primary Liver‐Cell Carcinoma: Noncorrelation with Alpha@Feto Protein. Concise Communication
58. 10.1097/00003072-199205000-0001010.1097/00003072-199205000-00010 ↗
59. Gallium Uptake in Benign Tumor of Liver: Case Report
60. 10.1148/116.3.67510.1148/116.3.675 ↗
61. Usefulness of Gallium Scintigraphy in Primary and Metastatic Breast Carcinoma
62. 10.1002/1097-0142(19880115)61:2<272::AID-CNCR2820610213>3.0.CO;2-V10.1002/1097-0142(19880115)61:2<272::AID-CNCR2820610213>3.0.CO;2-V ↗
63. 10.7326/0003-4819-97-5-69410.7326/0003-4819-97-5-694 ↗
64. Scintigraphy With Gallium‐67 Citrate in Staging of Soft‐Tissue Sarcomas of the Extremity
65. 10.1016/0090-4295(84)90353-410.1016/0090-4295(84)90353-4 ↗
66. 10.1097/00003072-198710000-0001410.1097/00003072-198710000-00014 ↗
67. 10.4103/0972-3919.12576010.4103/0972-3919.125760 ↗
68. Gallium‐67/Gallium‐68‐[DFO]‐Octreotide—a Potential Radiopharmaceutical for PET Imaging of Somatostatin Receptor‐Positive Tumors: Synthesis and Radiolabeling
69. 10.2214/AJR.11.729810.2214/AJR.11.7298 ↗
70. 10.1016/j.surg.2018.03.03010.1016/j.surg.2018.03.030 ↗
71. 10.1007/s00423-024-03254-710.1007/s00423-024-03254-7 ↗
72. 10.3390/jcm1106164110.3390/jcm11061641 ↗
73. 10.4274/mirt.galenos.2022.0692610.4274/mirt.galenos.2022.06926 ↗
74. 10.1097/JU.000000000000053110.1097/JU.0000000000000531 ↗
75. 10.4103/iju.iju_143_2410.4103/iju.iju_143_24 ↗
76. 10.1016/j.nucmedbio.2007.07.00310.1016/j.nucmedbio.2007.07.003 ↗
77. A Gallium‐Labeled DOTA‐α‐Melanocyte‐Stimulating Hormone Analog for PET Imaging of Melanoma Metastases
78. 10.1021/acs.molpharmaceut.2c0095710.1021/acs.molpharmaceut.2c00957 ↗
79. 10.3390/molecules2623727310.3390/molecules26237273 ↗
80. 10.3390/cancers1505156410.3390/cancers15051564 ↗
81. 10.1016/S0001-2998(79)80008-210.1016/S0001-2998(79)80008-2 ↗
82. Gallium‐67 Citrate Scanning—a New Adjunct in the Detection and Follow‐up of Extrapulmonary Tuberculosis: Concise Communication
83. Usefulness of Gallium‐67‐Citrate Scans in Patients With Acute Disseminated Tuberculosis and Comparison With Chest X‐Rays
84. 10.1053/j.semnuclmed.2022.07.00210.1053/j.semnuclmed.2022.07.002 ↗
85. 10.1016/j.cmi.2023.08.01010.1016/j.cmi.2023.08.010 ↗
86. 10.1007/s00330-022-09084-910.1007/s00330-022-09084-9 ↗
87. 10.1097/MNM.000000000000148110.1097/MNM.0000000000001481 ↗
88. 10.2214/ajr.174.4.174100510.2214/ajr.174.4.1741005 ↗
89. 10.1093/cid/cis19310.1093/cid/cis193 ↗
90. 10.2214/AJR.21.2732310.2214/AJR.21.27323 ↗
91. 10.1146/annurev-med-063014-12493610.1146/annurev-med-063014-124936 ↗
92. Technetium‐99m‐DTPA Aerosol and Gallium‐67 Scanning in Pulmonary Complications of Human Immunodeficiency Virus Infection
93. 10.1007/BF0316541710.1007/BF03165417 ↗
94. The Relationship Between the Tumor Uptake of Gallium‐67 and the Effect of Cisplatin‐Based Preoperative Chemotherapy or Chemoradiotherapy for Lung Cancer
95. 10.4103/ijnm.ijnm_193_2210.4103/ijnm.ijnm_193_22 ↗
96. 10.1021/mp400642s10.1021/mp400642s ↗
97. 10.1016/j.eprac.2023.12.00810.1016/j.eprac.2023.12.008 ↗
98. 10.1053/j.semnuclmed.2022.05.00210.1053/j.semnuclmed.2022.05.002 ↗
99. 10.1097/RLU.000000000000350210.1097/RLU.0000000000003502 ↗
100. 10.2967/jnumed.108.05722410.2967/jnumed.108.057224 ↗