Radiopharmaceuticals operate by combining radionuclides with carriers. The radiation energy emitted by radionuclides is utilized to selectively irradiate diseased tissues while minimizing damage to healthy tissues. In comparison to external beam radiation therapy, radionuclide drugs demonstrate research potential due to their biological targeting capabilities and reduced normal tissue toxicity. This article reviews the applications and research progress of radiopharmaceuticals in cancer treatment. Several key radionuclides are examined, including ²²³Ra, ⁹⁰Y, Lutetium-177 (¹⁷⁷Lu), ²¹²Pb, and Actinium-225 (²²⁵Ac). It also explores the current development trends of radiopharmaceuticals, encompassing the introduction of novel radionuclides, advancements in imaging technologies, integrated diagnosis and treatment approaches, and equipment-medication combinations. We review the progress in the development of new treatments, such as neutron capture therapy, proton therapy, and heavy ion therapy. Furthermore, we examine the challenges and breakthroughs associated with the clinical translation of radiopharmaceuticals and provide recommendations for the research and development of novel radionuclide drugs.
Humans ; Radiopharmaceuticals/therapeutic use* ; Neoplasms/radiotherapy* ; Radioisotopes/therapeutic use* ; Animals

OBJECTIVE: To investigate the feasibility of using thyroid ^99mTcO₄^- imaging ROI ratio instead of 24 h radioactive iodine uptake (RAIU) for estimating ¹³¹I dose in individualized treatment of hyperthyroidism. METHODS: We retrospectively analyzed the clinical data of 132 patients receiving ¹³¹I treatment in our department between January and June, 2019. According to their 3 h/24 h RAIU peak ratio, the patients were divided into peak forward (≥80%) group and no peak forward (< 80%) group. In the former group, the therapeutic ¹³¹I dose was calculated based the Marinelli formula (¹³¹I dose=thyroid mass×planned amount/24 h RAIU), and in the latter group, the correlation between the ROI ratio and the 24 h RAIU was analyzed, and the ¹³¹I dose was calculated using a modified Marinelli formula where 24 h RAIU was replaced by a converted ROI ratio. The two groups of patients were compared for antithyroid drug type and discontinuation time, thyroid hormones and related antibodies, thyroid area, thyroid mass and ¹³¹I dose. All the patients were and followed up for one year to analyze the treatment efficacy. The ROI ratios after the treatment were analyzed in the two groups using ROC curves. RESULTS: There was a significant positive correlation between the ROI ratio and 24 h RAUI in the no peak forward group (Y=58.13 + 0.2X, R²=0.118, P < 0.05), and the formula for calculating ¹³¹I dose was converted into: ¹³¹I dose=thyroid mass× planned amount/(58.13+0.2×ROI ratio)%. Before the treatment, therapeutic ¹³¹I dose, thyroid hormone levels, TRAb, 3 h and 24 h RAIU, thyroid area, thyroid mass, and ROI ratio all differed significantly between the two groups (P < 0.05). At 3 months after treatment, thyroid hormone levels, TRAb, TPOAb, thyroid area, thyroid mass, ROI ratio, response rate, hypothyroidism rate, cure rate, remission rate, and nonresponse rate were similar between two groups (P>0.05). At the 1-year follow-up, the composition ratios of hyperthyroidism, hypothyroidism and cured cases remained similar between two groups (P>0.05). ROC curve analysis showed that at 3 months after treatment, the optimal cutoff values of ROI ratio for predicting hyperthyroid recurrence and hypothyroidism were 15.79 and 6.33, respectively. CONCLUSION Thyroid ^99mTcO₄^- imaging ROI ratio can be used for calculating ¹³¹I dose in individualized treatment of hyperthyroidism and for prognostic evaluation of the patients.
Humans ; Iodine Radioisotopes/therapeutic use* ; Retrospective Studies ; Thyroid Neoplasms ; Hypothyroidism

Brachytherapy ; Carcinoma, Hepatocellular/drug therapy* ; Chemoembolization, Therapeutic ; Combined Modality Therapy ; Humans ; Iodine Radioisotopes ; Liver Neoplasms/drug therapy* ; Portal Vein ; Retrospective Studies ; Sorafenib/therapeutic use* ; Thrombosis ; Treatment Outcome

OBJECTIVE: To investigate the clinical application and efficacy of ¹²⁵Ⅰ radioactive seeds implantation in the treatment of recurrent salivary gland carcinoma after external radiotherapy. METHODS: From July 2004 to July 2016, 43 cases of recurrent salivary gland carcinoma of the neck after external radiotherapy or surgery combined with external radiotherapy were treated. According to the conventional segmentation radiotherapy for head and neck cancer (once a day, 1.8-2.0 Gy each time, 5 days per week), the cumulative radiation dose of the patients in this group was calculated. In the study, 26 patients received 50-60 Gy, 7 patients received less than 50 Gy, 4 patients received 60-70 Gy, and 6 patients received more than 80 Gy (range: 80-120 Gy). The interval between the last external irradiation and local recurrence was 4-204 months, and the median interval was 48 months. Among them, 25 cases were treated with ¹²⁵Ⅰ radioactive seeds implantation only and 18 cases were treated with ¹²⁵Ⅰ radioactive seeds implantation after operation. The prescription dose was 100-140 Gy. The control rate, survival rate and disease-free survival rate were recorded to evaluate the side effects. RESULTS: The median follow-up time was 27 months (ranging from 2.5 to 149.0 months). Among them, the median follow-up time of adenoid cystic carcinoma patients was 31 months (range: 2.5-112.0 months), and the median follow-up time of mucoepidermoid carcinoma patients was 18 months (range: 5-149 months). The local control rates for 1, 3 and 5 years were 66.5%, 48.8% and 42.7%, respectively. The 1-, 3- and 5- year survival rates were 88.0%, 56.7% and 45.8%, respectively. The disease-free survival rates of 1, 3 and 5 years were 58.3%, 45.4% and 38.1%, respectively. There was no statistically significant difference in local control rate, survival rate, and disease-free survival between the radioactive seeds implantation group and the radioactive seeds implantation group after surgical resection. There were 2 cases of acute radiation reaction Ⅰ/Ⅱ and 3 cases of reaction Ⅲ or above. In the late stage of radiotherapy, there were 8 cases with Ⅰ/Ⅱ grade reaction and 3 cases with Ⅲ grade or above reaction. The incidence of radiation reactions of Grade Ⅲ and above was 7%. CONCLUSION ¹²⁵Ⅰ radioactive seeds implantation provides an alternative method for the treatment of recurrent salivary gland carcinoma after external radiotherapy. The local control rate and survival rate are improved on the premise of low incidence of side effects.
Brachytherapy/adverse effects* ; Humans ; Iodine Radioisotopes/therapeutic use* ; Neoplasm Recurrence, Local/radiotherapy* ; Salivary Gland Neoplasms/radiotherapy* ; Salivary Glands

Adult ; Female ; Humans ; Hyperthyroidism ; drug therapy ; metabolism ; Iodine Radioisotopes ; pharmacokinetics ; therapeutic use ; urine ; Male ; Middle Aged ; Models, Biological ; Radiation Dosage ; Radiation Monitoring ; Radiopharmaceuticals ; pharmacokinetics ; therapeutic use ; urine ; Radiotherapy Dosage ; Young Adult

Bone metastases are the main driver of morbidity and mortality in advanced prostate cancer. Targeting the bone microenvironment, a key player in the pathogenesis of bone metastasis, has become one of the mainstays of therapy in men with advanced prostate cancer. This review will evaluate the data supporting the use of bone-targeted therapy, including (1) bisphosphonates such as zoledronic acid, which directly target osteoclasts, (2) denosumab, a receptor activator of nuclear factor-kappa B (RANK) ligand inhibitor, which targets a key component of bone stromal interaction, and (3) radium-223, an alpha-emitting calcium mimetic, which hones to the metabolically active areas of osteoblastic metastasis and induces double-strand breaks in the DNA. Denosumab has shown enhanced delay in skeletal-related events compared to zoledronic acid in patients with metastatic castration-resistant prostate cancer (mCRPC). Data are mixed with regard to pain control as a primary measure of efficacy. New data call into question dosing frequency, with quarterly dosing strategy potentially achieving similar effect compared to monthly dosing for zoledronic acid. In the case of radium-223, there are data for both pain palliation and improved overall survival in mCRPC. Further studies are needed to optimize timing and combination strategies for bone-targeted therapies. Ongoing studies will explore the impact of combining bone-targeted therapy with investigational therapeutic agents such as immunotherapy, for advanced prostate cancer. Future studies should strive to develop biomarkers of response, in order to improve efficacy and cost-effectiveness of these agents.
Bone Density Conservation Agents/therapeutic use* ; Bone Neoplasms/secondary* ; Denosumab/therapeutic use* ; Diphosphonates/therapeutic use* ; Endothelins/antagonists & inhibitors* ; Humans ; Male ; Prostatic Neoplasms/pathology* ; Protein Kinase Inhibitors/therapeutic use* ; Radioisotopes/therapeutic use* ; Radiopharmaceuticals/therapeutic use* ; Radium/therapeutic use* ; Samarium/therapeutic use* ; Strontium Radioisotopes/therapeutic use*

A 12-year-old girl presented with a history of cervical mass, and one week of throat discomfort and dyspnea. Five years ago, the patient was diagnosed as Hashimoto's thyroiditis and hyperthyroidism; she received antithyroid drug treatment, but the result was not satisfactory. B-ultrasonic showed that the size of thyroid gland was 8.1 cm×3.2 cm in the left and 8.2 cm×4.8 cm in the right. After iodine 131 combined with radiofrequency ablation (RFA) treatment, throat discomfort and recumbent breathing difficulties disappeared, and B-ultrasonic showed that the size of thyroid reduced to 2.3 cm×1.7 cm (left) and 2.8 cm×2.0 cm (right). No recurrence was observed during the two and a half years of follow-up.
Ablation Techniques ; methods ; Child ; Dyspnea ; etiology ; therapy ; Female ; Goiter ; complications ; diagnostic imaging ; pathology ; therapy ; Hashimoto Disease ; therapy ; Humans ; Hyperthyroidism ; therapy ; Iodine Radioisotopes ; therapeutic use ; Radio Waves ; therapeutic use ; Ultrasonography

Over 80% of the patients with prostate cancer (PCa) develop bone metastasis, which seriously affects the patients' quality of life and remains a major cause of morbidity. Radium-223 (Ra-223), a newly approved agent targeting bone metastasis of PCa, can improve the quality of life and prolong the overall survival of the PCa patients with bone metastasis. This article presents an overview of the clinical trials recently published on the management of bone metastasis of PCa with Ra-223.
Bone Neoplasms ; radiotherapy ; secondary ; Clinical Trials as Topic ; Humans ; Male ; Prostatic Neoplasms ; pathology ; Quality of Life ; Radioisotopes ; Radium ; therapeutic use

Objective To evaluate the impact of BRAF(V600E) gene status on clinical outcome of radioiodine((131)I) therapy in low-intermediate risk recurrent papillary thyroid carcinoma (PTC). Methods Totally 135 PTC patients were enrolled and divided into two groups according to BRAF(V600E) gene status:BRAF(V600E) mutation group(n=105) and BRAF(V600E) wild group(n=30). The median follow-up time was 2.16 years(1.03-4.06 years),and clinical outcome after initial (131)I ablation therapy was divided into excellent response(ER),acceptable response(AR),and incomplete response(IR) according to the serological and imageological follow-up results. The cinical outcomes were then compared between these two groups. Results There was no significant difference in clinicopathological features and initial radioactive iodine dose between BRAF(V600E) mutation and wild groups (P>0.05). ER,AR,and IR after (131)I ablation therapy accounted for 74.3%,20.0%,and 5.7% in BRAF(V600E) mutation group and 73.3%,20.0%,and 6.7% in BRAF(V600E) wild group,and no statistical difference was found (P=0.891). Conclusion For low-intermediate risk recurrent PTC,BRAF(V600E) gene status may have no impact on the response to (131)I ablation therapy,and thus this molecular feature should not be used as an independent weighting factor for risk assessment in this population.
Carcinoma ; genetics ; radiotherapy ; Carcinoma, Papillary ; Humans ; Iodine Radioisotopes ; therapeutic use ; Mutation ; Prognosis ; Proto-Oncogene Proteins B-raf ; genetics ; Thyroid Neoplasms ; genetics ; radiotherapy

Objective To dynamically observe the early change of thyroglobulin(Tg) levels after (131)I therapy in differentiated thyroid cancer(DTC) patients. Methods The study enrolled 22 post-total-thyroidectomy DTC patients and they were stratified as low to intermediate recurrence according to the 2009 American Thyroid Association Guidelines. The clinical data including pre-ablation stimulated Tg (ps-Tg),corresponding thyroid stimulating hormone(TSH),anti-thyroglobulin (TgAb) values,and the afterwards parameters were dynamically measured each week in the first month after (131)I therapy. Values collected at the first time were defined as Tg 0 and TSH0,while Tg1 and TSH1 were collected at the first week after (131)I therapy respectively. Then the variation trend curves of Tg were drawn,and factors influencing the variation of Tg were analyzed. Two groups were divided according to Tg levels:G1 (Tg≤0.1 ng/ml,n=9) and G2(Tg>0.1 ng/ml,n=13). Results The rates of negative Tg were 4.5%,18.0%,27.0%,36.0%,and 41.0%,respectively,exactly before (131)I therapy and the 1(st),2(nd),3(rd),and 4(th) week after the therapy. One-way analysis of variance showed that the two groups statistically differed in age (F=3.182,P=0.04) and remnant thyroid (U=4.849,P=0.026). Multivariate logistic regression analysis showed that early negative Tg was related to remnant thyroid tissue (OR:2.132;95%Cl:1.418- 6.532,P=0.009). Conclusions Negative Tg can be achieved in nearly half of DTC patients by the end of first month after (131)I therapy. The negative conversion is closely related with the volume of remnant thyroid tissue.
Autoantibodies ; blood ; Humans ; Iodine Radioisotopes ; therapeutic use ; Neoplasm Recurrence, Local ; Thyroglobulin ; blood ; Thyroid Neoplasms ; radiotherapy ; Thyroidectomy ; Thyrotropin ; blood