1.Sclera Vessel Segmentation Based on Fusion Filtering and Reflection Suppression
Ming-Xuan FAN ; Zong-Qing MA ; Chu-Xiang GAO ; Yi-Xuan SHI ; Zi-Hang ZHANG ; Zhe-Xuan JIA ; Fan FAN ; Guo-Liang HUANG ; Jiang ZHU
Progress in Biochemistry and Biophysics 2026;53(5):1195-1206
ObjectiveIn traditional Chinese medicine (TCM), the foundational doctrine that the eyes reflect the essence of the internal viscera establishes ocular observation as a cornerstone of diagnostic practice. Specifically, the morphological characteristics and coloration variations of the scleral microvasculature serve as critical clinical indicators for assessing the dynamic balance of Qi and Blood, as well as the pathological status of internal organs. Historically, however, TCM eye diagnosis has relied predominantly on the subjective clinical experience and visual acuity of individual practitioners, leading to inherent challenges in standardization and reproducibility. While automated computer-aided diagnostic systems offer a promising solution, existing vessel segmentation algorithms encounter significant domain-specific bottlenecks when applied to scleral imagery. These challenges primarily stem from the highly reflective and moist nature of the ocular surface, which generates severe reflective interference. Furthermore, the inherent low contrast of fine capillary networks against complex background textures, compounded by non-uniform illumination, frequently results in high false-positive rates, misdetections, and severe vessel fragmentation. To address these critical limitations and advance the objective quantification of TCM diagnostics, this paper proposes a novel, highly robust sclera vessel segmentation framework that innovatively integrates Frangi-Sato dual-filter adaptive enhancement with pixel-level reflection detection. MethodsThe proposed methodology systematically addresses the segmentation pipeline through three synergistic stages. First, to overcome the structural limitations of single-filter approaches, a multi-scale weighted fusion strategy is meticulously designed to harness the complementary extraction capabilities of both Frangi and Sato filters. This adaptive enhancement optimally balances the preservation of main vessel trunk continuity with the heightened sensitivity required for delineating delicate, low-contrast peripheral capillaries. Second, to tackle the persistent issue of reflective highlights, a sophisticated multi-feature synergistic reflection detection module is introduced. By jointly analyzing local information entropy, gradient field variations, and intensity statistical distributions, this module achieves precise, pixel-level identification and elimination of reflective artifacts without compromising the underlying vascular structures. Finally, a dual-level adaptive thresholding strategy, featuring an innovative “core protection” mechanism, is implemented. This critical step effectively suppresses complex background noise while rigorously preserving the structural and topological integrity of the intricate vessel network, preventing the structural breaks often seen in conventional binarization methods. ResultsThe efficacy of the proposed framework was rigorously evaluated using both self-constructed clinical datasets specifically acquired for TCM research and standardized public datasets. Extensive experimental results demonstrate that the proposed method consistently outperforms state-of-the-art traditional approaches and contemporary deep learning models. Specifically, the proposed method achieves a Dice similarity coefficient of approximately 0.71 on the private clinical dataset, and secures the best performance across the majority of quantitative metrics on both datasets. Notably, the framework exhibits exceptional robustness and generalization capabilities in highly challenging scenarios characterized by intense reflective interference, low signal-to-noise ratios, and cross-domain image variations. ConclusionThis study successfully realizes the high-integrity, automated segmentation of scleral vessel networks under complex clinical imaging conditions. By overcoming the fundamental algorithmic challenges of reflection interference and micro-vessel loss, the proposed methodology provides potential support for the digitization, objective standardization, and intelligent advancement of modern TCM eye diagnosis systems.
2.Sclera Vessel Segmentation Based on Fusion Filtering and Reflection Suppression
Ming-Xuan FAN ; Zong-Qing MA ; Chu-Xiang GAO ; Yi-Xuan SHI ; Zi-Hang ZHANG ; Zhe-Xuan JIA ; Fan FAN ; Guo-Liang HUANG ; Jiang ZHU
Progress in Biochemistry and Biophysics 2026;53(5):1195-1206
ObjectiveIn traditional Chinese medicine (TCM), the foundational doctrine that the eyes reflect the essence of the internal viscera establishes ocular observation as a cornerstone of diagnostic practice. Specifically, the morphological characteristics and coloration variations of the scleral microvasculature serve as critical clinical indicators for assessing the dynamic balance of Qi and Blood, as well as the pathological status of internal organs. Historically, however, TCM eye diagnosis has relied predominantly on the subjective clinical experience and visual acuity of individual practitioners, leading to inherent challenges in standardization and reproducibility. While automated computer-aided diagnostic systems offer a promising solution, existing vessel segmentation algorithms encounter significant domain-specific bottlenecks when applied to scleral imagery. These challenges primarily stem from the highly reflective and moist nature of the ocular surface, which generates severe reflective interference. Furthermore, the inherent low contrast of fine capillary networks against complex background textures, compounded by non-uniform illumination, frequently results in high false-positive rates, misdetections, and severe vessel fragmentation. To address these critical limitations and advance the objective quantification of TCM diagnostics, this paper proposes a novel, highly robust sclera vessel segmentation framework that innovatively integrates Frangi-Sato dual-filter adaptive enhancement with pixel-level reflection detection. MethodsThe proposed methodology systematically addresses the segmentation pipeline through three synergistic stages. First, to overcome the structural limitations of single-filter approaches, a multi-scale weighted fusion strategy is meticulously designed to harness the complementary extraction capabilities of both Frangi and Sato filters. This adaptive enhancement optimally balances the preservation of main vessel trunk continuity with the heightened sensitivity required for delineating delicate, low-contrast peripheral capillaries. Second, to tackle the persistent issue of reflective highlights, a sophisticated multi-feature synergistic reflection detection module is introduced. By jointly analyzing local information entropy, gradient field variations, and intensity statistical distributions, this module achieves precise, pixel-level identification and elimination of reflective artifacts without compromising the underlying vascular structures. Finally, a dual-level adaptive thresholding strategy, featuring an innovative “core protection” mechanism, is implemented. This critical step effectively suppresses complex background noise while rigorously preserving the structural and topological integrity of the intricate vessel network, preventing the structural breaks often seen in conventional binarization methods. ResultsThe efficacy of the proposed framework was rigorously evaluated using both self-constructed clinical datasets specifically acquired for TCM research and standardized public datasets. Extensive experimental results demonstrate that the proposed method consistently outperforms state-of-the-art traditional approaches and contemporary deep learning models. Specifically, the proposed method achieves a Dice similarity coefficient of approximately 0.71 on the private clinical dataset, and secures the best performance across the majority of quantitative metrics on both datasets. Notably, the framework exhibits exceptional robustness and generalization capabilities in highly challenging scenarios characterized by intense reflective interference, low signal-to-noise ratios, and cross-domain image variations. ConclusionThis study successfully realizes the high-integrity, automated segmentation of scleral vessel networks under complex clinical imaging conditions. By overcoming the fundamental algorithmic challenges of reflection interference and micro-vessel loss, the proposed methodology provides potential support for the digitization, objective standardization, and intelligent advancement of modern TCM eye diagnosis systems.
3.Risk factors for left atrial appendage thrombosis in elderly patients with non-valvular atrial fibrillation
Binhong TANG ; Ye ZHU ; Jia YOU ; Xiang GU
Chinese Journal of Geriatric Heart Brain and Vessel Diseases 2025;27(10):1345-1348
Objective To analyze the risk factors of left atrial appendage(LAA)thrombosis in elderly patients with NVAF.Methods A total of 210 NVAF patients admitted to our hospital from January 2019 to June 2023 were enrolled in this study.Transesophageal echocardiography was applied used to detect the LAA thrombus,and then according to the presence or absence of thrombus,the patients were divided into a thrombus group(n=42)and a non-thrombus group(n=168).The indicators of routine blood test within 48 h of admission and the characteristics of LAA were recorded.Multivariate logistic regression analysis was performed to identify the risk factors related to the occurrence of LAA thrombus.Results The thrombus group exhibited sig-nificantly larger proportions of diabetes and nonparoxysmal AF,higher total bilirubin,increased left ventricular end-systolic diameter and left ventricular end-diastolic diameter values,and elevat-ed ratio of complex LAA,but lower INR and left ventricular ejection fraction value than the non-thrombus group(P<0.05,P<0.01).After adjusting for confounding factors,multivariate logistic regression analysis showed that diabetes(OR=3.585,95%CI:1.003-12.808,P=0.049)and complex LAA(OR=5.572,95%CI:2.101-14.777,P=0.001)were independent risk factors for LAA thrombosis.Conclusion LAA morphology and diabetes are independent risk factors for the occurrence of LAA thrombus in NVAF patients.
4.Renal autotransplantation for traumatic ureteral injury with urinothorax as the first symptom in a child: one case report
Yijun ZHAO ; Fan YANG ; Linfeng ZHU ; Jia WEI ; Xiang YAN ; Guangjie CHEN
Chinese Journal of Urology 2025;46(8):619-621
A 13-year-old boy was admitted to the hospital due to 1 month after trauma in a traffic accident on September 29,2017. After admission,due to a large amount of pleural effusion through the chest tube,thoracoscopic exploration and fiberboard dissection were performed,and the postoperative pleural effusion was not significantly reduced. The creatinine of pleural effusion was 913 μmol/L,CT showed that left hydronephrosis and perirenal encapsulated effusion were closely related to the ureter,so ureteral injury and urinothorax were considered. Retrograde ureterography revealed a defect of left ureter,approximately 6 cm in length,and left nephrectomy + left kidney rupture repair + renal autotransplantation was performed. 7 years later,the patient recovered well and the renal blood supply was good,no left hydronephrosis was found by MRU. Early diagnosis of ureteral injury is challenging,especially when accompanied by urinothorax. When life is stable,early diagnosis and treatment can reduce the loss of renal function after combined trauma. Renal autotransplantation is safe and effective for the treatment of long segmental ureteral defects.
5.Effects of Sishen Pills and its separated prescriptions on human intestinal flora based on in vitro fermentation model.
Jia-Yang XI ; Qi-Qi WANG ; Xue CHENG ; Hui XIA ; Lu CAO ; Yue-Hao XIE ; Tian-Xiang ZHU ; Ming-Zhu YIN
China Journal of Chinese Materia Medica 2025;50(11):3137-3146
Sishen Pills and its separated prescriptions are classic prescriptions of traditional Chinese medicine to treat intestinal diseases. In this study, a high-performance liquid chromatography-electrospray ionization tandem mass spectrometry(HPLC-ESI-MS/MS) technology was used to identify the components of Sishen Pills, Ershen Pills, and Wuweizi Powder. The positive and negative ion sources of electrospray ionization were simultaneously collected by mass spectrometry. A total of 11 effective components were detected in Sishen Pills, with four effective components detected in Ershen Pills and eight effective components detected in Wuweizi Powder, respectively. To explore the effects of Sishen Pills and its separated prescriptions on the human intestinal flora, an in vitro anaerobic fermentation model was established, and the human intestinal flora was incubated with Sishen Pills, Ershen Pills, and Wuweizi Powder in vitro. The 16S rDNA sequencing technology was used to analyze the changes in the intestinal flora. The results showed that compared with the control group, Sishen Pills, and its separated prescriptions could decrease the intestinal flora abundance and increase the Shannon index after fermentation. The abundance of Bifidobacterium was significantly increased in the Sishen Pills and Ershen Pills groups. However, the abundance of Lactobacillus, Weissella, and Pediococcus was significantly increased in the Wuweizi Powder group. After fermentation for 12 h, the pH of the fermentation solution of three kinds of liquids with feces gradually decreased and was lower than that of the control group. The decreasing amplitude in the Wuweizi Powder group was the most obvious. The single-bacteria fermentation experiments further confirmed that Sishen Pills and Wuweizi Powder had inhibitory effects on Escherichia coli, Staphylococcus aureus, and Enterococcus faecalis, and the antibacterial activity of Wuweizi Powder was stronger than that of Sishen Pills. Both Sishen Pills and Ershen Pills could promote the growth of Lactobacillus brevis, and Ershen Pills could promote the growth of Bifidobacterium adolescentis. This study provided a more sufficient theoretical basis for the clinical application of Sishen Pills and its separated prescriptions.
Humans
;
Gastrointestinal Microbiome/drug effects*
;
Drugs, Chinese Herbal/chemistry*
;
Fermentation/drug effects*
;
Bacteria/drug effects*
;
Chromatography, High Pressure Liquid
;
Tandem Mass Spectrometry
;
Intestines/microbiology*
6.Three new chalcone C-glycosides from Carthami Flos.
Jia-Xu BAO ; Yong-Xiang WANG ; Xian ZHANG ; Ya-Zhu YANG ; Yue LIN ; Jiao-Jiao YIN ; Yun-Fang ZHAO ; Hui-Xia HUO ; Peng-Fei TU ; Jun LI
China Journal of Chinese Materia Medica 2025;50(13):3715-3745
The chemical components of Carthami Flos were investigated by using macroporous resin, silica gel column chromatography, reversed-phase octadecylsilane(ODS) column chromatography, Sephadex LH-20, and semi-preparative high-performance liquid chromatography(HPLC). The planar structures of the compounds were established based on their physicochemical properties and ultraviolet-visible(UV-Vis), infrared(IR), high-resolution electrospray ionization mass spectrometry(HR-ESI-MS), and nuclear magnetic resonance(NMR) spectroscopic technology. The absolute configurations were determined by comparing the calculated and experimental electronic circular dichroism(ECD). Six flavonoid C-glycosides were isolated from the 30% ethanol elution fraction of macroporous resin obtained from the 95% ethanol extract of Carthami Flos, and identified as saffloquinoside F(1), 5-hydroxysaffloneoside(2), iso-5-hydroxysaffloneoside(3), isosafflomin C(4), safflomin C(5), and vicenin 2(6). Among these, the compounds 1 to 3 were new chalcone C-glycosides. The compounds 1, 2, 4, and 5 could significantly increase the viability of H9c2 cardiomyocytes damaged by oxygen-glucose deprivation/reoxygenation(OGD/R) at a concentration of 50 μmol·L~(-1), showing their good cardioprotective activity.
Glycosides/pharmacology*
;
Flowers/chemistry*
;
Drugs, Chinese Herbal/pharmacology*
;
Carthamus tinctorius/chemistry*
;
Chalcones/pharmacology*
;
Animals
7.Comparison study on short-term efficacy between ROSA orthopedic surgical robotic-assisted and traditional manual total knee arthroplasty.
Jia-Liang HU ; Rui-Xiang MA ; Maimaitiabula ABASI ; Chen ZHU
China Journal of Orthopaedics and Traumatology 2025;38(10):1009-1018
OBJECTIVE:
To compare the short-term clinical outcomes and radiographic results of robotic-assisted total knee arthroplasty (RATKA) using the ROSA robot with those of traditional total knee arthroplasty (TKA).
METHODS:
A retrospective analysis was conducted on 55 patients who underwent unilateral TKA due to end-stage knee osteoarthritis(KOA), defined as Kellgren-Lawrence grade Ⅲ or Ⅳ, between June 2024 and December 2024. The patients were divided into two groups based on the surgical approach:the RATKA group and the conventional TKA group. The RATKA group included 25 patients, consisting of 6 males and 19 females, aged from 46 to 84 years old with a mean of ( 65.20±1.93 ) years old. Among them, 11 cases involved the left knee and 14 cases involved the right knee. The traditional TKA group included 30 patients, consisting of 5 males and 25 females, aged from 57 to 85 years old with an average of (68.73±1.36) years old. Among them, 13 cases involved the left knee and 17 cases involved the right knee. Operation time, total perioperative blood loss, and postoperative complications were compared between the two groups. Radiographic evaluation included preoperative and postoperative hip-knee-ankle (HKA) angle, and postoperative lateral tibial component angle (LTC), frontal femoral component angle (FFC), sagittal lateral femoral component angle(LFC), and frontal tibial component (FTC), for the assessment of lower extremity mechanical axis and prosthesis position. The American Knee Society score(KSS), visual analogue scale(VAS) for pain, and range of motion (ROM) of the knee joint preoperatively and postoperatively were compared between the two groups to evaluate the short-term clinical efficacy.
RESULTS:
All surgeries in both groups were successfully completed without intraoperative vascular or nerve injury. Primary wound healing (GradeⅠ) was achieved in all cases, and no infection occurred during follow-up. A total of 55 patients completed the follow-up, with a follow-up duration ranging from 3 to 6 months with a mean of (4.0±1.1) months. The average operation time was (106.56±9.70) minutes in the RATKA group and (90.10±10.97) minutes in the traditional TKA group, with a statistically significant difference between the two groups (P<0.05). However, there was no statistically significant difference in the total perioperative blood loss between the two groups(P>0.05). Postoperative X-ray examinations showed that the prosthesis was well-positioned in all patients of both groups, with no signs of prosthesis loosening or dislocation. On the 1st day postoperatively, the HKA and FFC angle in the RATKA group were (179.25±2.50)° and (89.24±1.58)°, while those in the traditional TKA group were (177.68±2.73)° and (88.25±1.91)°, both showing statistically significant differences(P<0.05). In contrast, there were no statistically significant differences in the FTC, LTC, or LFC angles between the two groups(P>0.05). At 1 month and 3 months postoperatively, the ROM values were (110.68±4.92)° and (117.28±4.91)° in the RATKA group, and (106.25±6.89)° and (113.43±7.91)° in the traditional TKA group, both showing statistically significant difference(P<0.05). Nevertheless, there were no statistically significant differences in the VAS (both at rest and during movement) or KSS between the two groups at 1 month and 3 months postoperatively(P>0.05). Compared with the preoperative data, both groups showed significant improvements in the HKA angle, VAS(at rest and during movement), knee ROM, and KSS (both clinical and functional scores) postoperatively, with statistically significant differences(P<0.05).
CONCLUSION
Compared to traditional TKA, ROSA robotic system-assisted TKA in patients with severe knee osteoarthritis achieved superior accuracy in prosthesis positioning and lower limb mechanical axis restoration, showing satisfactory clinical outcomes. Although short-term outcomes are favorable, long-term clinical efficacy requires further investigation.
Humans
;
Male
;
Female
;
Arthroplasty, Replacement, Knee/methods*
;
Aged
;
Middle Aged
;
Aged, 80 and over
;
Robotic Surgical Procedures/methods*
;
Retrospective Studies
;
Osteoarthritis, Knee/surgery*
;
Treatment Outcome
;
Knee Joint/physiopathology*
8.Preparation and Evaluation of Clinical-Grade Human Umbilical Cord-Derived Mesenchymal Stem Cells with High Expression of Hematopoietic Supporting Factors.
Jie TANG ; Pei-Lin LI ; Xiao-Yu ZHANG ; Xiao-Tong LI ; Fu-Hao YU ; Jia-Yi TIAN ; Run-Xiang XU ; Bo-Feng YIN ; Li DING ; Heng ZHU
Journal of Experimental Hematology 2025;33(3):892-898
OBJECTIVE:
To prepare clinical-grade human umbilical cord-derived mesenchymal stem cells (hUC-MSC) with high expression of hematopoietic supporting factors and evaluate their stem cell characteristics.
METHODS:
Fetal umbilical cord tissues were collected from healthy postpartum women during full-term cesarean section. Wharton's jelly was mechanically separated and hUC-MSCs were obtained by explant culture method and enzyme digestion method in an animal serum-free culture system with addition of human platelet lysate. The phenotypic characteristics of hUC-MSCs obtained by two methods were detected by flow cytometry. The differences in proliferation ability between the two groups of hUC-MSCs were identified through CCK-8 assay and colony forming unit-fibroblast (CFU-F) assay. The differences in multilineage differentiation potential between the two groups of hUC-MSCs were identified through induction of adipogenic, osteogenic, and chondrogenic differentiation. The mRNA expression levels of hematopoietic supporting factors such as SCF, IL-3, CXCL12, VCAM1 and ANGPT1 in the two groups of hUC-MSCs were identified by real-time fluorescence quantiative PCR(RT-qPCR).
RESULTS:
The results of flow cytometry showed that hUC-MSCs obtained by the two methods both expressed high levels of CD73, CD90 and CD105, while lowly expressed CD31, CD45 and HLA-DR. The results of CCK-8 and CFU-F assay showed that the proliferation ability of hUC-MSCs obtained by explant culture method was better than those obtained by enzyme digestion method. The results of the triple lineage differentiation experiment showed that there was no significant difference in multilineage differentiation potential between the two grous of hUC-MSCs. The results of RT-qPCR showed that the mRNA expression levels of hematopoietic supporting factors SCF, IL-3, CXCL12, VCAM1 and ANGPT1 in hUC-MSCs obtained by explant cultrue method were higher than those obtained by enzyme digestion method.
CONCLUSION
Clinical-grade hUC-MSCs with high expression levels of hematopoietic supporting factors were successfully cultured in an animal serum-free culture system.
Humans
;
Mesenchymal Stem Cells/metabolism*
;
Umbilical Cord/cytology*
;
Cell Differentiation
;
Female
;
Cell Proliferation
;
Cells, Cultured
;
Chemokine CXCL12/metabolism*
;
Angiopoietin-1/metabolism*
;
Vascular Cell Adhesion Molecule-1/metabolism*
;
Stem Cell Factor/metabolism*
;
Flow Cytometry
;
Pregnancy
9.Glucocorticoid Discontinuation in Patients with Rheumatoid Arthritis under Background of Chinese Medicine: Challenges and Potentials Coexist.
Chuan-Hui YAO ; Chi ZHANG ; Meng-Ge SONG ; Cong-Min XIA ; Tian CHANG ; Xie-Li MA ; Wei-Xiang LIU ; Zi-Xia LIU ; Jia-Meng LIU ; Xiao-Po TANG ; Ying LIU ; Jian LIU ; Jiang-Yun PENG ; Dong-Yi HE ; Qing-Chun HUANG ; Ming-Li GAO ; Jian-Ping YU ; Wei LIU ; Jian-Yong ZHANG ; Yue-Lan ZHU ; Xiu-Juan HOU ; Hai-Dong WANG ; Yong-Fei FANG ; Yue WANG ; Yin SU ; Xin-Ping TIAN ; Ai-Ping LYU ; Xun GONG ; Quan JIANG
Chinese journal of integrative medicine 2025;31(7):581-589
OBJECTIVE:
To evaluate the dynamic changes of glucocorticoid (GC) dose and the feasibility of GC discontinuation in rheumatoid arthritis (RA) patients under the background of Chinese medicine (CM).
METHODS:
This multicenter retrospective cohort study included 1,196 RA patients enrolled in the China Rheumatoid Arthritis Registry of Patients with Chinese Medicine (CERTAIN) from September 1, 2019 to December 4, 2023, who initiated GC therapy. Participants were divided into the Western medicine (WM) and integrative medicine (IM, combination of CM and WM) groups based on medication regimen. Follow-up was performed at least every 3 months to assess dynamic changes in GC dose. Changes in GC dose were analyzed by generalized estimator equation, the probability of GC discontinuation was assessed using Kaplan-Meier curve, and predictors of GC discontinuation were analyzed by Cox regression. Patients with <12 months of follow-up were excluded for the sensitivity analysis.
RESULTS:
Among 1,196 patients (85.4% female; median age 56.4 years), 880 (73.6%) received IM. Over a median 12-month follow-up, 34.3% (410 cases) discontinued GC, with significantly higher rates in the IM group (40.8% vs. 16.1% in WM; P<0.05). GC dose declined progressively, with IM patients demonstrating faster reductions (median 3.75 mg vs. 5.00 mg in WM at 12 months; P<0.05). Multivariate Cox analysis identified age <60 years [P<0.001, hazard ratios (HR)=2.142, 95% confidence interval (CI): 1.523-3.012], IM therapy (P=0.001, HR=2.175, 95% CI: 1.369-3.456), baseline GC dose ⩽7.5 mg (P=0.003, HR=1.637, 95% CI: 1.177-2.275), and absence of non-steroidal anti-inflammatory drugs use (P=0.001, HR=2.546, 95% CI: 1.432-4.527) as significant predictors of GC discontinuation. Sensitivity analysis (545 cases) confirmed these findings.
CONCLUSIONS
RA patients receiving CM face difficulties in following guideline-recommended GC discontinuation protocols. IM can promote GC discontinuation and is a promising strategy to reduce GC dependency in RA management. (Trial registration: ClinicalTrials.gov, No. NCT05219214).
Adult
;
Aged
;
Female
;
Humans
;
Male
;
Middle Aged
;
Arthritis, Rheumatoid/drug therapy*
;
Glucocorticoids/therapeutic use*
;
Medicine, Chinese Traditional
;
Retrospective Studies
10.Safety, pharmacokinetics, and dosimetry of 177Lu-AB-3PRGD2 in patients with advanced integrin α v β 3-positive tumors: A first-in-human study.
Huimin SUI ; Feng GUO ; Hongfei LIU ; Rongxi WANG ; Linlin LI ; Jiarou WANG ; Chenhao JIA ; Jialin XIANG ; Yingkui LIANG ; Xiaohong CHEN ; Zhaohui ZHU ; Fan WANG
Acta Pharmaceutica Sinica B 2025;15(2):669-680
Integrin α v β 3 is overexpressed in various tumor cells and angiogenesis. To date, no drug has been proven to target it for therapy. A first-in-human study was designed to investigate the safety, pharmacokinetics, and dosimetry of 177Lu-AB-3PRGD2, a novel integrin α v β 3-targeting radionuclide drug with an albumin-binding motif to optimize the pharmacokinetics. Ten patients (3 men, 7 women; aged 45 ± 16 years) with integrin α v β 3-avid tumors were recruited to accept 177Lu-AB-3PRGD2 injection in a dosage of 1.57 ± 0.08 GBq (42.32 ± 2.11 mCi), followed by serial scans to obtain its dynamic distribution in the body. Safety tests were performed before and every 2 weeks after the treatment for 6-8 weeks. No adverse event over grade 3 was observed. 177Lu-AB-3PRGD2 was excreted mainly through the urinary system, with intense radioactivity in the kidneys and bladder. Moderate distribution was found in the liver, spleen, and intestines. The estimated blood half-life was 2.85 ± 2.17 h. The whole-body effective dose was 0.251 ± 0.047 mSv/MBq. The absorbed doses were 0.157 ± 0.032 mGy/MBq in red bone marrow and 0.684 ± 0.132 mGy/MBq in kidneys. This first-in-human study of 177Lu-AB-3PRGD2 treatment indicates its promising potential for targeted radionuclide therapy of integrin α v β 3-avid tumors. It merits further studies in more patients with escalating doses and multiple treatment courses.

Result Analysis
Print
Save
E-mail