1.Safety, dosimetry, and efficacy of an optimized long-acting somatostatin analog for peptide receptor radionuclide therapy in metastatic neuroendocrine tumors: From preclinical testing to first-in-human study.
Wei GUO ; Xuejun WEN ; Yuhang CHEN ; Tianzhi ZHAO ; Jia LIU ; Yucen TAO ; Hao FU ; Hongjian WANG ; Weizhi XU ; Yizhen PANG ; Liang ZHAO ; Jingxiong HUANG ; Pengfei XU ; Zhide GUO ; Weibing MIAO ; Jingjing ZHANG ; Xiaoyuan CHEN ; Haojun CHEN
Acta Pharmaceutica Sinica B 2025;15(2):707-721
Peptide receptor radionuclide therapy (PRRT) with radiolabeled SSTR2 agonists is a treatment option that is highly effective in controlling metastatic and progressive neuroendocrine tumors (NETs). Previous studies have shown that an SSTR2 agonist combined with albumin binding moiety Evans blue (denoted as 177Lu-EB-TATE) is characterized by a higher tumor uptake and residence time in preclinical models and in patients with metastatic NETs. This study aimed to enhance the in vivo stability, pharmacokinetics, and pharmacodynamics of 177Lu-EB-TATE by replacing the maleimide-thiol group with a polyethylene glycol chain, resulting in a novel EB conjugated SSTR2-targeting radiopharmaceutical, 177Lu-LNC1010, for PRRT. In preclinical studies, 177Lu-LNC1010 exhibited good stability and SSTR2-binding affinity in AR42J tumor cells and enhanced uptake and prolonged retention in AR42J tumor xenografts. Thereafter, we presented the first-in-human dose escalation study of 177Lu-LNC1010 in patients with advanced/metastatic NETs. 177Lu-LNC1010 was well-tolerated by all patients, with minor adverse effects, and exhibited significant uptake and prolonged retention in tumor lesions, with higher tumor radiation doses than those of 177Lu-EB-TATE. Preliminary PRRT efficacy results showed an 83% disease control rate and a 42% overall response rate after two 177Lu-LNC1010 treatment cycles. These encouraging findings warrant further investigations through multicenter, prospective, and randomized controlled trials.
2.Establishment of UPLC characteristic spectrum of Liushenqu standard decoction and determination of related index components
Jiahui XIE ; Jiabao WEI ; Shuangyan TANG ; Kaiwei HUANG ; Weizhi ZHAO ; Yu HU ; Hui ZHANG
International Journal of Traditional Chinese Medicine 2025;47(5):669-675
Objective:To establish the characteristic spectrum of Liushenqu standard decoction using ultra-high performance liquid chromatography (UPLC); To determine the contents of related index components; To evaluate the quality of Liushenqu standard decoction.Methods:UPLC method was used to establish characteristic spectrum of Liushenqu standard decoction. Chromatographic Fingerprint Similarity Evaluation System (2012 edition) was used for similarity analysis, the characteristic peak was assigned, and the content of its index components was determined.Results:The characteristic peaks of Liushenqu standard decoction were calibrated and 8 components were identified, namely uridine, adenosine, guanosine, 5-hydroxymethylfurfural, tryptophan, vanillic acid, ferulic acid and shaftaside. The contents of uridine, adenosine, tryptophan ferulic acid and shaftaside in 10 batches of Liushenqu standard decoction were simultaneously determined, and ranged from 0.036 1~0.383 9 mg/g, 0.030 7~0.170 2 mg/g, 0.007 0~0.060 2 mg/g, 0.001 0~0.005 0 mg/g, 0.000 8~0.013 8 mg/g, respectively. The transfer rates ranged from 44.2% to 50.8%, 60.1% to 67.7%, 60.4% to 76.4%, 62.7% to 77.4%, 50.7% to 61.4%, respectively.Conclusion:The established UPLC characteristic spectrum and content determination method are accurate and repeatable, which can provide references for quality control of Liushenqu standard granules.
3.Study on quality standard of wine-processed Coptidis Rhizoma standard decoction
Huilin YANG ; Kaiwei HUANG ; Yanghua LI ; Suqin CAI ; Shuping XU ; Jiabao WEI ; Hui ZHANG ; Weizhi ZHAO ; Pei TAN
International Journal of Traditional Chinese Medicine 2025;47(9):1285-1292
Objective:To establish the quality standard of the standard decoction of wine-processed Coptidis Rhizoma by studying the extraction rate, fingerprint and component quantitative analysis.Methods:ccording to the Technical Requirements for Quality Control and Standard Formulation of Chinese Medicine Formula Granules, 15 batches of the standard decoction of wine-processed Coptidis Rhizoma were prepared, and the paste rate was determined; HPLC fingerprints of 15 batches of standard decoction of wine-processed Coptidis Rhizoma were established, and evaluated by combining similarity evaluation, clustering analysis, principal component analysis and orthogonal partial least squares discriminant analysis; the contents of berberine, epiberberine, pamadine, and safranine in the samples of the 15 batches were determined and analyzed their transfer rates.Results:A total of 15 batches of standard decoction samples were calibrated with 11 common peaks, referring to the recognition of 8 components. The similarity between the samples and the control product was greater than 0.900; the clustering analysis could cluster the 15 batches of samples into 2 classes; the results of the principal component analysis showed that the cumulative variance contribution rate of the 3 principal component factors was 89.388%; the OPLS-DA screened out the 3 components of the quality difference; the 15 batches of samples out of the paste rate was 15.7% -20.8%, and the mass fractions of berberine, epiberberine, safranine, and palmatine were 18.47%-24.38%, 2.82%-3.49%, 5.08%-6.69%, and 4.84%-6.68%, respectively, with transfer rates of 41.7%-61.7%, 46.9%-68.7%, 39.8%-61.5%, and 43.8%-65.2%.Conclusion:The fingerprint and content determination method established in this study is accurate, stable, simple, and can be used for the quality control and evaluation of the standard decoction of wine-processed Coptidis Rhizoma.
4.Insights from the Development Process of Traditional Chinese Medicine Chronic Disease Management Guidelines for Menopausal Women with Emotional Disorders(DB44/T 2547-2024)
Guanglian HE ; Jianong YU ; Xuchun HUANG ; Weizhi FAN ; Yuanxiu CHEN ; Jingling HE ; Xiaoyun WANG ; Qinghua GUO
Journal of Guangzhou University of Traditional Chinese Medicine 2025;42(11):2868-2876
This article outlines the formulation process of the local standard of Traditional Chinese Medicine Chronic Disease Management Guideline for Menopausal Women with Emotional Disorders(DB44/T 2547-2024;hereafter referred to as the"Guideline").By analyzing its structural framework and content,this study elucidates the TCM-specific chronic disease management strategies incorporated in the Guidelines,aiming to supply references to the development of similar standards and provide guidance for TCM chronic disease management practices.The development for the Guideline involved a multi-dimensional evidence collection process,including literature review,summary of expert experience,and expert consultations.By employing a multi-dimensional evidence-based approach,the Guideline has effectively integrated diverse evidence sources,and ensures the standard formulation being scientific and precise.The Guideline proposes the requirements for TCM-specific chronic disease management of menopausal women with emotional disorders firstly.By incorporating TCM lifestyle regulation,TCM emotional management,TCM dietary therapy,medication guidance,exercise therapies,and distinctive external treatments,the Guideline has developed into a comprehensive TCM chronic disease management system for prevention,treatment,rehabilitation and health preservation.The integrated approach effectively reduces the recurrence of emotional disorder and enhances quality of life of the patients.
5.Current status and advances in the diagnosis and treatment of inflammatory breast cancer
Wenjing ZENG ; Juan HUANG ; Shouman WANG ; Yangyi LI ; Weizhi XIA ; Yulong ZHANG ; Jun WU ; Taohong SHEN ; Fangli ZHOU ; Ayong CAO
Chinese Journal of General Surgery 2025;34(5):1044-1055
Inflammatory breast cancer(IBC)is a rare but highly aggressive subtype of breast cancer characterized by rapid clinical progression and poor prognosis.Although it accounts for only 2%-4%of all breast cancer cases,it is responsible for 8%-10%of breast cancer-related mortality.The etiology of IBC is multifactorial,involving genetic,hormonal,environmental,and socioeconomic factors.Pathologically,IBC is marked by the presence of dermal lymphatic tumor emboli,and molecular subtypes are predominantly HER2-positive and triple-negative,indicating high tumor invasiveness.Diagnosis relies on characteristic clinical manifestations and histopathological confirmation,while imaging techniques such as MRI and PET/CT play important roles in evaluating disease extent and metastasis.Given that IBC is often diagnosed at a locally advanced or metastatic stage,there is currently no specific treatment protocol.Instead,management generally follows the treatment paradigm of non-IBC,emphasizing systemic therapy within a multidisciplinary framework.HER2-positive IBC benefits from chemotherapy combined with dual-targeted anti-HER2 therapy;triple-negative IBC may respond to immune checkpoint inhibitors;and CDK4/6 inhibitors show potential efficacy in hormone receptor-positive subtypes.Despite advancements,the prognosis remains poor,with a high risk of early recurrence and distant metastasis.Prognostic factors include lymph node involvement,molecular subtype,and response to neoadjuvant therapy.As research into the tumor microenvironment and molecular mechanisms deepens,targeted and individualized therapies hold promise for improving outcomes.This review summarizes the epidemiology,pathology,diagnostic criteria,treatment strategies,and prognostic factors of IBC,aiming to inform clinical practice and future research.
6.Breast-conserving surgery vs. mastectomy in centrally located breast cancer
Wenjing ZENG ; Shouman WANG ; Ayong CAO ; Weizhi XIA ; Jinyue GAO ; Liya LI ; Ziqi TANG ; Hongmei WANG ; Juan HUANG
Chinese Journal of General Surgery 2025;34(8):1726-1737
Background and Aims:Centrally located breast cancer(CLBC),due to its proximity to the nipple-areolar complex,has long been treated primarily with mastectomy,while the oncologic safety of breast-conserving surgery(BCS)remains controversial.This study,based on a large-scale database combined with a real-world cohort,compared the survival outcomes of BCS and mastectomy to evaluate the feasibility and oncologic safety of BCS in CLBC patients.Methods:Data of 10 325 female CLBC patients diagnosed between 2010 and 2015 were extracted from the SEER database,including 5 601 patients who underwent BCS and 4 724 who underwent mastectomy.Propensity score matching(PSM)yielded 1 951 matched pairs,and disease-specific survival(DSS)and overall survival(OS)were compared between groups.Cox regression analyses were performed to identify prognostic factors,and subgroup analyses were conducted.Additionally,an independent validation cohort from Xiangya Hospital,Central South University(2015-2016)included 221 BCS and 636 mastectomy patients,with OS and progression-free survival(PFS)assessed.Results:After PSM,baseline characteristics between groups were well balanced.Kaplan-Meier analysis demonstrated no significant differences in DSS or OS between BCS and mastectomy,and 5-,7-,and 10-year OS rates were comparable(all P>0.05).Subgroup analyses revealed equivalent outcomes for BCS and mastectomy in patients with T1/T2 disease,different HER2 statuses,and those receiving chemotherapy,while in patients receiving radiotherapy,BCS showed significantly better DSS and OS than mastectomy(both P<0.05).Multivariate Cox regression identified T,N,and M stage,histologic grade,molecular subtype,ER/PR status,and chemotherapy as independent prognostic factors(all P<0.05),whereas surgical type was not(P>0.05).The validation cohort confirmed the SEER findings,with no significant differences in OS or PFS between the two groups(both P>0.05).Conclusions:BCS provides DSS and OS comparable to mastectomy in CLBC patients and may confer additional survival benefits when combined with radiotherapy.These findings suggest that CLBC should not be considered a contraindication to BCS,supporting BCS as a feasible and safe surgical strategy that offers valuable evidence for individualized clinical decision-making and may help improve patients' quality of life.
7.Current status and advances in the diagnosis and treatment of inflammatory breast cancer
Wenjing ZENG ; Juan HUANG ; Shouman WANG ; Yangyi LI ; Weizhi XIA ; Yulong ZHANG ; Jun WU ; Taohong SHEN ; Fangli ZHOU ; Ayong CAO
Chinese Journal of General Surgery 2025;34(5):1044-1055
Inflammatory breast cancer(IBC)is a rare but highly aggressive subtype of breast cancer characterized by rapid clinical progression and poor prognosis.Although it accounts for only 2%-4%of all breast cancer cases,it is responsible for 8%-10%of breast cancer-related mortality.The etiology of IBC is multifactorial,involving genetic,hormonal,environmental,and socioeconomic factors.Pathologically,IBC is marked by the presence of dermal lymphatic tumor emboli,and molecular subtypes are predominantly HER2-positive and triple-negative,indicating high tumor invasiveness.Diagnosis relies on characteristic clinical manifestations and histopathological confirmation,while imaging techniques such as MRI and PET/CT play important roles in evaluating disease extent and metastasis.Given that IBC is often diagnosed at a locally advanced or metastatic stage,there is currently no specific treatment protocol.Instead,management generally follows the treatment paradigm of non-IBC,emphasizing systemic therapy within a multidisciplinary framework.HER2-positive IBC benefits from chemotherapy combined with dual-targeted anti-HER2 therapy;triple-negative IBC may respond to immune checkpoint inhibitors;and CDK4/6 inhibitors show potential efficacy in hormone receptor-positive subtypes.Despite advancements,the prognosis remains poor,with a high risk of early recurrence and distant metastasis.Prognostic factors include lymph node involvement,molecular subtype,and response to neoadjuvant therapy.As research into the tumor microenvironment and molecular mechanisms deepens,targeted and individualized therapies hold promise for improving outcomes.This review summarizes the epidemiology,pathology,diagnostic criteria,treatment strategies,and prognostic factors of IBC,aiming to inform clinical practice and future research.
8.Breast-conserving surgery vs. mastectomy in centrally located breast cancer
Wenjing ZENG ; Shouman WANG ; Ayong CAO ; Weizhi XIA ; Jinyue GAO ; Liya LI ; Ziqi TANG ; Hongmei WANG ; Juan HUANG
Chinese Journal of General Surgery 2025;34(8):1726-1737
Background and Aims:Centrally located breast cancer(CLBC),due to its proximity to the nipple-areolar complex,has long been treated primarily with mastectomy,while the oncologic safety of breast-conserving surgery(BCS)remains controversial.This study,based on a large-scale database combined with a real-world cohort,compared the survival outcomes of BCS and mastectomy to evaluate the feasibility and oncologic safety of BCS in CLBC patients.Methods:Data of 10 325 female CLBC patients diagnosed between 2010 and 2015 were extracted from the SEER database,including 5 601 patients who underwent BCS and 4 724 who underwent mastectomy.Propensity score matching(PSM)yielded 1 951 matched pairs,and disease-specific survival(DSS)and overall survival(OS)were compared between groups.Cox regression analyses were performed to identify prognostic factors,and subgroup analyses were conducted.Additionally,an independent validation cohort from Xiangya Hospital,Central South University(2015-2016)included 221 BCS and 636 mastectomy patients,with OS and progression-free survival(PFS)assessed.Results:After PSM,baseline characteristics between groups were well balanced.Kaplan-Meier analysis demonstrated no significant differences in DSS or OS between BCS and mastectomy,and 5-,7-,and 10-year OS rates were comparable(all P>0.05).Subgroup analyses revealed equivalent outcomes for BCS and mastectomy in patients with T1/T2 disease,different HER2 statuses,and those receiving chemotherapy,while in patients receiving radiotherapy,BCS showed significantly better DSS and OS than mastectomy(both P<0.05).Multivariate Cox regression identified T,N,and M stage,histologic grade,molecular subtype,ER/PR status,and chemotherapy as independent prognostic factors(all P<0.05),whereas surgical type was not(P>0.05).The validation cohort confirmed the SEER findings,with no significant differences in OS or PFS between the two groups(both P>0.05).Conclusions:BCS provides DSS and OS comparable to mastectomy in CLBC patients and may confer additional survival benefits when combined with radiotherapy.These findings suggest that CLBC should not be considered a contraindication to BCS,supporting BCS as a feasible and safe surgical strategy that offers valuable evidence for individualized clinical decision-making and may help improve patients' quality of life.
9.A brief discussion on the Chinese translation of disease-modifying therapies
Chinese Journal of Neurology 2024;57(2):199-200
Ever since interferon-β was introduced into China more than 20 years ago and used in the disease-modifying therapies (DMT) of multiple sclerosis (MS) patients, the Chinese translations of DMT used in China are quite puzzling, even clinicians are also difficult to understand the meaning of DMT. The authors searched and traced the origins of current DMT translations, which may be mainly due to the fact that the word "modifying" in Chinese contains two meanings: correction and alleviation, obviously currently used names prefer to correct, while the exact meaning of DMT should be to alleviate disease. Considering that inaccurate translation is widely used in domestic academic conferences and academic journals, it is easy to cause misunderstanding and ambiguity. The authors believe that the meaning of DMT should be correctly and deeply understood in the specific context, and the original meaning of alleviating disease should be returned, which is also in line with the two endpoints of immunomodulatory therapy for MS and optic neuromyelitis spectrum disease, the primary endpoint being to reduce the annual recurrence rate of the diseases, the secondary one being to slow the progression of disease disability.
10.Characteristic spectrum of Rheum tanguticum Maxim,ex Balf.water decoction and analysis of different origins and different processed products
Kaiwei HUANG ; Hui ZHANG ; Shuping XU ; Huiling YANG ; Yanghua LI ; Weizhi ZHAO ; Zhijun GUO ; Pei TAN
Drug Standards of China 2024;25(4):330-338
Objective To establish an ultra-high liquid chromatography(UPLC)characteristic spectrum of Rheum tanguticum Maxim.ex Balf.water decoction and conduct chemical pattern recognition analysis,and to identify the medicinal materials of different origins and different processed products.Methods:UPLC was adopted to establish the characteristic spectra of 15 batches of Rheum tanguticum Maxim.ex Balf.Cluster analysis combined with principal component analysis was used to analyze their quality.Rhei Radix et Rhizoma from different origins and different processed products of Rheum tanguticum Maxim.ex Balf.were identified.Results:The characteristic spectrum of Rheum tanguticum Maxim.ex Balf.water decoction was established,18 common peaks were identi-fied,and 15 batches of Rheum tanguticum Maxim.ex Balf.were divided into 2 categories according to their origins by cluster analysis.The similarity between 15 batches of samples from different origins and the control spectrum was greater than 0.900.According to OPLS-DA analysis,a total of 6 markers(rhein-8-O-β-D-glu-cosid,resveratrol-4'-O-β-D-(6''-O-D-gallyl)glucopyranside,isolindleyin,rhein,epicatechin-3-O-D-gallate,and catechin)affecting the quality of Rheum tanguticum Maxim.ex Balf.water decoction samples were found.Rhei Radix et Rhizoma from different origins and different processed products of Rheum tanguticum Maxim.ex Balf.can be effectively distinguished.Conclusion:The established characteristic spectrum method is easy to operate and has good repeatability.It can be used for the quality control of Rheum tanguticum Maxim.ex Balf.water decoction,and can provide reference for the formulation of quality standard of formula granules of Rhei Radix et Rhizoma.

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