Outcomes of a 12-month course of early and late rituximab BCD020 biosimilar administration in juvenile systemic lupus erythematosus:A retrospective study

BACKGROUND Juvenile systemic lupus erythematosus(SLE)is a severe,life-threatening disease.However,the role of rituximab in managing juvenile SLE remains undefined,although early biological intervention may improve disease outcomes.AIM To assess the differences in the outcomes of different types of rituximab administration(early and late).METHODS In this retrospective cohort study,the information of 36 children with SLE with administration(LRA)was analyzed.We compared initial disease characteristics at onset,at baseline(start of rituximab),and at the end of the study(EOS)at 12 months,as well as outcomes and treatment characteristics.RESULTS The main differences at baseline were a higher daily median dose of corticosteroids,increased MAS frequency,and a higher Systemic Lupus Erythematosus Disease Activity Index(SLEDAI)in the ERA group.No differences in the main SLE outcomes between groups at the EOS were observed.The part of lupus nephritis patients who achieved remission changed from 44%to 31%in ERA and 32%to 11%in the LRA group.Patients with ERA had a shorter time to achieve low daily corticosteroid dose(≤0.2 mg/kg)at 1.2(0.9;1.4)years compared to 2.8(2.3;4.0)years(P=0.000001)and higher probability to achieve this low dose[hazard ratio(HR)=57.8(95%confidence interval(CI):7.2-463.2),P=0.00001 and remission(SLEDAI=0);HR=37.6(95%CI:4.45-333.3),P=0.00001].No differences in adverse events,including severe adverse events,were observed.CONCLUSION ERA demonstrated a better steroid-sparing effect and a possibility of earlier remission or low disease activity,except for lupus nephritis.Further investigations are required.

Comparison of inebilizumab or rituximab in addition to glucocorticoid therapy for neuromyelitis optica spectrum disorders

AIM:To investigate the short-term efficacy and safety of inebilizumab for neuromyelitis optica spectrum disorders(NMOSD).METHODS:A total of 33 patients with NMOSD treated with inebilizumab(Group INB,n=15)or rituximab(Group RTX,n=18)in addition to high-dose glucocorticoids were included.Both groups underwent hormone shock therapy during the acute phase.Subsequently,Group INB received inebilizumab injections during the remission phase,while Group RTX received rituximab injections.A comparison of aquaporins 4(AQP4)titer values,peripheral blood B lymphocyte counts,and visual function recovery was conducted before and 8wk after treatment.Additionally,adverse reactions and patient tolerability were analyzed after using inebilizumab treatment regimes.RESULTS:Following inebilizumab treatment,there was a significantly improvement in the visual acuity of NMOSD patients(P<0.05),accompanied by a notable decrease in AQP4 titer values and B lymphocyte ratio(P<0.05).Moreover,inebilizumab treatment showed a partial effect in preventing optic nerve atrophy(P<0.05).However,there were no significant differences in other therapeutic effects compared to rituximab,which has previously demonstrated substantial therapeutic efficacy(P>0.05).Furthermore,inebilizumab exhibited higher safety levels than that of rituximab injections.CONCLUSION:The combination of inebilizumab and high-dose glucocorticoids proves to be effective.In comparison to rituximab injections,inebilizumab displays better tolerance and safety.Moreover,it demonstrates a partial effect in preventing optic nerve atrophy.Thus,it stands as an effective method to reduce the disability rates and improve the daily living ability of patients with NMOSD.

Bendamustine and rituximab as frontline therapy in extranodal marginal zone lymphoma:a single-institution experience

Extranodal marginal zone lymphoma(EMZL)encompasses 70%of cases of marginal zone lymphoma.Frontline bendamustine and rituximab(BR)were derived from trials involving other indolent non-Hodgkin’s lymphomas.Only one trial has evaluated frontline BR prospectively in EMZL.This retrospective study reports outcomes among EMZL patients receiving frontline BR.Twenty-five patients were included with a median age of 69 years(40–81).Five(20.0%)patients had stage Ⅰ/Ⅱ disease,and 20(80.0%)had stage Ⅲ/Ⅳ disease.The median number of cycles was 6.0(3.0–6.0).Maintenance rituximab was administered to 10(41.7%)individuals.Overall response rate(ORR)was 100.0%(60.0%complete response,40.0%partial response).Medians of overall survival and progression-free survival were not reached.The estimated 2-year progression-free survival was 85.2%and overall survival was 100.0%.Four(16.6%)patients had infections related to treatment;3(12.0%)transformed to diffuse large B-cell lymphoma;5(20.8%)had a relapse or progression of EMZL;and 3(12.0%)died unrelated to BR.BR is an efficacious and well-tolerated front-line regimen for EMZL with response data consistent with existing literature.

Rituximab Induced Vasculitis: Dose the Antigen-Antibody Complex of Rituximab Play a Role in Developing Leukocytoclastic Vasculitis?—A Case Report and Review of the Literature

Rituximab is a monoclonal antibody that targets CD20, which is a specific B-cell surface antigen. It was the first monoclonal antibody that was approved for the treatment of non-Hodgkin lymphoma, rheumatoid arthritis, and other cutaneous lymphoid malignancies. There are many off-label uses of rituximab, such as systemic lupus erythematosus, autoimmune hemolytic anemia, multiple sclerosis, graft-versus-host disease, chronic lymphocytic leukemia, and chronic immune-mediated thrombocytopenia. Among the rare side effects associated with rituximab treatment is vasculitis, more specifically, leukocytoclastic vasculitis. Here, we describe a 21-year-old Saudi female with leukocytoclastic vasculitis occurring three months after treatment with rituximab.

Review of plasma exchange and rituximab for prevention of recurrent focal segmental glomerulosclerosis after a prior graft loss

BACKGROUND Focal segmental glomerulosclerosis(FSGS)often recurs after transplantation,leading to graft dysfunction and graft loss.Patients who have lost prior grafts due to recurrence are at particularly high risk of re-recurrence in subsequent grafts.Rituximab and plasma exchange have been used pre-emptively to prevent post-transplant recurrence.However,the efficacy of such preventative measures remains unclear.AIM To investigate the outcomes of preventative rituximab and plasma exchange for recurrent FSGS in transplant recipients after prior graft loss.METHODS We conducted a systematic review of 11 studies with 32 patients who had experienced prior graft loss due to post-transplant FSGS recurrence and were treated with either pre-emptive plasma exchange alone,rituximab alone,or a combination of both.RESULTS Overall,47%of the 32 patients experienced recurrence despite prophylactic treatment.Re-recurrence was seen in 25%(1/4)with pre-emptive rituximab alone,and 45%recurrence(9/20)with plasma exchange alone.Re-recurrence was noted in 63%with the use of combined plasma exchange and rituximab.CONCLUSION There is a paucity of available evidence in the literature to draw clear conclusions on the benefits of pre-emptive measures to prevent FSGS re-recurrence.The small sample sizes and variations in protocols call for larger and controlled studies to serve this patient population at high risk of recurrence and graft loss.

BCD020 rituximab bioanalog compared to standard treatment in juvenile systemic lupus erythematosus: The data of 12 months casecontrol study

BACKGROUND Systemic lupus erythematosus(SLE)is the most frequent and serious systemic connective tissue disease.Nowadays there is no clear guidance on its treatment in childhood.There are a lot of negative effects of standard-of-care treatment(SOCT),including steroid toxicity.Rituximab(RTX)is the biological B-lymphocyte-depleting agent suggested as a basic therapy in pediatric SLE.AIM To compare the benefits of RTX above SOCT.METHODS The data from case histories of 79 children from the Saint-Petersburg State Pediatric Medical University from 2012 to 2022 years,were analyzed.The diagnosis of SLE was established with SLICC criteria.We compared the outcomes of treatment of SLE in children treated with and without RTX.Laboratory data,doses of glucocorticosteroids,disease activity measured with SELENA-SLEDAI,RESULTS Patients,treated with RTX initially had a higher degree of disease activity with prevalence of central nervous system and kidney involvement,compared to patients with SOCT.One year later the disease characteristics became similar between groups with a more marked reduction of disease activity(SELENA-SLEDAI activity index)in the children who received RTX[-19 points(17;23)since baseline]compared to children with SOCT[-10(5;15.5)points since baseline,P=0.001],the number of patients with active lupus nephritis,and daily proteinuria.During RTX therapy,infectious diseases had three patients;one patient developed a bi-cytopenia.CONCLUSION RTX can be considered as the option in the treatment of severe forms of SLE,due to its ability to arrest disease activity compared to SOCT.

Clinical Observation of Serum Anti-PLA2R Antibody Levels in the Treatment of Idiopathic Membranous Nephropathy with Rituximab

Objective:To investigate the efficacy of rituximab in the treatment of idiopathic membranous nephropathy with varying levels of serum phospholipase A2 receptor antibodies.Methods:A total of 137 patients with idiopathic membranous nephropathy admitted to Beijing Sixth Hospital were selected.Based on their blood PLA2R antibody levels before rituximab treatment,patients were categorized into the PLA2R antibody positive group(n=94)and the PLA2R antibody negative group(n=43).They were followed up for at least 1 year,during which the efficacy,measured through 24-hour urine protein quantification and serum albumin levels,were compared between the two groups before and after treatment.Results:After 3 months of treatment,there was no significant difference in the quantitative levels of 24-hour urine protein between the two groups(P>0.05).However,after 6 and 12 months of treatment,there was a significant difference in the levels of 24-hour urine protein between the two groups(P<0.05).Additionally,after 3 months of treatment,there was a notable difference in the serum albumin levels between the two groups(P<0.05).However,after 6 and 12 months of treatment,there was no significant difference in serum albumin levels between the two groups(P>0.05).Analysis of complications in the two groups revealed that in the positive group,9 individuals experienced thrombosis,5 had infections,and 11 developed acute kidney injury(AKI).In contrast,in the negative group,5 individuals had thrombosis,2 had infections,and 3 developed AKI.There was no statistically significant difference in complications between the two groups(P>0.05).Conclusion:Serum anti-PLA2R antibody levels provide valuable insights into the clinical observation of rituximab treatment for idiopathic membranous nephropathy.They aid in understanding the disease’s pathogenesis,evaluating treatment efficacy,and predicting disease prognosis.

Successful treatment of patients with refractory idiopathic membranous nephropathy with low-dose Rituximab:A single-center experience

BACKGROUND The recognition of idiopathic membranous nephropathy(IMN)as an autoimmune disease has paved the way for the use of B-cell-depleting agents,such as Rituximab(RTX),which is now a first-line drug for treating IMN with proven safety and efficacy.Nevertheless,the usage of RTX for the treatment of refractory IMN remains controversial and challenging.AIM To evaluate the efficacy and safety of a new low-dose RTX regimen for the treatment of patients with refractory IMN.METHODS A retrospective study was performed on refractory IMN patients that accepted a low-dose RTX regimen(RTX,200 mg,once a month for five months)in the Xiyuan Hospital of Chinese Academy of Chinese Medical Sciences’Department of Nephrology from October 2019 to December 2021.To assess the clinical and immune remission data,we performed a 24 h urinary protein quantification(UTP)test and measured the serum albumin(ALB)and serum creatinine(SCr)levels,phospholipase A2 receptor(PLA2R)antibody titer,and CD19+B-cell count every three months.RESULTS A total of nine refractory IMN patients were analyzed.During follow-up conducted twelve months later,the results from the 24 h UTP decreased from baseline[8.14±6.05 g/d to 1.24±1.34 g/d(P<0.05)]and the ALB levels increased from baseline[28.06±8.42 g/L to 40.93±5.85 g/L(P<0.01)].Notably,after administering RTX for six months,the SCr decreased from 78.13±16.49μmol/L to 109.67±40.87μmol/L(P<0.05).All of the nine patients were positive for serum anti-PLA2R at the beginning,and four patients had normal anti-PLA2R titer levels at six months.The level of CD19+B-cells decreased to 0 at three months,and CD19+B-cell count remained at 0 up until six months of follow-up.CONCLUSION Our low-dose RTX regimen appears to be a promising treatment strategy for refractory IMN.

The Beneficial Effect of 3-Month-Induction Therapy with Corticosteroids and Mycophenolate Mofetil Followed by Maintenance Therapy with Yearly Rituximab Infusions as Sole Maintenance Therapy in Cryptogenic Chronic Hypersensitivity Pneumonitis

Background: The available data on cryptogenic chronic hypersensitivity pneumonitis (ccHP) indicate an inherited predisposition to disease with triggering autoimmune phenomena. Hence, we evaluated prospectively the role of a new autoimmune regimen in treatment of its severe and progressive disease. Patients and Methods: A total of 9 patients were included in the study. They had criteria for ccHP viz. 1) clinical features of cryptogenic progressive restrictive lung disease, 2) high-resolution computed tomographic pulmonary abnormalities, and 3) bronchoalveolar lavage lymphocytosis (>30%). The regimen consisted of an initial induction phase of 3-month Solumedrol 1 g IV daily for 3 days followed by 1 month of Prednisone (P) 60 mg/day to tapered down to discontinuation by 3rd month. They also had received Mycophenolate mofetil (MMF) 1 g twice daily for 3 months. This stage was followed by a maintenance phase of yearly Rituximab infusions (1 g followed by 1 g 2 weeks later). Results: compared to their previous 6 months deterioration;all patients showed significant improvement in their forced vital volume, diffusion capacity for carbon monoxide, 6-minutes-walk after the induction phase (at 3 months) which improved further at 15 months with Rituximab therapy. Conclusion: After 3-month induction therapy with P and MMF;yearly R treatment is a safe, practical and effective long-term therapy for ccHP.

Efficacy and safety of Revlimid combined with Rituximab in the treatment of follicular lymphoma: A meta-analysis

Objective:To evaluate the clinical efficacy and safety of lenalidomide combined with rituximab for treating follicular lymphoma.Methods:We searched PubMed,Web of Science,Cochrane Library,Embase,China Medical Biological Service system(CBM),VIP database(VIP),Wan fang database(Wan Fang Data),China Knowledge Network(CNKI),and ClinicTrails.gov for literature related to lenalidomide combined with rituximab for treating follicular lymphoma(until June 23,2022).The literature that met the requirements were screened out according to the established criteria,and the data were analyzed by RevMan5.4 and Stata14.0 to conduct a meta-analysis.Results:Eight studies involving 865 patients with follicular lymphoma were included.The results of the meta-analysis showed that the objective remission rate(RR=1.43,95%CI:1.26–1.61)and complete remission rate(RR=1.67,95%CI:1.27–2.21)of lenalidomide combined with rituximab for treating follicular lymphoma were significantly higher than those of rituximab alone.However,adverse reactions(neutropenia,diarrhea,nausea and vomiting,rash)were more likely to occur in the lenalidomide combined with the rituximab group,albeit at a low level.Conclusion:Compared to rituximab alone,lenalidomide combined with rituximab could significantly improve the objective and complete remission rates of patients with follicular lymphoma.However,as combination therapy may be associated with adverse reactions,timely corresponding measures should be taken during treatment.Therefore,to confirm the efficacy and safety of lenalidomide combined with rituximab for treating follicular lymphoma,it is necessary to conduct multicenter,multi-sample,randomized double-blind controlled trials,and single-arm trials.

Membranous nephropathy with systemic light-chain amyloidosis of remission after rituximab therapy:A case report

BACKGROUND About 70%-80%of patients with primary membranous nephropathy(MN)have phospholipase A2 receptor(PLA2R)in renal tissue.Systemic light-chain(AL)amyloidosis is the most common type of amyloidosis.MN complicated with amyloidosis is rare.CASE SUMMARY A 48-year-old Chinese male presented with nephrotic syndrome,positive serum PLA2R antibody,and positive serum and urine IgG-lambda type M-protein,with a normal ratio of serum-free light-chain level.The patient was diagnosed with MN accompanied by AL amyloidosis.He was treated with rituximab with glucocorticoids and CyBorD regimen of chemotherapy.After 21 mo of follow-up,the patient achieved complete remission regarding nephrotic syndrome without adverse effects of chemotherapy.CONCLUSION We report a case of PLA2R-related MN complicated with primary AL amyloidosis only with renal involvement and successfully treated with rituximab,glucocorticoids and chemotherapy.

Rituximab combined with Bruton tyrosine kinase inhibitor to treat elderly diffuse large B-cell lymphoma patients: Two case reports

BACKGROUND Diffuse large B-cell lymphoma(DLBCL)is a common aggressive non-Hodgkin's lymphoma(NHL),accounting for 30%-40%of adult NHLs.This report aims to explore the efficacy and safety of rituximab combined with Bruton tyrosine kinase inhibitors(BTKis)in the treatment of elderly patients with DLBCL.CASE SUMMARY The clinical data of two elderly patients with DLBCL who received rituximab combined with BTKi in our hospital were retrospectively analyzed,and the literature was reviewed.The patients were treated with chemotherapy using the R-miniCHOP regimen for two courses.Then,they received rituximab in combination with BTKi.CONCLUSION The treatment experience in these cases demonstrates the potential efficacy of rituximab combined with BTKi to treat elderly DLBCL patients,thus providing a new treatment strategy.

Rituximab Therapy for Persistent, Severe and Extensive Idiopathic Bullous Pemphigoid

Background: Idiopathic Bullous Pemphigoid (IBP) is a rare blistering autoimmune disease. Its morbidity and mortality have remained high owing to complications of extensive skin involvement as well as its conventional steroid therapy. We reviewed the medical literature and found indicators of an autoimmune etiology for its pathogenesis triggering genetically predisposed patients. Objective: to evaluate, prospectively, the role of Rituximab (R) therapy in its persistent, severe and extensive form. Patients and methods: A total of 12 patients, with disease duration of 6 ± 1 months, were treated with yearly R infusions (1 g followed by 1 g 2 weeks later). Results: Significant clinical improvement was achieved as documented by decrease in total score of Bullous Pemphigoid Disease Area Index from 60 ± 3 to 6 ± 2 that persisted for 26 ± 11 months of follow up. Moreover, IBP autoantibodies (anti-BP 180 and anti-320 IgG) levels fell from to 91 ± 3 and 81 ± 2 to 8 ± 2 and 9 ± 2, respectively. Conclusions: R is a safe and effective treatment for severe IBP and such response further confirms its autoimmune pathogenesis.

Efficacy of Low-Dose Rituximab in Primary Immune Thrombocytopenia

Objective:To explore the effect of low-dose rituximab in primary immune thrombocytopenia.Methods:From January 2022 to January 2023,60 patients with primary immune thrombocytopenia were randomly divided into two groups.The control group was treated with standard doses of rituximab,and the observation group was treated with low doses of rituximab.Rituximab was used for treatment,and the clinical curative effect of the two groups was observed.Results:Before treatment,there was no statistically significant difference in platelet count(PLT),anti-GPⅡb/Ⅲa antibody,and anti-GPⅠb/Ⅸantibody between the two groups(P>0.05).After treatment,the PLT of the two groups increased significantly.Antibodies were all decreased,and there was no significant difference between the two groups(P>0.05).The incidence of adverse reactions in the observation group was 13.33%,and that in the control group was 40.00%.The adverse reactions in the observation group were significantly lower than the control group(P<0.05).Conclusion:In the clinical treatment of primary immune thrombocytopenia,low-dose rituximab can control the progression of the disease,improve blood routine indicators,and have fewer adverse reactions.

^(99)Tc^(m)-rituximab改良模式引导技术在原发性乳腺癌内乳前哨淋巴结活检的观察

目的探讨^(99)Tc^(m)-rituximab在乳腺癌内乳前哨淋巴结活检(IM-SLNB)中的应用,以及采用超声引导下大体积腺体内注射技术对乳腺癌患者内乳前哨淋巴结(IM-SLN)检出率的影响。资料与方法回顾性分析2017年9月—2022年1月福建省立医院行手术治疗的女性乳腺癌患者119例,根据注射部位分为3组:2针组45例,4针组19例,瘤周组55例。比较各组不同注射方法、注射部位的IM-SLN检出率及腋窝前哨淋巴结检出率及原发肿瘤位置对IM-SLN检出率的影响。结果2针组IMSLN(64.44%,29/45)和4针组IM-SLN的检出率(52.63%,10/19)均显著高于瘤周组IM-SLN(9.09%,5/55;χ^(2)=13.981、33.794,均P=0.000)。瘤周组与2针组及4针组检出的腋窝前哨淋巴结平均个数差异无统计学意义(2.38枚比2.46枚比2.53枚;χ^(2)=0.284,P=0.867)。原发肿瘤位置不同,IM-SLN检出率差异无统计学意义(χ^(2)=1.444,P=0.486)。结论采用超声引导下大体积腺体内注射技术后,^(99)Tc^(m)-rituximab引导的IM-SLNB检出率显著提高,为内乳区淋巴结活检创造了微创治疗的重要条件,并为准确的淋巴结分期提供了重要的技术支持。

Efficacy of Rituximab Combined with Plasma Exchange in the Treatment of Thrombotic Thrombocytopenic Purpura(TTP)

Objective:To analyze the curative effect of rituximab combined with plasma exchange in the treatment of thrombotic thrombocytopenic purpura.Methods:70 patients with thrombotic thrombocytopenic purpura that were treated in our hospital from January 2022 to January 2023 were selected for this study.They were divided into two groups according the treatment method they were about to receive.The patients in the control group received plasma exchange.The observation group was given rituximab in addition to plasma exchange.Then,the therapeutic effects of the two groups were observed,and the incidence of adverse reactions was compared.Results:The rate of effectiveness of the treatment received in observation group and the control group was 97.14%and 82.86%,respectively.The treatment received in observation group had a better therapeutic effect(P<0.05).The incidence of adverse reactions in the observation group(22.86%)was lower than that of the control group(5.71%),with P<0.05.Conclusion:Rituximab combined with plasma exchange is relatively more effective than plasma exchange alone,with less adverse reaction,making it a viable treatment option.

Effect of Rituximab Versus Mycophenolate Mofetil or Cyclophosphamide as Control in Lupus Nephritis:A Meta-Analysis

Objective:To evaluate the effects of rituximab versus mycophenolate mofetil or cyclophosphamide as control in lupus nephritis by meta-analysis.Methods:A systematic search was carried out up to January 2022,obtaining 7 studies involving 645 participants with lupus nephritis at the commencement of the investigation;198 of them were treated with rituximab,while 447 were treated with mycophenolate mofetil or cyclophosphamide.We determined the odds ratio(OR)and mean difference(MD)with 95%confidence index(CI)to compare rituximab’s efficacy to that of mycophenolate mofetil or cyclophosphamide as control in lupus nephritis using random-or fixed-effects model by dichotomous or continuous techniques.Results:The rituximab group showed significantly higher complete renal remission rate(OR=2.52;95%CI 1.30-4.91,P=0.006)and total renal remission rates(OR=2.22;95%CI 1.36-3.63,P=0.001)than the control group.However,there was no significant difference in terms of end Systemic Lupus Erythematosus Disease Activity Index(SLEDAI)score(MD-1.16;95%CI-2.88-0.57,P=0.19),proteinuria(MD-0.31;95%CI-0.70-0.09,P=0.013),and serum creatinine(MD 0.01;95%CI-0.04-0.07,P=0.64)between the rituximab group and the control.Conclusion:Rituximab exhibited significantly greater complete renal remission rate and total renal remission rates,with no significant difference in terms of shorter-end SLEDAI,proteinuria,and serum creatinine,compared with the control in individuals with lupus nephritis.

前哨淋巴结显像剂^(99)Tc^m-IT-Rituximab的制备及其定位性能

目的研究前哨淋巴结(SLN)显像剂 ^(99)Tc^m-亚氨基噻吩(IT)-美罗华(Rituximab)的标记方法及其定位效应。方法采用2-IT 作为双功能连接剂,制备 ^(99)Tc^m-IT-Rituxinlab,确定最佳反应条件,评价标记抗体分子完整性及生物活性。观察比较 ^(99)Tc^m-IT-Rituximab 及 ^(99)Tc^m-硫胶体(SC)2种示踪剂在小鼠淋巴结中的定位性能。将 ^(99)Tc^m-IT-Rituximab 作为显像剂,对10例乳腺癌患者行乳腺癌 SLN动态显像。结果 2-IT 与 Rituximab 连接的最佳物质的量比为10:1,4℃反应45 min 后,每分子抗体螯合上的游离巯基数平均为2.1个。IT-Rituximab 分子保持完整、免疫活性保留完全。^(99)Tc^m-IT-Ritux-imab 的标记率>90%,其与 B 淋巴瘤细胞株 Raji 细胞的结合率为69.4%。动物显像结果显示 ^(99)Tc^m-IT-Rituximab 可清晰定位小鼠 SLN,注射后30 min～24 h SLN 均可显影,2 h 后 SLN 显影清晰,至24 h未见次级淋巴结显影。动物体内分布数据显示 ^(99)Tc^m-IT-Rituximab 定位性能明显优于 ^(99)Tc^m-SC,24 h时 SLN 百分注射剂量率(%ID)为4.49%,次级及第3级淋巴结基本无摄取,24 h 注射点滞留率为22.14% 结论该标记方法简单,标记率高;^(99)Tc^m-IT-Rituximab 在 SLN 中定位性能良好,是一种潜在的新型 SLN 显像剂。

特异性前哨淋巴结显像剂^(99)Tc^m-rituximab药盒的制备及生物评价

采用2-巯基乙醇修饰Rituximab(利妥昔单克隆抗体),制得其冻干药盒。所制得的冻干药盒性质稳定,可在-20℃冷冻保存3个月以上。利用99 Tcm-葡庚糖酸钠(GH)交换法,标记冻干药盒得到99 Tcm-ritux-imab,标记率和放化纯度均大于90%。生物分布结果显示:SD大鼠经前脚掌皮下注射99 Tcm-rituximab后,前哨淋巴结的摄取值在1～4h内逐渐增加,在4h时达到(2.14±0.46)%ID,前哨淋巴结与注射点的放射性摄取比在4h时达到最大(14.80%±2.11%),且在18h时,这一比值基本保持不变。SPECT显像结果表明,在30min～18h内,大鼠的前哨淋巴结清晰可见,无次级淋巴结显影。本研究提供了一种特异性前哨淋巴结显像剂的药盒化制备方法,该方法操作简便,性能稳定,便于在临床推广应用。

前哨淋巴结示踪剂^(99)Tc^m-IT-Rituximab的制备及初步动物实验研究

目的研究新型特异性前哨淋巴结(SLN)示踪剂^(99)Tc^m-IT-Rituximab的定位效应。方法采用2-亚氨基噻吩(2-IT)修饰法制备^(99)Tc^m-IT-Rituximab,并评价其定位SLN的生物性能,监测注射显像剂的化学剂量及注射体积对SLN摄取的影响。结果^(99)Tc^m-IT-Rituximab标记率大于90%,分子保持完整。^(99)Tc^m-IT-Rituximab可清晰定位小鼠SLN,注射后30min到24h SLN均可显影,未见次级淋巴结显影。注药后24h SLNID%值为4.49%,次级及第三级淋巴结ID%摄取率比值相当于本底,24h注射点滞留率为22.14%。示踪剂的化学量及注射体积均影响SLN显像。随着二者的增加,SLN%ID值逐渐减少,次级及第三级淋巴结%ID值均逐渐上升。结论^(99)Tc^m-IT-Rituximab的标记方法简单,研究结果表明其具有潜在的临床应用价值。