Inetetamab combined with tegafur as second-line treatment for human epidermal growth factor receptor-2-positive gastric cancer: A case report

BACKGROUND Human epidermal growth factor receptor-2(HER-2)plays a vital role in tumor cell proliferation and metastasis.However,the prognosis of HER2-positive gastric cancer is poor.Inetetamab,a novel anti-HER2 targeting drug independently developed in China,exhibits more potent antibody-dependent cell-mediated cytotoxicity than trastuzumab,which is administered as the first-line treatment for HER2-positive gastric cancer in combination with chemotherapy.In this case,the efficacy and safety of inetetamab combined with tegafur was investigated as a second-line treatment for HER2-positive gastric cancer.CASE SUMMARY A 52-year-old male patient with HER2-positive gastric cancer presented with abdominal distension,poor appetite,and fatigue two years after receiving six cycles of oxaliplatin combined with tegafur as first-line treatment after surgery,followed by tegafur monotherapy for six months.The patient was diagnosed with postoperative recurrence of gastric adenocarcinoma.He received 17 cycles of a combination of inetetamab,an innovative domestically developed anti-HER2 monoclonal antibody,and tegafur chemotherapy as the second-line treatment(inetetamab 200 mg on day 1,every 3 wk combined with tegafur twice daily on days 1–14,every 3 wk).Evaluation of the efficacy of the second-line treatment revealed that the patient achieved a stable condition and progression-free survival of 17 months.He tolerated the treatment well without exhibiting any grade 3-4 adverse events.CONCLUSION Inetetamab combined with chemotherapy for the treatment of metastatic HER2-positive gastric cancer demonstrates significant survival benefits and acceptable safety.

Thermodynamic study on the interaction between anti-tumor drug tegafur and human serum albumin

The changes of thermodynamic properties of the system on interaction between tegafur and human serum albumin （HSA） and the changes of secondary structure units of HSA in the system at 298.15 K have been investigated by the Nano-Watt-Scale isothermal titration calorimetry （ITC）, the Langmuirs binding model and the circular dichroism （CD） spectrometry.

Tegafur-uracil-induced rapid development of advanced hepatic fibrosis

Tegafur-uracil has been reported to have only minor adverse effects and is associated with liver injury in 1.79% of Japanese patients. The development of tegafur-uracil-induced hepatic fibrosis with portal hypertension is rare. Here, we report a case of a 74-year-old woman with rapidly developing tegafururacil-induced hepatic fibrosis. The patient had no history of liver disease and had been treated with tegafur-uracil for 8 mo after breast cancer surgery. The patient was admitted to our hospital for abdominal distension and leg edema associated with liver dysfunction. Computed tomography imaging revealed massive ascites and splenomegaly, and a non-invasive assessment of liver fibrosis indicated advanced fibrosis. The histopathological findings revealed periportal fibrosis and bridging fibrosis with septation. The massive ascites resolved after discontinuing tegafururacil. These findings suggest that advanced hepatic fibrosis can develop from a relatively short-term administration of tegafur-uracil and that non-invasive assessment is useful for predicting hepatic fibrosis.

TEGAFUR PLUS MMC OR ACNU IN THE TREATMENT OF ADVANCED GASTRIC CANCER-A PILOT STUDY

Twenty four cases of advanced gastric cancer were divided into two groups according to the general condition of the patients (PS 0-2 and 3-4), further subdivided into localized abdominal form, liver metastatic form, ascitic form and distant metastatic form. These patients were allocated randomly into Regimen A or B. Regimen A: Tegafur 600 mg daily and Mitomycin C (MMC) 5 mg/m2/1-2 weeks. Regimen B: Tegafur 600 mg daily and ACNU (Nimustine, water-soluble Nitrosourea) 60 mg/week for 2 weeks. After a course of ACNU, it was with drawn for 4 weeks and then resumed again. The response rate of Regimen A was 3/11 (27%), that of Regimen B was 3/13 (23%).

A Case of Advanced Multiple Hepatocellular Carcinomas with Portal Vein Tumor Thrombosis Successfully Treated by Oral Tegafur/Uracil

A case of advanced multiple hepatocellular carcinomas (HCC) with portal vein tumor thrombosis successfully treated by oral tegafur/uracil is reported. A 69-year-old Japanese woman with advanced HCC with tumor thrombosis underwent transcatheter arterial infusion chemotherapy in April 2001. However, 1 year later, the patient experieced a recurrence with advanced multiple HCC with portal vein tumor thrombosis and ascites. Treatment with oral tegafur/uracil was started in May 2002 and resulted in the partial response of liver tumors and the complete improvement of ascites. She remained in good health for about 6 years. This case strongly suggests that oral tegafur/uracil is an effective treatment for some cases of advanced HCC with portal vein tumor thrombosis.

Feasibility and Efficacy Study of Biweekly Irinotecan Combined with Oral Tegafur/Uracil in Advanced Colorectal Cancer

Background: We evaluated the feasibility and efficacy of irinotecan (CPT-11) plus tegafur/uracil (UFT) combination chemotherapy in patients with advanced colorectal cancer. Patients and Methods: PK parameters were concurrently measured to confirm the presence of drug interactions in this treatment schedule. CPT-11 was administered intravenously at the dose of 150 mg/m2 on days 1, 15. UFT was administered at the dose of 375 mg/m2/day (B.I.D.) on days 3 - 7, 10 - 14, 17 - 21, 24 - 28 repeated every 5 weeks. Results: 31 patients were enrolled. PK parameters for CPT-11, FT, 5-FU and uracil are available from 5 patients. The overall response rate was 16.1%. The median time to treatment discontinuation was 3.9 months. There was no significant difference in PK parameters of CPT-11 between day 1 and day 15 and of UFT between day 3 and day 10. Conclusion: CPT-11 plus UFT combination chemotherapy exhibited a tolerable toxicity profile with acceptable efficacy. Pharmacokinetic analysis showed that there were no drug interactions in this treatment schedule.

Clinical Efficacy and Safety of Oxaliplatin-tegafur,Gimeracil and Oteracil Potassium and Vinorelbine-Pt in the Treatment of Advanced Triple Negative Breast Cancer

The purpose of this study was to investigate the efficacy and safety of oxaliplatin combined with tegafur,gimeracil and oteracil potassium(SOX regimen)and vinorelbine combined with Pt(NP regimen)in the treatment of advanced triple negative breast cancer(TNBC).First of all,88 patients with advanced breast cancer were selected and divided into observation group and control group with 44 cases each by random number method.Both groups received conventional supportive therapy.On this basis,SOX regimen was adopted in the observation group and NP regimen in the control group,and the efficacy,occurrence of toxic and side effects in the two groups were compared.The results showed that the objective effective rates and clinical benefit rates of the two groups were statistically significant(P<0.05).In addition,both groups had hand foot syndrome,diarrhea,liver function damage,decreased platelet(PLT)and other toxic side effects,but the incidence of rash,oral ulcer and pigmentation in the observation group was significantly lower than that in the control group(P<0.05).Therefore,both SOX regimen and NP regimen can effectively treat advanced TNBC adverse reactions,but SOX regimen was more effective.

Multicenter Analysis of mFOLFOX6 with Oxaliplatin Stop-and-Go Strategy Using Oral Uracil-Tegafur with Leucovorin for Unresectable Colorectal Cancer in Elderly Patients

Background: This study evaluated the tolerability and efficacy of intermittent oxaliplatin treatment based on mFOLFOX6 using oral uracil-tegafur(UFT) and leucovorin(LV) maintenance therapy in the treatment of elderly patients with advanced colorectal cancer. Methods: Ten non-elderly patients (70 years) with advanced/recurrent colorectal cancer were enrolled in this prospective, multicenter cooperative group clinical trial. The mFOLFOX6 regimen was administered for eight cycles with maintenance therapy with oral UFT/LV treatment until progression. In cases with disease progression, mFOLFOX6 was reintroduced. Results: Grade 2 peripheral neuropathy was noted in 30.0% and 25.0% of the elderly and non-elderly patients, respectively. The observed time to treatment failure (TTF) was 6.3 months in the elderly patients and 6.4 months in the non-elderly patients. The disease control rate was 83.3% in each group. Conclusion: Our new stop-and-go strategy using oral UFT/LV is well-tolerated and effective even in elderly patients.

Effect of Tegafur Gimeracil Oteracil Potassium Capsule + Kangai injection + intensity-modulated radiation therapy on the cellular malignant biological processes in advanced cervical cancer lesion

Objective:To study the effect of Tegafur Gimeracil Oteracil Potassium Capsule + Kangai injection + intensity-modulated radiation therapy on the cellular malignant biological processes in advanced cervical cancer lesion.Methods: Patients who were diagnosed with advanced cervical cancer in the Second People Hospital of Banan District Chongqing between April 2015 and March 2017 were selected and divided into two groups, group A received Tegafur Gimeracil Oteracil Potassium Capsule + Kangai injection + intensity-modulated radiation therapy, and group B received cisplatin + intensity-modulated radiation therapy. Serum contents of tumor markers, tumor invasion molecules and tumor proliferation molecules of two groups of patients were detected before treatment as well as 2 weeks and 4 weeks after treatment.Results: Serum E-cad, STMN1, Fas and p53 levels of both groups of patients 2 weeks and 4 weeks after treatment were significantly higher than those before treatment while TSGF, TK1, SCC-Ag, CA125, OPN, MMP9, NGAL, CyclinE, CyclinD1 and PCNA levels were significantly lower than those before treatment, and serum E-cad, STMN1, Fas and p53 levels of group A 2 weeks and 4 weeks after treatment were significantly higher than those of group B while TSGF, TK1, SCC-Ag, CA125, OPN, MMP9, NGAL, CyclinE, CyclinD1 and PCNA levels were significantly lower than those of group B.Conclusion: Tegafur Gimeracil Oteracil Potassium Capsule + Kangai injection + intensity-modulated radiation therapy for advanced cervical cancer can induce cancer cell apoptosis and inhibit cancer cell proliferation and invasion.

Clinical Analysis of Gemcitabine Combined with Tegafur Chemotherapy after Radical Surgery on Pancreatic Cancer

Objective:To study and analyze the clinical efficacy of gemcitabine combined with Tegafur chemotherapy after radical resection of pancreatic cancer.Methods:The subjects of the study were 200 patients who were admitted to the hospital from January 2018 to February 2021 requiring chemotherapy after radical resection of pancreatic cancer.According to the different treatment methods,they were divided into a experimental group(gemcitabine combined with Tegafur chemotherapy)and a control group(single gemcitabine chemotherapy),and the treatment efficacy of the two groups of patients was observed and compared.Results:Compared with the control group,patients in the experimental group had significantly better treatment efficacy,quality of life scores and post-treatment anxiety and depression scores.The difference between the groups was significant(p<0.05).Conclusion:Gemcitabine combined with Tegafur chemotherapy for patients requiring chemotherapy after radical resection of pancreatic cancer can significantly improve the treatment efficacy for the disease,improve the patient's quality of life,and ensure that the patient's emotional state during treatment is more positive.

Chemotherapy with enteric-coated tegafur/uracil for advanced hepatocellular carcinoma

Hepatocellular carcinoma (HCC) is one of the most common malignancies worldwide, including Japan. Although the development of imaging modalities has made the early diagnosis of HCC possible, surgically resectable cases are relatively uncommon because of hepatic function reserve and/or an advanced stage at presentation. Several modalities, such as transcatheter arterial chemoembolization, percutaneous ethanol injection, microwave coagulation therapy and radiofrequency ablation are reportedly useful in treating patients with non-resectable disease. However, unfortunately, many HCC patients have tumor recurrence. The overall prognosis of patients with HCC is very poor, and treatment of the advanced form is still problematic. In this article, we review the clinical efficacy and toxicity of enteric-coated tegafur/uracil in the treatment of patients with advanced non-resectable HCC.

Nab-paclitaxel plus tegafur gimeracil oteracil potassium capsule (S-1) as first-line treatment for advanced biliary tract adenocarcinoma: a phase 2 clinical trial

Background:This study aimed to evaluate the efficacy and safety of a new combination of nab-paclitaxel plus tegafur gimeracil oteracil potassium capsule(S-1)for patients with advanced biliary tract carcinoma(BTC).Methods:Patients were treated with nab-paclitaxel at a dose of 125 mg/m2 on day 1 and 8,and S-1,80 to 120 mg/day on days 1-14 of a 21-day cycle.Treatments were repeated until disease progression or unacceptable toxicity occurred.The primary endpoint was objective response rate(ORR).The secondary endpoints were median progression-free survival(PFS),overall survival(OS),and adverse events(AEs).Results:The number of patients enrolled were 54,and 51 patients were evaluated for efficacy.A total of 14 patients achieved partial response(PR)with an ORR of 27.5%.The ORR varied by sites,with 53.8%(7/13)for gallbladder carcinoma,18.4%(7/38)for cholangiocarcinoma.The most common grade 3 or 4 toxicities were neutropenia and stomatitis.The median PFS and OS were 6.0 and 13.2 months,respectively.Conclusions:The combination of nab-paclitaxel with S-1 showed explicit antitumor activities and favorable safety profile in advanced BTC and could serve as a potential non-platinum and-gemcitabine-based regimen.

替吉奥联合放疗治疗胃癌疗效及安全性的Meta分析

目的 采用Meta分析评价替吉奥联合放疗治疗胃癌的疗效及安全性。方法 通过计算机检索PubMed、Embase、万方数据知识服务平台、中国知网、维普网数据库中关于替吉奥联合放疗治疗胃癌的研究文献,文献检索时间为从建库到2023年3月。按纳入及排除标准筛选文献,对文献进行风险偏倚评价并提取文献信息,采用RevMan 5.3软件进行Meta分析。结果 纳入文献9篇,共包含648例患者,Meta分析结果显示,替吉奥联合放疗与单纯放疗相比,可提高胃癌患者的完全缓解率[危险比(RR)=2.31,95%CI(1.60,3.32),P<0.000 01]、部分缓解率[RR=1.82,95%CI(1.43,2.32),P<0.000 01]、客观缓解率[RR=1.98,95%CI(1.66,2.35),P<0.000 01],但增加了消化道反应[RR=1.32,95%CI(1.08,1.62),P=0.008]、骨髓抑制[RR=1.65,95%CI(1.28,2.14),P=0.000 1]的发生率。结论 替吉奥联合放疗可以提高胃癌的近期疗效,但增加了不良反应的发生率。

甲磺酸阿帕替尼片联合替吉奥治疗老年进展期胃癌患者的临床研究

目的 研究甲磺酸阿帕替尼片联合替吉奥治疗老年进展期胃癌患者的效果。方法 选择老年进展期胃癌患者60例,将所有研究对象进行随机数字序号编码,最终确认序号编排为1~30患者为对照组,序号编排为31~60患者为研究组。对照组患者接受替吉奥治疗,研究组患者接受甲磺酸阿帕替尼片联合替吉奥治疗。对比两组临床治疗效果,不良反应发生情况,治疗后第1、2、3年的生存情况。结果 研究组的缓解率53.33%、控制率80.00%高于对照组的16.67%、46.67%(P<0.05)。研究组不良反应发生率为26.67%,对照组则为20.00%,对比无统计学意义(P>0.05)。对照组第2、3年生存20例(66.67%)和18例(60.00%),研究组则为27例(90.00%)和25例(83.33%),研究组第2、3年生存率高于对照组(P<0.05)。两组第1年生存率比较无统计学意义(P>0.05)。结论 老年进展期胃癌患者在甲磺酸阿帕替尼片联合替吉奥治疗后,显著缓解并控制了疾病的进展,不会增加不良反应的发生,并延长生存时间,值得临床推广。

替吉奥联合三维适形放疗治疗食管癌疗效及对心脏损伤和毒副反应的影响

目的探讨替吉奥联合三维适形放疗治疗食管癌疗效及对心脏损伤和毒副反应的影响。方法选取行放化疗的92例中晚期食管癌患者,随机分为试验组和对照组,每组46例。对照组患者采用三维适形放疗治疗,试验组患者采用三维适形放疗联合替吉奥治疗,均持续治疗6周。观察两组患者的近期临床疗效,分别于治疗前后抽取患者空腹静脉外周血,检测患者的细胞角化素蛋白片段19(CYFRA21-1)、癌胚抗原(CEA)、鳞状上皮细胞癌抗原(SCC)、心肌肌钙蛋白I(cTnI)、肌红蛋白(Mb)、肌酸激酶同工酶(CK-MB)水平。记录两组患者在放疗期间的毒副反应发生情况。结果试验组患者的总缓解率为50.00%,与对照组的41.30%比较差异无统计学意义(P>0.05);试验组患者的疾病控制率为93.48%,高于对照组的78.26%(P<0.05)。治疗后,两组患者CYFRA21-1、CEA、SCC水平均有下降(P<0.05),试验组患者的CYFRA21-1、CEA、SCC水平低于对照组(P<0.05);两组患者的cTnI、Mb、CK-MB水平均有上升(P<0.05),试验组患者的CYFRA21-1、CEA、SCC水平与对照组比较差异无统计学意义(P<0.05);两组患者的毒副反应情况比较差异无统计学意义(P>0.05)。结论三维适形放疗联合替吉奥治疗食管癌的临床疗效优于单独三维适形放疗,且安全性较好。

Polyethylenimine-cyclodextrin-tegafur conjugate shows anti-cancer activity and a potential for gene delivery

Polyethylenimine-cyclodextrin-tegafur(PEI-CyD-tegafur) conjugate was synthesized as a novel multifunctional prodrug of tegafur for co-delivery of chemotherapeutic agent tegafur and enhanced green fluorescent protein(EGFP) reporter plasmid DNA.Conjugation of tegafur to PEI-CyD via chemical linkage was characterized by 1 H NMR spectrometry and ultraviolet(UV) spectrometry.PEI-CyD-tegafur was able to condense plasmid DNA into complexes of around 150 nm with positive charge at the N/P ratio of 25,in accordance with electron microscopy observation of compact and monodisperse nanoparticles.The results of in vitro experiments showed enhanced cytotoxicity and considerable transfection efficiency in B16F10 cell line.Therefore,PEI-CyD-tegafur may have great potential as a co-delivery system with anti-cancer activity and potential for gene delivery.

替加氟-焦脱镁叶绿酸A胶束的制备

目的以替加氟和焦脱镁叶绿酸A为原料合成缀合物,并将其制备成胶束,实现光动力治疗和化疗的协同抗肿瘤作用。方法以丁二酸酐连接替加氟衍生物与焦脱镁叶绿酸A,通过核磁共振氢谱、质谱进行结构表征;通过溶剂挥发法制备载药胶束,以载药量、形貌、粒径、ζ电位、体外抗肿瘤活性等对载药胶束进行制剂学评价。结果替加氟-焦脱镁叶绿酸A复合物的结构得以确证;通过马尔文激光粒度仪和透射电镜验证所制备载药胶束粒径为143.9 nm,粒度均一;载药胶束可持续释药72 h以上,且激光照射可加速药物释放;载药胶束经激光照射可增强体外抗肿瘤效果,IC_(50)值为14.81μg·mL^(-1),其细胞毒性相较于单独给药替加氟增加至1.43倍。结论替加氟-焦脱镁叶绿酸A前药负载的胶束可实现替加氟的缓释作用,并可通过光动力治疗联合化疗有效提高替加氟体外抗肿瘤效果。

康艾注射液联合SOX化疗方案治疗晚期胃癌的临床研究

目的:观察康艾注射液联合SOX(替吉奥和奥沙利铂)化疗方案治疗晚期胃癌的临床疗效。方法:选择100例同意化疗的晚期胃癌患者,通过随机数字表法分为对照组和观察组,每组50例。对照组使用SOX治疗方案,静注奥沙利铂注射液,同时口服替吉奥胶囊。观察组在对照组基础上联合静脉注射康艾注射液,两组均连续治疗14天,停药7天,以21天为1个治疗周期,连续治疗3个周期。观察两组临床总有效率、疾病控制率、血清肿瘤标记物水平、卡式(Karnofsky,KPS)评分及不良反应发生率。结果:治疗3个周期后,观察组总有效率[64.0%(32/50)]优于对照组[48.0%(24/50)](P<0.05);观察组疾病控制率[84.0%(42/50)]优于对照组[70.0%(35/50)](P<0.05)。治疗后,观察组血清肿瘤标志物癌胚抗原(carcinoembryonic antigen,CEA)、糖类抗原199(carbohydrate antigen199,CA199)、糖类抗原724(carbohydrate antigen724,CA724)水平低于对照组,KPS评分高于对照组(P<0.05);观察组不良反应发生率[28.0%(14/50)]低于对照组[42.0%(21/50)](P<0.05)。结论:康艾注射液联合SOX化疗方案治疗晚期胃癌可降低患者肿瘤标志物水平,提高其生活质量,减少不良反应发生率。

替吉奥联合奥沙利铂治疗晚期胃癌的效果分析

目的:分析替吉奥联合奥沙利铂治疗晚期胃癌的效果。方法:选取2018年5月—2019年5月广东省深圳市南雅医疗美容门诊部收治的78例晚期胃癌患者作为研究对象,采用随机数字表法分为两组,各39例。对照组实施卡培他滨联合奥沙利铂治疗,观察组实施替吉奥联合奥沙利铂治疗。比较两组治疗效果。结果:观察组近期治疗总有效率、临床控制率高于对照组,胃肠道反应、白细胞减少、血小板减少、血红蛋白减少发生率低于对照组,差异有统计学意义(P<0.05)。治疗后,两组癌抗原19-9、糖类抗原125、癌胚抗原、人可溶性细胞间黏附分子-1、基质金属蛋白酶-2、基质金属蛋白酶-9、血管内皮生长因子水平低于治疗前,且观察组低于对照组,差异有统计学意义(P<0.05)。结论:替吉奥联合奥沙利铂治疗晚期胃癌的效果显著,可抑制肿瘤增殖、侵袭和转移,且不良反应较少,值得临床推广。

阿帕替尼联合替吉奥对老年晚期胃癌患者肠道微生态、外周血肿瘤异常蛋白水平及Th1/Th2细胞因子水平的影响

目的:分析老年晚期胃癌患者接受替吉奥联合阿帕替尼治疗对其肠道微生态、外周血肿瘤异常蛋白水平及Th1/Th2细胞因子水平的影响。方法:抽签法将2020年2月至2022年6月我科95例老年晚期胃癌患者分组,对照组47例患者口服替吉奥胶囊,观察组48例患者联合阿帕替尼口服,均28d为1周期。治疗2个周期后,采用菌落计数法(Colony forming units,CFU)测定乳酸杆菌、双歧杆菌、粪肠球菌及大肠埃希菌计数;采用免疫放射法测定癌胚抗原(Carcino-embryonic antigen,CEA)、肿瘤特异性生长因子(Tumor specific growth factor,TSGF)、糖类抗原19-9(Carbohydrate antigen199,CA19-9)、白细胞介素-10(Interleukin-10,IL-10)、白细胞介素-4(Interleukin-4,IL-4)、肿瘤坏死因子-α(Tumor necrosis factor-α,TNF-α)及γ-干扰素(Interferon-γ,INF-γ)水平;采用随访方法记录各患者不良反应。结果:观察组治疗后,乳酸杆菌、双歧杆菌和粪肠球菌、外周血CEA、TSGF、CA19-9、IL-10、IL-4较对照组低,大肠埃希菌、TNF-α及INF-γ较对照组高(P<0.05),血压升高和手足综合征高于对照组(P<0.05);但两组患者腹泻、恶心呕吐、中性粒细胞减少和血小板减少无统计学差异(P>0.05)。结论:老年晚期胃癌患者接受替吉奥联合阿帕替尼治疗,患者肠道微生态、肿瘤异常蛋白及Th1/Th2细胞因子水平均得到有效改善,且不明显增加严重不良反应。