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.

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.

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.

Synthesis of a novel series of amino acid prodrugs based on tegafur and evaluation of their antitumor activity

As an oral chemotherapy prodrug,tegafur,can be converted to 5-fluorouracil,which is activated to kill tumor cells mainly by the inhibition of thymidylate synthase.In the present study,we synthesized 20 new tegafur derivatives containing amino acid ester groups by substitution,hydrolysis,and condensation.Their structures were confirmed by 1H NMR,13C NMR,and H RMS,and their inhibitory effects on tumor cell growth were studied.The results showed that some of the compounds had good anti-tumor activity.

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.

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.

替吉奥联合奥沙利铂对老年胃癌患者胃动力相关激素及基质金属蛋白酶-2、基质金属蛋白酶-9的影响

目的探讨替吉奥联合奥沙利铂对老年胃癌患者胃动力相关激素及基质金属蛋白酶-2(MMP-2)、基质金属蛋白酶-9(MMP-9)的影响。方法选取128例老年胃癌患者为研究对象,随机分成对照组(n=64)与观察组(n=64)。对照组给予替吉奥治疗,观察组给予替吉奥联合奥沙利铂治疗。观察2组的胃动力相关激素[胃动素(MTL)、血管活性肠肽(VIP)]、MMP-2与MMP-9、肿瘤标志物[癌胚抗原(CEA)、糖类抗原125(CA125)、糖类抗原19-9(CA19-9)]、临床疗效以及不良反应发生情况。分析胃动力相关激素与MMP-2、MMP-9及肿瘤标记物水平的相关性。结果治疗后,2组MTL低于治疗前,VIP高于治疗前,且观察组MTL低于对照组,VIP高于对照组,差异有统计学意义(P<0.05)。治疗后,2组MMP-2、MMP-9及CEA、CA125、CA19-9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)。观察组总有效率为70.31%,高于对照组的53.13%,差异有统计学意义(P<0.05)。2组不良反应发生率比较,差异无统计学意义(P>0.05)。MTL与MMP-2、MMP-9、CEA、CA125、CA19-9呈负相关(P<0.05);VIP与MMP-2、MMP-9、CEA、CA125、CA19-9呈正相关(P<0.05)。结论替吉奥联合奥沙利铂治疗老年胃癌患者的效果较好,且安全性较高。MTL、VIP与MMP-2、MMP-9及CEA、CA125、CA19-9在老年胃癌患者的疾病发展中起相互关联作用。

以替吉奥为基础联合阿帕替尼三药方案对进展期胃癌患者的影响

目的研究以替吉奥为基础联合阿帕替尼对进展期胃癌患者免疫功能及血清细胞因子水平的影响。方法选取本院89例进展期胃癌患者,采用随机数字表法分组,对常规组44例采用奥沙利铂、替吉奥治疗,对研究组45例增加阿帕替尼,对比两组患者血清肿瘤标志物水平、血清细胞因子水平、免疫功能和不良反应。结果研究组治疗后癌胚抗原(CEA)、糖类抗原125(CA125)水平低于常规组(P<0.05);研究组治疗后血清γ-干扰素(IFN-γ)、正常上皮细胞特异性-1基因(NES1)、白介素-10(IL-10)和肿瘤坏死因子-α(TNF-α)水平高于常规组(P<0.05);研究组治疗后T淋巴细胞(CD8+)水平低于常规组,CD3+、CD4+水平高于常规组(P<0.05)。结论以替吉奥为基础联合阿帕替尼三药方案对进展期胃癌患者效果确切,能够有效提高患者的免疫功能,改善血清细胞因子水平,降低血清肿瘤标志物水平,安全性高。

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。

安罗替尼与阿帕替尼分别联合替吉奥治疗晚期食管癌的效果比较

目的 探讨安罗替尼与阿帕替尼分别联合替吉奥治疗晚期食管癌的临床效果。方法 选取2020年10月~2021年10月本院收治的126例晚期食管癌患者作为研究对象,按随机数字表法分为两组。对照组63例给予阿帕替尼联合替吉奥治疗,观察组63例给予安罗替尼联合替吉奥治疗。对比两组客观缓解率(ORR)、疾病控制率(DCR)、中位总生存期(OS)、无进展生存期(PFS)、治疗期间不良反应发生情况;另比较两组治疗前后Karnofsky功能状态(KPS)评分和食管癌专用量表(QLQ-OES24)评分。结果 观察组ORR、DCR均高于对照组(30.16%比14.29%、76.19%比58.73%,P<0.05);观察组患者的OS、PFS均长于对照组[(7.23±1.32)个月比(6.43±1.22)个月、(3.67±0.69)个月比(3.23±0.58)个月,P<0.05];两组不良反应发生率差异无统计学意义(P>0.05);治疗后两组KPS、QLQ-OES24评分均升高(P<0.05),且观察组均高于对照组(P<0.05)。结论 安罗替尼与阿帕替尼联合替吉奥治疗晚期食管癌均有一定的治疗效果,但相较于阿帕替尼联合替吉奥,安罗替尼联合替吉奥治疗更有利于延长患者无进展生存时间和中位总生存期,提高近期疗效,改善患者生活质量,且安全性良好。

替雷利珠单抗联合白蛋白结合型紫杉醇和替吉奥二线治疗晚期胃癌的效果

目的探讨替雷利珠单抗联合白蛋白结合型紫杉醇和替吉奥二线治疗晚期胃癌的效果。方法选取2020年1月至2023年1月宝鸡市陈仓医院肿瘤科收治的100例晚期胃癌患者,随机将其分为对照组和观察组,各50例。对照组给予白蛋白结合型紫杉醇和替吉奥二线治疗,观察组在对照组基础上给予替雷利珠单抗治疗。比较两组的治疗效果。结果观察组的治疗总有效率高于对照组(P<0.05)。治疗后,观察组的癌胚抗原(CEA)、糖类抗原72-4(CA72-4)及糖类抗原199(CA199)水平低于对照组(P<0.05)。治疗后,观察组的CD4^(+)、CD4^(+)/CD8^(+)高于对照组,CD8^(+)低于对照组(P<0.05)。两组的不良反应发生率无明显差异(P>0.05)。结论替雷利珠单抗联合白蛋白结合型紫杉醇和替吉奥二线治疗晚期胃癌患者有助于提高治疗效果,降低肿瘤标志物水平,改善免疫功能,值得推广。

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。