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Synthesis of a novel series of amino acid prodrugs based on tegafur and evaluation of their antitumor activity 被引量:3
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作者 Shiqi Xu Liyan Zhu +4 位作者 Chao Hao Wenqian Liu Chenglong Chen Yongyi Chen Aiqin Liu 《Journal of Chinese Pharmaceutical Sciences》 CAS CSCD 2021年第9期743-753,共11页
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 der... 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. 展开更多
关键词 tegafur 5-FLUOROURACIL Amino acid ester Synthesis EVALUATION Antitumor activity
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Thermodynamic study on the interaction between anti-tumor drug tegafur and human serum albumin 被引量:2
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作者 Lin Wei Li Dong Dong Wang De Zhi Sun Min Liu You Ying Di Hua Chao Yan 《Chinese Chemical Letters》 SCIE CAS CSCD 2007年第7期891-894,共4页
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... 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. 展开更多
关键词 tegafur Human serum albumin Isothermal titration calorimetry Circular dichroism
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Polyethylenimine-cyclodextrin-tegafur conjugate shows anti-cancer activity and a potential for gene delivery 被引量:1
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作者 Qi-da HU Hui FAN +2 位作者 Wei-jian LOU Qing-qing WANG Gu-ping TANG 《Journal of Zhejiang University-Science B(Biomedicine & Biotechnology)》 SCIE CAS CSCD 2011年第9期720-729,共10页
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(E... 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. 展开更多
关键词 POLYETHYLENIMINE Β-CYCLODEXTRIN tegafur CO-DELIVERY Gene therapy
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Chemotherapy with enteric-coated tegafur/uracil for advanced hepatocellular carcinoma 被引量:1
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作者 Toru Ishikawa 《World Journal of Gastroenterology》 SCIE CAS CSCD 2008年第18期2797-2801,共5页
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 case... 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. 展开更多
关键词 Advanced hepatocellular carcinoma Tumor dormancy Enteric-coated tegafur/uracil CHEMOTHERAPY Portal vein tumor thrombus Lung metastasis
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Tegafur-uracil-induced rapid development of advanced hepatic fibrosis 被引量:1
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作者 shuya honda koji sawada +3 位作者 takumu hasebe shunsuke nakajima mikihiro fujiya toshikatsu okumura 《World Journal of Gastroenterology》 SCIE CAS 2017年第31期5823-5828,共6页
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 hypertensio... 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. 展开更多
关键词 tegafur-uracil Drug-induced liver injury Hepatic fibrosis Portal hypertension Non-invasive assessment
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TEGAFUR PLUS MMC OR ACNU IN THE TREATMENT OF ADVANCED GASTRIC CANCER-A PILOT STUDY
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作者 张达荣 萧树东 +1 位作者 江绍基 Minoru Kurihara 《Chinese Journal of Cancer Research》 SCIE CAS CSCD 1990年第4期63-66,共4页
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, a... 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%). 展开更多
关键词 ACNU tegafur PLUS MMC OR ACNU IN THE TREATMENT OF ADVANCED GASTRIC CANCER-A PILOT STUDY BCNU MMC
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A Case of Advanced Multiple Hepatocellular Carcinomas with Portal Vein Tumor Thrombosis Successfully Treated by Oral Tegafur/Uracil
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作者 Hiroto Tanaka Huuta Koga +8 位作者 Masako Hasegawa Hiroshi Takihara Eri Kimura Tarou Inoue Chie Ueda Wataru Ono Seigou Takamatsu Yasushi Nakamura Hiroki Ueda 《Journal of Cancer Therapy》 2010年第3期160-164,共5页
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 thrombos... 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. 展开更多
关键词 ADVANCED Hepatocellular Carcinoma Portal VEIN THROMBOSIS ORAL tegafur/Uracil Chemotherapy
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Feasibility and Efficacy Study of Biweekly Irinotecan Combined with Oral Tegafur/Uracil in Advanced Colorectal Cancer
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作者 Masataka Ikeda Mitsugu Sekimoto +5 位作者 Ichiro Takemasa Tsunekazu Mizushima Hirofumi Yamamoto Hideshi Ishii Yuichiro Doki Masaki Mori 《Journal of Cancer Therapy》 2013年第6期8-14,共7页
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 con... 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. 展开更多
关键词 Colorectal NEOPLASMS PHARMACOKINETICS Drug Therapy Fluorouracil tegafur/Uracil UFT
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Inetetamab combined with tegafur as second-line treatment for human epidermal growth factor receptor-2-positive gastric cancer: A case report
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作者 Jing-Hao Zhou Qi-Jun Yi +4 位作者 Ming-Yan Li Yan Xu Qi Dong Cong-Ying Wang Hai-Yan Liu 《World Journal of Clinical Cases》 SCIE 2024年第4期820-827,共8页
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 target... 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. 展开更多
关键词 Inetetamab Gastric cancer Human epidermal growth factor receptor-2 protein tegafur Case report
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Clinical Efficacy and Safety of Oxaliplatin-tegafur,Gimeracil and Oteracil Potassium and Vinorelbine-Pt in the Treatment of Advanced Triple Negative Breast Cancer
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作者 Miroslav Samaržija Lela Bitar 《Advances in Modern Oncology Research》 2019年第5期21-24,共4页
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 ad... 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. 展开更多
关键词 OXALIPLATIN tegafur gimeracil and oteracil potassium VINORELBINE PT
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Multicenter Analysis of mFOLFOX6 with Oxaliplatin Stop-and-Go Strategy Using Oral Uracil-Tegafur with Leucovorin for Unresectable Colorectal Cancer in Elderly Patients
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作者 Tetsu Yamamoto Kuniyuki Katano +7 位作者 Shinichi Sugimoto Akiyoshi Kanazawa Eiji Hira Hiroshi Takeda Yoshitoshi Sato Yutaka Yamashiro Yoshitsugu Tajima Masahide Ikeguchi 《Journal of Cancer Therapy》 2014年第2期147-154,共8页
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 ... 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. 展开更多
关键词 Colorectal Cancer OXALIPLATIN Uracil-tegafur (UFT) LEUCOVORIN Elderly Patient Stop-and-Go
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Effect of Tegafur Gimeracil Oteracil Potassium Capsule + Kangai injection + intensity-modulated radiation therapy on the cellular malignant biological processes in advanced cervical cancer lesion
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作者 Ji-Fan Yang Hong-Bo Ren +3 位作者 Chun-Mei Li Zhong-Hui Bao Yi Jiang Shao-Lin Li 《Journal of Hainan Medical University》 2017年第17期103-107,共5页
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 lesio... 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. 展开更多
关键词 Advanced CERVICAL cancer tegafur Gimeracil Oteracil POTASSIUM INTENSITY-MODULATED radiation therapy Invasion Proliferation
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Clinical Analysis of Gemcitabine Combined with Tegafur Chemotherapy after Radical Surgery on Pancreatic Cancer
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作者 Wei Zheng Xiang Yan Xiaoxue Song 《Proceedings of Anticancer Research》 2021年第3期7-10,共4页
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... 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. 展开更多
关键词 Radical resection of pancreatic cancer GEMCITABINE tegafur CHEMOTHERAPY Clinical efficacy
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Nab-paclitaxel plus tegafur gimeracil oteracil potassium capsule (S-1) as first-line treatment for advanced biliary tract adenocarcinoma: a phase 2 clinical trial 被引量:6
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作者 Wen Zhang Yongkun Sun +3 位作者 Zhichao Jiang Wang Qu Caifeng Gong Aiping Zhou 《Hepatobiliary Surgery and Nutrition》 SCIE 2023年第1期37-44,共8页
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).Meth... 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. 展开更多
关键词 Biliary tract adenocarcinoma chemotherapy NAB-PACLITAXEL tegafur gimeracil oteracil potassium capsule(S-1)
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信迪利单抗联合替吉奥与奥沙利铂治疗晚期胃癌的效果及对血清炎性因子的影响
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作者 胡青 《临床合理用药》 2026年第8期4-7,共4页
目的观察信迪利单抗联合替吉奥与奥沙利铂治疗晚期胃癌的效果及对血清炎性因子的影响。方法选取2022年2月—2024年12月连云港市赣榆区人民医院收治的晚期胃癌患者106例,根据信封法随机分为免疫治疗联合组和SOX方案组,各53例。SOX方案组... 目的观察信迪利单抗联合替吉奥与奥沙利铂治疗晚期胃癌的效果及对血清炎性因子的影响。方法选取2022年2月—2024年12月连云港市赣榆区人民医院收治的晚期胃癌患者106例,根据信封法随机分为免疫治疗联合组和SOX方案组,各53例。SOX方案组给予替吉奥+奥沙利铂治疗,免疫治疗联合组在SOX方案组基础上给予信迪利单抗治疗,21 d为1个周期,2组均治疗3个周期。比较2组近期疗效,治疗前后血清炎性因子[C反应蛋白(CRP)、白介素-6(IL-6)、肿瘤坏死因子-α(TNF-α)]、肿瘤标志物[癌胚抗原(CEA)、糖类抗原125(CA125)、糖类抗原19-9(CA19-9)]及不良反应。结果免疫治疗联合组客观缓解率、疾病控制率分别为71.70%、94.34%,高于SOX方案组的50.94%、79.25%(χ^(2)=4.813,P=0.028;χ^(2)=5.267,P=0.022)。治疗3个周期后,2组CRP、IL-6、TNF-α、CEA、CA125、CA19-9水平降低,且免疫治疗联合组低于SOX方案组(P<0.01)。免疫治疗联合组与SOX方案组不良反应总发生率比较差异无统计学意义(20.75%vs.24.53%,χ^(2)=0.215,P=0.643)。结论信迪利单抗联合替吉奥与奥沙利铂治疗晚期胃癌效果显著,可明显缓解炎性反应,降低肿瘤标志物水平,且安全性较高。 展开更多
关键词 晚期胃癌 信迪利单抗 替吉奥 奥沙利铂 炎性因子 肿瘤标志物
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替加氟-原卟啉IX脂质体的制备及抗肿瘤研究
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作者 李安宁 王晨 +2 位作者 郑琰 林睿铨 张志强 《沈阳药科大学学报》 2026年第2期138-149,共12页
替加氟(Tegafur,TF)为一种辅助化疗药物,抗肿瘤效果较弱且有一定副作用,原卟啉IX(Protoporphyrin IX,PpIX)为一种光敏剂,可产生活性氧发挥光动力的抗肿瘤作用,为增强TF的抗肿瘤效果,并延长其作用时间,本研究将TF与PpIX化学结合,并负载... 替加氟(Tegafur,TF)为一种辅助化疗药物,抗肿瘤效果较弱且有一定副作用,原卟啉IX(Protoporphyrin IX,PpIX)为一种光敏剂,可产生活性氧发挥光动力的抗肿瘤作用,为增强TF的抗肿瘤效果,并延长其作用时间,本研究将TF与PpIX化学结合,并负载至缓释脂质体内,通过化学键合延长作用时间,通过化疗和光动力治疗增强抗肿瘤效果,并通过控制其粒径实现被动肿瘤靶向增强抗肿瘤效果并降低不良反应。经1 H-NMR、质谱、红外光谱等表征,验证了TF和PpIX缀合物(TSP)的成功合成,并且荧光光谱扫描结果说明合成的TSP成功保留了PpIX的荧光性质。经过粒径测量、透射电镜表征等发现,所制备的TSP脂质体载药量为(6.84±0.16)%,包封率为(68.25±1.57)%,呈球状,粒径均一,约为152.2 nm,ζ电位-25.8 mV,可缓慢释药长达120 h以上。经体外抗肿瘤研究发现TSP脂质体在激光照射下能显著增加对TF和PpIX对4T1细胞的毒性。本研究作者所制备的TSP前药脂质体具有良好理化性质和体外抗肿瘤效果,为增强TF的临床疗效提供了有效给药途径。 展开更多
关键词 光动力治疗 活性氧 化疗 脂质体 替加氟
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乌苯美司片联合奥沙利铂+替吉奥治疗晚期胃癌的效果及对T淋巴细胞水平的影响
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作者 徐鸣潞 惠佳君 丁宁 《临床医学研究与实践》 2026年第4期82-85,共4页
目的分析乌苯美司片联合奥沙利铂+替吉奥治疗晚期胃癌的效果及对T淋巴细胞水平的影响。方法回顾性分析南通大学杏林学院附属惠山医院/无锡市惠山区人民医院肿瘤血液科2021年8月至2024年6月收治的88例晚期胃癌患者的诊疗资料,以诊疗方案... 目的分析乌苯美司片联合奥沙利铂+替吉奥治疗晚期胃癌的效果及对T淋巴细胞水平的影响。方法回顾性分析南通大学杏林学院附属惠山医院/无锡市惠山区人民医院肿瘤血液科2021年8月至2024年6月收治的88例晚期胃癌患者的诊疗资料,以诊疗方案差异分为两联组(奥沙利铂+替吉奥治疗)和三联组(乌苯美司片+奥沙利铂+替吉奥治疗),每组44例。比较两组患者的临床疗效、免疫指标及治疗期间不良反应发生率。结果三联组的肿瘤控制率显著高于两联组(P<0.05)。两组患者治疗前的CD3^(+)、CD4^(+)、CD8^(+)、CD4^(+)/CD8^(+)比较,差异无统计学意义(P>0.05);治疗后,两组的CD3^(+)、CD4^(+)、CD4^(+)/CD8^(+)均较治疗前升高,CD8^(+)较治疗前降低,且三联组优于两联组(P<0.05)。两组患者治疗前的癌胚抗原(CEA)、糖类抗原199(CA199)、糖类抗原724(CA724)水平比较,差异无统计学意义(P>0.05);治疗后,两组患者的CEA、CA199、CA724水平均较治疗前降低,且三联组低于两联组(P<0.05)。两组患者治疗期间的不良反应总发生率比较,差异无统计学意义(P>0.05)。结论乌苯美司片联合奥沙利铂+替吉奥治疗晚期胃癌可取得显著疗效,且安全性较高,具有临床可行性。 展开更多
关键词 晚期胃癌 奥沙利铂 替吉奥 乌苯美司片 肿瘤预后
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替吉奥胶囊致胃癌患者重症间质性肺炎1例分析
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作者 孟德辉 王超 +1 位作者 李华 丁春雷 《中国药物警戒》 2026年第2期207-209,共3页
目的探讨口服替吉奥胶囊导致胃癌患者重症间质性肺炎的不良反应,为临床安全用药提供参考。方法对1例口服替吉奥治疗胃癌过程中出现重症间质性肺炎的临床资料进行分析,并对国内外相关文献进行回顾总结。结果本例患者重启替吉奥治疗3 d出... 目的探讨口服替吉奥胶囊导致胃癌患者重症间质性肺炎的不良反应,为临床安全用药提供参考。方法对1例口服替吉奥治疗胃癌过程中出现重症间质性肺炎的临床资料进行分析,并对国内外相关文献进行回顾总结。结果本例患者重启替吉奥治疗3 d出现发热伴恶心呕吐,胸部CT示双肺间质性肺炎症状较1周前加重,经多学科会诊讨论及关联性分析判断间质性肺炎为替吉奥所致,停用替吉奥,给予甲泼尼龙及呼吸机辅助通气治疗,患者逐渐改善。结论替吉奥致间质性肺炎虽罕见,但可能导致严重的呼吸衰竭而危及生命。临床使用替吉奥应注意药品不良反应,做好用药评估。若患者出现发热、呼吸困难等症状,应及时完善相关检查,根据间质性肺炎分级采取相应的处理措施,改善患者预后。 展开更多
关键词 替吉奥 甲泼尼龙 间质性肺炎 胃癌 药品不良反应
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区域动脉栓塞联合替吉奥治疗局部进展期胃癌的效果及对血红蛋白水平、纤溶与凝血功能的影响
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作者 惠佳君 丁胜军 丁宁 《临床医学研究与实践》 2026年第6期85-88,共4页
目的 探讨区域动脉栓塞联合替吉奥治疗局部进展期胃癌(LAGC)患者的临床效果,并分析其对血红蛋白(Hb)水平、纤溶与凝血功能的影响。方法 选取2022年11月至2024年11月本院68例LAGC患者,根据治疗方式的不同将其分成对照组和观察组,各34例... 目的 探讨区域动脉栓塞联合替吉奥治疗局部进展期胃癌(LAGC)患者的临床效果,并分析其对血红蛋白(Hb)水平、纤溶与凝血功能的影响。方法 选取2022年11月至2024年11月本院68例LAGC患者,根据治疗方式的不同将其分成对照组和观察组,各34例。对照组采用替吉奥治疗,观察组采用区域动脉栓塞联合替吉奥治疗。对比两组的临床疗效、血管内皮生长因子(VEGF)、Hb水平、纤溶与凝血功能、不良反应发生情况。结果 观察组的治疗总有效率为61.76%,较对照组的32.35%高(P<0.05)。观察组治疗后的VEGF水平低于对照组,Hb水平高于对照组(P<0.05)。观察组治疗后的纤维蛋白原降解产物(FDP)、D-二聚体(D-D)水平低于对照组,活化部分凝血活酶时间(APTT)、凝血酶原时间(PT)长于对照组(P<0.05)。观察组的不良反应总发生率低于对照组(P<0.05)。结论 区域动脉栓塞联合替吉奥治疗LAGC患者能有效提升Hb水平,改善纤溶和凝血功能,且治疗安全性高,值得推广。 展开更多
关键词 替吉奥 区域动脉栓塞 局部进展期胃癌 血红蛋白 凝血功能
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全程同步加量调强放疗同步替吉奥对食管癌患者血清CA19-9、CEA水平的影响
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作者 王丹丹 宋光辉 +1 位作者 刘畅 魏继军 《河北医药》 2026年第1期35-38,43,共5页
目的 探讨全程同步加量调强放疗同步替吉奥对食管癌患者血清糖类抗原19-9(CA19-9)、癌胚抗原(CEA)水平的影响。方法 选择2020年10月至2024年4月进行食管癌治疗的106例患者,随机分为对照组和研究组,每组53例。对照组给予全程同步加量调... 目的 探讨全程同步加量调强放疗同步替吉奥对食管癌患者血清糖类抗原19-9(CA19-9)、癌胚抗原(CEA)水平的影响。方法 选择2020年10月至2024年4月进行食管癌治疗的106例患者,随机分为对照组和研究组,每组53例。对照组给予全程同步加量调强放疗治疗,研究组给予全程同步加量调强放疗同步替吉奥治疗。记录2组在进行调强放疗过程中患者心脏、脊髓、右肺、左肺所进行的照射剂量;采用医院自制胃肠功能紊乱评分量表,评估患者自身胃肠功能情况;检测白细胞计数(WBC)、血红蛋白(HGB)、血小板计数(PLT)、丙氨酸转氨酶(ALT)、天冬氨酸转氨酶(AST)、ALT/AST比值、CA19-9、CEA水平;对比2组治疗效果及不良反应。结果 与对照组比较,研究组心脏V30照射剂量、脊髓最大照射剂量、右肺平均照射剂量、左肺平均照射剂量水平均降低(P<0.05);研究组腹痛、上腹胀、恶心呕吐评分水平均降低(P<0.05);研究组WBC、HGB、PLT比值、CA19-9、CEA水平均降低(P<0.05),ALT、AST、ALT/AST水平升高(P<0.05);研究组治疗总有效率显著高于对照组(P<0.05);研究组不良反应低于对照组,但差异无统计学意义(P>0.05)。结论 经全程同步加量调强放疗同步替吉奥对食管癌患者治疗,降低照射剂量,减轻炎性反应,缓解患者病情,提高临床治疗效果,降低毒副反应发生率。 展开更多
关键词 全程同步加量调强放疗 替吉奥 糖类抗原19-9 癌胚抗原
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