替加氟/亚叶酸钙/吉莫斯特/氧嗪酸钾(Tegafur/Leucovorin calcium/Gimeracil/Oteracil Potassium)

概要

基本信息

药物类型

小分子化药

别名

Folinic acid/S-1、Gimeracil/oteracil potassium/tegafur/calcium folinate、Gimeracil/oteracil potassium/tegafur/folinic acid

+ [6]

靶点

TYMS

作用方式

抑制剂

作用机制

TYMS抑制剂(胸苷酸合成酶抑制剂)、DNA合成抑制剂

治疗领域

肿瘤消化系统疾病

在研适应症-

非在研适应症

晚期胃癌

原研机构

Taiho Pharmaceutical Co., Ltd.

在研机构-

非在研机构

Taiho Pharmaceutical Co., Ltd.

权益机构-

最高研发阶段无进展临床3期

首次获批日期-

最高研发阶段(中国)-

特殊审评-

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结构/序列

分子式C5H4ClNO2

InChIKeyZPLQIPFOCGIIHV-UHFFFAOYSA-N

CAS号103766-25-2

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关联

7

项与替加氟/亚叶酸钙/吉莫斯特/氧嗪酸钾相关的临床试验

ChiCTR1900020948

/ Recruiting临床4期IIT

Androtinib Combined with S - 1 in the Treatment of Advanced Non - small Cell Lung Cancer: A Phase II Clinical Study

开始日期2019-01-25

申办/合作机构

绵阳市中心医院

JPRN-UMIN000024688

/ CompletedN/AIIT

The feasibility study of TAS-118 plus Oxaliplatin or TAS-118 monotherapy as perioperative chemotherapy for locally advanced gastric cancer - The feasibility study of TAS-118 plus Oxaliplatin or TAS-118 monotherapy as perioperative chemotherapy for locally advanced gastric cancer (APOLLO-11)

开始日期2016-11-18

申办/合作机构-

JPRN-JapicCTI-132379

/ Unknown status临床1期

Food effect and dosage form comparison study of TAS-118

开始日期2014-01-01

申办/合作机构

Taiho Pharmaceutical Co., Ltd.

100 项与替加氟/亚叶酸钙/吉莫斯特/氧嗪酸钾相关的临床结果

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100 项与替加氟/亚叶酸钙/吉莫斯特/氧嗪酸钾相关的转化医学

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100 项与替加氟/亚叶酸钙/吉莫斯特/氧嗪酸钾相关的专利（医药）

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7

项与替加氟/亚叶酸钙/吉莫斯特/氧嗪酸钾相关的文献（医药）

2023-07-01·Gastric cancer : official journal of the International Gastric Cancer Association and the Japanese Gastric Cancer Association

Perioperative TAS-118 plus oxaliplatin in patients with locally advanced gastric cancer: APOLLO-11 study.

Article

作者: Wakatsuki, Takeru ; Ishizuka, Naoki ; Mikami, Shinya ; Wada, Takeyuki ; Yoshikawa, Takaki ; Nakayama, Izuma ; Ohashi, Manabu ; Shoji, Hirokazu ; Nunobe, Souya ; Boku, Narikazu ; Doi, Ayako ; Takashima, Atsuo ; Kumagai, Koshi ; Sano, Takeshi ; Chin, Keisho ; Yamaguchi, Kensei ; Izawa, Naoki ; Iwasa, Satoru ; Ida, Satoshi ; Takahari, Daisuke ; Katai, Hitoshi

BACKGROUNDWe investigated the feasibility of perioperative chemotherapy with S-1 and leucovorin (TAS-118) plus oxaliplatin in patients with locally advanced gastric cancer.METHODSPatients with clinical T3-4N1-3M0 gastric cancer received four courses of TAS-118 (40-60 mg/body, orally, twice daily for seven days) plus oxaliplatin (85 mg/m², intravenously, day one) every two weeks preoperatively followed by gastrectomy with D2 lymphadenectomy, followed by postoperative chemotherapy with either 12 courses of TAS-118 monotherapy (Step 1) or eight courses of TAS-118 plus oxaliplatin (Step 2). The primary endpoints were completion rates of preoperative chemotherapy with TAS-118 plus oxaliplatin and postoperative chemotherapy with TAS-118 monotherapy (Step 1) or TAS-118 plus oxaliplatin (Step 2).RESULTSAmong 45 patients enrolled, the preoperative chemotherapy completion rate was 88.9% (90% CI 78.0-95.5). Major grade ≥ 3 adverse events (AEs) were diarrhoea (17.8%) and neutropenia (8.9%). The R0 resection rate was 95.6% (90% CI 86.7-99.2). Complete pathological response was achieved in 6 patients (13.3%). Dose-limiting toxicity was not observed in 31 patients receiving postoperative chemotherapy (Step 1, n = 11; Step 2, n = 20), and completion rates were 90.9% (95% CI 63.6-99.5) for Step 1 and 80.0% (95% CI 59.9-92.9) for Step 2. No more than 10% of grade ≥ 3 AEs were observed in patients receiving Step 1. Hypokalaemia and neutropenia occurred in 3 and 2 patients, respectively, receiving Step 2. The 3-year recurrence-free and overall survival rates were 66.7% (95% CI 50.9-78.4) and 84.4% (95% CI 70.1-92.3), respectively.CONCLUSIONSPerioperative chemotherapy with TAS-118 plus oxaliplatin with D2 gastrectomy is feasible.

2020-08-01·The Lancet Oncology1区 · 医学

TAS-118 plus oxaliplatin in advanced gastric cancer: is it worth it?

1区 · 医学

Article

作者: Adenis, Antoine ; Samalin, Emmanuelle

A review.Practices are changing overtime,and geog. differences in the treatment of localised and metastatic gastric cancer are becoming increasingly less pronounced,even though some medications are not available or are not reimbursed equally in all countries.Regarding the use of fluoropyrimidines,capecitabine or S-1 can be used as an alternative to infusional fluorouracil in doublet regimens.In addition ciplatin or oxaliplatin are viewed as platinum agents with similar effectiveness when incorporated in doublet or triplet regimens although this aspect remains a matter of debate.S-1 plus cisplatin has been widely used in eastern Asia,whereas infusional fluorouracil (plus leucovorin) or capecitabine,combined with oxaliplatin or cisplatin,are standard practices in Europe and North America.As a conclusion to the SOLAR study,Kang and colleagues suggest that the combination of TAS-118 plus oxaliplatin could be a new first-line standard chemotherapy for advanced gastric cancer,in Asian patients.First,it would have been reasonable to the added value of leucovorin to S-1,by comparing TAS-118 (S-1 plus leucovorin) plus oxaliplatin with S-1 plus oxaliplatin (rather than S-1 plus cisplatin).Second,as the TAS-118 plus oxalipaltin combination appears effective in patients with Lauren's diffuse-type histol. and poor prognosis,we suggest clin. research should focus on this group.Third,TAS-118 plus oxaliplatin deserves to also be tested in non-Asian patients,although it is known that S-1 is not equally tolerated in non-Asian patients and Asian patients.Finally,ongoing phase 3 trials will elucidate the role of many promising compounds such as trifluridine-tipiracil,anti-CLDN18.2 monoclonal antibodies (zolbetuximab), or checkpoint inhibitors, in other clin. relevant subsets of patients with advanced HER2-neg. gastric cancer ,including frail or fit patients, with diffuse type histol., and CLDN18.2-pos. or microsatellite-unstable tumors.

2020-08-01·The Lancet Oncology1区 · 医学

S-1 plus leucovorin and oxaliplatin versus S-1 plus cisplatin as first-line therapy in patients with advanced gastric cancer (SOLAR): a randomised, open-label, phase 3 trial

1区 · 医学

Article

作者: Ryu, Min-Hee ; Miyata, Yoshinori ; Baba, Hideo ; Kang, Yoon-Koo ; Hara, Hiroki ; Tsuda, Masahiro ; Nakayama, Norisuke ; Chung, Ik-Joo ; Chung, Hyun Cheol ; Chin, Keisho ; Kadowaki, Shigenori ; Lee, Keun-Wook ; Bang, Yung-Jue ; Hyodo, Ichinosuke ; Hosaka, Hisashi ; Hironaka, Shuichi ; Park, Se Hoon ; Boku, Narikazu ; Oh, Sang Cheul

BACKGROUNDS-1 plus leucovorin and oxaliplatin showed promising efficacy for treatment of advanced gastric cancer in a randomised phase 2 study. We aimed to evaluate the efficacy and safety of oral TAS-118 (S-1 plus leucovorin) and oxaliplatin versus S-1 plus cisplatin in patients with advanced gastric cancer.METHODSWe did a randomised, open-label, phase 3 trial in 62 centres across Japan and South Korea. Patients aged 20 years or older, with a histologically confirmed advanced gastric cancer with negative or unknown HER2 status, with Eastern Cooperative Oncology Group performance status of 0 or 1, measurable or evaluable metastatic lesions, and no previous treatment were randomly assigned (1:1) via an interactive web response system using the minimisation method, stratified by performance status, presence of a measurable lesion, and country, to receive TAS-118 (S-1 40-60 mg and leucovorin 25 mg orally twice daily for 7 days) plus oxaliplatin (85 mg/m² intravenously on day 1) every 2 weeks, or S-1 (40-60 mg orally twice daily) for 21 days plus cisplatin (60 mg/m² intravenously on day 1 or 8) every 5 weeks. The primary endpoint was overall survival in patients who had advanced gastric cancer with measurable or evaluable metastatic lesions and who received the study drug. Safety was assessed in all patients who received the study drug. This study was registered at ClinicalTrials.gov, NCT02322593.FINDINGSBetween Jan 28, 2015, and Dec 5, 2016, 711 patients were randomised to TAS-118 plus oxaliplatin (n=356) or S-1 plus cisplatin (n=355). 11 untreated patients and 19 ineligible patients were excluded from the primary analysis (TAS-118 plus oxaliplatin group n=347, S-1 plus cisplatin group n=334) following recommendation from the independent data monitoring committee. After median follow-up of 26·0 months (IQR 22·0-32·8), median overall survival was 16·0 months (95% CI 13·8-18·3) in the TAS-118 plus oxaliplatin group and 15·1 months (95% CI 13·6-16·4) in the S-1 plus cisplatin group (hazard ratio 0·83, 95% CI 0·69-0·99; p=0·039). The most common grade 3 or higher adverse events in the 352 patients in the TAS-118 plus oxaliplatin group and the 348 patients in the S-1 plus cisplatin group were anaemia (56 [16%] vs 64 [18%]), neutropenia (54 [15%] vs 88 [25%]), decreased appetite (53 [15%] vs 46 [13%]), diarrhoea (33 [9%] vs 15 [4%]), and peripheral sensory neuropathy (30 [9%] vs one [<1%]). Serious adverse events were observed in 155 (44%) of 352 patients in the TAS-118 plus oxaliplatin group and 159 (46%) of 348 patients in the S-1 plus cisplatin group. Two treatment-related deaths occurred in the TAS-118 plus oxaliplatin group (pulmonary tuberculosis and viral pneumonia).INTERPRETATIONTAS-118 plus oxaliplatin showed a clinically meaningful improvement in efficacy compared with S-1 plus cisplatin, and could be considered a new first-line treatment option for advanced gastric cancer in Asian patients.FUNDINGTaiho Pharmaceutical and Yakult Honsha.

100 项与替加氟/亚叶酸钙/吉莫斯特/氧嗪酸钾相关的药物交易

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研发状态

10 条进展最快的记录,

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适应症	最高研发状态	国家/地区	公司	日期
晚期胃癌	临床3期	日本	Taiho Pharmaceutical Co., Ltd.	2014-12-01
晚期胃癌	临床3期	韩国	Taiho Pharmaceutical Co., Ltd.	2014-12-01

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临床结果

适应症

分期

评价

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研究	分期	人群特征	评价人数	分组	结果	评价	发布日期


JPRN-UMIN000024688 (APOLLO-11, ASCO_GI2021)	N/A	晚期胃癌	45	TAS-118 + L-OHP	(艱範網憲艱膚糧蓋糧選) = One pt in step 2 discontinued post-op chemo due to AE 製顧糧觸網鹽艱顧夢繭 (範膚獵鹹蓋繭壓膚獵醖 ) 更多	-	2021-01-22
JPRN-UMIN000024688 (APOLLO-11, ASCO_GI2021)	N/A	晚期胃癌	45	TAS-118		-	2021-01-22
JPRN-UMIN000024688 (APOLLO-11, ASCO_GI2020)	N/A	晚期胃癌	45	TAS-118 + oxaliplatin	壓鹽糧鹹糧積遞築積襯(鬱醖夢艱構夢艱廠鬱廠) = 鹽艱獵衊鹽選蓋廠繭構願願膚齋艱醖鹹鹽網遞 (構鹹襯簾膚製淵壓憲夢, 86.7 ~ 99.2) 更多	-	2020-02-04
EPOC1604 (ESMO2019)	临床2期	晚期胃癌	20	TAS-114 and S-1 combination	(糧襯繭壓積艱觸壓淵鬱) = 艱壓衊鬱遞衊繭獵窪壓鹹鏇壓簾積簾遞鏇鹽蓋 (鑰艱鏇憲範構夢憲醖膚, 0.1 ~ 24.9) 更多	-	2019-09-29
JPRN-JapicCTI-132172 (GRAPE, ASCO2017)	临床3期	胰腺癌	-	TAS-118 (S-1 plus leucovorin)	(襯夢鏇選膚製選壓鹹網) = 鏇艱獵繭鹹齋艱顧築願構網壓獵夢窪遞遞壓壓 (繭壓醖製範構艱顧齋範 ) 更多	不佳	2017-05-30
JPRN-JapicCTI-132172 (GRAPE, ASCO2017)	临床3期	胰腺癌	-	S-1	(襯夢鏇選膚製選壓鹹網) = 襯鹽艱餘襯鹽繭願選衊構網壓獵夢窪遞遞壓壓 (繭壓醖製範構艱顧齋範 ) 更多	不佳	2017-05-30
ASCO2013	临床2期	转移性结直肠癌	36	Gemcitabine and S-1 combination	(獵蓋衊願衊顧衊蓋繭膚) = 遞觸鬱廠簾鏇製獵窪築餘築觸繭鬱齋觸醖壓製 (顧衊繭積繭積襯膚簾鹽, 4.5 ~ 28.9) 更多	积极	2013-05-20
ASCO2012	临床2期	复发性非小细胞肺癌一线	23	Tailored S-1 regimen	(願願製範簾壓艱憲鬱憲) = 遞齋憲獵簾膚鏇壓醖願衊窪醖獵遞淵膚獵鏇襯 (膚廠壓淵膚製膚蓋築鏇, 50.8 ~ 88.4) 更多	-	2012-05-20
Study 0601 (ASCO2009)	临床2期	非小细胞肺癌一线	40	Irinotecan and S-1 combination	(鏇顧範艱願鹽鹽餘膚獵) = 遞廠鬱鬱醖構鹹構鹽壓糧築襯蓋簾膚憲淵獵選 (襯夢鹹繭蓋網鹹鹽醖積, 16.6–46.5) 更多	-	2009-05-20