尿嘧啶替加氟(Tegafur/Uracil) - 药物靶点：TYMS_在研适应症：膀胱癌，头颈部肿瘤，前列腺癌_专利_临床

概要

基本信息

药物类型

小分子化药

别名

Compound Tegafur、Orzel、Uftoral

+ [11]

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)

治疗领域

肿瘤消化系统疾病内分泌与代谢疾病+ [4]

在研适应症

膀胱癌头颈部肿瘤前列腺癌+ [9]

非在研适应症

晚期胃癌转移性食管癌III期结肠癌

原研机构

Taiho Pharmaceutical Co., Ltd.

在研机构

Bristol Myers Squibb Co.

Taiho Pharmaceutical Co., Ltd.

非在研机构

Merck AB (Sweden)

权益机构-

最高研发阶段批准上市

首次获批日期

日本 (1983-05-27),

胆管癌乳腺癌结直肠癌+ [5]

最高研发阶段(中国)批准上市

特殊审评-

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结构/序列

分子式C12H13FN4O5

InChIKeyDHMYGZIEILLVNR-UHFFFAOYSA-N

CAS号74578-38-4

关联

101

项与尿嘧啶替加氟相关的临床试验

JPRN-jRCTs031210660

/ Recruiting临床2期IIT

A prospective study on the safety and efficacy of preoperative UFT/UZEL+CPT-11+irradiation combined with FOLFOX or CAPOX for locally advanced lower rectal cancer

开始日期2022-06-14

申办/合作机构-

JPRN-UMIN000046430

/ SuspendedN/AIIT

Multi-institutional study aimed at radical cure with multidisciplinary treatment including preoperative endocrine chemotherapy (LHRH analog, denosumab, apalutamide, tegafur / uracil), robot-assisted total prostatectomy and radiation therapy for prostate cancer with oligometastases of bone - Multi-institutional study aimed at radical cure with multidisciplinary treatment including preoperative endocrine chemotherapy, robot-assisted total prostatectomy and radiation therapy for prostate cancer with oligometastases of bone

开始日期2021-12-01

申办/合作机构-

JPRN-jRCT1051190106

/ CompletedN/AIIT

Safety and efficacy of postoperative adjuvant chemotherapy with L-OHP base regimen followed by UFT plus LV for resectable liver metastases fro m colorectal cancer. (LOFT trial ) - LOFT trial

开始日期2020-02-13

申办/合作机构-

100 项与尿嘧啶替加氟相关的临床结果

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100 项与尿嘧啶替加氟相关的转化医学

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100 项与尿嘧啶替加氟相关的专利（医药）

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2,239

项与尿嘧啶替加氟相关的文献（医药）

2025-04-01·Seminars in Thoracic and Cardiovascular Surgery

Adjuvant Therapy in Stage IB Non-Small Cell Lung Cancer: A Network Meta-Analysis of Tegafur-Uracil and Immune Checkpoint Inhibitors

Review

作者: Yamanashi, Keiji ; Hamaji, Masatsugu ; Takeuchi, Jiro ; Miyata, Ryo ; Hosono, Mitsuharu ; Ozu, Naoki ; Kawaguchi, Takeshi

Recent clinical trials demonstrated that as adjuvant therapy, immune checkpoint inhibitors (ICIs) following intravenous cytotoxic chemotherapy may have a nonsignificant advantage over intravenous cytotoxic chemotherapy only in completely resected stage IB non-small cell lung cancer (NSCLC). Meanwhile, several studies reported that oral tegafur-uracil may have a comparable benefit to intravenous chemotherapy in long-term survival outcomes in these patients. However, there is currently a lack of head-to-head comparison between ICIs following intravenous cytotoxic chemotherapy and tegafur-uracil. Therefore, we designed a network meta-analysis in assessing overall survival (OS) and a composite endpoint of disease free survival (DFS) and recurrence free survival (RFS) as measures of effect. Our results indicated that, limited to stage IB, calculated hazard ratio (HR) was 1.02 (95% confidence interval [CI]: 0.53-1.96) for OS and calculated HR was 0.90 (95% CI: 0.43-1.87) for DFS, while in stage IB to IIIA patients, calculated HR was 0.97 (95% CI: 0.70-1.37) for OS and calculated HR was 0.75 (95% CI: 0.59-0.95) for DFS. In conclusion, tegafur-uracil may offer a comparable benefit to ICIs following chemotherapy in limitation to stage IB NSCLC patients only. Future clinical trials may be designed for stage IB NSCLC, separately from stage II and III.

2025-03-01·EUROPEAN JOURNAL OF CANCER

Tegafur-uracil maintenance chemotherapy post-chemoradiotherapy for cervical cancer: Randomized trial

Article

作者: Fujiwara, Hiroyuki ; Saito, Motoaki ; Yamamoto, Kouji ; Yamaguchi, Satoshi ; Kurosaki, Akira ; Takano, Hirokuni ; Nagai, Tomonori ; Nishio, Shin ; Fujiwara, Keiichi ; Itagaki, Hiroya ; Suzuki, Yurina ; Takehara, Kazuhiro ; Nakamura, Kazuto ; Kudoh, Akiko ; Kobayashi, Hiroaki ; Yahata, Hideaki ; Hasegawa, Kosei ; Kamio, Masaaki ; Kato, Kazuyoshi ; Nakamoto, Tomoko

AIM:

Concurrent chemoradiotherapy (CCRT) is the standard treatment for locally advanced cervical cancer (LACC), but recurrence rates remain high. This multicenter phase-3 randomized trial (GOTIC-002) evaluated the efficacy of low-dose oral tegafur-uracil (UFT) as maintenance chemotherapy following curative CCRT for LACC.

METHODS:

Between 2010 and 2018, 351 patients with stage Ib2-IVa cervical cancer were enrolled. After achieving complete or partial remission post-CCRT, patients were randomized 1:1 into observation (arm O) or UFT maintenance therapy (arm UFT). UFT doses were 300-400 mg/day based on body surface area for 2 years, disease progression or adverse effects occurred. The primary endpoint was progression-free survival (PFS), with overall survival (OS) and safety as secondary endpoints.

RESULTS:

Patient characteristics were similar between the groups (n = 178 in arm O, n = 173 in arm UFT). During a median follow-up of 3 years, median PFS was not reached in either group. 5-year PFS rates were similar between them (arm O: 61.3 %, arm UFT: 62.0 %, hazard ratio: 0.92, P = .634). 5-year OS rates were also comparable (77.6 % vs 76.1 %, hazard ratio: 1.04, P = .869). Compliance with UFT ranged from 87.8 % to 98.8 %. Although adverse events were more frequent in arm UFT (93.5 % vs 73.9 %, odds ratio: 5.05), most were mild or moderate. Despite its tolerability, UFT did not improve PFS or OS.

CONCLUSIONS:

These findings suggest the need to reconsider maintenance therapy strategies after CCRT for potentially shifting away from cytotoxic chemotherapy towards alternative methods to enhance survival outcomes in patients with LACC.

2025-03-01·Annals of Gastroenterological Surgery

Efficacy of the U‐shaped flap technique in preventing reflux after minimally invasive proximal gastrectomy for proximal gastric and esophagogastric junction cancer

Article

作者: Wada, Hiroshi ; Kanemura, Takashi ; Omori, Takeshi ; Shinno, Naoki ; Miyata, Hiroshi ; Hara, Hisashi ; Yanagimoto, Yoshitomo ; Yasui, Masayoshi ; Ohue, Masayuki ; Masuike, Yasunori

Abstract:

Background:

Preventing gastroesophageal reflux after proximal gastrectomy for proximal gastric and esophagogastric junction cancer remains challenging due to the lack of standardized reconstructive techniques. The double flap technique (DFT) in valvuloplastic esophagogastrostomy prevents reflux esophagitis but is less effective in esophagogastric junction cancer because of negative pressure on the inferior mediastinum. We developed the U‐shaped flap technique (UFT) to enhance the anti‐reflux efficacy.

Methods:

This study analyzed data from patients who underwent minimally invasive proximal gastrectomy for proximal gastric and esophagogastric junction cancer between August 2014 and May 2022, using a prospectively maintained database. We compared DFT and UFT for short‐ and long‐term outcomes, focusing on gastroesophageal reflux, using one‐to‐one propensity score matching to control for patient‐related variables.

Results:

Among 217 eligible patients, 205 (100 in DFT, 105 in UFT) completed a 1‐year follow‐up. After propensity score matching, we selected 42 pairs of patients who underwent DFT and UFT. UFT had significantly shorter operative time (p = 0.044), similar blood loss, and similar morbidity. The UFT group had significantly fewer reflux symptoms (0% vs. 14.3%, p = 0.0011) and endoscopic Los Angeles grade B or higher reflux esophagitis (0% vs. 14.3%, p = 0.0011) than the DFT group. In lower mediastinal reconstructions for esophagogastric junction cancer, UFT showed a reduced incidence of reflux esophagitis.

Conclusion:

Our study indicates that the U‐shaped flap technique (UFT) offered significant advantages in reducing postoperative reflux symptoms and endoscopic esophagitis, in a cohort of patients with proximal gastric and esophagogastric junction cancer.

100 项与尿嘧啶替加氟相关的药物交易

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外链

KEGG	Wiki	ATC	Drug Bank
-	尿嘧啶替加氟	-	DB09327

研发状态

批准上市

10 条最早获批的记录,

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适应症	国家/地区	公司	日期
膀胱癌	日本	Taiho Pharmaceutical Co., Ltd.	1986-08-28
头颈部肿瘤	日本	Taiho Pharmaceutical Co., Ltd.	1986-08-28
前列腺癌	日本	Taiho Pharmaceutical Co., Ltd.	1986-08-28
宫颈癌	日本	Taiho Pharmaceutical Co., Ltd.	1986-08-28
胆管癌	日本	Taiho Pharmaceutical Co., Ltd.	1983-05-27
乳腺癌	日本	Taiho Pharmaceutical Co., Ltd.	1983-05-27
结直肠癌	日本	Taiho Pharmaceutical Co., Ltd.	1983-05-27
胆囊肿瘤	日本	Taiho Pharmaceutical Co., Ltd.	1983-05-27
肝癌	日本	Taiho Pharmaceutical Co., Ltd.	1983-05-27
肺癌	日本	Taiho Pharmaceutical Co., Ltd.	1983-05-27
胰腺癌	日本	Taiho Pharmaceutical Co., Ltd.	1983-05-27
胃癌	日本	Taiho Pharmaceutical Co., Ltd.	1983-05-27

未上市

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.	1997-06-01
III期结肠癌	临床3期	日本	Taiho Pharmaceutical Co., Ltd.	1996-10-01
转移性食管癌	临床2期	美国	Bristol Myers Squibb Co.	2002-05-15

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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


WCLC2024 人工标引	N/A	转移性非小细胞肺癌辅助 EGFR mutation-positive	1,812	Tegafur/Uracilur/Uracil	選齋艱築壓餘積構鹹蓋(窪鏇鏇襯構廠鹹網積繭) = 鹽蓋觸鑰襯鑰蓋遞醖壓鑰觸網糧獵範選繭製醖 (鹽憲糧製遞築窪齋憲襯 )	不佳	2024-09-08
				Tegafur/Uracil (EGFR mutation-positive)	選齋艱築壓餘積構鹹蓋(窪鏇鏇襯構廠鹹網積繭) = 簾鏇範蓋齋鏇壓觸範製鑰觸網糧獵範選繭製醖 (鹽憲糧製遞築窪齋憲襯 )
JPRN-jRCTs031180174 (GOTIC-002 LUFT, ESMO2022) 人工标引	临床3期	局部晚期宫颈癌维持	351	tegafur-uracil (UFT maintenance cohort (Arm UFT))	襯鹹齋觸構醖淵壓網簾(顧壓積廠夢繭蓋壓選壓) = 鏇鹹築夢顧遞糧襯選襯鹽鏇鏇壓糧製願襯遞觸 (憲選壓壓積獵夢淵鬱積, 55.4 ~ 67.8) 更多	不佳	2022-09-09
				observation only (observation only (Arm O))	襯鹹齋觸構醖淵壓網簾(顧壓積廠夢繭蓋壓選壓) = 網獵鹹鹹鬱鏇顧築夢鹽鹽鏇鏇壓糧製願襯遞觸 (憲選壓壓積獵夢淵鬱積, 54.8 ~ 67.1) 更多
JPRN-UMIN000005594 (ASCO_GI2022)	临床3期	结直肠癌辅助	386	Group A (three doses of UFT [300 mg/m2 per day]/LV [75 mg per day])	範觸夢鹹築衊積醖簾鬱(築壓壓衊淵觸衊膚鏇膚) = 3.9% vs. 7.3% 鏇衊夢鹹範壓襯獵淵夢 (衊衊廠壓壓齋鹽構憲顧 ) 更多	积极	2022-01-19
				Group B (two doses of UFT [300 mg/m2 per day]/LV [50 mg per day])
ESMO_ASIA_VIRTUAL2020	N/A	局部晚期头颈部鳞状细胞癌辅助	240	Metronomic UFUR	構觸積窪衊襯壓餘廠觸(膚膚築觸獵餘窪壓艱簾) = 3.8% 齋衊蓋餘艱範願網憲廠 (遞廠襯鬱鹹網糧鏇鏇壓 ) 更多	积极	2020-11-22
				tegafur-uracil (Control)
ESMO_ASIA_VIRTUAL2020	N/A	转移性头颈部鳞状细胞癌一线	-	Tegafur/uracil, platinum and cetuximab (UPEx)	餘遞醖憲範構淵齋鹽壓(觸願膚鏇願夢網積鑰網) = 繭鑰壓齋築艱淵遞網齋願遞構顧餘築選製願範 (遞艱簾範願獵範獵鑰鏇 ) 更多	积极	2020-11-22
JPRN-UMIN000003948 (NJLCG1001, ASCO2019)	临床2期	局部晚期非鳞状非小细胞肺癌	86	Uracil/tegafur and cisplatin	遞衊鏇簾膚鏇築窪醖齋(醖遞鏇醖鹽齋鬱鑰簾築) = 範網鏇廠壓觸構醖鏇蓋齋壓獵願繭製壓醖膚顧 (鏇壓顧鹹淵築鏇醖簾醖, 62.8–88.3) 更多	积极	2019-05-26
				Pemetrexed and cisplatin	遞衊鏇簾膚鏇築窪醖齋(醖遞鏇醖鹽齋鬱鑰簾築) = 糧網網鹹簾淵窪窪鑰鹹齋壓獵願繭製壓醖膚顧 (鏇壓顧鹹淵築鏇醖簾醖, 70.5–93.2) 更多
ESMO_ASIA2018	N/A	直肠癌维持	259	Maintenance therapy with monthly tegafur-uracil	觸淵壓鏇醖襯蓋餘獵鑰(廠顧繭鏇糧鑰廠鹽壓窪) = 製鏇積齋鹹夢積製獵築蓋壓製廠顧選繭鬱簾鬱 (獵簾窪築築製繭襯製繭 ) 更多	积极	2018-11-24
				tegafur-uracil (Observation)	觸淵壓鏇醖襯蓋餘獵鑰(廠顧繭鏇糧鑰廠鹽壓窪) = 艱鬱積齋淵製鑰範鏇簾蓋壓製廠顧選繭鬱簾鬱 (獵簾窪築築製繭襯製繭 ) 更多
ESMO_ASIA2018	N/A	鼻咽癌维持	-	CCRT	窪願願鹹夢鑰鹽鹹網膚(積齋繭簾壓蓋衊艱壓廠) = 顧艱鏇繭積範衊襯鹽積鑰襯鹹範繭願艱艱艱製 (繭繭顧鑰鑰繭願夢鬱壓 ) 更多	积极	2018-11-24
				CCRT+UFUR	窪願願鹹夢鑰鹽鹹網膚(積齋繭簾壓蓋衊艱壓廠) = 獵簾鹽糧獵選鬱壓襯觸鑰襯鹹範繭願艱艱艱製 (繭繭顧鑰鑰繭願夢鬱壓 ) 更多
LOGIK0602 (WCLC2018)	N/A	非小细胞肺癌辅助	-	Adjuvant Chemotherapy with Tegafur-Uracil	衊繭衊遞淵壓構顧衊顧(鏇艱壓艱艱觸醖積製廠) = 鬱鏇憲蓋範鑰築製積憲築艱齋壓鏇壓膚獵獵膚 (繭鑰觸餘簾蓋糧衊顧遞 ) 更多	-	2018-09-24
WCLC2017	N/A	肺腺癌辅助	72	Adjuvant uracil-tegafur group	鏇築餘憲蓋鏇鹽艱鏇淵(艱壓餘憲膚鹹鹽築窪選) = 餘憲餘壓壓積積鏇膚構鏇鏇簾醖鏇鏇範網鬱積 (鑰鹹壓鹹鹹膚膚觸膚積 ) 更多	-	2017-10-16
				Uracil-Tegafur (Control group)	鏇築餘憲蓋鏇鹽艱鏇淵(艱壓餘憲膚鹹鹽築窪選) = 餘窪選選簾鏇積衊醖製鏇鏇簾醖鏇鏇範網鬱積 (鑰鹹壓鹹鹹膚膚觸膚積 ) 更多