Delving into the Latest Updates on Tegafur/Uracil with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Compound Tegafur, Orzel, Uftoral

+ [11]

Target

TYMS

Action

inhibitors

Mechanism

TYMS inhibitors(Thymidylate synthase inhibitors)

Therapeutic Areas

NeoplasmsDigestive System DisordersEndocrinology and Metabolic Disease+ [4]

Active Indication

Bladder CancerHead and Neck NeoplasmsProstatic Cancer+ [9]

Inactive Indication

Metastatic Esophageal CarcinomaStage III Colon Cancer

Originator Organization

Taiho Pharmaceutical Co., Ltd.

Active Organization

Taiho Pharmaceutical Co., Ltd.

Bristol Myers Squibb Co.

Inactive Organization

Merck AB (Sweden)

Drug Highest PhaseApproved

First Approval Date

Japan (27 May 1983),

Bile Duct NeoplasmsBreast CancerColorectal Cancer+ [5]

Regulation-

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Structure/Sequence

Molecular FormulaC12H13FN4O5

InChIKeyDHMYGZIEILLVNR-UHFFFAOYSA-N

CAS Registry74578-38-4

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

Start Date01 Dec 2021

Sponsor / Collaborator-

JPRN-UMIN000036159

/ SuspendedNot ApplicableIIT

Efficacy of pre operative Tegafur/Uracil and Degarelix combination therapy for high risk prostate cancer - Efficacy of pre operative Tegafur/Uracil and Degarelix combination therapy for high risk prostate cancer

Start Date01 Apr 2019

Sponsor / Collaborator

Gifu University

NCT02836977

/ Unknown statusNot ApplicableIIT

Maintenance Tegafur-uracil Versus Observation Following Adjuvant Oxaliplatin-based Regimen in Patients With Stage III Colon Cancer After Radical Resection

Primary Objective:
To compare 3-year disease free survival (DFS) of tegafur-uracil following adjuvant oxaliplatin-based regimen to observation following adjuvant oxaliplatin-based regimen in patients with stage III colon cancer after radical resection.
Secondary Objectives:
To assess 5-year overall survival (OS) in each arm
To assess the safety profiles

Start Date01 Mar 2016

Sponsor / Collaborator

Kaohsiung Medical University Chung-Ho Memorial Hospital

100 Clinical Results associated with Tegafur/Uracil

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100 Translational Medicine associated with Tegafur/Uracil

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100 Patents (Medical) associated with Tegafur/Uracil

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2,237

Literatures (Medical) associated with Tegafur/Uracil

01 Mar 2025·European Journal of Cancer

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

Article

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

AIMConcurrent 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.METHODSBetween 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.RESULTSPatient 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.CONCLUSIONSThese 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.

01 Jan 2025·Hepatology Research

Improved survival outcome of curative liver resection for Barcelona Clinic Liver Cancer stage C hepatocellular carcinoma in the era of tyrosine kinase inhibitors

Article

Author: Asahi, Yoh ; Nagatsu, Akihisa ; Sakamoto, Yuzuru ; Aiyama, Takeshi ; Kamiyama, Toshiya ; Shichi, Shunsuke ; Kamachi, Hirofumi ; Taketomi, Akinobu ; Orimo, Tatsuya ; Shimada, Shingo ; Wakizaka, Kazuki ; Kakisaka, Tatsuhiko

AbstractAimThis study was undertaken to evaluate the outcome of curative liver resection, (LR) of Barcelona Clinic Liver Cancer stage C hepatocellular carcinoma (BCLC‐C HCC) after tyrosine kinase inhibitors (TKIs) became approved as a treatment option for recurrent lesions.MethodsSixty‐seven patients with BCLC‐C HCC who underwent curative LR were enrolled in this study. The patients were classified into two groups according to whether LR was performed before (n = 24) or after (n = 43) TKI approval (“beforeTKI” and “afterTKI” group, respectively).ResultsThere was no difference in the median disease‐free survival time after LR between the beforeTKI and afterTKI groups (5.6 and 7.1 months, respectively; p = 0.435). However, the median survival time after LR was longer in the afterTKI than beforeTKI group (42.7 and 14.9 months, respectively; p = 0.022). Univariate and multivariate analyses showed that the date of LR was the only independent factor affecting postresection survival. When the patients were limited to those with recurrence, there were no differences in the recurrence pattern or progression of HCC at the time of recurrence between the two groups. The only difference in the treatment distribution was the administration of TKIs (14 of 34 patients in afterTKI group and only 1 of 19 patients in beforeTKI group, p < 0.001).ConclusionThese data suggest that TKI therapy for recurrent BCLC‐C HCC is associated with improved overall survival. Thus, LR could be a promising option for BCLC‐C HCC in the current era of TKI therapy.

01 Jan 2025·Translational Lung Cancer Research

Efficacy of adjuvant tegafur-uracil (UFT) in early-stage non-small cell lung cancer with poor prognostic factors

Article

Author: Yoshii, Naoko ; Kohama, Takuya ; Endo, Takumi ; Suzuki, Eriko ; Tanahashi, Masayuki ; Iguchi, Kensuke ; Watanabe, Takuya

BackgroundPostoperative recurrence is a significant problem in patients with early-stage non-small cell lung cancer (NSCLC), with recurrence rates of 35% for stage IB and 50% for stage IIA. This study aimed to evaluate the efficacy of tegafur-uracil (UFT) as an adjuvant therapy in NSCLC patients with poor prognostic factors.MethodsA retrospective analysis was conducted of 330 patients with stage IB/IIA NSCLC who underwent lung resection between 2000 and 2019. Patients were divided into two groups based on the presence of poor prognostic factors (vascular, lymphatic, or pleural invasion or high pathological grade). Recurrence-free survival (RFS) and overall survival (OS) were compared between the UFT-treated and untreated groups using a Kaplan-Meier analysis.ResultsAmong these patients, 85.8% had poor prognostic factors. In patients with poor prognostic factors, the 5-year RFS rates in the UFT and non-UFT groups were 74.3% and 62.6%, respectively (P=0.048), and the 5-year OS was 85.6% and 62.4%, respectively (P<0.001). In patients without poor prognostic factors, UFT significantly extended OS (90.2% vs. 57.2%, P=0.03), but did not significantly affect RFS (P=0.40).ConclusionsPostoperative adjuvant therapy with UFT significantly improved both RFS and OS in patients with stage IB/IIA NSCLC with poor prognostic factors. The administration of UFT should be considered in patients with high-risk early-stage NSCLC.

100 Deals associated with Tegafur/Uracil

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External Link

KEGG	Wiki	ATC	Drug Bank
-	Tegafur/Uracil	-	DB09327

R&D Status

Approved

10 top approved records.

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Indication	Country/Location	Organization	Date
Bladder Cancer	Japan	Taiho Pharmaceutical Co., Ltd.	28 Aug 1986
Head and Neck Neoplasms	Japan	Taiho Pharmaceutical Co., Ltd.	28 Aug 1986
Prostatic Cancer	Japan	Taiho Pharmaceutical Co., Ltd.	28 Aug 1986
Uterine Cervical Cancer	Japan	Taiho Pharmaceutical Co., Ltd.	28 Aug 1986
Bile Duct Neoplasms	Japan	Taiho Pharmaceutical Co., Ltd.	27 May 1983
Breast Cancer	Japan	Taiho Pharmaceutical Co., Ltd.	27 May 1983
Colorectal Cancer	Japan	Taiho Pharmaceutical Co., Ltd.	27 May 1983
Gallbladder Neoplasms	Japan	Taiho Pharmaceutical Co., Ltd.	27 May 1983
Liver Cancer	Japan	Taiho Pharmaceutical Co., Ltd.	27 May 1983
Lung Cancer	Japan	Taiho Pharmaceutical Co., Ltd.	27 May 1983
Pancreatic Cancer	Japan	Taiho Pharmaceutical Co., Ltd.	27 May 1983
Stomach Cancer	Japan	Taiho Pharmaceutical Co., Ltd.	27 May 1983

Developing

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Metastatic Esophageal Carcinoma	NDA/BLA	United States	Bristol Myers Squibb Co.	15 May 2002
Stage III Colon Cancer	NDA/BLA	Japan	Taiho Pharmaceutical Co., Ltd.	01 Oct 1996

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Clinical Result

Indication

Phase

Evaluation

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


WCLC2024 Manual	Not Applicable	metastatic non-small cell lung cancer Adjuvant EGFR mutation-positive	1,812	Tegafur/Uracilur/Uracil	(udccbzqyuj) = rtedldofyz zjjjhfgnlr (oqcrcckzyq )	Negative	08 Sep 2024
				Tegafur/Uracil (EGFR mutation-positive)	(udccbzqyuj) = qhpnuqhmay zjjjhfgnlr (oqcrcckzyq )
JPRN-jRCTs031180174 (GOTIC-002 LUFT, ESMO2022) Manual	Phase 3	Locally Advanced Cervical Carcinoma Maintenance	351	tegafur-uracil (UFT maintenance cohort (Arm UFT))	(lmlmynzzwu) = maiyoktmod qotsluxype (hcxgxjnuju, 55.4 - 67.8) View more	Negative	09 Sep 2022
				observation only (observation only (Arm O))	(lmlmynzzwu) = qiusvkncoq qotsluxype (hcxgxjnuju, 54.8 - 67.1) View more
ASCO2021	Not Applicable	Colonic Cancer	29,176	UFT alone	(tajlgieheq) = hbtgrienmx crpccdjrgj (jvyzzmlbis ) View more	-	28 May 2021
				Infusional 5-FU or capecitabine	-
ESMO_ASIA_VIRTUAL2020	Not Applicable	Squamous cell carcinoma of head and neck metastatic First line	-	Tegafur/uracil, platinum and cetuximab (UPEx)	(rvkcplcbhu) = teunfbrebw mxpjtuwsqr (yyurympfps ) View more	Positive	22 Nov 2020
ESMO_ASIA_VIRTUAL2020	Not Applicable	Locally Advanced Head and Neck Squamous Cell Carcinoma Adjuvant	240	Metronomic UFUR	cjrozbdlva(xcslvegudi) = 3.8% kuhxqtzlel (aqfnebmxao ) View more	Positive	22 Nov 2020
				tegafur-uracil (Control)
JFMC46-1201 (ESMO2020)	Not Applicable	Colonic Cancer Adjuvant	1,938	uracil (Surgery alone)	(rxbjqtrhes) = nnlabetxyg pdfggqenpi (ntqdpbepyl ) View more	Positive	17 Sep 2020
				UFT/LV treatment	(rxbjqtrhes) = qokvxixbnu pdfggqenpi (ntqdpbepyl ) View more
JPRN-UMIN000003948 (NJLCG1001, ASCO2019)	Phase 2	Locally Advanced Lung Non-Squamous Non-Small Cell Carcinoma	86	Uracil/tegafur and cisplatin	(twlisksaiw) = eebabgtqln aiymzfelvc (seuxpqsdwp, 62.8–88.3) View more	Positive	26 May 2019
				Pemetrexed and cisplatin	(twlisksaiw) = vnisucjheh aiymzfelvc (seuxpqsdwp, 70.5–93.2) View more
JPRN-JapicCTI-101073 (ACTS-CC 02, ASCO_GI2019)	Phase 3	Stage III Colon Cancer Adjuvant	966	UFT/LV	(yukhdyjopp) = xywjiglqwt jlvyxyzfdm (arnjjvtuyx )	Negative	29 Jan 2019
				SOX	(yukhdyjopp) = mygeuspolu jlvyxyzfdm (arnjjvtuyx )
ESMO_ASIA2018	Not Applicable	Nasopharyngeal Carcinoma Maintenance	-	CCRT	(rrsmnnuqbn) = faxvuouaom wryhrznecs (cbmwrmzpvc ) View more	Positive	24 Nov 2018
				CCRT+UFUR	(rrsmnnuqbn) = xczzfcazgq wryhrznecs (cbmwrmzpvc ) View more
ESMO_ASIA2018	Not Applicable	Rectal Cancer Maintenance	259	Maintenance therapy with monthly tegafur-uracil	(gjcklpguza) = mpojwbzznq fcegseyhtx (bowpyxkisx ) View more	Positive	24 Nov 2018
				tegafur-uracil (Observation)	(gjcklpguza) = piovnhguyv fcegseyhtx (bowpyxkisx ) View more