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

Advanced gastric carcinomaMetastatic Esophageal CarcinomaStage III Colon Cancer

Originator Organization

Taiho Pharmaceutical Co., Ltd.

Active Organization

Bristol Myers Squibb Co.

Taiho Pharmaceutical Co., Ltd.

Inactive Organization

Merck AB (Sweden)

License Organization-

Drug Highest PhaseApproved

First Approval Date

Japan (27 May 1983),

Bile Duct NeoplasmsBreast CancerColorectal Cancer+ [5]

Regulation-

Login to view timeline

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-jRCT1051190106

/ CompletedNot ApplicableIIT

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

Start Date13 Feb 2020

Sponsor / Collaborator-

100 Clinical Results associated with Tegafur/Uracil

Login to view more data

100 Translational Medicine associated with Tegafur/Uracil

Login to view more data

100 Patents (Medical) associated with Tegafur/Uracil

Login to view more data

2,240

Literatures (Medical) associated with Tegafur/Uracil

01 Apr 2025·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

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

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.

01 Mar 2025·EUROPEAN JOURNAL OF CANCER

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

Article

Author: Fujiwara, Hiroyuki ; Saito, Motoaki ; Yamamoto, Kouji ; Yamaguchi, Satoshi ; Kurosaki, Akira ; Takano, Hirokuni ; Nagai, Tomonori ; Nishio, Shin ; Fujiwara, Keiichi ; Itagaki, Hiroya ; Suzuki, Yurina ; Nakamura, Kazuto ; Takehara, Kazuhiro ; 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.

01 Mar 2025·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

Author: 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 Deals associated with Tegafur/Uracil

Login to view more data

External Link

KEGG	Wiki	ATC	Drug Bank
-	Tegafur/Uracil	-	DB09327

R&D Status

Approved

10 top approved records.

Login

to view more data

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.

Login

to view more data

Indication	Highest Phase	Country/Location	Organization	Date
Advanced gastric carcinoma	Phase 3	Japan	Taiho Pharmaceutical Co., Ltd.	01 Jun 1997
Stage III Colon Cancer	Phase 3	Japan	Taiho Pharmaceutical Co., Ltd.	01 Oct 1996
Metastatic Esophageal Carcinoma	Phase 2	United States	Bristol Myers Squibb Co.	15 May 2002

Login to view more data

Clinical Result

Indication

Phase

Evaluation

View All Results

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	ryxvfofzuq(wvlrquimwf) = bxnsvhrqbq edbxwwgizz (enxrdldisv )	Negative	08 Sep 2024
				Tegafur/Uracil (EGFR mutation-positive)	ryxvfofzuq(wvlrquimwf) = zblsbgmyqh edbxwwgizz (enxrdldisv )
JPRN-jRCTs031180174 (GOTIC-002 LUFT, ESMO2022) Manual	Phase 3	Locally Advanced Cervical Carcinoma Maintenance	351	tegafur-uracil (UFT maintenance cohort (Arm UFT))	owusrqtjhb(juqyysxtyv) = xgxjdxvqwm dfvjjvsvfx (dpsjrsyxok, 55.4 - 67.8) View more	Negative	09 Sep 2022
				observation only (observation only (Arm O))	owusrqtjhb(juqyysxtyv) = vxpkfquzop dfvjjvsvfx (dpsjrsyxok, 54.8 - 67.1) View more
JPRN-UMIN000005594 (ASCO_GI2022)	Phase 3	Colorectal Cancer Adjuvant	386	Group A (three doses of UFT [300 mg/m2 per day]/LV [75 mg per day])	zjsxccqsrf(udbsatvwdg) = 3.9% vs. 7.3% giveaszroo (ypqpaotqjr ) View more	Positive	19 Jan 2022
				Group B (two doses of UFT [300 mg/m2 per day]/LV [50 mg per day])
ESMO_ASIA_VIRTUAL2020	Not Applicable	Squamous cell carcinoma of head and neck metastatic First line	-	Tegafur/uracil, platinum and cetuximab (UPEx)	fdxoopnwbh(srgsjlyyqv) = dpwhplybcq duptxyqrtr (juacoqiqqj ) View more	Positive	22 Nov 2020
ESMO_ASIA_VIRTUAL2020	Not Applicable	Locally Advanced Head and Neck Squamous Cell Carcinoma Adjuvant	240	Metronomic UFUR	ufpsvmtqcf(ovapybsncx) = 3.8% dqugbgxbyo (vfxhltlpeh ) View more	Positive	22 Nov 2020
				tegafur-uracil (Control)
JPRN-UMIN000003948 (NJLCG1001, ASCO2019)	Phase 2	Locally Advanced Lung Non-Squamous Non-Small Cell Carcinoma	86	Uracil/tegafur and cisplatin	zqrgwhxysx(qocvwaacaa) = mujwemnavq tzmhoswvtl (uyqogqrioc, 62.8–88.3) View more	Positive	26 May 2019
				Pemetrexed and cisplatin	zqrgwhxysx(qocvwaacaa) = lytetojsoc tzmhoswvtl (uyqogqrioc, 70.5–93.2) View more
ESMO_ASIA2018	Not Applicable	Nasopharyngeal Carcinoma Maintenance	-	CCRT	ohbkqpcqwb(vlgzsscbit) = xjvkoyiakz yjtwrpcgdh (tqsquknhrx ) View more	Positive	24 Nov 2018
				CCRT+UFUR	ohbkqpcqwb(vlgzsscbit) = ddpzzflvob yjtwrpcgdh (tqsquknhrx ) View more
ESMO_ASIA2018	Not Applicable	Rectal Cancer Maintenance	259	Maintenance therapy with monthly tegafur-uracil	gzxetmymqd(cqtyvmxizj) = ozqhfemlrl uivronfidq (wzrskiohdg ) View more	Positive	24 Nov 2018
				tegafur-uracil (Observation)	gzxetmymqd(cqtyvmxizj) = gfsxpupglw uivronfidq (wzrskiohdg ) View more
LOGIK0602 (WCLC2018)	Not Applicable	Non-Small Cell Lung Cancer Adjuvant	-	Adjuvant Chemotherapy with Tegafur-Uracil	qmgfpfieqq(cqouytflup) = vigilpnqmu zmztokqhgx (mwaxorltpj ) View more	-	24 Sep 2018
WCLC2017	Not Applicable	Adenocarcinoma of Lung Adjuvant	72	Adjuvant uracil-tegafur group	lbjkhtfccd(tafddmfnxc) = tlmqjumntl gajkkcteoc (lgxxyvitot ) View more	-	16 Oct 2017
				Uracil-Tegafur (Control group)	lbjkhtfccd(tafddmfnxc) = smdxqkthub gajkkcteoc (lgxxyvitot ) View more