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-

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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-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

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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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1,984

Literatures (Medical) associated with Tegafur/Uracil

01 Sep 2025·ANTICANCER RESEARCH

Tegafur-uracil as a Maintenance Therapy for Non-metastatic Nasopharyngeal Carcinoma: Insights from the Literature

Review

Author: Jhou, Hong-Jie ; Chen, Po-Huang ; Lee, Cho-Hao ; Chen, Jia-Hong ; Lee, Jih-Chin ; Chu, Yueng-Hsiang ; Yang, Tung-Lung ; Lee, Hsu-Lin

Nasopharyngeal carcinoma (NPC) remains a challenging malignancy with high rates of recurrence following definitive therapy. This meta-analysis aimed to evaluate the efficacy of tegafur-uracil (UFT) maintenance therapy in patients with non-metastatic NPC after curative treatment. A systematic literature search of PubMed, Embase, and the Cochrane Library was performed to identify eligible studies. Three retrospective cohort studies including a total of 558 patients were analyzed. Random-effects meta-analysis demonstrated that UFT maintenance therapy significantly improved both progression-free survival [hazard ratio (HR)=0.53, 95% confidence interval (CI)=0.35-0.81] and overall survival (HR=0.37, 95%CI=0.21-0.65) compared to observation alone. Sensitivity analyses confirmed the robustness of these findings. However, trial sequential analysis indicated that the cumulative evidence did not meet the a priori information size required for a conclusive result, highlighting the need for further high-quality studies. In summary, UFT maintenance therapy may represent a promising option to reduce recurrence and improve survival in non-metastatic NPC, particularly in settings where access to novel agents is limited, but additional prospective studies are needed to confirm its clinical benefit.

01 Aug 2025·Gan to kagaku ryoho. Cancer & chemotherapy

[A Case of Long-Term Complete Remission with Solitary Metastasis Following Surgery and Chemotherapy for Ascending Colon Cancer].

Review

Author: Nakata, Yasuhiko ; Murai, Kaiki ; Matsumoto, Ikuko ; Kaiga, Teruo ; Katsuno, Gotaro ; Kurokawa, Tomoharu ; Mamiya, Takao

We report a rare case of a solitary metastasis in which long-term complete remission was achieved with chemotherapy alone. An 81-year-old woman underwent a right hemicolectomy and D3 lymph node dissection for ascending colon cancer. Pathological findings showed type 2, 40×20 mm, tub2>muc, pT3, int, INF b, ly1, v0, pN1(1/32), pPM0, pDM0, and fStage Ⅲa. However, the patient chose not to undergo adjuvant chemotherapy and opted for further observation. Five months after the surgery, lymph node metastasis was observed near the right external iliac artery. Because the patient did not wish to undergo surgical treatment, SOX therapy was initiated. Owing to considerable side effects, the patient's treatment was switched to oral S-1. Gradually, the lesion disappeared, and the treatment was changed to UFT. The patient has maintained complete long-term remission for 10 years postoperatively. Here, we report this case along with a literature review.

01 Aug 2025·LUNG CANCER

Adjuvant therapy in pStage IA1–IIA lung adenocarcinoma (pN0): A multicenter study focusing on EGFR mutations and recurrence patterns (CReGYT-01 EGFR study)

Article

Author: Fujino, K ; Soh, J ; Ikeda, K ; Kinoshita, F ; Notsuda, H ; Katsumata, S ; Muto, S ; Shinchi, Y ; Shien, K ; Nomura, K ; Motooka, Y ; Shimokawa, M ; Hayasaka, K ; Suzawa, K ; Suda, K ; Ohde, Y ; Koga, T ; Matsushima, R ; Yoshikawa, M ; Saishoji, H ; Suzuki, M ; Takamori, S

BACKGROUND:

Adjuvant treatment strategies based on EGFR mutation status remain unestablished in stage I-II lung adenocarcinoma. Although UFT is an established adjuvant therapy in Japan for resected pathological N0 (pN0) lung adenocarcinoma, its clinical utility according to EGFR mutation status remains unclear. This study aimed to evaluate the efficacy of UFT and recurrence patterns in pStage IA1-IIA disease, with a primary focus on pStage IA3-IIA and the influence of EGFR mutation status.

METHODS:

This multicenter retrospective study included 2,462 patients with pStage IA1-IIA lung adenocarcinoma (TNM 8th edition) who underwent complete resection at 21 institutions in Japan (2015-2018). Propensity score matching was employed to adjust for baseline differences between treatment groups. We evaluated the survival benefit of UFT by EGFR mutation status and analyzed recurrence patterns based on EGFR status and other clinicopathological variables.

RESULTS:

In the post-PSM cohort (N = 600), UFT significantly improved overall survival (OS) (p = 0.007, HR = 0.546), particularly in EGFR wild-type patients (p < 0.001, HR = 0.403). UFT also prolonged recurrence-free survival (RFS) in EGFR wild-type cases (p = 0.004, HR = 0.604). No OS or RFS benefit was observed in EGFR mutation-positive patients. Subgroup analysis showed that UFT provided significant OS benefit in patients with high-malignancy histological subtypes such as solid/micropapillary (HR = 0.32, 95 % CI: 0.13-0.80). EGFR mutation and lymphovascular invasion were independent predictors of recurrence, with EGFR mutations associated specifically with distant and CNS recurrence.

CONCLUSIONS:

Adjuvant UFT improves OS and RFS in EGFR wild-type pStage IA3-IIA lung adenocarcinoma, particularly in patients with high-risk pathological features. In contrast, UFT is ineffective in EGFR mutation-positive cases, highlighting the need for refined adjuvant treatment strategies tailored to EGFR status and tumor biology in early-stage lung adenocarcinoma with pathological N0 (pN0).

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
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

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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	Adjuvant EGFR mutation-positive	1,812	Tegafur/Uracilur/Uracil	waabyekddy(mqgoaevles) = bqbeceuftl urmrvkjgcu (jgkumrzssl )	Negative	08 Sep 2024
				Tegafur/Uracil (EGFR mutation-positive)	waabyekddy(mqgoaevles) = bnfshulcug urmrvkjgcu (jgkumrzssl )
JPRN-jRCTs031180174 (GOTIC-002 LUFT, ESMO2022) Manual	Phase 3	Locally Advanced Cervical Carcinoma Maintenance	351	tegafur-uracil (UFT maintenance cohort (Arm UFT))	fitxzcsipd(vzsvblsmlf) = xpuwmyekrk fnbshzbvou (dxmxuubebh, 55.4 - 67.8) View more	Negative	09 Sep 2022
				observation only (observation only (Arm O))	fitxzcsipd(vzsvblsmlf) = paneutedpc fnbshzbvou (dxmxuubebh, 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])	cjogriclzh(spbnlfgipb) = 3.9% vs. 7.3% bgznzdrrht (pzutswhjjw ) 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	Locally Advanced Head and Neck Squamous Cell Carcinoma Adjuvant	240	Metronomic UFUR	irtieknroe(hhqzvaxfqm) = 3.8% jncuplgewi (fxqxdlhhpj ) View more	Positive	22 Nov 2020
				tegafur-uracil (Control)
ESMO_ASIA_VIRTUAL2020	Not Applicable	Squamous cell carcinoma of head and neck metastatic First line	-	Tegafur/uracil, platinum and cetuximab (UPEx)	yipusddonl(mrhjznobpn) = jfrjxbdyby hpjetphyue (nfjpzrvuej ) View more	Positive	22 Nov 2020
JPRN-UMIN000003948 (NJLCG1001, ASCO2019)	Phase 2	Locally Advanced Lung Non-Squamous Non-Small Cell Carcinoma	86	Uracil/tegafur and cisplatin	xeoidghwvm(bgecfczkcg) = kvfkdkktky imrwyyfjhm (zbydjljlvy, 62.8–88.3) View more	Positive	26 May 2019
				Pemetrexed and cisplatin	xeoidghwvm(bgecfczkcg) = tpdpunxewr imrwyyfjhm (zbydjljlvy, 70.5–93.2) View more
ESMO_ASIA2018	Not Applicable	Rectal Cancer Maintenance	259	Maintenance therapy with monthly tegafur-uracil	ldbhdgnvsh(tlfeuywphv) = tvdjgmgvmh pdgshqzwiv (pugebgmxwb ) View more	Positive	24 Nov 2018
				tegafur-uracil (Observation)	ldbhdgnvsh(tlfeuywphv) = drxrmswhux pdgshqzwiv (pugebgmxwb ) View more
LOGIK0602 (WCLC2018)	Not Applicable	Non-Small Cell Lung Cancer Adjuvant	-	Adjuvant Chemotherapy with Tegafur-Uracil	pwwxlbqghq(vegvcsczfm) = poeriqrbsk feanlrlffx (oqqqlfmduu ) View more	-	24 Sep 2018
JPRN-C000000013 (ASCO_GI2017)	Phase 3	Colorectal Liver Metastases Adjuvant	180	UFT/LV	foenrmvdwl(uygznjcxmr) = suksooxthg kzkpxvdheq (suxkbucfbj ) View more	Positive	21 Mar 2017
ISRCTN17533723 (ASCO2016)	Phase 1/2	Recurrent Squamous Cell Carcinoma of the Head and Neck	43	Cisplatin/UFUR/irinotecan triple combination therapy	uvpsjhcocq(yzenalydsu) = zwhrqvpidi vetmwmbaxo (byjquqkmqx ) View more	Positive	20 May 2016