Tegafur

Summary

Tegafur (CHEMBL20883) is an approved small molecule (ATC L01BC03); indicated across 43 conditions including neoplasm and colorectal adenocarcinoma; with CIViC clinical evidence for 3 variant-indication associations (e.g. DPYD DPYD*13 HOMOZYGOSITY in cancer).

At a glance

• Status: Approved (max clinical phase 4)
• Modality: Small molecule
• ATC class: L01BC03 (+1 more)
• Indications: 43 conditions
• Clinical trials: 44
• Precision-oncology evidence (CIViC): 3 variant–indication associations
• Chemistry: 200.17 Da · C8H9FN2O3

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL20883
Name	Tegafur
Type	Small molecule
Max phase	4
FDA approved	no
PubChem CID	5386
ATC	L01BC03, L01BC53
Molecular formula	C8H9FN2O3
Molecular weight	200.17
InChIKey	WFWLQNSHRPWKFK-UHFFFAOYSA-N

SMILES: C1CC(OC1)N2C=C(C(=O)NC2=O)F

IUPAC name: 5-fluoro-1-(oxolan-2-yl)pyrimidine-2,4-dione

Also known as: Atillon, BMS-200604, Citofur, Coparogin, Exonal, Fental, Franrose, FT-207, Ftorafur, Fulaid, Fulfeel, Furafluor

Patent coverage: 13,760 distinct patent families (52,494 SureChEMBL compound mentions), from 2 matched compound structure(s). One matched structure accounts for 52,489 (100%) of the total. Mentions count patents naming the compound (not distinct inventions), so promiscuous / reference molecules inflate the mention figure — families are the dedup metric.

Targets

Targets

Broader ChEMBL bioactivity targets: 5 (assay-derived). Sample: Microtubule-associated protein tau, Nuclear receptor ROR-gamma, Prelamin-A/C, Beta-lactamase, Estrogen receptor.

Bioactivity

ChEMBL activities: 5 potent at pChembl ≥ 5 of 7 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

Target	pChembl	Type	Value	Unit	Activity ID
P00811	5.8	Potency	1585	nM	CHEMBL_ACT_4648205
ESR1	5.38	AC50	4131	nM	CHEMBL_ACT_25138722
P51450	5.3	Potency	5012	nM	CHEMBL_ACT_4778100
MAPT	5.1	Potency	7943	nM	CHEMBL_ACT_4501875
P51450	5	Potency	10000	nM	CHEMBL_ACT_4074494

Target pathways

No target-pathway data for this drug (no mapped target genes).

Indications & clinical

Indications

43 indications (2 at ChEMBL trial phase 4). Phase below is the highest clinical-trial phase recorded for this drug against each disease — not the molecule’s overall approval status (that is in the Summary).

Indication	Trial phase	MONDO	EFO
neoplasm	4	MONDO:0005070	EFO:0000616
colorectal adenocarcinoma	3	MONDO:0005008	EFO:0000365
gastric adenocarcinoma	3	MONDO:0005036	EFO:0000503
exocrine pancreatic carcinoma	3	MONDO:0005192	EFO:0002618
carcinoma of esophagus	3	MONDO:0019086	EFO:0002916
breast neoplasm	3	MONDO:0021100	EFO:0003869
biliary tract neoplasm	3	MONDO:0005304	EFO:0003891
gastric neoplasm	3	MONDO:0021085	EFO:0003897
colorectal neoplasm	3	MONDO:0005335	EFO:0004142
cholangiocarcinoma	3	MONDO:0019087	EFO:0005221
esophageal squamous cell carcinoma	3	MONDO:0005580	EFO:0005922
head and neck cancer	3	MONDO:0005627	EFO:0006859
rectal cancer	3	MONDO:0006519	EFO:1000657
adenocarcinoma	3	MONDO:0004970	EFO:0000228
rectal neoplasm	3	MONDO:0002165	MONDO:0044937
pancreatic neoplasm	3	MONDO:0021040	EFO:0003860
gastric carcinoma	3	MONDO:0004950	EFO:0000178
malignant pancreatic neoplasm	3	MONDO:0009831	EFO:1000359
head and neck squamous cell carcinoma	2	MONDO:0010150	EFO:0000181
hepatocellular carcinoma	2	MONDO:0007256	EFO:0000182
non-small cell lung carcinoma	2	MONDO:0005233	EFO:0003060
pancreatic neuroendocrine tumor	2	MONDO:0019954	EFO:1000045
neuroendocrine neoplasm	2	MONDO:0019496	EFO:1001901
gallbladder carcinoma	2	MONDO:0003220	EFO:1001956
small cell lung carcinoma	2	MONDO:0008433	EFO:0000702
neuroendocrine carcinoma	2	MONDO:0002120	MONDO:0002120
oral cavity squamous cell carcinoma	2	MONDO:0004958	EFO:0000199
pancreatic ductal adenocarcinoma	2	MONDO:0005184	MONDO:0005184
nasopharyngeal carcinoma	2	MONDO:0015459	MONDO:0015459
liver disorder	1	MONDO:0005154	EFO:0001421
kidney disorder	1	MONDO:0005240	EFO:0003086

12 further indication records had no mapped disease name (EFO/MeSH-only) or were duplicates, and are omitted.

Clinical trials

Total trials: 44.

Phase distribution

Phase	Trials
PHASE2	23
PHASE3	8
PHASE1	6
PHASE2/PHASE3	3
Not specified	3
PHASE4	1

Top trials by phase / activity

NCT	Phase	Status	Title
NCT02887365	PHASE4	UNKNOWN	A Phase II Study of Tegafur-Uracil as Maintenance Chemotherapy in Patients With Stage II of Colon Cancer
NCT04415853	PHASE3	RECRUITING	Study of Larotinib in Unresectable Advanced or Recurrent Esophageal Cancer
NCT05914610	PHASE3	NOT_YET_RECRUITING	Envollizumab Combined With Fruquintinib and SOX Versus SOX for Conversion Therapy in Advanced Gastric Cancer
NCT00207831	PHASE3	TERMINATED	Trial Testing Ftorafur (UFT) Associated With Neoadjuvant Radiotherapy Versus Radiotherapy Alone in Rectal Adenocarcinoma
NCT00336947	PHASE3	UNKNOWN	S-1 or Tegafur-Uracil in Treating Patients With Previously Treated Stage III or Stage IV Head and Neck Cancer
NCT00378716	PHASE3	COMPLETED	Combination Chemotherapy in Treating Patients With Resected Colon Cancer
NCT00385970	PHASE3	UNKNOWN	A Phase III Trial Comparing UFT+PSK to UFT+LV in Stage IIB, III Colorectal Cancer
NCT00503321	PHASE2/PHASE3	TERMINATED	Phase II Study of TS-1 Therapy and TS-1+PSK Therapy Against Advanced Gastric Carcinoma
NCT00660894	PHASE3	COMPLETED	Tegafur-Uracil and Leucovorin or S-1 in Treating Patients With Stage III Colon Cancer That Has Been Completely Removed by Surgery
NCT04135781	PHASE3	UNKNOWN	Nab-paclitaxel Combined With S-1 as Adjuvant Chemotherapy for Stage Ⅲ Gastric Cancer
NCT05325528	PHASE2/PHASE3	UNKNOWN	Study of Tislelizumab in Combination With SOX for the Treatment of Gastric Cancer With Liver Metastases
NCT05817201	PHASE2/PHASE3	UNKNOWN	Toripalimab Plus Radiotherapy for Elderly Esophageal Cancer Patients Treated With Non-chemotherapy Strategy
NCT05451290	PHASE2	ACTIVE_NOT_RECRUITING	Camrelizumab Plus Apatinib in Combination With GEMOX (Gemcitabine and Oxaliplatin ) in Patients With Locally Advanced Biliary Tract Cancer
NCT06339619	PHASE2	RECRUITING	Combination Immunotherapy of Adebrelimab With Apatinib and Tegafur for Immune Rechallenge Therapy in Esophageal Squamous Cell Carcinoma
NCT06354140	PHASE2	RECRUITING	PPIO-008 Tislelizumab Combined With S-1 in Patients With ypT+N0 ESCC After Radical Resection With Neoadjuvant STUDY
NCT06383078	PHASE2	NOT_YET_RECRUITING	HR070803 in Combination With Oxaliplatin, S-1 Versus NALIRIFOX as Adjuvant Therapy for Pancreatic Cancer
NCT06396585	PHASE2	NOT_YET_RECRUITING	The Efficacy and Safety of Tislelizumab Combined With Anlotinib and S1 Plus Oxaliplatin as Neoadjuvant Therapy for the Locally Advanced Adenocarcinoma of Esophagogastric Junction
NCT06439550	PHASE2	NOT_YET_RECRUITING	Adjuvant Treatment With Serplulimab，Trastuzumab and SOX in the HER-2 Positive GC/GEJC
NCT06461910	PHASE2	RECRUITING	Efficacy and Safety of Anti-PD-1, Thymalfasin, and SOX in Neoadjuvant Treatment of cStage III Gastric/Gastroesophageal Junction Adenocarcinoma
NCT06988956	PHASE2	RECRUITING	Nimotuzumab Plus Definite Chemoradiotherapy(dCRT) in Elderly Patients With Esophageal Squamous Cell Carcinoma
NCT07165847	PHASE2	RECRUITING	Neoadjuvant Radiotherapy Plus Tegafur, Oxaliplatin and Iparomlimab and Tuvonralimab in Resectable Gastric and GE-junction Cancer : A Randomized, Two-arm, Prospective Trial (TRIUNITE-05)
NCT00004860	PHASE2	COMPLETED	Fluorouracil-Uracil and Leucovorin in Treating Elderly Patients With Metastatic Colorectal Cancer
NCT00005608	PHASE2	TERMINATED	Fluorouracil-Uracil and Leucovorin in Treating Women With Metastatic Breast Cancer
NCT00464919	PHASE2	COMPLETED	Sorafenib Plus Tegafur/Uracil (UFUR®) for Hepatocellular Carcinoma (HCC)
NCT00519688	PHASE2	COMPLETED	UFUR Plus Thalidomide for Advanced Hepatocellular Carcinoma
NCT00855881	PHASE2	UNKNOWN	Metronomic Chemotherapy With Tegafur/Uracil for Head and Neck Squamous Cell Carcinoma
NCT02447679	PHASE2	COMPLETED	Oral Thalidomide and Tegafur-uracil to Decrease Hepatocellular Carcinoma Recurrence
NCT03121313	PHASE2	UNKNOWN	Maintenance Tegafur-uracil in Resected Oral Cavity Cancer With ECS+
NCT03204019	PHASE2	UNKNOWN	A Study of Tegafur Combined With Temozolomide Versus Tegafur Combined With Temozolomide and Thalidomide in Subjects With Advanced Pancreatic Neuroendocrine Tumor
NCT03204032	PHASE2	UNKNOWN	A Study of Tegafur Combined With Temozolomide Versus Tegafur Combined With Temozolomide and Thalidomide in Subjects With Advanced Extrapancreatic Neuroendocrine Tumor
NCT03406299	PHASE2	COMPLETED	Phase II Randomized Trial of SLOG vs GC in Locally Advanced or Metastatic Biliary Tract Cancer
NCT03702491	PHASE2	UNKNOWN	Apapitatin Combined With SOX for Palliative Adjuvant Chemotherapy in Patients With Advanced Gallbladder Carcinoma
NCT04216758	PHASE2	UNKNOWN	Nab-P and Gem Compared With Gem and Tegafur in Adjuvant Chemotherapy After Radical Resection of Pancreatic Cancer
NCT05070598	PHASE2	UNKNOWN	Camrelizumab Combined With Chemotherapy in First-line Treatment of HER2-positive Gastric Cancer
NCT05223088	PHASE2	COMPLETED	Tislelizumab Combined With Apatinib and Oxaliplatin Plus S1 as Neoadjuvant Therapy for Borrmann IV、Large Borrmann III Type and Bulky N Positive Advanced Gastric Cancer
NCT00002801	PHASE1	COMPLETED	Combination Chemotherapy and Radiation Therapy in Treating Patients With Colorectal Cancer
NCT00003925	PHASE1	COMPLETED	Combination Chemotherapy In Treating Patients With Advanced Cancer
NCT00009815	PHASE1	WITHDRAWN	Combination Chemotherapy in Treating Patients With Advanced Solid Tumors
NCT00009828	PHASE1	WITHDRAWN	Paclitaxel Combined With Fluorouracil-Uracil and Leucovorin in Treating Patients With Solid Tumors
NCT03175679	PHASE1	COMPLETED	Adoptive Transfer of iNKT Cells for Treating Patients With Relapsed/Advanced HCC

Clinical evidence (CIViC)

Variant × indication × effect (3 predictive associations from 3 curated evidence items):

Variant	Indication	Effect	Therapy	Level	CIViC
DPYD DPYD*13 HOMOZYGOSITY	Cancer	Adverse Response	Capecitabine + Fluorouracil + Tegafur	CIViC A	EID1801
DPYD DPYD*2A HOMOZYGOSITY	Cancer	Adverse Response	Tegafur + Capecitabine + Fluorouracil	CIViC A	EID1800
DPYD RS67376798 HOMOZYGOSITY	Cancer	Adverse Response	Tegafur + Fluorouracil + Capecitabine	CIViC A	EID1803

Pharmacology

Pharmacogenomics

PharmGKB dosing guidelines (4) — CPIC / DPWG genotype-guided dosing for this drug (drug × pharmacogene):

Guideline	Source	Gene(s)	Dosing	Recommendation
Annotation of DPWG Guideline for tegafur and DPYD	DPWG	DPYD	yes	yes
Annotation of CPIC Guideline for tegafur and DPYD	CPIC	DPYD
Annotation of SEFF/SEOM Guideline for capecitabine, fluorouracil, tega	SEFF/SEOM	DPYD	yes	yes
Annotation of AIOM Guideline for capecitabine, fluorouracil, tegafur a	AIOM	DPYD	yes	yes

PharmGKB also curates 10 clinical and 42 variant annotation(s) for this drug (gene-keyed; see PharmGKB).

Related molecules

Related molecules

No competitor molecules sharing a primary target (ChEMBL phase ≥2 or PubChem drug-class).