> Trialight public data. Index of pages: https://trialight.com/llms.txt
> Web page: https://trialight.com/data/asset/tegafur-373c07a7-2961-4c06-af1a-16fedfad4fd1
> Record changed: 2026-10-13

# Tegafur

Highest phase reached

Approved

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL20883)

Drug type

Small molecule

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL20883)

## Development status

**Listing at source**

Listed

**Highest phase reached**

Approved

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL20883)

## Names and chemistry

**Drug type**

Small molecule

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL20883)

**Drug name**

Tegafur

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL20883)

**Molecular weight**

200.17

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL20883)

**Structure (SMILES)**

O=c1\[nH\]c(=O)n(C2CCCO2)cc1F

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL20883)

### Brand names (12)

- citofur
- Citofur
- riol
- Riol
- tegafur component of s 1
- Tegafur component of s-1
- tegafur component of teysuno
- Tegafur component of teysuno
- tegafur component of ts 1
- Tegafur component of ts-1
- uftoral
- Uftoral

### Other names (75)

- atillon
- Atillon
- bms 200604
- BMS-200604
- camrelizumab oxaliplatin tegafur
- coparogin
- Coparogin
- exonal
- Exonal
- fental
- Fental
- franrose
- Franrose
- ft 207
- FT-207
- ftorafur
- Ftorafur
- fulaid
- Fulaid
- fulfeel
- Fulfeel
- furafluor
- Furafluor
- furofutran
- Furofutran

And 50 more, listed on the interactive page.

## Identifiers

**CAS registry numbers**

- 17902-23-7

**ChEMBL ID**

CHEMBL20883

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL20883)

**InChIKey**

WFWLQNSHRPWKFK-UHFFFAOYSA-N

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL20883)

**PubChem compound IDs**

- 5386

**RxNorm IDs (RxCUI)**

- 4582

**FDA ingredient codes (UNII)**

- 1548R74NSZ

### ATC classification codes (2)

- L01BC03
- L01BC53

Sources for recorded values

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL20883)

## Regulatory information

### Other regulatory facts

**First in class**

No

**Orphan designation**

No

## Pharmacology

### Drug classification

**Pharmacology name**

tegafur

**Type**

Synthetic organic

**Approval recorded by Guide to Pharmacology**

Yes

### Mechanisms of action (3)

- **Mechanism**  
DNA inhibitor

**Action type**  
Inhibitor

**Target**  
DNA
- **Mechanism**  
RNA inhibitor

**Action type**  
Inhibitor

**Target**  
RNA
- **Mechanism**  
Thymidylate synthase inhibitor

**Action type**  
Inhibitor

**Target**  
Thymidylate synthase

**Protein identifier**  
P04818

### Open Targets mechanisms

- **Mechanism**  
Thymidylate synthase inhibitor

**Action type**  
Inhibitor

**Target**  
Thymidylate synthase

### Investigated indications (43)

- **Condition**  
Stomach Neoplasms

**Highest recorded phase**  
3

**Condition identifier**  
EFO:0000178

**Subject identifier**  
D013274
- **Condition**  
Carcinoma, Squamous Cell

**Highest recorded phase**  
2

**Condition identifier**  
EFO:0000181

**Subject identifier**  
D002294
- **Condition**  
Carcinoma, Hepatocellular

**Highest recorded phase**  
2

**Condition identifier**  
EFO:0000182

**Subject identifier**  
D006528
- **Condition**  
Squamous Cell Carcinoma of Head and Neck

**Highest recorded phase**  
2

**Condition identifier**  
EFO:0000199

**Subject identifier**  
D000077195
- **Condition**  
Adenocarcinoma

**Highest recorded phase**  
3

**Condition identifier**  
EFO:0000228

**Subject identifier**  
D000230
- **Condition**  
Colorectal Neoplasms

**Highest recorded phase**  
3

**Condition identifier**  
EFO:0000365

**Subject identifier**  
D015179
- **Condition**  
Stomach Neoplasms

**Highest recorded phase**  
3

**Condition identifier**  
EFO:0000503

**Subject identifier**  
D013274
- **Condition**  
Neoplasms

**Highest recorded phase**  
4

**Condition identifier**  
EFO:0000616

**Subject identifier**  
D009369
- **Condition**  
Small Cell Lung Carcinoma

**Highest recorded phase**  
2

**Condition identifier**  
EFO:0000702

**Subject identifier**  
D055752
- **Condition**  
Liver Diseases

**Highest recorded phase**  
1

**Condition identifier**  
EFO:0001421

**Subject identifier**  
D008107
- **Condition**  
Pancreatic Neoplasms

**Highest recorded phase**  
3

**Condition identifier**  
EFO:0002618

**Subject identifier**  
D010190
- **Condition**  
Esophageal Neoplasms

**Highest recorded phase**  
3

**Condition identifier**  
EFO:0002916

**Subject identifier**  
D004938
- **Condition**  
Carcinoma, Non-Small-Cell Lung

**Highest recorded phase**  
2

**Condition identifier**  
EFO:0003060

**Subject identifier**  
D002289
- **Condition**  
Kidney Diseases

**Highest recorded phase**  
1

**Condition identifier**  
EFO:0003086

**Subject identifier**  
D007674
- **Condition**  
Pancreatic Neoplasms

**Highest recorded phase**  
3

**Condition identifier**  
EFO:0003860

**Subject identifier**  
D010190
- **Condition**  
Breast Neoplasms

**Highest recorded phase**  
3

**Condition identifier**  
EFO:0003869

**Subject identifier**  
D001943
- **Condition**  
Biliary Tract Neoplasms

**Highest recorded phase**  
3

**Condition identifier**  
EFO:0003891

**Subject identifier**  
D001661
- **Condition**  
Stomach Neoplasms

**Highest recorded phase**  
3

**Condition identifier**  
EFO:0003897

**Subject identifier**  
D013274
- **Condition**  
Colorectal Neoplasms

**Highest recorded phase**  
3

**Condition identifier**  
EFO:0004142

**Subject identifier**  
D015179
- **Condition**  
Cholangiocarcinoma

**Highest recorded phase**  
3

**Condition identifier**  
EFO:0005221

**Subject identifier**  
D018281
- **Condition**  
Esophageal Neoplasms

**Highest recorded phase**  
3

**Condition identifier**  
EFO:0005922

**Subject identifier**  
D004938
- **Condition**  
Head and Neck Neoplasms

**Highest recorded phase**  
3

**Condition identifier**  
EFO:0006859

**Subject identifier**  
D006258
- **Condition**  
Neuroendocrine Tumors

**Highest recorded phase**  
2

**Condition identifier**  
EFO:1000045

**Subject identifier**  
D018358
- **Condition**  
Pancreatic Neoplasms

**Highest recorded phase**  
3

**Condition identifier**  
EFO:1000359

**Subject identifier**  
D010190
- **Condition**  
Rectal Neoplasms

**Highest recorded phase**  
3

**Condition identifier**  
EFO:1000657

**Subject identifier**  
D012004

And 18 more, listed on the interactive page.

### Open Targets indications (67)

- **Condition identifier**  
EFO\_0000181

**Highest recorded phase**  
2
- **Condition identifier**  
EFO\_0000182

**Highest recorded phase**  
2
- **Condition identifier**  
EFO\_0000199

**Highest recorded phase**  
2
- **Condition identifier**  
EFO\_0000365

**Highest recorded phase**  
3
- **Condition identifier**  
EFO\_0000503

**Highest recorded phase**  
3
- **Condition identifier**  
EFO\_0000616
- **Condition identifier**  
EFO\_0000702

**Highest recorded phase**  
2
- **Condition identifier**  
EFO\_0002618

**Highest recorded phase**  
3
- **Condition identifier**  
EFO\_0003060
- **Condition identifier**  
EFO\_0003086

**Highest recorded phase**  
1
- **Condition identifier**  
EFO\_0003860

**Highest recorded phase**  
2
- **Condition identifier**  
EFO\_0003897
- **Condition identifier**  
EFO\_0004142

**Highest recorded phase**  
2
- **Condition identifier**  
EFO\_0005221

**Highest recorded phase**  
3
- **Condition identifier**  
EFO\_0005922

**Highest recorded phase**  
3
- **Condition identifier**  
EFO\_0006859
- **Condition identifier**  
EFO\_1000359

**Highest recorded phase**  
2
- **Condition identifier**  
EFO\_1000657

**Highest recorded phase**  
3
- **Condition identifier**  
EFO\_1001956

**Highest recorded phase**  
2
- **Condition identifier**  
MONDO\_0001056
- **Condition identifier**  
MONDO\_0001056

**Highest recorded phase**  
4
- **Condition identifier**  
MONDO\_0001187

**Highest recorded phase**  
3
- **Condition identifier**  
MONDO\_0002120

**Highest recorded phase**  
2
- **Condition identifier**  
MONDO\_0002169

**Highest recorded phase**  
3
- **Condition identifier**  
MONDO\_0002974

And 42 more, listed on the interactive page.

### Reported adverse events (53)

- **Event**  
acute myeloid leukaemia

**Reports**  
4

**Reporting signal score**

8.74867
- **Event**  
alanine aminotransferase increased

**Reports**  
29

**Reporting signal score**

62.5694
- **Event**  
anaemia

**Reports**  
18

**Reporting signal score**

15.454
- **Event**  
anorexia

**Reports**  
8

**Reporting signal score**

21.137
- **Event**  
aspartate aminotransferase increased

**Reports**  
26

**Reporting signal score**

56.1503
- **Event**  
bile culture positive

**Reports**  
1

**Reporting signal score**

7.58686
- **Event**  
biliary tract disorder

**Reports**  
2

**Reporting signal score**

7.0277
- **Event**  
blood bilirubin increased

**Reports**  
13

**Reporting signal score**

29.2243
- **Event**  
blood lactate dehydrogenase increased

**Reports**  
8

**Reporting signal score**

18.309
- **Event**  
bone marrow failure

**Reports**  
18

**Reporting signal score**

48.3854
- **Event**  
carbohydrate antigen 15-3 increased

**Reports**  
2

**Reporting signal score**

8.58673
- **Event**  
cardiotoxicity

**Reports**  
5

**Reporting signal score**

12.6017
- **Event**  
cholangitis acute

**Reports**  
2

**Reporting signal score**

7.8713
- **Event**  
decreased appetite

**Reports**  
21

**Reporting signal score**

27.4507
- **Event**  
diarrhoea

**Reports**  
41

**Reporting signal score**

35.4556
- **Event**  
disease progression

**Reports**  
9

**Reporting signal score**

8.5991
- **Event**  
disseminated intravascular coagulation

**Reports**  
6

**Reporting signal score**

15.0951
- **Event**  
eosinophil count increased

**Reports**  
3

**Reporting signal score**

6.25957
- **Event**  
eosinophil percentage increased

**Reports**  
2

**Reporting signal score**

7.80229
- **Event**  
febrile neutropenia

**Reports**  
7

**Reporting signal score**

6.55445
- **Event**  
gamma-glutamyltransferase increased

**Reports**  
6

**Reporting signal score**

9.11971
- **Event**  
hepatic function abnormal

**Reports**  
19

**Reporting signal score**

45.7949
- **Event**  
hyperbilirubinaemia

**Reports**  
6

**Reporting signal score**

14.4356
- **Event**  
hypoalbuminaemia

**Reports**  
3

**Reporting signal score**

6.28463
- **Event**  
interstitial lung disease

**Reports**  
8

**Reporting signal score**

10.7618

And 28 more, listed on the interactive page.

### Trial references (265)

- NCT00002801  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT00002801)
- NCT00004860  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT00004860)
- NCT00152230  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT00152230)
- NCT00209651  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT00209651)
- NCT00284258  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT00284258)
- NCT00378716  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT00378716)
- NCT00385970  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT00385970)
- NCT00660894  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT00660894)
- NCT00905047  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT00905047)
- NCT00974389  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT00974389)
- NCT03397199  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT03397199)
- NCT03769935  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT03769935)
- NCT00003925  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT00003925)
- NCT00009815  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT00009815)
- NCT00009828  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT00009828)
- NCT00400023  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT00400023)
- NCT00479076  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT00479076)
- NCT01128998  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT01128998)
- NCT01610479  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT01610479)
- NCT02454062  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT02454062)
- NCT04566380  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT04566380)
- NCT00005608  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT00005608)
- NCT00152178  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT00152178)
- NCT00152191  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT00152191)
- NCT00994968  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT00994968)

And 240 more, listed on the interactive page.

## Chemical properties

**Hydrogen bond acceptors**

4

**Hydrogen bond donors**

1

**Polar surface area**

64.09

**Calculated partition coefficient (ALogP)**

\-0.02

**Calculated partition coefficient (XLogP)**

\-0.3

**Prodrug**

Yes

**Chirality**

Racemic

**Inorganic**

No

**Rule-of-five violations**

0

**Rotatable bonds**

1

**Heavy atoms**

14

**Molecular formula**

C8H9FN2O3

**Monoisotopic mass**

200.05972032

**Natural product**

No

## Evidence counts

**Recorded assays**

2,225

**Active assays**

19

### Active assay types (3)

- Confirmatory
- Other
- Screening

## Pharmacologic actions

- Antimetabolites, Antineoplastic  
Source: [id.nlm.nih.gov](https://id.nlm.nih.gov/mesh/D000964.html)

## Related records

### Trials (67)

- [A LM-302 Combination With Other Anti-Tumor Therapies Phase ll Study](https://trialight.com/data/trial/a-lm-302-combination-with-other-anti-tumor-therapies-phase-f867e7b8-f10d-4281-8491-ff6441459c77.md)
- A Phase II Study of Gimatecan (ST1481) in Locally Advanced or Metastatic Pancreatic Cancer
- A Phase II Study of Paclitaxel, UFT, and Leucovorin in Patients With Metastatic Esophageal Cancer
- A Phase II Study of Tegafur-Uracil as Maintenance Chemotherapy in Patients With Stage II of Colon Cancer
- A Phase II Study of Tegafur/Uracil (UFUR®)Plus Thalidomide for the Treatment of Advanced or Metastatic Hepatocellular Carcinoma (HCC)
- A Phase III Trial Comparing UFT+PSK to UFT+LV in Stage IIB, III Colorectal Cancer
- A Phase lb/lI Clinical Study in Advanced or Metastatic Esophageal Squamous Cell Carcinoma
- A Randomized Controlled Study of Postoperative Adjuvant Chemotherapy of Uracil- Tegafur (UFT) Compared With Surgery Alone (NSAS-CC)
- A Randomized Controlled Study of Postoperative Adjuvant Chemotherapy of Uracil- Tegafur (UFT) Compared With Surgery Alone (NSAS-GC)
- A Randomized Controlled Study of Postoperative Adjuvant Therapy of Uracil-tegafur (UFT) Compared With Cyclophosphamide/Methotrexate/5-fluorouracil (CMF) in Breast Cancer (NSAS-BC)
- A Study of Intraperitoneal Paclitaxel in Combination With SOX Compared With SOX Alone in Gastric Cancer With Malignant Ascites
- A Study of Tegafur Combined With Temozolomide Versus Tegafur Combined With Temozolomide and Thalidomide in Subjects With Advanced Extrapancreatic Neuroendocrine Tumor
- A Study of Tegafur Combined With Temozolomide Versus Tegafur Combined With Temozolomide and Thalidomide in Subjects With Advanced Pancreatic Neuroendocrine Tumor
- Adjuvant Treatment With Serplulimab，Trastuzumab and SOX in the HER-2 Positive GC/GEJC
- Adoptive Transfer of iNKT Cells for Treating Patients With Relapsed/Advanced HCC
- Adoptive Transfer of Specific HCC Antigens CD8+ T Cells for Treating Patients With Relapsed/Advanced HCC
- Apapitatin Combined With SOX for Palliative Adjuvant Chemotherapy in Patients With Advanced Gallbladder Carcinoma
- Camrelizumab Combined With Chemotherapy in First-line Treatment of HER2-positive Gastric Cancer
- Camrelizumab Plus Apatinib in Combination With GEMOX (Gemcitabine and Oxaliplatin ) in Patients With Locally Advanced Biliary Tract Cancer
- CCRT Followed by Tegafur, Gimeracil and Oteracil Potassium in Cervical Cancer

### Approved for (2)

- [Cancer](https://trialight.com/data/condition/cancer-703b1dfc-4812-50eb-83f4-d7a205d16bdb.md)
- Neoplasm

### In development for (40)

- [Adenocarcinoma](https://trialight.com/data/condition/adenocarcinoma-b5c321d1-7c49-5bf9-abd0-dfa99dbd5f29.md) Phase 3
- [Adult hepatocellular carcinoma](https://trialight.com/data/condition/adult-hepatocellular-carcinoma-c10a1a4b-50f0-572a-8bff-bf597d4b7fae.md) Phase 2
- [Biliary tract cancer](https://trialight.com/data/condition/biliary-tract-cancer-6b9535c9-ccaa-5b47-8c46-0d05d39d7c62.md) Phase 3
- [Biliary tract neoplasm](https://trialight.com/data/condition/biliary-tract-neoplasm-5b757066-5940-52f7-aa7d-e5aafdc5b54e.md) Phase 3
- [Breast cancer](https://trialight.com/data/condition/breast-cancer-8ac10da3-93bd-54c5-a93b-265bc6699689.md) Phase 3
- [Breast neoplasm](https://trialight.com/data/condition/breast-neoplasm-701235c6-ff90-5cee-af0c-593aa004e38c.md) Phase 3
- Carcinoma of esophagus Phase 3
- [Cervical cancer](https://trialight.com/data/condition/cervical-cancer-10fb8f6c-5aac-5281-8f06-7238adeec443.md) Phase 1
- [Cholangiocarcinoma](https://trialight.com/data/condition/cholangiocarcinoma-3777afe4-5189-5eb1-82f8-0c3446cb902f.md) Phase 3
- [Colorectal adenocarcinoma](https://trialight.com/data/condition/colorectal-adenocarcinoma-49107d5a-ece1-5f2b-8783-f2077e298ffa.md) Phase 3
- [Colorectal cancer](https://trialight.com/data/condition/colorectal-cancer-09c643cf-146c-5e27-a5b7-3c891b3368c2.md) Phase 3
- [Colorectal neoplasm](https://trialight.com/data/condition/colorectal-neoplasm-31f0a633-3abe-5df4-9d3a-9292c6541f1d.md) Phase 3
- [Esophageal cancer](https://trialight.com/data/condition/esophageal-cancer-a3b5271c-e6d4-537b-8dfd-9391c60e2af2.md) Phase 3
- [Esophageal squamous cell carcinoma](https://trialight.com/data/condition/esophageal-squamous-cell-carcinoma-c10bd9c9-02f9-5805-8008-b021f4604e7a.md) Phase 3
- Exocrine pancreatic carcinoma Phase 3
- [Gallbladder carcinoma](https://trialight.com/data/condition/gallbladder-carcinoma-0f30c5c6-4ee3-58f9-a97d-6499bb1158fb.md) Phase 2
- [Gastric adenocarcinoma](https://trialight.com/data/condition/gastric-adenocarcinoma-6bb74a55-7ba6-53e3-a113-22296a84d6ae.md) Phase 3
- [Gastric cancer](https://trialight.com/data/condition/gastric-cancer-3c1e2785-2672-5b3e-afce-9335f684c159.md) Phase 3
- Gastric carcinoma Phase 3
- [Gastric neoplasm](https://trialight.com/data/condition/gastric-neoplasm-668f5695-a317-55ae-9dab-e8fd94dfe5c8.md) Phase 3

### Targets (1)

- [TYMS](https://trialight.com/data/target/tyms-8b1d20f5-3314-546a-bd58-610c1db66b0f.md) Thymidylate synthase inhibitor

---

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