> Trialight public data. Index of pages: https://trialight.com/llms.txt
> Web page: https://trialight.com/data/asset/trifluridine-cf1f965b-3efb-4c26-a766-cb4c7c73675f
> Record changed: 2026-10-13

# Trifluridine

Highest phase reached

Approved

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL1129)

Drug type

Small molecule

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL1129)

First approval year

1980

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL1129)

## Development status

**First approval year**

1980

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL1129)

**Listing at source**

Listed

**Highest phase reached**

Approved

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL1129)

## Names and chemistry

**Drug type**

Small molecule

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL1129)

**Drug name**

Trifluridine

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL1129)

**Molecular weight**

296.2

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL1129)

**Structure (SMILES)**

O=c1\[nH\]c(=O)n(\[C@H\]2C\[C@H\](O)\[C@@H\](CO)O2)cc1C(F)(F)F

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL1129)

### Brand names (14)

- t f t
- T.f.t.
- trifluridine
- Trifluridine
- trifluridine component of lonsurf
- Trifluridine component of lonsurf
- trifluridine component of s 95005
- Trifluridine component of s-95005
- trifluridine component of tas 102
- Trifluridine component of tas-102
- triherpine
- Triherpine
- viroptic
- Viroptic

### Other names (38)

- f3dthd
- F3dthd
- f3t
- F3T
- nsc 529182
- nsc 75520
- NSC-529182
- NSC-75520
- s 95005 component trifluridine
- S-95005 COMPONENT TRIFLURIDINE
- tas 102 component trifluridine
- TAS-102 COMPONENT TRIFLURIDINE
- trifluridina
- Trifluridina
- trifluridine
- Trifluridine
- TRIFLURIDINE \[EP MONOGRAPH\]
- trifluridine \[INN\]
- TRIFLURIDINE \[JAN\]
- TRIFLURIDINE \[MART.\]
- TRIFLURIDINE \[MI\]
- TRIFLURIDINE \[ORANGE BOOK\]
- TRIFLURIDINE \[USAN\]
- TRIFLURIDINE \[USP MONOGRAPH\]
- TRIFLURIDINE \[USP-RS\]

And 13 more, listed on the interactive page.

## Identifiers

**CAS registry numbers**

- 70-00-8

**ChEMBL ID**

CHEMBL1129

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL1129)

**InChIKey**

VSQQQLOSPVPRAZ-RRKCRQDMSA-N

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL1129)

**PubChem compound IDs**

- 6256

**RxNorm IDs (RxCUI)**

- 10803

**FDA ingredient codes (UNII)**

- RMW9V5RW38

### ATC classification codes (2)

- L01BC59
- S01AD02

Sources for recorded values

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL1129)

## Regulatory information

### United States

**Applicant**

TAIHO ONCOLOGY

**Approval date**

22 Sept 2015

**Application number**

NDA207981

### Other regulatory facts

**First in class**

No

**Orphan designation**

No

**Availability**

Prescription only

## Pharmacology

### Drug classification

**Pharmacology name**

trifluridine

**Type**

Synthetic organic

**Drug name stem**

\-uridine

**Approval recorded by Guide to Pharmacology**

Yes

#### Administration routes

- Oral
- topical

### Mechanisms of action

- **Mechanism**  
DNA inhibitor

**Action type**  
Inhibitor

**Target**  
DNA

### Investigated indications (17)

- **Condition**  
Colorectal Neoplasms

**Highest recorded phase**  
4

**Condition identifier**  
EFO:0000365

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

**Highest recorded phase**  
1

**Condition identifier**  
EFO:0000503

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

**Highest recorded phase**  
4

**Condition identifier**  
EFO:0000616

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

**Highest recorded phase**  
1

**Condition identifier**  
EFO:0003060

**Subject identifier**  
D002289
- **Condition**  
Breast Neoplasms

**Highest recorded phase**  
2

**Condition identifier**  
EFO:0003869

**Subject identifier**  
D001943
- **Condition**  
Colorectal Neoplasms

**Highest recorded phase**  
4

**Condition identifier**  
EFO:0004142

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

**Highest recorded phase**  
2

**Condition identifier**  
EFO:0005221

**Subject identifier**  
D018281
- **Condition**  
Rectal Neoplasms

**Highest recorded phase**  
2

**Condition identifier**  
EFO:1000657

**Subject identifier**  
D012004
- **Condition**  
Eye Infections

**Highest recorded phase**  
4

**Condition identifier**  
EFO:1001888

**Subject identifier**  
D015817
- **Condition**  
Colonic Neoplasms

**Highest recorded phase**  
2

**Condition identifier**  
EFO:1001950

**Subject identifier**  
D003110
- **Condition**  
Colorectal Neoplasms

**Highest recorded phase**  
4

**Condition identifier**  
EFO:1001951

**Subject identifier**  
D015179
- **Condition**  
Herpes Simplex

**Highest recorded phase**  
4

**Condition identifier**  
EFO:1002022

**Subject identifier**  
D006561
- **Condition**  
Keratoconjunctivitis

**Highest recorded phase**  
4

**Condition identifier**  
MONDO:0004768

**Subject identifier**  
D007637
- **Condition**  
Colorectal Neoplasms

**Highest recorded phase**  
4

**Condition identifier**  
MONDO:0005575

**Subject identifier**  
D015179
- **Condition**  
Breast Neoplasms

**Highest recorded phase**  
2

**Condition identifier**  
MONDO:0007254

**Subject identifier**  
D001943
- **Condition**  
Esophageal Neoplasms

**Highest recorded phase**  
3

**Condition identifier**  
MONDO:0007576

**Subject identifier**  
D004938
- **Condition**  
Rectal Neoplasms

**Highest recorded phase**  
2

**Condition identifier**  
MONDO:0044937

**Subject identifier**  
D012004

### Open Targets indications (45)

- **Condition identifier**  
EFO\_0000365
- **Condition identifier**  
EFO\_0000616
- **Condition identifier**  
EFO\_0000763
- **Condition identifier**  
EFO\_0003869

**Highest recorded phase**  
2
- **Condition identifier**  
EFO\_0004142
- **Condition identifier**  
EFO\_0005221

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

**Highest recorded phase**  
2
- **Condition identifier**  
EFO\_1001480

**Highest recorded phase**  
3
- **Condition identifier**  
EFO\_1001888
- **Condition identifier**  
EFO\_1001888

**Highest recorded phase**  
4
- **Condition identifier**  
EFO\_1002022
- **Condition identifier**  
MONDO\_0001056

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

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

**Highest recorded phase**  
3
- **Condition identifier**  
MONDO\_0002271

**Highest recorded phase**  
1
- **Condition identifier**  
MONDO\_0003060

**Highest recorded phase**  
2
- **Condition identifier**  
MONDO\_0003219

**Highest recorded phase**  
2
- **Condition identifier**  
MONDO\_0003220

**Highest recorded phase**  
2
- **Condition identifier**  
MONDO\_0004609

**Highest recorded phase**  
4
- **Condition identifier**  
MONDO\_0004768
- **Condition identifier**  
MONDO\_0004768

**Highest recorded phase**  
4
- **Condition identifier**  
MONDO\_0004970

**Highest recorded phase**  
2
- **Condition identifier**  
MONDO\_0005008

**Highest recorded phase**  
4
- **Condition identifier**  
MONDO\_0005028

**Highest recorded phase**  
2
- **Condition identifier**  
MONDO\_0005036

**Highest recorded phase**  
3

And 20 more, listed on the interactive page.

### Reported adverse events (26)

- **Event**  
abdominal pain

**Reports**  
149

**Reporting signal score**

78.0084
- **Event**  
abdominal pain upper

**Reports**  
82

**Reporting signal score**

36.6816
- **Event**  
alopecia

**Reports**  
95

**Reporting signal score**

72.6481
- **Event**  
anaemia

**Reports**  
143

**Reporting signal score**

68.6087
- **Event**  
asthenia

**Reports**  
134

**Reporting signal score**

35.7944
- **Event**  
blood alkaline phosphatase abnormal

**Reports**  
13

**Reporting signal score**

43.0673
- **Event**  
blood count abnormal

**Reports**  
42

**Reporting signal score**

66.0398
- **Event**  
carcinoembryonic antigen increased

**Reports**  
18

**Reporting signal score**

52.0837
- **Event**  
colorectal cancer metastatic

**Reports**  
16

**Reporting signal score**

49.8779
- **Event**  
constipation

**Reports**  
104

**Reporting signal score**

50.9111
- **Event**  
cytopenia

**Reports**  
50

**Reporting signal score**

104.882
- **Event**  
decreased appetite

**Reports**  
247

**Reporting signal score**

301.545
- **Event**  
diarrhoea

**Reports**  
432

**Reporting signal score**

297.907
- **Event**  
disease progression

**Reports**  
532

**Reporting signal score**  
1,285.51
- **Event**  
drug hypersensitivity

**Reports**  
2

**Reporting signal score**

43.0462
- **Event**  
dysgeusia

**Reports**  
62

**Reporting signal score**

61.6506
- **Event**  
fatigue

**Reports**  
553

**Reporting signal score**

469.278
- **Event**  
intestinal obstruction

**Reports**  
52

**Reporting signal score**

68.7468
- **Event**  
malignant neoplasm progression

**Reports**  
72

**Reporting signal score**

62.6329
- **Event**  
nausea

**Reports**  
486

**Reporting signal score**

307.112
- **Event**  
neutropenia

**Reports**  
145

**Reporting signal score**

101.809
- **Event**  
neutrophil count decreased

**Reports**  
48

**Reporting signal score**

39.6399
- **Event**  
red blood cell count decreased

**Reports**  
36

**Reporting signal score**

38.6141
- **Event**  
stoma site haemorrhage

**Reports**  
13

**Reporting signal score**

41.124
- **Event**  
vomiting

**Reports**  
255

**Reporting signal score**

115.312

And 1 more, listed on the interactive page.

### Trial references (20)

- NCT01867866  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT01867866)
- NCT04393298  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT04393298)
- NCT05029882  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT05029882)
- NCT03297710  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT03297710)
- NCT03799731  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT03799731)
- NCT05077839  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT05077839)
- NCT05198934  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT05198934)
- NCT05364489  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT05364489)
- NCT06379399  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT06379399)
- NCT03844620  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT03844620)
- NCT04076761  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT04076761)
- NCT04104139  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT04104139)
- NCT05965531  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT05965531)
- NCT04149444  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT04149444)
- NCT04457297  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT04457297)
- NCT04776148  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT04776148)
- NCT04489173  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT04489173)
- NCT04879368  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT04879368)
- NCT05062889  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT05062889)
- NCT05927857  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT05927857)

## Dosing

**Dose**

35 mg/m2

**Route**

Oral

**How often**

Twice daily on Days 1-5 and 8-12 of each 28-day cycle

### Conditions of use

- Take with food

## Chemical properties

**Hydrogen bond acceptors**

6

**Hydrogen bond donors**

3

**Polar surface area**

104.55

**Calculated partition coefficient (ALogP)**

\-0.8

**Calculated partition coefficient (XLogP)**

\-0.5

**Prodrug**

No

**Chirality**

Single enantiomer

**Inorganic**

No

**Rule-of-five violations**

0

**Rotatable bonds**

2

**Heavy atoms**

20

**Molecular formula**

C10H11F3N2O5

**Monoisotopic mass**

296.06200594

**Natural product**

No

## National Drug Codes

- 61314-044
- 64842-1020
- 64842-1025

## Evidence counts

**Recorded assays**

1,683

**Active assays**

164

### Active assay types (4)

- Confirmatory
- Other
- Screening
- Summary

## Pharmacologic actions

- Antimetabolites  
Source: [id.nlm.nih.gov](https://id.nlm.nih.gov/mesh/D000963.html)
- Antiviral Agents  
Source: [id.nlm.nih.gov](https://id.nlm.nih.gov/mesh/D000998.html)

## Biological measurements

### Observed measurements

#### Liver toxicity assay

**Median**

3,370

**Mean**

3,370

**Minimum**

3,370

**Maximum**

3,370

**Unit**

nM

**Assays**

1

**Standard deviation**

0

**Summary method**

median

**Censored results excluded**

0

**Other units excluded**

0

**Unknown units excluded**

0

#### Measurement types

- EC50

## Related records

### Trials (105)

- - IKF/AIO-QUINTIS - Evaluating Fruquintinib in Combination With Tislelizumab in Microsatellite Stable / Proficient Mismatch Repair (MSS/pMMR) Metastatic Colorectal Cancer Without Active Liver Metastases
- 5-Fluorouracil/Leucovorin (5FU/LV) in Combination With Regorafenib in Patients With Metastatic Colorectal Cancer
- A Clinical Study to Evaluate Injection TQB2102 for the Treatment of Patients With HER2 IHC3+ Advanced Colorectal Cancer Who Progressed After Treatment With Oxaliplatin, Irinotecan and Fluoropyrimidine-Based Drugs
- A Phase Ib/III Study of Suvemcitug Plus FTD/TPI in Participants With Refractory Metastatic Colorectal Cancer
- A Prospective, Single-arm, Exploratory Study of Trifluridine/Tipiracil (TAS-102) Combined With Apatinib as Third-line Therapy for Advanced Gastric Cancer
- A Randomized Phase 2 Trial of Fruquintinib and TAS-102 as Compared to Fruquintinib in Patients With Refractory Advanced/Metastatic Colorectal Cancer
- A Real-world Study of Trifluridine/Tipiracil Containing Regimen for the Treatment of Patients With mCRC (REFLECT Study)
- A Study Evaluating S 95005 Plus Bevacizumab and Capecitabine Plus Bevacizumab in Patients With Previously Untreated Colorectal Cancer Who Are Non-eligible for Intensive Therapy
- A Study in Advanced or Metastatic Gastrointestinal Cancers Exploring Treatment Combinations With Pelareorep and Atezolizumab
- [A Study of ASP1002 in Adults for Treatment of Solid Tumors](https://trialight.com/data/trial/a-study-of-asp1002-in-adults-for-treatment-of-solid-tumors-b7c15848-a6e0-44a0-9928-39a39c4086cf.md)
- A Study of ASP1570 Taken by Itself, or ASP1570 Taken Together With Either Pembrolizumab, Standard Therapies, or Both, in Adults With Solid Tumors
- A Study of Brontictuzumab With Chemotherapy for Subjects With Previously Treated Metastatic Colorectal Cancer
- [A Study of Precemtabart Tocentecan With or Without Bevacizumab Compared to Trifluridine/Tipiracil Plus Bevacizumab in Participants With Previously Treated Metastatic Colorectal Cancer (PROCEADE-CRC-03)](https://trialight.com/data/trial/a-study-of-precemtabart-tocentecan-with-or-without-21c5d54c-43a5-4347-a5d0-44bb5990e16c.md)
- A Study of Rivoceranib and Trifluridine/Tipiracil for Metastatic Colorectal Cancer (mCRC)
- A Study of Trifluridine/ Tipiracil in Chemorefractory mCRC in Greece
- A Study of Trifluridine/Tipiracil (Also Known as S 95005 or TAS-102) in Patients With a Pretreated Colorectal Cancer That Has Spread (Metastatic).
- A Study of Trifluridine/Tipiracil in Triple Negative Metastatic Breast Cancer
- A Study to Access Intravenous (IV) Telisotuzumab Adizutecan in Combination With IV Bevacizumab Compared to Standard of Care IV Bevacizumabin Combination With Oral Trifluridine and Tipiracil in Adult Participants With Refractory Metastatic Colorectal Cancer
- A Study to Assess the Safety, Pharmacokinetics and Anti Tumor Activity of UCB6114 Administered Intravenously to Participants With Advanced Solid Tumors
- A Study to Evaluate Sacituzumab Tirumotecan (MK-2870) in Advanced/Metastatic Gastroesophageal Adenocarcinoma (MK-2870-015)

### Approved for (8)

- [Colorectal adenocarcinoma](https://trialight.com/data/condition/colorectal-adenocarcinoma-49107d5a-ece1-5f2b-8783-f2077e298ffa.md)
- [Colorectal cancer](https://trialight.com/data/condition/colorectal-cancer-09c643cf-146c-5e27-a5b7-3c891b3368c2.md)
- [Colorectal carcinoma](https://trialight.com/data/condition/colorectal-carcinoma-51401c02-7884-5c5c-bb91-90106e7d0d4a.md)
- [Colorectal neoplasm](https://trialight.com/data/condition/colorectal-neoplasm-31f0a633-3abe-5df4-9d3a-9292c6541f1d.md)
- Eye infectious disorder
- [Herpes simplex infectious disease](https://trialight.com/data/condition/herpes-simplex-infectious-disease-e68e9e47-8d4d-542b-bba5-bb8aaa1ebd60.md)
- Keratoconjunctivitis
- Neoplasm

### In development for (9)

- [Breast cancer](https://trialight.com/data/condition/breast-cancer-8ac10da3-93bd-54c5-a93b-265bc6699689.md) Phase 2
- [Breast neoplasm](https://trialight.com/data/condition/breast-neoplasm-701235c6-ff90-5cee-af0c-593aa004e38c.md) Phase 2
- [Cholangiocarcinoma](https://trialight.com/data/condition/cholangiocarcinoma-3777afe4-5189-5eb1-82f8-0c3446cb902f.md) Phase 2
- Colon carcinoma Phase 2
- [Esophageal cancer](https://trialight.com/data/condition/esophageal-cancer-a3b5271c-e6d4-537b-8dfd-9391c60e2af2.md) Phase 3
- [Gastric adenocarcinoma](https://trialight.com/data/condition/gastric-adenocarcinoma-6bb74a55-7ba6-53e3-a113-22296a84d6ae.md) Phase 1
- [Non-small cell lung carcinoma](https://trialight.com/data/condition/non-small-cell-lung-carcinoma-a86c1d60-523f-5ea7-a5e1-39ed4a2296f8.md) Phase 1
- Rectal cancer Phase 2
- Rectal carcinoma Phase 2

### Other linked conditions (1)

- [Viral infectious disease](https://trialight.com/data/condition/viral-infectious-disease-43db42a3-adad-5b9d-b74c-f17df0674c21.md)

---

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