Trifluridine

Highest phase reached

Approved

www.ebi.ac.uk

Drug type

Small molecule

www.ebi.ac.uk

First approval year

1980

www.ebi.ac.uk

First approval year: 1980
www.ebi.ac.uk

Listing at source: Listed

Highest phase reached: Approved
www.ebi.ac.uk

Drug type: Small molecule
www.ebi.ac.uk

Drug name: Trifluridine
www.ebi.ac.uk

Molecular weight: 296.2
www.ebi.ac.uk

Structure (SMILES): O=c1[nH]c(=O)n([C@H]2C[C@H](O)[C@@H](CO)O2)cc1C(F)(F)F
www.ebi.ac.uk

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

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.

CAS registry numbers

70-00-8

ChEMBL ID: CHEMBL1129
www.ebi.ac.uk

InChIKey: VSQQQLOSPVPRAZ-RRKCRQDMSA-N
www.ebi.ac.uk

PubChem compound IDs

6256

RxNorm IDs (RxCUI)

10803

FDA ingredient codes (UNII)

RMW9V5RW38

L01BC59
S01AD02

Sources for recorded values

www.ebi.ac.uk

Applicant: TAIHO ONCOLOGY
Approval date: 22 Sept 2015
Application number: NDA207981

First in class: No
Orphan designation: No
Availability: Prescription only

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

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

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.

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.

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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

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

61314-044
64842-1020
64842-1025

Recorded assays: 1,683
Active assays: 164

Confirmatory
Other
Screening
Summary

Antimetabolites
id.nlm.nih.gov
Antiviral Agents
id.nlm.nih.gov

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
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)
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)

In development for (9)

Breast cancer Phase 2
Breast neoplasm Phase 2
Cholangiocarcinoma Phase 2
Colon carcinoma Phase 2
Esophageal cancer Phase 3
Gastric adenocarcinoma Phase 1
Non-small cell lung carcinoma Phase 1
Rectal cancer Phase 2
Rectal carcinoma Phase 2

Trifluridine

Development status

Names and chemistry

Brand names (14)

Other names (38)

Identifiers

ATC classification codes (2)

Regulatory information

United States

Other regulatory facts

Pharmacology

Drug classification

Administration routes

Mechanisms of action

Investigated indications (17)

Open Targets indications (45)

Reported adverse events (26)

Trial references (20)

Dosing

Conditions of use

Chemical properties

National Drug Codes

Evidence counts

Active assay types (4)

Pharmacologic actions

Biological measurements

Observed measurements

Liver toxicity assay

Measurement types

Related records

Trials (105)

Approved for (8)

In development for (9)

Other linked conditions (1)