> Trialight public data. Index of pages: https://trialight.com/llms.txt
> Web page: https://trialight.com/data/asset/tipiracil-hydrochloride-c5072dfa-12fa-4ccc-9e35-c488a67c9673
> Record changed: 2026-10-13

# Tipiracil hydrochloride

Highest phase reached

Approved

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL65375)

Drug type

Small molecule

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL65375)

First approval year

2015

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL65375)

## Development status

**First approval year**

2015

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL65375)

**Listing at source**

Listed

**Highest phase reached**

Approved

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL65375)

## Names and chemistry

**Drug type**

Small molecule

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL65375)

**Drug name**

Tipiracil hydrochloride

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL65375)

**Molecular weight**

279.13

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL65375)

**Structure (SMILES)**

Cl.N=C1CCCN1Cc1\[nH\]c(=O)\[nH\]c(=O)c1Cl

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL65375)

### Brand names (6)

- tipiracil hydrochloride component of lonsurf
- Tipiracil hydrochloride component of lonsurf
- tipiracil hydrochloride component of s 95005
- Tipiracil hydrochloride component of s-95005
- tipiracil hydrochloride component of tas 102
- Tipiracil hydrochloride component of tas-102

### Other names (22)

- lonsurf component tipiracil hydrochloride
- LONSURF COMPONENT TIPIRACIL HYDROCHLORIDE
- s 95005 component tipiracil hydrochloride
- S-95005 COMPONENT TIPIRACIL HYDROCHLORIDE
- tas 1 462
- tas 102 component tipiracil hydrochloride
- TAS-1-462
- TAS-102 COMPONENT TIPIRACIL HYDROCHLORIDE
- tipiracil hydrochloride
- Tipiracil hydrochloride
- TIPIRACIL HYDROCHLORIDE \[JAN\]
- TIPIRACIL HYDROCHLORIDE \[MI\]
- TIPIRACIL HYDROCHLORIDE \[ORANGE BOOK\]
- TIPIRACIL HYDROCHLORIDE \[USAN\]
- Tipiracil hydrochloride \[WHO-DD\]
- tipiracil hydrochloride jan
- tipiracil hydrochloride mi
- tipiracil hydrochloride orange book
- tipiracil hydrochloride usan
- tipiracil hydrochloride who dd
- tpi
- TPI

## Identifiers

**CAS registry numbers**

- 183204-72-0

**ChEMBL ID**

CHEMBL65375

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL65375)

**InChIKey**

KGHYQYACJRXCAT-UHFFFAOYSA-N

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL65375)

**RxNorm IDs (RxCUI)**

- 1670303

**FDA ingredient codes (UNII)**

- 4H59KLQ0A4

### PubChem compound IDs (2)

- 9903778
- 44306451

## 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

**Drug name stem**

\-racil

#### Administration routes

- Oral

### Mechanisms of action

- **Mechanism**  
Thymidine phosphorylase inhibitor

**Action type**  
Inhibitor

**Target**  
Thymidine phosphorylase

**Protein identifier**  
P19971

### Open Targets mechanisms

- **Mechanism**  
Thymidine phosphorylase inhibitor

**Action type**  
Inhibitor

**Target**  
Thymidine phosphorylase

### Investigated indications (15)

- **Condition**  
Colorectal Neoplasms

**Highest recorded phase**  
4

**Condition identifier**  
EFO:0000365

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

**Highest recorded phase**  
1

**Condition identifier**  
EFO:0000616

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

**Highest recorded phase**  
2

**Condition identifier**  
EFO:0000702

**Subject identifier**  
D055752
- **Condition**  
Carcinoma, Squamous Cell

**Highest recorded phase**  
2

**Condition identifier**  
EFO:0000708

**Subject identifier**  
D002294
- **Condition**  
Pancreatic Neoplasms

**Highest recorded phase**  
2

**Condition identifier**  
EFO:0002618

**Subject identifier**  
D010190
- **Condition**  
Pancreatic Neoplasms

**Highest recorded phase**  
2

**Condition identifier**  
EFO:0003860

**Subject identifier**  
D010190
- **Condition**  
Colorectal Neoplasms

**Highest recorded phase**  
4

**Condition identifier**  
EFO:0004142

**Subject identifier**  
D015179
- **Condition**  
Nasopharyngeal Neoplasms

**Highest recorded phase**  
2

**Condition identifier**  
EFO:0004252

**Subject identifier**  
D009303
- **Condition**  
Rectal Neoplasms

**Highest recorded phase**  
2

**Condition identifier**  
EFO:1000657

**Subject identifier**  
D012004
- **Condition**  
Pulmonary Disease, Chronic Obstructive

**Highest recorded phase**  
1

**Condition identifier**  
EFO:1001949

**Subject identifier**  
D029424
- **Condition**  
Colorectal Neoplasms

**Highest recorded phase**  
4

**Condition identifier**  
EFO:1001951

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

**Highest recorded phase**  
3

**Condition identifier**  
MONDO:0001056

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

**Highest recorded phase**  
4

**Condition identifier**  
MONDO:0005575

**Subject identifier**  
D015179
- **Condition**  
Colonic Neoplasms

**Highest recorded phase**  
2

**Condition identifier**  
MONDO:0021063

**Subject identifier**  
D003110
- **Condition**  
Rectal Neoplasms

**Highest recorded phase**  
2

**Condition identifier**  
MONDO:0044937

**Subject identifier**  
D012004

### Open Targets indications (28)

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

**Highest recorded phase**  
1
- **Condition identifier**  
EFO\_0000708

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

**Highest recorded phase**  
2
- **Condition identifier**  
EFO\_0004252

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

**Highest recorded phase**  
1
- **Condition identifier**  
EFO\_1001480

**Highest recorded phase**  
3
- **Condition identifier**  
MONDO\_0001056
- **Condition identifier**  
MONDO\_0001056

**Highest recorded phase**  
3
- **Condition identifier**  
MONDO\_0003060

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

**Highest recorded phase**  
3
- **Condition identifier**  
MONDO\_0004970

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

**Highest recorded phase**  
4
- **Condition identifier**  
MONDO\_0005036

**Highest recorded phase**  
3
- **Condition identifier**  
MONDO\_0005097

**Highest recorded phase**  
2
- **Condition identifier**  
MONDO\_0005184

**Highest recorded phase**  
1
- **Condition identifier**  
MONDO\_0005575
- **Condition identifier**  
MONDO\_0005575

**Highest recorded phase**  
4
- **Condition identifier**  
MONDO\_0006047

**Highest recorded phase**  
2
- **Condition identifier**  
MONDO\_0006519

**Highest recorded phase**  
2
- **Condition identifier**  
MONDO\_0008433

**Highest recorded phase**  
2
- **Condition identifier**  
MONDO\_0008903

**Highest recorded phase**  
2
- **Condition identifier**  
MONDO\_0009831

**Highest recorded phase**  
1
- **Condition identifier**  
MONDO\_0015459

**Highest recorded phase**  
2
- **Condition identifier**  
MONDO\_0019087

**Highest recorded phase**  
2

And 3 more, listed on the interactive page.

### Reported adverse events (26)

- **Event**  
abdominal pain

**Reports**  
149

**Reporting signal score**

81.3691
- **Event**  
abdominal pain upper

**Reports**  
82

**Reporting signal score**

38.4239
- **Event**  
alopecia

**Reports**  
94

**Reporting signal score**

73.4139
- **Event**  
anaemia

**Reports**  
138

**Reporting signal score**

65.7487
- **Event**  
asthenia

**Reports**  
133

**Reporting signal score**

37.3387
- **Event**  
blood alkaline phosphatase abnormal

**Reports**  
13

**Reporting signal score**

43.4639
- **Event**  
blood count abnormal

**Reports**  
42

**Reporting signal score**

67.2381
- **Event**  
carcinoembryonic antigen increased

**Reports**  
18

**Reporting signal score**

52.6293
- **Event**  
colorectal cancer metastatic

**Reports**  
14

**Reporting signal score**

42.2272
- **Event**  
constipation

**Reports**  
103

**Reporting signal score**

51.9697
- **Event**  
cytopenia

**Reports**  
50

**Reporting signal score**

106.365
- **Event**  
decreased appetite

**Reports**  
247

**Reporting signal score**

308.537
- **Event**  
dehydration

**Reports**  
74

**Reporting signal score**

31.696
- **Event**  
diarrhoea

**Reports**  
423

**Reporting signal score**

295.135
- **Event**  
disease progression

**Reports**  
532

**Reporting signal score**  
1,302.97
- **Event**  
dysgeusia

**Reports**  
62

**Reporting signal score**

63.2796
- **Event**  
fatigue

**Reports**  
550

**Reporting signal score**

479.273
- **Event**  
intestinal obstruction

**Reports**  
52

**Reporting signal score**

70.1909
- **Event**  
malignant neoplasm progression

**Reports**  
71

**Reporting signal score**

62.752
- **Event**  
nausea

**Reports**  
484

**Reporting signal score**

316.461
- **Event**  
neutropenia

**Reports**  
130

**Reporting signal score**

83.3413
- **Event**  
neutrophil count decreased

**Reports**  
48

**Reporting signal score**

40.8448
- **Event**  
red blood cell count decreased

**Reports**  
36

**Reporting signal score**

39.5713
- **Event**  
stoma site haemorrhage

**Reports**  
13

**Reporting signal score**

41.5197
- **Event**  
vomiting

**Reports**  
254

**Reporting signal score**

119.727

And 1 more, listed on the interactive page.

### Trial references (29)

- NCT01607957  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT01607957)
- NCT01955837  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT01955837)
- NCT03223779  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT03223779)
- NCT03974594  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT03974594)
- NCT04920032  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT04920032)
- NCT05064059  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT05064059)
- NCT05314101  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT05314101)
- NCT05343013  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT05343013)
- NCT05364489  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT05364489)
- NCT05600309  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT05600309)
- NCT01867866  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT01867866)
- NCT01867879  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT01867879)
- NCT01916447  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT01916447)
- NCT02261532  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT02261532)
- NCT02301104  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT02301104)
- NCT02301117  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT02301117)
- NCT01904253  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT01904253)
- NCT02500043  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT02500043)
- NCT02920476  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT02920476)
- NCT02921737  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT02921737)
- NCT03297710  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT03297710)
- NCT03844620  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT03844620)
- NCT04104139  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT04104139)
- NCT05806931  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT05806931)
- NCT04627961  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT04627961)

And 4 more, listed on the interactive page.

## Chemical properties

**Hydrogen bond acceptors**

3

**Hydrogen bond donors**

3

**Polar surface area**

92.81

**Calculated partition coefficient (ALogP)**

0.29

**Prodrug**

No

**Chirality**

Achiral

**Inorganic**

No

**Rule-of-five violations**

0

**Rotatable bonds**

2

**Heavy atoms**

17

**Molecular formula**

C9H12Cl2N4O2

**Monoisotopic mass**

278.0337310

**Natural product**

No

## National Drug Codes

- 64842-1020
- 64842-1025

## Evidence counts

**Recorded assays**

107

**Active assays**

19

### Active assay types (2)

- Confirmatory
- Other

## Biological measurements

### Observed measurements

#### Oral bioavailability

**Median**

52

**Mean**

52

**Minimum**

52

**Maximum**

52

**Unit**

%

**Assays**

1

**Standard deviation**

0

**Summary method**

median

**Censored results excluded**

0

**Other units excluded**

0

**Unknown units excluded**

0

#### Measurement types

- F

## Related records

### Trials (99)

- - IKF/AIO-QUINTIS - Evaluating Fruquintinib in Combination With Tislelizumab in Microsatellite Stable / Proficient Mismatch Repair (MSS/pMMR) Metastatic Colorectal Cancer Without Active Liver Metastases
- 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 Multicenter, Phase 3 Study of IBI343 Monotherapy Versus Treatment of Investigator's Choice in Subjects With Previously Treated, Claudin (CLDN) 18.2-positive, HER2-negative, Gastric or Gastroesophageal Junction Adenocarcinoma (G-HOPE-001)
- 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 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 the Safety and Efficacy of Selinexor With or Without Pembrolizumab Versus Standard of Care in Previously Treated Metastatic Colorectal Cancer With RAS Mutations
- A Vaccine (PolyPEPI1018 Vaccine) and TAS-102 for the Treatment of Metastatic Colorectal Cancer
- ADG126 in Combination With Pembrolizumab in Patients With Advanced/Metastatic Solid Tumors

### Approved for (4)

- [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)

### In development for (11)

- Colon adenocarcinoma Phase 1
- Exocrine pancreatic carcinoma Phase 2
- [Gastric cancer](https://trialight.com/data/condition/gastric-cancer-3c1e2785-2672-5b3e-afce-9335f684c159.md) Phase 3
- Malignant colon neoplasm Phase 2
- [Nasopharyngeal neoplasm](https://trialight.com/data/condition/nasopharyngeal-neoplasm-48691b20-fad8-5218-b6aa-4dd6c49469e4.md) Phase 2
- Neoplasm Phase 1
- [Pancreatic neoplasm](https://trialight.com/data/condition/pancreatic-neoplasm-de300cc3-339a-5c06-97d8-2d9155fc3a7b.md) Phase 2
- Rectal cancer Phase 2
- Rectal carcinoma Phase 2
- [Small cell lung carcinoma](https://trialight.com/data/condition/small-cell-lung-carcinoma-505ad14d-ce79-5398-b171-f724c32e1b4e.md) Phase 2
- [Squamous cell lung carcinoma](https://trialight.com/data/condition/squamous-cell-lung-carcinoma-9debeb10-0511-5be7-aeaa-3901bc5b9a67.md) Phase 2

### Targets (1)

- [TYMP](https://trialight.com/data/target/tymp-d3e9f860-719a-5bf3-88de-e36378c4ce8c.md) Thymidine phosphorylase inhibitor

---

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