Tipiracil hydrochloride
Highest phase reached
Approved
Drug type
Small molecule
First approval year
2015
- First approval year
- 2015
- Listing at source
- Listed
- Highest phase reached
- Approved
- Drug type
- Small molecule
- Drug name
- Tipiracil hydrochloride
- Molecular weight
- 279.13
- Structure (SMILES)
- Cl.N=C1CCCN1Cc1[nH]c(=O)[nH]c(=O)c1Cl
- 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
- 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
- CAS registry numbers
- 183204-72-0
- ChEMBL ID
- CHEMBL65375
- InChIKey
- KGHYQYACJRXCAT-UHFFFAOYSA-N
- RxNorm IDs (RxCUI)
- 1670303
- FDA ingredient codes (UNII)
- 4H59KLQ0A4
- 9903778
- 44306451
- Applicant
- TAIHO ONCOLOGY
- Approval date
- 22 Sept 2015
- Application number
- NDA207981
- First in class
- No
- Orphan designation
- No
- Availability
- Prescription only
- 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
- 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
- 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.
- 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.
- NCT01607957
- NCT01955837
- NCT03223779
- NCT03974594
- NCT04920032
- NCT05064059
- NCT05314101
- NCT05343013
- NCT05364489
- NCT05600309
- NCT01867866
- NCT01867879
- NCT01916447
- NCT02261532
- NCT02301104
- NCT02301117
- NCT01904253
- NCT02500043
- NCT02920476
- NCT02921737
- NCT03297710
- NCT03844620
- NCT04104139
- NCT05806931
- NCT04627961
And 4 more, listed on the interactive page.
- 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
- 64842-1020
- 64842-1025
- Recorded assays
- 107
- Active assays
- 19
- Confirmatory
- Other
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)
- 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)
In development for (11)
- Colon adenocarcinoma Phase 1
- Exocrine pancreatic carcinoma Phase 2
- Gastric cancer Phase 3
- Malignant colon neoplasm Phase 2
- Nasopharyngeal neoplasm Phase 2
- Neoplasm Phase 1
- Pancreatic neoplasm Phase 2
- Rectal cancer Phase 2
- Rectal carcinoma Phase 2
- Small cell lung carcinoma Phase 2
- Squamous cell lung carcinoma Phase 2
Targets (1)
- TYMP Thymidine phosphorylase inhibitor