Drugs / Tipiracil
Tipiracil
also known as
tipiracil hydrochloride · TPI · TAS-1-462 · Tipiracil hydrochloride component of lonsurf · Tipiracil hydrochloride component of s-95005 · Tipiracil hydrochloride component of tas-102 · Tipiracilo · TPI (freebase)
Small molecule targets TYMP via inhibition
Regulatory milestones approvals, filings & regulatory actions · 2 recorded
| Milestone | Jurisdiction | Brand | Indication | Date | Sentence it was read from |
|---|---|---|---|---|---|
| Approved | EU (EMA) | Lonsurf | — | 2016-04-25 | europa.eu ↗ |
| Approved | US (FDA) | LONSURF | — | 2015-09-22 | fda.gov ↗ |
Trials 28 · a red edge is where a trial was stopped
| Phase | Registry id | Dates | Indication | Sponsor | Status | Outcome |
|---|---|---|---|---|---|---|
| Phase 14 trials | ||||||
| Phase 1 | NCT04511039 | Jun 2021 → Sep 2028 expected | colorectal adenocarcinoma, gastroesophageal junction adenocarcinoma | Roswell Park Cancer Institute | Recruiting | No outcome recorded |
| Phase 1 | NCT04104139 | Dec 2019 → Sep 2024 overdue | rectum adenocarcinoma | OHSU Knight Cancer Institute | Active not recruiting | No outcome recorded |
| Phase 1 | NCT03616574 | Apr 2019 → Feb 2022 | colorectal cancer | Holy Stone Healthcare Co., Ltd | Completed | No outcome recorded |
| Phase 1 | NCT03317119 | Apr 2018 → Jul 2023 | colon carcinoma, rectal carcinoma | City of Hope Medical Center | Completed | No outcome recorded |
| Phase 1/23 trials | ||||||
| Phase 1/2 | NCT05927857 | Apr 2024 → Dec 2027 expected | gastric adenocarcinoma | National Health Research Institutes, Taiwan | Recruiting | No outcome recorded |
| Phase 1/2 | NCT04177602 | Nov 2019 → Sep 2022 | — | University Medical Center Hamburg-Eppendorf | Terminated | No outcome recorded |
| Phase 1/2 | NCT03368963 | Jan 2018 → Jun 2025 overdue | cholangiocarcinoma, colorectal adenocarcinoma, gastric adenocarcinoma, pancreatic adenocarcinoma | Emory University | Active not recruiting | No outcome recorded |
| Phase 214 trials | ||||||
| Phase 2 | NCT07535632 | Jun 2026 → Jun 2028 expected | colorectal neoplasm | Shanghai Zhongshan Hospital | Not yet recruiting | No outcome recorded |
| Phase 2 | NCT07146646 | Dec 2025 → Feb 2027 expected | cholangiocarcinoma, gallbladder carcinoma | Case Comprehensive Cancer Center | Recruiting | No outcome recorded |
| Phase 2 | NCT07011550 | Aug 2025 → Jul 2028 | colorectal cancer | M.D. Anderson Cancer Center | Suspended | No outcome recorded |
| Phase 2 | NCT06711471 | Nov 2024 → Nov 2026 expected | gastric adenocarcinoma | LIN YANG | Recruiting | No outcome recorded |
| Phase 2 | NCT06485713 | Mar 2024 → Jun 2026 overdue | colorectal cancer | First Affiliated Hospital of Wenzhou Medical University | Recruiting | No outcome recorded |
| Phase 2 | NCT05356897 | Oct 2023 → Sep 2024 | colon adenocarcinoma, rectum adenocarcinoma | Academic and Community Cancer Research United | Withdrawn | No outcome recorded |
| Phase 2 | NCT04660760 | Jun 2021 → Jul 2024 | gastric adenocarcinoma, gastroesophageal adenocarcinoma, gastroesophageal junction adenocarcinoma | Academic and Community Cancer Research United | Unknown | No outcome recorded |
| Phase 2 | NCT04076761 | Dec 2019 → Sep 2022 | cholangiocarcinoma | Sunnybrook Health Sciences Centre | Terminated | No outcome recorded |
| Phase 2 | NCT03981614 | Oct 2019 → Aug 2021 | colorectal carcinoma | Academic and Community Cancer Research United | Completed | No outcome recorded |
| Phase 2 | NCT04042714 | Aug 2019 → Sep 2025 | neuroendocrine neoplasm | Baylor Research Institute | Terminated | No outcome recorded |
| Phase 2 | NCT04294264 | Feb 2019 → Mar 2024 overdue | colon carcinoma | Rutgers, The State University of New Jersey | Active not recruiting | No outcome recorded |
| Phase 2 | NCT03844620 | Jan 2019 → Aug 2026 overdue | colorectal carcinoma | M.D. Anderson Cancer Center | Active not recruiting | No outcome recorded |
| Phase 2 | NCT03274882 | Mar → Dec 2017 | colorectal cancer | Servier | Completed | No outcome recorded |
| Phase 2 | NCT01904253 | Jul 2013 → Jun 2014 | small cell lung carcinoma | Taiho Oncology, Inc. | Terminated | No outcome recorded |
| Phase 35 trials | ||||||
| Phase 3 | NCT07525206 | May 2026 → May 2029 expected | colorectal cancer | AbbVie | Recruiting | No outcome recorded |
| Phase 3 | NCT07483684 | Mar 2026 → Aug 2027 expected | carcinoma | Chia Tai Tianqing Pharmaceutical Group Nanjing Shunxin Pharmaceutical Co., Ltd. | Not yet recruiting | No outcome recorded |
| Phase 3 | NCT04457297 | Jul 2020 → Jul 2024 | colorectal cancer | National Cancer Center Hospital East | Completed | No outcome recorded |
| Phase 3 | NCT03306394 | Oct 2016 → Nov 2020 | colorectal cancer | Servier | Completed | No outcome recorded |
| Phase 3 | NCT01607957 | Jun 2012 → Jan 2014 | colorectal cancer | Taiho Oncology, Inc. | Completed | No outcome recorded |
| Phase not applicable2 trials | ||||||
| — | NCT07371871 | Jan 2026 → Dec 2027 expected | gastric cancer | Anhui Provincial Cancer Hospital | Not yet recruiting | No outcome recorded |
| — | NCT06495463 | Mar 2022 → Aug 2024 | colorectal cancer | Chang Gung Memorial Hospital | Unknown | No outcome recorded |
Also used as a comparator or background therapy in 18 trials
| Phase | Registry id | Dates | Indication | Sponsor | Status | Outcome |
|---|---|---|---|---|---|---|
| Phase 01 trial | ||||||
| Phase 0 | NCT07318389 Background | Jun 2026 → Nov 2027 expected | colorectal cancer | M.D. Anderson Cancer Center | Not yet recruiting | No outcome recorded |
| Phase 12 trials | ||||||
| Phase 1 | NCT05130060 Background | Jan 2022 → Jun 2023 | colon adenocarcinoma, metastatic malignant neoplasm in the colon, rectum adenocarcinoma | Mayo Clinic | Completed | No outcome recorded |
| Phase 1 | NCT03715933 Background | Oct 2018 → Dec 2028 expected | Ewing sarcoma, colorectal adenocarcinoma | Inhibrx Biosciences, Inc | Recruiting | No outcome recorded |
| Phase 1/23 trials | ||||||
| Phase 1/2 | NCT05405595 Background | Jun 2022 → Oct 2026 expected | — | Adagene Inc | Recruiting | No outcome recorded |
| Phase 1/2 | NCT05083481 Background | Oct 2021 → May 2026 | — | Astellas Pharma Global Development, Inc. | Terminated | No outcome recorded |
| Phase 1/2 | NCT04393298 Background | Jul 2020 → Apr 2024 | cancer | UCB Biopharma SRL | Completed | No outcome recorded |
| Phase 28 trials | ||||||
| Phase 2 | NCT07353268 Comparator | Jan 2026 → Aug 2027 expected | colorectal cancer | Tao Zhang | Not yet recruiting | No outcome recorded |
| Phase 2 | NCT07387081 Background | Dec 2025 → May 2028 expected | — | LaNova Medicines Limited | Recruiting | No outcome recorded |
| Phase 2 | NCT06856837 Comparator | Oct 2025 → Dec 2029 expected | colorectal cancer | Institut für Klinische Krebsforschung IKF GmbH at Krankenhaus Nordwest | Recruiting | No outcome recorded |
| Phase 2 | NCT06680622 Background | Mar 2025 → Sep 2027 expected | gastroesophageal adenocarcinoma | Institut für Klinische Krebsforschung IKF GmbH at Krankenhaus Nordwest | Active not recruiting | No outcome recorded |
| Phase 2 | NCT06039202 Background | Jan 2024 → Feb 2025 | colorectal cancer | Holy Stone Healthcare Co., Ltd | Unknown | No outcome recorded |
| Phase 2 | NCT05608044 Comparator | Nov 2022 → Sep 2027 expected | colorectal cancer | Agenus Inc. | Active not recruiting | No outcome recorded |
| Phase 2 | NCT04854434 Comparator | Jun 2021 → Jun 2022 | colorectal cancer | Karyopharm Therapeutics Inc | Terminated | No outcome recorded |
| Phase 2 | NCT03992456 Comparator | Apr 2020 → Dec 2023 | colon adenocarcinoma, rectum adenocarcinoma | Academic and Community Cancer Research United | Unknown | No outcome recorded |
| Phase 34 trials | ||||||
| Phase 3 | NCT06992648 Comparator | Apr 2025 → Dec 2027 expected | colorectal cancer | Second Affiliated Hospital, School of Medicine, Zhejiang University | Recruiting | No outcome recorded |
| Phase 3 | NCT05198934 Comparator | Apr 2022 → Jul 2025 | colorectal cancer | Amgen | Completed | No outcome recorded |
| Phase 3 | NCT04879368 Comparator | May 2021 → Jan 2025 | gastroesophageal cancer | Australasian Gastro-Intestinal Trials Group | Completed | No outcome recorded |
| Phase 3 | NCT03717038 Comparator | Feb 2019 → Dec 2023 | colorectal carcinoma | Symphogen A/S | Withdrawn | No outcome recorded |
Evidence & citations 13 cited values
Every value below carries the sentence it was read from. 49 sources stand behind the page.
| Field | Value | Cited text |
|---|---|---|
| Known as | tipiracil | “TAS-102 is a novel combination medicinal product consisting of a thymidine-based nucleoside analogue (trifluridine; FTD) as the active component and the thymidine phosphorylase...” NCT04042714 ↗36“OBJECTIVES: TAS-102 is an oral combination treatment comprised of an antimetabolite, trifluridine, a thymidine-based nucleoside analog, and tipiracil hydrochloride, at a molar...” PMID 27597276 ↗ Jun 2016 “LONSURF is a cytotoxic combination treatment of 2 new drugs: trifluridine, a thymidine-based nucleoside analog, and tipiracil, an inhibitor of thymidine phosphorylase.” NCT03616574 ↗ “TAS-102 is a cytotoxic combination treatment of 2 drugs: trifluridine, a thymidine-based nucleoside analogue, and tipiracil an inhibitor of thymidine phosphorylase.” NCT06039202 ↗ “TAS-102 is a combination of trifluridine, a thymidine-based nucleic acid analogue, and tipiracil, a thymidine phosphorylase inhibitor.” NCT03717038 ↗ “TAS-102 is a combination of the thymidine-based nucleoside analog trifluridine and the thymidine phosphorylase inhibitor tipiracil.” PMID 27443414 ↗ Jul 2016 “The drug consists of the cytotoxin trifluridine and the thymidine phosphorylase inhibitor (TPI) tipiracil.” NCT04879368 ↗ “Regorafenib. Fruquintinib. Trifluridine/Tipiracil (TAS-102) with or without Bevacizumab.” NCT07353268 ↗ “Drug:Trifluridine and Tipiracil Hydrochloride Tablets BID,Oral Administration” NCT07387081 ↗ “Regorafenib or trifluridine and tipiracil.” NCT05608044 ↗ |
| Known as | TAS-1-462 | ChEMBL registry synonym — accepted as the source's own label CHEMBL235668 ↗ |
| Known as | tipiracil hydrochloride | “Film-coated tablet containing 15 mg of trifluridine and 7.065 mg of tipiracil hydrochloride, or 20 mg of trifluridine and 9.42 mg of tipiracil hydrochloride (with a molar ratio...” NCT03274882 ↗11“TAS-102 is a novel combination medicinal product consisting of a thymidine-based nucleoside analogue (trifluridine; FTD) as the active component and the thymidine phosphorylase...” NCT04042714 ↗ “FTD/TPI is an orally administered combination of a thymidine-based nucleic acid analogue, trifluridine, and a thymidine phosphorylase inhibitor, tipiracil hydrochloride.” NCT04076761 ↗ “TAS-102, an oral agent that combines trifluridine and tipiracil hydrochloride, was effective in the treatment of refractory colorectal cancer.” PMID 25970050 ↗ May 2015 |
| Known as | Tipiracil hydrochloride component of lonsurf | ChEMBL registry synonym — accepted as the source's own label CHEMBL235668 ↗ |
| Known as | Tipiracil hydrochloride component of s-95005 | ChEMBL registry synonym — accepted as the source's own label CHEMBL235668 ↗ |
| Known as | Tipiracil hydrochloride component of tas-102 | ChEMBL registry synonym — accepted as the source's own label CHEMBL235668 ↗ |
| Known as | Tipiracilo | ChEMBL registry synonym — accepted as the source's own label CHEMBL235668 ↗ |
| Known as | TPI | “TAS-102 is a novel combination medicinal product consisting of a thymidine-based nucleoside analogue (trifluridine; FTD) as the active component and the thymidine phosphorylase...” NCT04042714 ↗1“The phase II J003 (N = 169) and phase III RECOURSE (N = 800) trials demonstrated a significant improvement in survival with trifluridine (FTD)/tipiracil (TPI) versus placebo in...” PMID 31912801 ↗ Jan 2020 |
| Known as | TPI (freebase) | ChEMBL registry synonym — accepted as the source's own label CHEMBL235668 ↗ |
| Action | Inhibit | “the thymidine phosphorylase inhibitor tipiracil” PMID 27443414 ↗ Jul 2016 |
| Modality | Small molecule | “Tipiracil is in a class of medications called thymidine phosphorylase inhibitors.” NCT05356897 ↗ |
| Route | Oral | “TAS-102, an oral agent that combines trifluridine and tipiracil hydrochloride” PMID 25970050 ↗ May 2015 |
| Target | TYMP | “tipiracil an inhibitor of thymidine phosphorylase” NCT06039202 ↗ |