Drugs / Tipiracil
last change Aug 2026 re-read 8 days ago

Tipiracil

Small molecule targets TYMP via inhibition

Developed for
colorectal cancer · gastric adenocarcinoma · cholangiocarcinoma · colon carcinoma · colorectal adenocarcinoma · colorectal carcinoma · gastroesophageal junction adenocarcinoma · rectum adenocarcinoma
+11 more · carcinoma · colon adenocarcinoma · colorectal neoplasm · gallbladder carcinoma · gastric cancer · gastroesophageal adenocarcinoma · neuroendocrine neoplasm · pancreatic adenocarcinoma · rectal carcinoma · small cell lung carcinoma · gastroesophageal cancer
Investigated by
National Cancer Institute (NCI) · Taiho Oncology, Inc. · Academic and Community Cancer Research United · ADIR, a Servier Group company · Chang Gung Memorial Hospital · M.D. Anderson Cancer Center
+33 more · Servier · Taiho Pharmaceutical Co., Ltd. · AbbVie · Alpha-A, Inc. · Anhui Provincial Cancer Hospital · Baylor Research Institute · Case Comprehensive Cancer Center · Chia Tai Tianqing Pharmaceutical Group Nanjing Shunxin Pharmaceutical Co., Ltd. · China Medical University Hospital · City of Hope Medical Center · Clinical Trial Center North (CTC North GmbH & Co. KG) · Emory University · First Affiliated Hospital of Wenzhou Medical University · Holy Stone Healthcare Co., Ltd · Innovent Biologics (Suzhou) Co. Ltd. · Ipsen · Kaohsiung Medical University Chung-Ho Memorial Hospital · LIN YANG · National Cancer Center Hospital East · National Cheng-Kung University Hospital · National Comprehensive Cancer Network · National Health Research Institutes, Taiwan · OHSU Knight Cancer Institute · Oregon Health and Science University · Pfizer · Roswell Park Cancer Institute · Rutgers, The State University of New Jersey · Servier · Shanghai Zhongshan Hospital · Strategic Alliance · Sunnybrook Health Sciences Centre · Taipei Veterans General Hospital, Taiwan · University Medical Center Hamburg-Eppendorf

Regulatory milestones approvals, filings & regulatory actions · 6 recorded

MilestoneJurisdictionBrandIndicationDateSentence it was read from
Filed colorectal cancer 3 milestones
Filed US (FDA) LONSURF colorectal cancer 2023-04-18

“the U.S. Food and Drug Administration (FDA) has accepted for Priority Review the supplemental new drug application (sNDA) for trifluridine/tipiracil (LONSURF®)” taihooncology.com ↗

Filed Other — colorectal cancer 2017-10-20

“Health Canada accepted for review Taiho’s New Drug Submission (NDS) for trifluridine (FTD) and tipiracil (TPI)” taihooncology.com ↗

Filed US (FDA) — colorectal cancer 2014-12-22

“the New Drug Application (NDA) for TAS-102 (nonproprietary names: trifluridine and tipiracil hydrochloride), has been accepted for review by the U.S. Food and Drug Administration (FDA)” taihooncology.com ↗

Filed gastroesophageal adenocarcinoma 1 milestone
Filed US (FDA) LONSURF gastroesophageal adenocarcinoma 2018-10-25

“the United States Food and Drug Administration (FDA) has accepted and granted priority review for the supplemental New Drug Application (sNDA) for LONSURF®...” taihooncology.com ↗

Approved Indication not stated 2 milestones
Approved EU (EMA) Lonsurf — 2016-04-25 europa.eu ↗
Approved US (FDA) LONSURF — 2015-09-22 fda.gov ↗

Trials 28

PhaseRegistry idDatesIndicationSponsorStatusOutcome
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 Stop: Business
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 Stop: Business
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 Stop: Enrollment
Phase 35 trials · 1 met primary · 1 missed
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 Missed primary
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 Met primary
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 → Dec 2024 colorectal cancer Chang Gung Memorial Hospital Completed No outcome recorded
Comparator or background therapy19 trials
Phase 0 NCT07318389 Background Jun 2026 → Nov 2027 expected colorectal cancer M.D. Anderson Cancer Center Not yet recruiting No outcome recorded
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 1/2 NCT05405595 Background Jun 2022 → Oct 2026 expected — Adagene Inc Recruiting No outcome recorded
Phase 1/2 NCT05438459 Comparator Jun 2022 → Mar 2032 expected gastric cancer, malignant pancreatic neoplasm Kyushu University Recruiting No outcome recorded

News releases announcing trial results or a regulatory action · 24

DateIssuerRelease
2025-10-13 AbbVie Results AbbVie to Present New Data at ESMO 2025 Reinforcing Leadership in Advancing Targeted Therapies for Solid Tumors abbvie.com ↗
Grade ≥3 treatment emergent adverse events (TEAEs) occurred in 67% and 65% of patients, respectively.
2025-01-22 Agenus Inc. Results Agenus Presents Data at ASCO GI Demonstrating Impact of BOT/BAL in Colorectal Cancer Across Neoadjuvant and Advanced Disease agenusbio.com ↗
Standard of care had no responses.
2023-08-02 Taiho Oncology, Inc. Regulatory FDA Approves LONSURF® (trifluridine/tipiracil) in Combination With Bevacizumab for Adult Patients With Metastatic Colorectal Cancer (mCRC) taihooncology.com ↗
2023-05-03 Taiho Oncology, Inc. Results Taiho Oncology and Servier Announce Publication in the New England Journal of Medicine of Pivotal Phase 3 Data for Trifluridine/Tipiracil (LONSURF®) in Combination With Bevacizumab in Patients With Refractory Metastatic Colorectal Cancer taihooncology.com ↗
In addition, the median time to worsening of ECOG (Eastern Cooperative Oncology Group) performance-status score was significantly delayed in patients receiving the investigational combination of trifluridine/tipiracil and bevacizumab.
2023-04-18 Taiho Oncology, Inc. Regulatory U.S. Food and Drug Administration Accepts for Priority Review Taiho Oncology’s Supplemental New Drug Application for the Use of Trifluridine/Tipiracil (LONSURF®) in Combination With Bevacizumab for Refractory Metastatic Colorectal Cancer taihooncology.com ↗
2023-01-17 Taiho Oncology, Inc. Results Servier and Taiho Oncology Present Overall Survival Data for Trifluridine/Tipiracil (LONSURF®) In Combination With Bevacizumab in Patients With Refractory Metastatic Colorectal Cancer at 2023 ASCO Gastrointestinal Cancers Symposium taihooncology.com ↗
This improvement in OS represents a 39% reduction in the risk of death in patients with refractory mCRC.
2022-09-12 Taiho Oncology, Inc. Results Drug Combination Meets Survival Endpoint in Phase III Pivotal Trial Involving Participants With Refractory Metastatic Colorectal Cancer taihooncology.com ↗
Combining trifluridine/tipiracil with bevacizumab demonstrated the potential to extend survival in these patients who have limited therapeutic options.
2020-01-25 Taiho Oncology, Inc. Results Taiho Oncology Presents Data on LONSURF® (trifluridine and tipiracil) and Futibatinib (TAS-120) at ASCO 2020 Gastrointestinal Cancers Symposium (ASCO GI) taihooncology.com ↗
hematologic adverse events with LONSURF in subgroups of patients with mild to moderate renal impairment and mild hepatic impairment were manageable and similar to those in the overall patient population.
2019-10-14 Taiho Oncology, Inc. Results Analysis of Patients with Prior Gastrectomy Treated with LONSURF® (trifluridine and tipiracil) Published in JAMA Oncology taihooncology.com ↗
The safety profile of LONSURF was consistent with studies of the drug in metastatic colorectal cancer (mCRC), and no new safety concerns were reported.
2019-02-25 Taiho Oncology, Inc. Regulatory FDA Approves Taiho Oncology’s LONSURF® (trifluridine/tipiracil) for Adult Patients with Previously Treated Advanced Gastric or Gastroesophageal Junction (GEJ) Adenocarcinoma taihooncology.com ↗
2019-01-17 Taiho Oncology, Inc. Results Taiho Oncology and Servier Present Data on LONSURF® (trifluridine/tipiracil) at ASCO 2019 Gastrointestinal Cancers Symposium (ASCO GI) taihooncology.com ↗
The results confirmed that LONSURF prolonged survival versus placebo regardless of prior gastrectomy.
2018-10-25 Taiho Oncology, Inc. Regulatory FDA Accepts Supplemental New Drug Application for LONSURF® (trifluridine/tipiracil) for the Treatment of Metastatic Gastric/Gastroesophageal Junction (GEJ) Adenocarcinoma; Grants Priority Review taihooncology.com ↗

All press releases naming this drug 33 releases

DateIssuerRelease

Evidence & citations 13 cited values

Every value below carries the sentence it was read from. 50 sources stand behind the page.

FieldValueCited 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 ↗
37

“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 ↗

NCT05927857 ↗

Show 27 more sources

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

NCT03317119 ↗

NCT03992456 ↗

NCT04660760 ↗

NCT04294264 ↗

NCT05130060 ↗

NCT03844620 ↗

NCT03368963 ↗

Show 1 more source

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
1

“Thymidine phosphorylase inhibitor” CHEMBL235668 ↗

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 “Thymidine phosphorylase inhibitor” CHEMBL235668 ↗