Drugs / Raltitrexed
last change Jul 2026 re-read 2 minutes ago

Raltitrexed

Small molecule targets TYMS via inhibition

Developed for
colorectal cancer · hepatocellular carcinoma · gastric cancer · rectal cancer · metastasis from malignant tumor of colon · cancer of unknown primary site · colon carcinoma · colorectal carcinoma
+19 more · head and neck squamous cell carcinoma · malignant mesothelioma · rectal carcinoma · bile duct adenoma · childhood acute lymphoblastic leukemia · childhood acute myeloid leukemia · colorectal neoplasm · esophageal cancer · esophageal squamous cell carcinoma · gastroesophageal junction adenocarcinoma · intrahepatic cholangiocarcinoma · malignant colon neoplasm · malignant pancreatic neoplasm · nasopharyngeal carcinoma · neoplasm · peritoneal carcinomatosis · colon adenocarcinoma · metastatic neoplasm · rectum adenocarcinoma
Investigated by
Fudan University · National Cancer Institute (NCI) · Jiangsu Cancer Institute & Hospital · Second Affiliated Hospital, School of Medicine, Zhejiang University · The First Affiliated Hospital of Dalian Medical University · AstraZeneca
+62 more · China Medical University, China · Chinese Academy of Medical Sciences · European Organisation for Research and Treatment of Cancer - EORTC · Gang Wu · Pfizer · The Second Affiliated Hospital of Dalian Medical University · Abramson Cancer Center at Penn Medicine · Affiliated Hospital of Jiangnan University · Anshan Tumor Hospital · BeiGene · Beijing Xisike Clinical Oncology Research Foundation · Benxi Cental Hospital · Centre Georges Francois Leclerc · Centre Hospitalier Universitaire de Besancon · Changzhou Cancer Hospital of Soochow University · Chinese PLA General Hospital · Donghai People's Hospital · First Affiliated Hospital of Wenzhou Medical University · First Affiliated Hospital of Zhejiang University · Fox Chase Cancer Center · General Hospital of Shenyang Military Region · Guangzhou Development District Hospital · Hebei Tumor Hospital · Henan Cancer Hospital · Huai'an First People's Hospital · Hubei Cancer Hospital · IRCCS Azienda Ospedaliero-Universitaria di Bologna · Institut du Cancer de Montpellier - Val d'Aurelle · Jinhua Central Hospital · Liaoning Cancer Hospital & Institute · Medical Research Council · Memorial Sloan Kettering Cancer Center · Meng Qiu · Nanfang Hospital, Southern Medical University · Nanjing BenQ Hospital · Nanjing Chia-tai Tianqing Pharmaceutical · National Cancer Institute, France · Northern Jiangsu People's Hospital · Peking University Cancer Hospital & Institute · People's Hospital of Ganyu · Qilu Hospital of Shandong University · RenJi Hospital · Second Affiliated Hospital of Guangzhou Medical University · Second Affiliated Hospital of Wenzhou Medical University · Shanxi Province Cancer Hospital · Shaoxing People's Hospital · Shengjing Hospital · Shenzhen People's Hospital · The Affiliated Shunde Hospital of Jinan University · The East Hospital of Lianyungang · The First Affiliated Hospital of Nanchang University · The First Affiliated Hospital with Nanjing Medical University · The First People's Hospital of Lianyungang · The People's Hospital of Liaoning Province · The Second Hospital of Nanjing Medical University · The Third Affiliated Hospital of Wenzhou Medical University · Zhejiang Cancer Hospital · Zhejiang University · Zhongnan Hospital · Zhongshan People's Hospital, Guangdong, China · Zhu Xu · Zhujiang Hospital

Trials 62 · started per year

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PhaseRegistry idDatesIndicationSponsorStatusOutcome
Phase 01 trial
Phase 0 NCT05007587 Jul 2021 → Jun 2022 hepatocellular carcinoma Zhejiang Cancer Hospital Unknown No outcome recorded
Phase 17 trials
Phase 1 NCT07349043 Jan 2026 → Oct 2027 expected colorectal cancer, peritoneal carcinomatosis Second Affiliated Hospital, School of Medicine, Zhejiang University Recruiting No outcome recorded
Phase 1 NCT04761185 Sep 2020 → Dec 2024 colorectal cancer Fudan University Completed No outcome recorded
Phase 1 NCT00003528 Sep 1998 → Jun 2002 childhood acute lymphoblastic leukemia, childhood acute myeloid leukemia National Cancer Institute (NCI) Completed No outcome recorded
Phase 1 NCT00003109 Dec 1997 → Oct 2000 cancer of unknown primary site Fox Chase Cancer Center Completed No outcome recorded
Phase 1 NCT00002902 Apr 1997 → ? cancer of unknown primary site Abramson Cancer Center at Penn Medicine Completed No outcome recorded
Phase 1 NCT00002828 Apr 1995 → Nov 2001 colorectal cancer Memorial Sloan Kettering Cancer Center Completed No outcome recorded
Phase 1 NCT00001341 Sep 1993 → Jun 2001 neoplasm National Cancer Institute (NCI) Completed No outcome recorded
Phase 1/21 trial
Phase 1/2 NCT05426811 Jul 2022 → Jul 2025 colorectal neoplasm China Medical University, China Unknown No outcome recorded
Phase 242 trials
Phase 2 NCT07327788 Dec 2025 → Dec 2027 expected hepatocellular carcinoma, portal vein thrombosis Nanfang Hospital, Southern Medical University Recruiting No outcome recorded
Phase 2 NCT06812039 Jan 2025 → Dec 2026 expected hepatocellular carcinoma Fudan University Recruiting No outcome recorded
Phase 2 NCT06665087 Nov 2024 → Nov 2027 expected colon carcinoma, rectal cancer Fudan University Not yet recruiting No outcome recorded
Phase 2 NCT06652412 Nov 2024 → Nov 2027 expected colon carcinoma, rectal carcinoma Fudan University Not yet recruiting No outcome recorded
Phase 2 NCT06475287 Jul 2024 → Jul 2025 overdue hepatocellular carcinoma Fudan University Not yet recruiting No outcome recorded
Phase 2 NCT06441019 Jul 2024 → May 2025 hepatocellular carcinoma Fudan University Unknown No outcome recorded
Phase 2 NCT06397235 May 2024 → Apr 2027 expected hepatocellular carcinoma Second Affiliated Hospital of Guangzhou Medical University Recruiting No outcome recorded
Phase 2 NCT06423937 May 2024 → Jul 2026 overdue colorectal cancer Fudan University Not yet recruiting No outcome recorded
Phase 2 NCT06427005 Feb 2023 → Aug 2025 Meng Qiu Unknown No outcome recorded
Phase 2 NCT05628038 Nov 2022 → Dec 2024 overdue rectal carcinoma Fudan University Recruiting No outcome recorded
Phase 2/31 trial
Phase 2/3 NCT00234429 Nov 2003 → Jun 2006 colorectal cancer AstraZeneca Completed No outcome recorded
Phase 35 trials
Phase 3 NCT05766605 Jan 2023 → Jan 2026 hepatocellular carcinoma Zhujiang Hospital Unknown No outcome recorded
Phase 3 NCT02453490 Oct 2015 → Sep 2018 metastasis from malignant tumor of colon Zhejiang University Terminated No outcome recorded
Phase 3 NCT02485548 Jun 2015 → Jun 2018 head and neck squamous cell carcinoma Jiangsu Cancer Institute & Hospital Unknown No outcome recorded
Phase 3 NCT00004920 Nov 1999 → Jan 2003 malignant mesothelioma European Organisation for Research and Treatment of Cancer - EORTC Completed No outcome recorded
Phase 3 NCT00002893 Jun 1995 → ? colorectal cancer Medical Research Council Unknown No outcome recorded
Phase 44 trials
Phase 4 NCT06118762 Oct 2023 → Oct 2026 expected colorectal cancer The First Affiliated Hospital of Nanchang University Recruiting No outcome recorded
Phase 4 NCT03196843 Sep 2017 → Aug 2020 head and neck squamous cell carcinoma The First Affiliated Hospital of Dalian Medical University Unknown No outcome recorded
Phase 4 NCT02557490 Jan 2015 → Dec 2016 metastasis from malignant tumor of colon Zhu Xu Unknown No outcome recorded
Phase 4 NCT01959061 Sep 2013 → Dec 2017 colorectal cancer Nanjing Chia-tai Tianqing Pharmaceutical Unknown No outcome recorded
Phase not applicable1 trial
NCT06519578 Aug 2024 → Jul 2026 overdue hepatocellular carcinoma RenJi Hospital Recruiting No outcome recorded
Also used as a comparator or background therapy in 7 trials
PhaseRegistry idDatesIndicationSponsorStatusOutcome
Phase 25 trials
Phase 2 NCT06525428 Background Apr 2024 → Dec 2026 expected colorectal cancer Fudan University Recruiting No outcome recorded
Phase 2 NCT06841159 Background Mar 2024 → Mar 2026 overdue colorectal cancer Fudan University Recruiting No outcome recorded
Phase 2 NCT03823079 Background Feb → Sep 2019 colorectal carcinoma, thrombocytopenia Fudan University Unknown No outcome recorded
Phase 2 NCT01703910 Comparator Nov 2012 colon adenocarcinoma, metastatic neoplasm, rectum adenocarcinoma Spanish National Cancer Research Centre Completed No outcome recorded
Phase 2 NCT01481545 Background Dec 2006 → Jul 2011 rectal cancer National Cancer Institute, Naples Completed No outcome recorded
Phase 31 trial
Phase 3 NCT05701436 Background Sep 2022 → Jan 2026 liver cancer Zhujiang Hospital Unknown No outcome recorded
Phase not applicable1 trial
NCT02678806 Comparator Nov 2017 → Nov 2018 hepatocellular carcinoma Guangxi Medical University Unknown No outcome recorded

Evidence & citations 9 cited values

Every value below carries the sentence it was read from. 71 sources stand behind the page.

FieldValueCited text
Known as raltitrexed “Second-line standard systemic therapies in cohort B include: FOLFOX/XELOX+ bevacizumab, FOLFOX/XELOX+cetuximab (KRAS/NRAS/BRAF WT),...” NCT06841159
66

“transarterial chemoembolization (TACE) plus Hepatic Arterial Infusion Chemotherapy (HAIC) with oxaliplatin and raltitrexed for Barcelona stage C hepatocellular carcinoma (HCC)” NCT04597970

“The ROX regimen was administered via hepatic artery: oxaliplatin , 100mg/m2 , from hour 0 to 4 on day1 ;raltitrexed , 3mg/m2 , from hour 4 to 5 on day 1.” NCT05007587

“RALOX-based regimen for hepatic arterial infusion chemotherapy: oxaliplatin, 85 mg/m2 infusion for 2 hours; Raltitrexed, 3 mg/m2 infusion for 0.5 hour.” NCT06397235

“Arterial infusion chemotherapy (THP + oxaliplatin + raltitrexed) and THP combined with lipiodol embolization for 2 times, with an interval of 1 month.” NCT05361161

Raltitrexed contained regimen: Raltitrexed 3mg/m2 on day 1; ± Bevacizumab 7.5mg/kg, repeating every 3 weeks; Raltitrexed 2mg/m2 on day 1” NCT03485027

“The chemotherapy regimen consists of oxaliplatin 85 mg/m² over 2 hours and raltitrexed 2 mg/m² over 1 hour.” NCT06812039

“TOMOX(Raltitrexed 2 mg/m2, Oxaliplatin 85mg/m2)/ TOMIRI(Raltitrexed 2 mg/m2 ,Irinotecan 120mg/m2)” NCT06423937

“Then, 50 mg of lobaplatin plus 4 mg of raltitrexed was injected into the vascular artery.” NCT02678806

“Oxaliplatin 85 mg/m² over 2 to 4 hours, and Raltitrexed 3 mg/m² over 1 to 2 hours” NCT07327788

“Oxaliplatin(85 mg/m2); Raltitrexed (3 mg/m2) ,continuous infusion for 3 hours.” NCT06239532

“Transarterial infusion chemotherapy: Oxaliplatin(85mg/m\^2)+Raltitrexed(3mg)” NCT05340231

Raltitrexed: 3 mg/m2 intravenously, on the first day of each cycle” NCT06118762

Raltitrexed is a potent thymidylate synthase (TS) inhibitor.” NCT02821559

“15 min intravenous infusion Raltitrexed (Tomudex ®) 3 mg/m2” NCT02723253

“FOLFIRI/irinotecan+raltitrexed/irinotecan/+bevacizumab” NCT06525428

Raltitrexed 3 mg/m\^2” NCT06519578

RaltitrexedNCT01703910

NCT00004254

NCT03083613

NCT01836120

NCT00002828

NCT03196843

NCT05148143

NCT05160896

NCT03392103

NCT04581876

NCT03053167

NCT03813641

NCT00002893

NCT02618356

NCT01732380

NCT00003528

NCT01532804

NCT06475287

NCT03823079

NCT04582981

NCT00002902

NCT02557490

NCT06427005

NCT04761185

NCT03126071

NCT05435313

NCT02485548

NCT06665087

NCT02562599

NCT05766605

NCT02072317

NCT07349043

NCT05701436

NCT03585530

NCT00004920

NCT00003109

NCT01481545

NCT01959061

NCT06652412

NCT00234429

NCT03344614

NCT01348412

NCT02376452

NCT02992886

NCT06441019

NCT04499586

NCT05628038

NCT04241731

NCT05426811

NCT02453490

Known as raltitrexed for injection “Drug: raltitrexed for injectionNCT04581876
Known as Tomudex “We investigated the activity and toxicity of raltitrexed (Tomudex) as a single agent treatment in patients with Malignant Pleural Mesothelioma (MPM) in a multicentre phase II...” PMID 12565988 Feb 2003
3

“15 min intravenous infusion Raltitrexed (Tomudex ®) 3 mg/m2” NCT02723253

“ZD1694 (TOMUDEX)” NCT00001341

NCT00590278

Known as ZD-16 ChEMBL registry synonym — accepted as the source's own label CHEMBL225071
Known as ZD1694 ClinicalTrials.gov intervention name — accepted as the source's own label NCT00001341
Action Inhibit “Thymidylate synthase inhibitor” CHEMBL225071
1

“directly inhibits TS” NCT00001341

Modality Small molecule “new quinazolone folate analog” NCT00001341
Route Intravenous “administered as a 15 minute IV infusion” NCT00001341
Target TYMS “Thymidylate synthase inhibitor” CHEMBL225071