生物活性

• 描述Trifluridine is a nucleoside metabolic inhibitor used to treat keratoconjunctivitis and epithelial keratitis caused by simplex virus, and as a part of chemotherapy for certain types of metastatic gastrointestinal cancers^[3]. Phase III trial of trifluridine showed significant improvement of overall survival and progression-free survival in refractory gastric cancer and gastroesophageal junction cancer^[4].
• 临床研究

• NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
  NCT02943733	Neuroendocrine Tumors ... more >> Neoplasms Cancer Tumors Collapse <<	Phase 1	Recruiting	August 2020	United States, Wisconsin ... more >> University of Wisconsin Carbone Cancer Center Recruiting Madison, Wisconsin, United States, 53792 Contact: Cancer Connect    800-622-8922    cancerconnect@uwcarbone.wisc.edu    Principal Investigator: Nataliya Uboha Collapse <<
  NCT01916447	Advanced Gastrointestinal Tumo... more >>rs Collapse <<	Phase 1	Completed	-	United States, California ... more >> Los Angeles Clinical Site Los Angeles, California, United States, 90095 United States, Illinois Chicago Clinical Site Chicago, Illinois, United States, 60611 United States, New York Memorial Sloan-Kettering Cancer Center New York, New York, United States, 10065 United States, Tennessee Vanderbilt Ingram Cancer Center Nashville, Tennessee, United States, 37212 Collapse <<
  NCT01904253	Small Cell Lung Cancer (SCLC)	Phase 2	Terminated(The preliminary dat... more >>a does not suggest any safety signal, but an ad hoc interim analysis showed an imbalance of PFS between the two arms) Collapse <<	-	Germany ... more >> Klinikum Mannheim GmbH Universitaetsklinikum Mannheim, Baden-Württemberg, Germany Lungenklinik Heckeshorn- HELIOS Kliniken GmbH Berlin, Germany LungenClinic Grosshansdorf Grosshansdorf, Germany Klinikum Koeln-Merheim Koplin, Germany St. Hildegardis-Krankenhaus- Katholisches Klinikum Mainz Mainz, Germany LMU-Campus Innenstadt Muenchen, Germany Italy Azienda Ospedaliero-Universitaria S. Luigi Gonzaga Orbassano, Turin, Italy IRCCS Centro di Riferimento Oncologico di Aviano, Divisione Oncologia Medica A Aviano, Italy Istituto Tumori Giovanni Paolo II IRCCS Ospedale Oncologico Bari Bari, Italy Azienda Ospedaliera Univ. Policlinico Gaspare Rodolico Catania, Italy Azienda Ospedaliera Instituti Ospitalieri di Cremona Cremona, Italy Azienda Ospedaliera Universitaria Careggi Firenze, Italy IEO Istituto Europeo di Oncologia Milano, Italy Azienda Ospedaliera San Gerardo U.O Oncologia Medica Monza, Italy Arcispedale S. Maria Nuova Azienda Ospedaliera di Reggio Emilia Reggio Emilia, Italy A.O.V.V. Ospedale Eugenio Morelli-Sondalo Sondalo, Italy Japan National Cancer Center Hospital East Chiba, Japan, 277-8577 National Kyushi Cancer Center Fukuoka, Japan, 811-1395 Hyogo Cancer Center Hyogo, Japan, 673-8588 Saitama Cancer Center Saitama, Japan, 362-0806 Shizuoka Cancer Center Shizuoka, Japan, 411-8777 Nippon Medical School Hospital Tokyo, Japan, 113-8603 Cancer Institute Hospital of Japanese Foundation for Cancer Research Tokyo, Japan, 135-8550 Collapse <<

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• 参考文献

• [1] Sakamoto K, Yokogawa T, et al. Crucial roles of thymidine kinase 1 and deoxyUTPase in incorporating the antineoplastic nucleosides trifluridine and 2'-deoxy-5-fluorouridine into DNA. Int J Oncol. 2015;46(6):2327-34.

  [2] Germano A, Rapa I, et al. Cytotoxic activity of gemcitabine, alone or in combination with mitotane, in adrenocortical carcinoma cell lines. Mol Cell Endocrinol. 2014 Jan 25;382(1):1-7.

  [3] Carmine AA, Brogden RN, Heel RC, Speight TM, Avery GS. Trifluridine: a review of its antiviral activity and therapeutic use in the topical treatment of viral eye infections. Drugs. 1982;23(5):329-353.

  [4] Fostea RM, Arkenau HT. Trifluridine/tipiracil in the treatment of gastric cancer. Future Oncol. 2022;18(12):1511-1517.