The safety and efficacy of trifluridine-tipiracil for metastatic colorectal cancer: A pharmacy perspective

American Journal of Health-system Pharmacy : AJHP : Official Journal of the American Society of Health-System Pharmacists
Betty M ChanHeinz-Josef Lenz

Abstract

The pharmacology, pharmacokinetics, clinical efficacy, safety, dosing, and place in therapy of trifluridine-tipiracil are reviewed. Trifluridine-tipiracil is an oral antineoplastic agent consisting of trifluridine (a trifluorothymidine, a thymidine-based nucleoside analog) and tipiracil (a thymidine phosphorylase inhibitor), at a molar ratio of 1:0.5. Tipiracil blocks the degradation of trifluridine by thymidine phosphorylase, which improves the bioavailability of trifluridine and allows for oral administration. A Phase III study comparing trifluridine-tipiracil versus placebo in metastatic colorectal cancer (mCRC) patients refractory to or intolerant of standard therapy (n = 800) showed a benefit in overall survival (the primary endpoint) and progression-free survival compared with placebo. The most common grade ≥ 3 adverse events in trifluridine-tipiracil groups in Phase II and III trials were neutropenia, anemia, and leukopenia. The recommended dose of trifluridine-tipiracil is 35 mg/m2 twice a day after meals in a 28-day cycle comprising 2 weeks of 5 days of treatment and 2 days of rest (days 1-5 and 8-12 [every] 28 days), followed by 2 weeks of rest. Trifluridine-tipiracil is approved for the treatment of patients with mCR...Continue Reading

References

May 2, 2003·Nature Reviews. Cancer·Daniel B LongleyPatrick G Johnston
Feb 3, 2005·The Lancet Oncology·Rohini SharmaStephen J Clarke
Jun 6, 2008·Investigational New Drugs·Michael J OvermanJames L Abbruzzese
Sep 18, 2008·Cancer Investigation·Michael J OvermanJames L Abbruzzese
Apr 16, 2014·Nature Reviews. Clinical Oncology·Peter M WilsonRobert D Ladner
May 15, 2015·The New England Journal of Medicine·Robert J MayerUNKNOWN RECOURSE Study Group
Sep 16, 2015·Cancer Chemotherapy and Pharmacology·Johanna C BendellManish R Patel
Oct 3, 2015·Cancer Treatment Reviews·Heinz-Josef LenzFotios Loupakis
Dec 1, 2015·Future Oncology·Nataliya Uboha, Howard S Hochster
Jan 21, 2016·Cancer Chemotherapy and Pharmacology·James J LeeJan Hendrik Beumer
May 7, 2016·Cancer Chemotherapy and Pharmacology·Johanna C BendellHendrik-Tobias Arkenau
May 23, 2016·European Journal of Cancer : Official Journal for European Organization for Research and Treatment of Cancer (EORTC) [and] European Association for Cancer Research (EACR)·Hideaki BandoAtsushi Ohtsu
Aug 16, 2016·Clinical Colorectal Cancer·Satoshi HamauchiHiroya Taniguchi
Jan 10, 2018·CA: a Cancer Journal for Clinicians·Rebecca L SiegelAhmedin Jemal

❮ Previous
Next ❯

Citations

Aug 6, 2020·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·William H Gmeiner
Sep 24, 2020·Archives of Medical Research·Krishnaprasad BabyYogendra Nayak
Jun 26, 2021·European Journal of Medicinal Chemistry·Hongfei JiangRenshuai Zhang

❮ Previous
Next ❯

Related Concepts

Related Feeds

Anemia

Anemia develops when your blood lacks enough healthy red blood cells. Anemia of inflammation (AI, also called anemia of chronic disease) is a common, typically normocytic, normochromic anemia that is caused by an underlying inflammatory disease. Here is the latest research on anemia.