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Antimicrobials during Pregnancy
Published in “Bert” Bertis Britt Little, Drugs and Pregnancy, 2022
Trifluridine is used to treat ophthalmic herpes infections. It is an FDA category C drug. The manufacturer reports that it was not teratogenic in rats or rabbits at doses up to 23 times the usual human dose. Systemic absorption of the drug through the eye is reported to be negligible.
Trifluridine
Published in Anton C. de Groot, Monographs in Contact Allergy, 2021
Trifluridine is a fluorinated pyrimidine nucleoside with antiviral activity against Herpes simplex virus type 1 and 2 and vacciniavirus and with potential antineoplastic activity. In anticancer therapy, trifluridine is incorporated into DNA and inhibits thymidylate synthase, resulting in inhibition of DNA synthesis, inhibition of protein synthesis, and apoptosis. Trifluridine in ophthalmic solutions is indicated for the treatment of primary keratoconjunctivitis and recurrent epithelial keratitis due to Herpes simplex virus types 1 and 2. Oral trifluridine, in combination with tipiracil, is indicated for the treatment of metastatic colorectal cancer (1).
Acute and Recurrent Genital Herpes Simplex Virus Infection
Published in Marie Studahl, Paola Cinque, Tomas Bergström, Herpes Simplex Viruses, 2017
In the event of further deterioration, or where an aciclovir-resistant virus is demonstrated, the following treatment options are recommended. Topical trifluridine every 8 hours until complete healing can be used for accessible lesions.IV foscarnet 50 mg/kg twice daily until complete healing is used for inaccessible or systemic lesions.
The discovery of novel antivirals for the treatment of mpox: is drug repurposing the answer?
Published in Expert Opinion on Drug Discovery, 2023
Ahmed A. Ezat, Jameel M. Abduljalil, Ahmed M. Elghareib, Ahmed Samir, Abdo A. Elfiky
For more than a half-century, a group of deoxyuridines analogs has been known for their antiviral potential against DNA viruses. 5-substituted 2´-deoxyuridine analogs are the most important among these analogs. Three 5-substituted 2́-deoxyuridine derivatives (idoxuridine, trifluridine, and brivudine) have been approved as antiviral drugs that inhibit viral DNA biosynthesis [43]. These drugs required a phosphorylation reaction before exerting their inhibitory effect. Both idoxuridine and trifluridine are activated by cellular kinases to the 5́-triphosphate or the 5́-monophosphate forms, respectively, while Brivudine is phosphorylated to mono- or diphosphate forms by viral thymidine kinase. Idoxuridine and trifluridine are approved for keratitis caused by herpes simplex virus as topical medications.
Evolving therapies in advanced oesophago-gastric cancers and the increasing role of immunotherapy
Published in Expert Review of Anticancer Therapy, 2021
Hossameldin Attia, Elizabeth Smyth
A third treatment that has recently become available for patients with chemo-refractory gastric cancer is trifluridine/tipiracil [72,73]. The approval of trifluridine/tipiracil was based on the results from the global, randomized, placebo-controlled, phase 3 TAGS study [85]. The trial enrolled 507 patients across 17 countries (14% were from Japan). After a median follow-up of 10.7 months, trifluridine/tipiracil met the primary endpoint to improve OS (5.7 months vs 3.6 months for placebo, p = 0.0003). It has marginally improved median PFS when compared to placebo (median PFS was 2.0 months versus 1.8 months, HR 0.57; p < 0.0001). TRAEs were seen in 81% of the patients treated with trifluridine/tipiracil (n = 335) vs 57% of the patients on placebo (n = 168). The most frequent nonhematological adverse events reported were nausea, decreased appetite, fatigue, vomiting, and diarrhea. Grade 3 or 4 neutropenia occurred in 34% of patients receiving trifluridine/tipiracil and in none in the placebo group however rates of febrile neutropenia were low (2%). A prespecified analysis demonstrated the following factors to be prognostic in terms of improved OS in the TAGS study (all p < 0.05): ECOG performance status 0 versus 1, age <65 versus ⩾65 years, number of prior regimens 2 versus ⩾3, number of metastatic sites 1 or 2 versus ⩾3 and HER-2 status negative vs positive or not done. After adjusting for these factors, the treatment effect for trifluridine/tipiracil was maintained with an HR of 0.69.
The safety of trifluridine and tipiracil for the treatment of metastatic colorectal cancer
Published in Expert Opinion on Drug Safety, 2018
Julia Martinez-Perez, M. Carmen Riesco-Martinez, Rocio Garcia-Carbonero
Pharmacokinetic–pharmacodynamic analyses were explored by comparing safety and efficacy of TAS102 in patients with a high trifluridine exposure (FTD AUC > median) and in patients with a low trifluridine exposure (AUC ≤ median). OS appeared more favorable in the high AUC group compared to the low AUC group (median OS of 9.3 vs. 8.1 months, respectively). All AUC groups performed better than placebo throughout the follow-up period. The incidence of Grade ≥3 neutropenia was higher in patients with higher trifluridine exposure (47.8% vs. 30.4% in the high- vs. low-trifluridine AUC groups, respectively).