更新于：2024-11-01

5 Alpha Fluorouracil Toxicity

5α-氟尿嘧啶毒性

更新于：2024-11-01

基本信息

别名

5 alpha Fluorouracil toxicity、5α-氟尿嘧啶毒性

简介-

关联

项与 5α-氟尿嘧啶毒性相关的药物

Uridine Triacetate

尿苷三乙酸酯

靶点

DPD

作用机制

DPD agonists

在研机构

Wellstat Therapeutics Corp. [+1]

原研机构

Wellstat Therapeutics Corp.

在研适应症

药物中毒 [+2]

非在研适应症

躁郁症 [+2]

最高研发阶段批准上市

首次获批国家/地区

美国

首次获批日期2015-09-04

项与 5α-氟尿嘧啶毒性相关的临床试验

NCT06258525 / Not yet recruiting临床2期IIT

A Phase II, Open-Label Trial of S-Adenosylmethionine (SAMe) in Prevention of Oxaliplatin Associated Liver Injury

This is an open-label, phase II study that may provide evidence that taking S-adenosylmethionine (SAMe) supplementation prevents oxaliplatin, a type of chemotherapy drug, associated liver toxicity in patients with resectable colorectal liver metastases. Resectable means that it is able to removed with surgery. Patients will take two SAMe tablets in the morning and one tablet in the evening for 3-6 months (about 6-8 cycles of chemotherapy) in addition to oxaliplatin based chemotherapy followed by surgical removal of the colorectal liver metastases.

开始日期2024-08-01

申办/合作机构

Cedars-Sinai Medical Center

[+1]

NCT06048458 / RecruitingN/AIIT

Cancer Treatment Related Cardiovascular Toxicity: Comprehensive Myocardial and Vascular Phenotyping

Observational prospective cohort study designed to assess the mechanisms of fluoropyrimidine induced cardiovascular toxicity.

开始日期2022-05-18

申办/合作机构

University College London

NL-OMON55582 / CompletedN/AIIT

Identification of the mechanisms of 5-fluorouracil (5-FU)-induced Gastrointestinal (GI) toxicity in human colon - 5-FU-induced toxicity in GI system

开始日期2019-06-26

申办/合作机构-

100 项与 5α-氟尿嘧啶毒性相关的临床结果

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100 项与 5α-氟尿嘧啶毒性相关的转化医学

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0 项与 5α-氟尿嘧啶毒性相关的专利（医药）

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项与 5α-氟尿嘧啶毒性相关的文献（医药）

2023-08-01·Saudi Pharmaceutical Journal

The protective effects of silymarin nanoemulsion on 5-fluorouracil-induced gastrointestinal toxicity in rats

Article

作者: Safarpour, Samaneh ; Ebrahimpour, Anahita ; Akbar Moghadamnia, Ali ; Safarpour, Soheila ; Shirafkan, Fatemeh ; Kazemi, Sohrab

5-Fluorouracil (5FUra) is the third most popular chemotherapeutic component employed to treat solid tumors. In the present study, we aimed to appraise the silymarin (SM) and silymarin nanoemulsion (SMN) effect on 5FUra-induced gastrointestinal toxicity in adult male rats. A total of 30 male Wistar rats were divided into 6 groups including the control (Crl) group, and groups treated with SMN (5 mg.kg^-1), SM (5 mg.kg^-1), 5FUra + SMN (5 mg.kg^-1), and 5FUra + SM (5 mg.kg^-1) by IP injection for 14 days. And gastrointestinal toxicity was induced by a single intraperitoneal (IP) injection of 5FUra (100 mg.kg^-1) for the last group in the study. Treating rats with SM and SMN diminished elevating malondialdehyde (MDA) levels, and improved total antioxidant capacity (TAC) levels. Also, the intensity of mRNA expression of interleukin-2 (IL-2) and tumor necrosis factor-alpha (TNF-α) caused by 5FUra in the gastrointestinal tissue tract, and macroscopic oral ulcerations decreased, ass well as weight loss was prevented, particularly in the SMN group. Moreover, in the microscopic scope, there were significant improvements in the levels of hyperemia, hyaline, and inflammatory cell infiltration in the tongue, esophagus, and intestinal tissues in the FUra + SMN and FUra + SM groups compared to 5FUra. Hence, treatment with SM and SMN reduced oxidative stress, histopathological degeneration, and gene expression of inflammatory markers in the gastrointestinal tract. According to the results, treatment with SM and SMN markedly decreases the gastrointestinal toxicity caused by 5FUra.

2023-08-01·Inflammopharmacology

Mito-TEMPO mitigates 5-fluorouracil-induced intestinal injury via attenuating mitochondrial oxidative stress, inflammation, and apoptosis: an in vivo study.

Article

作者: Bharati, Sanjay ; Tambe, Prasad Kisan ; Qsee, H S

BACKGROUNDRecent evidences highlight role of mitochondria in the development of 5-fluorouracil (5-FU)-induced intestinal toxicity. Mitochondria-targeted antioxidants are well-known for their protective effects in mitochondrial oxidative stress- mediated diseases. In the present study, we investigated protective effect of Mito-TEMPO in 5-FU-induced intestinal toxicity.METHODSMito-TEMPO (0.1 mg/kg b.w.) was administered intraperitoneally to male BALB/c mice for 7 days, followed by co-administration of 5-FU for next 4 days (intraperitoneal 12 mg/kg b.w.). Protective effect of Mito-TEMPO on intestinal toxicity was assessed in terms of histopathological alterations, modulation in inflammatory markers, apoptotic cell death, expression of 8-OhDG, mitochondrial functional status and oxidative stress.RESULTS5-FU administered animals showed altered intestinal histoarchitecture wherein a shortening and atrophy of the villi was observed. The crypts were disorganized and inflammatory cell infiltration was noted. Mito-TEMPO pre-protected animals demonstrated improved histoarchitecture with normalization of villus height, better organized crypts and reduced inflammatory cell infiltration. The inflammatory markers and myeloperoxidase activity were normalized in mito-TEMPO protected group. A significant reduction in intestinal apoptotic cell death and expression of 8-OhDG was also observed in mito-TEMPO group as compared to 5-FU group. Further, mtROS, mtLPO and mitochondrial antioxidant defense status were improved by mito-TEMPO.CONCLUSIONMito-TEMPO exerted significant protective effect against 5-FU-induced intestinal toxicity. Therefore, it may be used as an adjuvant in 5-FU chemotherapy.

2023-05-01·Journal of Veterinary Emergency and Critical Care

Successful treatment of 5‐fluorouracil toxicosis with hemodialysis

作者: Istvan, Stephanie A ; Buoncompagni, Simona ; Press, Saya A ; Cowgill, Larry D ; Ross, Sheri ; Rizzo, Kaila ; Henry, Jessica S

AbstractObjectiveTo describe the successful treatment of lethal dose 5‐fluorouracil (5‐FU) toxicosis using hemodialysis.Case SummaryA 4‐month‐old intact female Golden Retriever was presented to the emergency department after ingesting 20 g of 5% 5‐FU cream. The puppy developed refractory seizures and became comatose with uncontrolled tonic–clonic convulsions. Because of the low molecular weight and minimal protein binding of 5‐FU, a single hemodialysis treatment was employed for detoxification. The puppy improved clinically posttreatment and was successfully discharged 3 days after admission. Postingestion leukopenia and neutropenia occurred but were responsive to treatment with filgrastim. The puppy is neurologically normal and has no lasting effects 1 year postingestion.New or Unique Information ProvidedTo the authors’ knowledge, this is the first reported case in veterinary medicine of a potentially fatal 5‐FU ingestion that has been treated with intermittent hemodialysis.