Tegafur, an anticancer prodrug, is reported to be bioactivated to 5-fluorouracil (5-FU) by cytochrome P450 (P450) enzymes. Liver microsomal P450 enzymes involved in the biotransformation of tegafur into 5-FU in rats and the effect of tegafur in vivo on P450 levels in rats were investigated. Of 12 cDNA-expressed rat P450 enzymes tested, CYP1A2, CYP3A1, and CYP2C11 had high 5-FU formation rates from 100 microM and 1.0 mM tegafur concentrations. The contributions of CYP1A, CYP2C, and CYP3A enzymes to 5-FU formation in male rat liver microsomes were supported by immunoinhibition studies. 5-FU formation from tegafur, at substrate concentrations of 100 microM and 1.0 mM, was increased by intraperitoneal treatment of tegafur (50 mg/kg for 5 days) as well as by beta-naphthoflavone, phenobarbital, and dexamethasone. Orally administered tegafur (100 mg/kg daily for 20 days) caused the induction of CYP2B (5-fold) and of CYP1A and CYP3A (approximately 2-fold) and of 5-FU formation (approximately 2-fold) in rat liver microsomes. These results suggest that CYP1A and CYP3A enzymes, autoinduced by tegafur, have important roles in 5-FU formation from tegafur in rat liver microsomes. Coadministration of tegafur and P450-inducing drugs could markedly enhance the biotransformation of tegafur into 5-FU via P450 induction.

Rat cytochrome p450 1A and 3A enzymes involved in bioactivation of tegafur to 5-fluorouracil and autoinduced by tegafur in liver microsomes.

Objective: Taxanes and fluoropyrimidines are active in metastatic breast cancer (MBC), and their combination has proven effective in anthracycline-refractory patients. We conducted

Phase I Study of Paclitaxel and Uracil plus Tegafur Combination in Patients with Pretreated Metastatic Breast Cancer: Drug Sequencing Based on Preclinical Modelling Studies

Cancer is the major health problem worldwide, according to WHO in 2018 cancer is responsible for an estimated 9.6 mill death out of 18.1 million new cases and globally 6 deaths occur due to cancer. Cancer is the abnormal, unwanted growth of cells, when abnormal cells divide in an uncontrolled way within the body and destroy normal tissue that can lead to death. Normal body cell grows, divide, and die in an orderly way or cancer cells are different because they do not die, grow continuously, and divide in orderly way. There are more than 200 types of cancer. Any agent that converts a body cell to develop abnormally can cause cancer. The cancer causative agents include- radiations, chemical or toxic compound exposure, lifestyle, hormones, and human genetics. Most tumors can be categorized as one of the three main groups: carcinomas, sarcomas and leukemia or lymphomas. Carcinomas, which associated around 90% of human cancer, are malignancies of epithelial cell. Sarcomas, which are uncommon in human, are solid tumor of connective tissue including muscle, bone, cartilage, and fibrous tissue. Leukemia and lymphomas, which represent around 8% of human malignancies, emerge from the blood forming cell and from cell of immune system. Carcinoma of breast is a malignant disease with variable outcomes. Breast carcinoma is second most common cause of death in females though it can also occur in men but are very uncommon. This type of cancer is malignant cell growth in breast. This study was done to compare and analyze adverse drug reactions of cancer chemotherapy in breast cancer in a rural hospital. Objectives included- a) To study adverse drug reactions of various chemotherapeutic agents used in patients suffering breast cancer b) To compare various side-effects as a result of different combination protocols to identify the drug protocol with least amounts of adverse drug reactions. However, an extremely significant difference was found between all of the comparison groups studied.

A retrospective and prospective study for adverse drug reaction of cancer chemotherapy in breast cancer

BACKGROUND

Chronic oral tegafur (a 5-fluorouracil prodrug) modulated by folinic acid has antitumor activity in patients with metastatic breast carcinoma resistant to 5-fluorouracil or doxorubicin-based regimens. In this study, bolus 5-fluorouracil was substituted with chronic oral tegafur and folinic acid in a cyclophosphamide, methotrexate, and 5-fluorouracil-based regimen to study the activity of this novel regimen in patients with advanced breast carcinoma.



METHODS

This study was comprised of patients with advanced breast carcinoma and measurable or evaluable disease. Patients with prior chemotherapy were eligible. The regimen was comprised of cyclophosphamide, 600 mg/m2, and methotrexate, 40 mg/m2, both given intravenously on Day 1, and tegafur, 750 mg/m2, with folinic acid, 45 mg/day, both given orally in 3 daily fractions on Days 2-14, every 3 weeks.



RESULTS

Forty-seven patients were included, 44 of whom were fully assessable. Three patients (7%) achieved a complete remission and 17 (38.6%) achieved a partial remission, for an objective response rate of 45.5% (95% confidence interval, 29-59%). The median duration of response was 11 months. In previously untreated patients the response rate was 54.5%. In patients previously treated with anthracycline or 5-fluorouracil-based regimens the response rates were 41% and 39%, respectively. Sixteen patients (36.4%) had disease stabilization. The median overall time to progression was 10 months. Toxicities usually were mild and were comprised of leukocytopenia, mucositis, emesis, and diarrhea.



CONCLUSIONS

Chronic oral tegafur and folinic acid combined with intravenous cyclophosphamide and methotrexate at the dose and schedule used in the current study has significant antitumor activity both as first-line chemotherapy as well as in other patients with advanced breast carcinoma who had prior chemotherapy. This regimen is well tolerated, with gastrointestinal toxicity being the most frequent and dose-limiting toxicity. Cancer 1998;82:878-85. © 1998 American Cancer Society.

Cyclophosphamide, methotrexate, and chronic oral tegafur modulated by folinic acid in the treatment of patients with advanced breast carcinoma

Handle everyday research tasks with reliable, citation-backed results

Your personal Research Agent to handle research tasks with citation-backed results

Popular Tasks used by Researchers

How can I help with your research?

Meet SciSpace

Get more enhanced response by uploading the PDFs you want me to reference.

No relevant PDFs in your library

SciSpace is the AI research assistant for academics. Run systematic literature reviews on 280M+ papers, and write papers with cited sources. Trusted by 1M+ students, PhDs & researchers.

SciSpace | AI for Research

Analyze PDFs

Code & Manuscripts

Funding & Grants

Literature & Patents

Medical & Clinical Data

Systematic Review

Visualize & Present

Web & Data

Build a Google Scholar-like website for your research.

Build a website

Create charts and images for your research

Create a Chart

Write a paper for submission to a journal

Draft a manuscript

Patent Search

Design eye-catching scientific posters in minutes.

Scientific Poster Generation

Systematic Literature Review

One task is running at the moment. Your messages will be shown right after.

Drag and drop or click here to browse

Loved by <highlight>1 million+</highlight> researchers

Extract a list of specific topics and their sources from unstructured text

Topics

Compare and analyze relevant papers that matches with your search

Papers

Get insights from PDFs and bookmarked papers from your library

My library

Recent searches

Try searching for:

Catch AI-generated content in scholarly and non-scholarly content

{ai} Detector

Ai Writer

Get PDF Summaries, highlighted text explanations 

Chat with PDF

Effortlessly create in-text citations and bibliographies in APA and 2,500 other formats

Citation generator

Get explanations, summaries, and answers on academic papers

Ease up your research workflow with {scispace}'s cohort of exciting AI tools

Elevate your academic writing skills and convey your ideas the way you want

Paraphraser

Explore our range of reading and writing tools

Your file is being prepared and should be ready in a few minutes. If it's a large file, it might take a bit longer. You can close this window, and we'll email you the file when it's done.

You have reached a maximum limit of <strong>{limit}</strong> columns in the table. Remove at least <strong>1</strong> column to add or create another one.

Rosó Vidal

Author Tools

Chat about Author

Papers

Cyclophosphamide, methotrexate, and chronic oral tegafur modulated by folinic acid in the treatment of patients with advanced breast carcinoma