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PubMed2005

[Preparation of 5-fluorouracil-peanut agglutinin conjugate and determination of the ratio of drug to conjugate].

5-fluorouracil was combined with peanut agglutinin by a water-soluble carbodiimide to prepare the tumor target conjugate of 5-fluorouracil-peanut agglutinin and the ratio of drug to conjugate was determined by the modified trinitrobenzenesulfonic acid method (TNBS). The ratio of drug to conjugate was 76.33%. The result showed that 5-fluorouracil could link to the peanut agglutinin by EDC/NHS crosslinking with high drug ratio.

Antineoplastic Agents↗
PubMedDate not supplied

Release stability of 5-fluorouracil liposomal concentrates, gels and lyophilized powder.

Possible leakage of 5-fluorouracil from stable plurilamellar vesicles was monitored during storage of the liposomal concentrates, gels and lyophilized powders. Changes in release profile of dibucaine were taken as indicator of instability. Release profiles were obtained using the dialysis technique for a freshly prepared liposomal concentrate, gel or reconstituted lyophilized powder (zero time) and storage for one, two and four weeks in well closed tubes at 4 degrees C for the liposomal concentrate or gel and at 25 degrees C for liposomal lyophilized powder. Aiming at increasing stability of 5-fluorouracil liposomal dispersion, freshly prepared liposomal concentrates were directly incorporated in hydroxypropyl methylcellulose gel. Stability release profiles of liposomal gels and concentrates indicated a significant increase in stability of liposomal formulations. Also, lyophilization increases the shelf life of liposomes by preserving it in a dry form as a lyophilized cake to be reconstituted immediately prior to administration or direct incorporation into a final dosage form. Release and physico-chemical stability studies showed superior potentials of the lyophilized product after reconstitution in comparison to concentrate and gel forms. It could be concluded that lyophilization of liposomes loaded with a water-soluble drug such as 5-fluorouracil could significantly increase the stability of the liposomal vesicles and decrease leakage from it.

Antimetabolites, Antineoplastic↗
PubMed2006

One-week treatment with 0.5% fluorouracil cream prior to cryosurgery in patients with actinic keratoses: a double-blind, vehicle-controlled, long-term study.

Topical fluorouracil is currently approved for the treatment of actinic keratosis (AK) and is often used prior to or following cryosurgery as interval therapy in patients with severe AK lesions. No randomized, controlled studies are available to confirm anecdotal evidence suggesting pretreatment with fluorouracil is beneficial. This prospective, randomized, double-blind, vehicle-controlled study evaluated the effect of pretreatment with 0.5% fluorouracil cream (FC; Carac) or a vehicle cream (VC) once daily for 7 days to the face plus scalp, ears, neck, and/or lips in patients with > or = 5 visible or palpable AKs on the face prior to cryosurgery. Efficacy was determined by evaluating AK reduction and clearance (complete lack of AK lesions in the treatment area) at 4 weeks follow-up. Statistically significant decreases from baseline number of AKs were observed on all treatment areas in both groups. However, the mean number of facial AKs was significantly lower in the FC group at each treatment cycle (p = .011). No serious adverse events were considered related to treatment.

Antimetabolites, Antineoplastic↗
PubMed2006

Bilateral comparison of the efficacy and tolerability of 3% diclofenac sodium gel and 5% 5-fluorouracil cream in the treatment of actinic keratoses of the face and scalp.

Actinic keratoses (AKs) are a common precancerous condition and are said to account for 14% of visits to dermatologists in the US each year. Along with cryotherapy, topical treatments are a mainstay of therapy for these lesions. One of the potential benefits of topical therapy is less pain and irritation as compared to cryotherapy. Additionally, topical therapies have a perceived benefit of treating subclinical lesions along with clinically evident keratoses. We conducted a bilateral comparison study of the efficacy and tolerability of diclofenac 3% gel used for 90 days and 5% fluorouracil cream used for 28 days in thirty patients with AK of the face and scalp. The diclofenac gel and 5-fluorouracil cream each demonstrated substantial efficacy in the number of lesions cleared and the proportion of patients with significant lesion clearing. In most patients, diclofenac induced only mild signs of inflammation compared to 5-fluoruracil, despite a longer treatment period. A greater number of patients expressed significant satisfaction with diclofenac gel compared to the 5-fluorouracil cream.

Anti-Inflammatory Agents, Non-Steroidal↗
PubMed2006

[Clinical study on keloid treatment with intralesional injection of low concentration 5-fluorouracil].

OBJECTIVE: To explore the effect of intralesional injection of low concentration 5-fluorouracil (5-FU) on inhibition of angiogenesis of keloid. METHODS: 35 patients with 51 keloids were treated with intralesional injection of 5-FU (2-5 mg/ml) biweekly. After 3-6 times of injection, the keloids were treated with intralesional injection of corticosteroid. The average period of treatment was 10.29 months. RESULTS: The efficacy of inhibiting keloid angiogenesis by low concentration of 5-fluorouracil was 96.77%. For the patients who were treated over 6 months with both 5-FU and corticosteroid, the total efficacy was 97.14%. Among them, 45.71% of keloids achieved complete remission, 48.57% mostly remission, 2.86% partial remission and 2.86% no remission. CONCLUSION: Inhibition of keloid angiogenesis with intralesional injection of low concentration of 5-fluorouracil along with corticosteroid injection can achieve satisfactory result.

Adrenal Cortex Hormones↗
PubMedDate not supplied

Oxaliplatin combined with 5-fluorouracil and methotrexate in advanced colorectal cancer.

BACKGROUND: A promising regimen including 5-Fluorouracil, methotrexate and oxaliplatin is reported. PATIENTS AND METHODS: Patients with untreated measurable metastatic disease received bolus 5-Fluorouracil (600 mg/m2) on days 2 and 16, modulated by methotrexate (200 mg/m2) 24 h earlier, alternated with 4 weeks of continuous infusion of 5-Fluorouracil (200 mg/m2/daily) plus oxaliplatin (130 mg/m2) on days 29 and 56, followed by 2 weeks of rest. Serum vascular endothelial growth factor (VEGF) was analyzed at baseline and before every cycle. RESULTS: Fifty-eight patients were enrolled. Objective remissions were reported in 45.6% (95% CI=34.3%, 57.3%). The median progression-free survival was 7.8 months and the median overall survival was 19.4 months. No grade 4 toxicity was reported, except for one case of diarrhea. The serum VEGF evaluated in 23 patients showed a decreasing trend during therapy. CONCLUSION: The regimen was active, well tolerated and may be a possible option in patients not suitable for radical surgery.

Adult↗
PubMed2006

[Clinical evaluation of DLF, CLF and DFM regimens based on platinum compound plus 5-fluorouracil for treatment of advanced esophageal carcinoma].

BACKGROUND & OBJECTIVE: Combination chemotherapy with 5-fluorouracil (5-FU) and cisplatin is regarded as the standard regimen for advanced esophageal carcinoma. This study was to evaluate the efficacy and safety of DLF, CLF and DFM regimens, based on platinum compound plus 5-fluorouracil in the treatment of advanced esophageal carcinoma, and to further explore prognostic factors of advanced esophageal carcinoma. METHODS: From October 1999 to December 2004, 98 patients with advanced esophageal carcinoma were enrolled in the study. They were non-randomly assigned to receive a 2-hour infusion of folinic acid 200 mg/m(2), followed by a 5-FU bolus 400 mg/m(2) and 48-hour infusion of 5-FU 3,000 mg/m(2) every 3 weeks, combined with cisplatin 80 mg/m(2) (DLF, n=48) or with carboplatin AUC=5 on day 1 (CLF, n=32), or with cisplatin 80 mg/m(2), 5-fluorouracil bolus 400 mg/m(2) on day 1-5 plus pingyangmycin 5 mg/m(2) on day 1, 3, 5 (DFM, n=18). Survival analysis and prognostic factors were evaluated by Kaplan-Meier method and Cox regression analysis. RESULTS: All 98 patients were assessable for response and toxicity. There were 13 complete response, 36 partial response, 45 no changes and 4 progressive disease with a total response rate of 46.86%. The response rates of DLF, CLF and DFM regimens were 60.42%,46.86% and 27.78%, respectively (DLF vs DFM, P=0.027). The major side effects were nausea-vomiting, alopecia, bone marrow suppression and mucositis, and the others were uncommon. All side effects were tolerable and mild except for nausea-vomiting. Nausea-vomiting was mildest in CLF among the three regimens. After a median follow-up of 9 months, the overall median survival was 9 months (95% CI, 6.67 to 11.33 months), the median survival of the patients treated with DLF, CLF or DFM regimen was 10, 9 and 7 months, respectively (P=0.7402). Better prognosis was correlated with good conditions of patients before chemotherapy (KPS> or =80, P=0.000) and metastasis to lymph node, parenchyma or bone in stead of visceral organs (P=0.026). There was no correlation between the prognosis and age, sex, types of pathology and the regimen of therapy. CONCLUSIONS: The DLF regimen is tolerable and more effective, thus could be recommended as a front-line standard treatment for advanced esophageal carcinoma. The CLF regimen is more suitable for feeble and older patients since it has the mildest side effects. The prognostic factors of advanced esophageal carcinoma include conditions before chemotherapy and the location of metastasis.

Adenocarcinoma↗
PubMed1991

Mechanisms of interaction of interferon and 5-fluorouracil in solid tumors.

Recent clinical trials demonstrate the combined activity of 5-fluorouracil (5-FU) and interferon (IFN) in advanced colon cancer. Several possibilities exist for explaining the interaction. Interferon may alter the pharmacokinetics of 5-FU infusion by increasing the steady state concentration. Interferon enhances the inhibitory effects of 5-FU for tumor cells in culture. This enhancement is blocked by thymidine. Interferon reduces the concentration of thymidylate synthetase, and this may account for the thymidine-reversible interaction. An alternative mechanism invokes the immunomodulatory effects of IFN. Interferon augments the activity of killer cells with possible anti-tumor activity, both in vitro and in vivo. Also, by increasing the expression of human leukocyte class I antigens, IFN reduces the sensitivity of tumor cell lines to cell-mediated killing, an effect termed resistance. 5-Fluorouracil reverses the resistance in a time- and dose-dependent manner. The effect is mediated through inhibition of protein synthesis, since thymidine cannot reverse it. Fluorouridine is more active in reversing resistance than fluorodeoxyuridine. 5-Fluorouracil also reverses the induction of human leukocyte antigens by IFN. Studies in the resistance model suggest that high doses of 5-FU by infusion for several days might be the optimal method for modulation of IFN-induced effects.

Clinical Trials as Topic↗
PubMed1991

Adjuvant treatment of node-positive colon carcinoma with levamisole and 5-fluorouracil.

Levamisole, an anthelminthic drug, has been studied clinically as a nonspecific immunomodulator in the adjuvant treatment of a variety of malignancies. Over a decade ago, a small, non-randomized trial of levamisole versus no further therapy after primary surgical resection of colorectal carcinoma showed a survival benefit for the cohort receiving levamisole, particularly among patients with transmural penetration or positive regional nodes. Since this seminal trial, numerous adjuvant trials of levamisole alone or in combination with 5-fluorouracil have been conducted. Two randomized, placebo-controlled trials failed to show a benefit of levamisole in patients with node-positive colon carcinoma. Three adjuvant trials have shown a therapeutic benefit of levamisole plus 5-fluorouracil compared to observation. Adjuvant therapy with levamisole and 5-fluorouracil reduced the risk of cancer recurrence by 41% and the death rate by 33% in patients with node-positive disease. The results of this trial have defined a new standard of care in the treatment of patients with Stage C colon carcinoma.

Antineoplastic Combined Chemotherapy Protocols↗
PubMed1991

Pharmacology and phase I trial of high-dose oral leucovorin plus 5-fluorouracil in children with refractory cancer: a report from the Children's Cancer Study Group.

Because of the synergy seen in adult trials when 5-fluorouracil is combined with leucovorin, we initiated a Phase I trial of this combination in children's refractory cancer. Leucovorin, an equal mixture of the (6R,S)-diastereoisomers, was administered p.o. for 6 consecutive days as 4 equal doses at 0, 1, 2, and 3 h totaling 500 mg/m2/day. 5-Fluorouracil was given daily on days 2 to 6 as an i.v. bolus immediately following the last dose of leucovorin. The leucovorin dose was held constant while the 5-fluorouracil dose was escalated in cohorts of patients from 300 mg/m2/day to its maximally tolerated dose. Thirty-five patients (19 with acute leukemia and 16 with solid tumors) were evaluable for toxicity. The maximally tolerated dose of FUra was 450 mg/m2/day for 5 treatments for patients with solid tumors and 650 mg/m2/day for 5 treatments for the children with leukemia. The dose-limiting toxicities were myelosuppression and stomatitis. Other side effects included transient, mild elevations of serum transaminases, mild nausea, vomiting, and diarrhea. The pharmacokinetics of high-dose p.o. leucovorin was studied in 23 children. There was considerable interpatient variability in the plasma concentrations of total bioactive folates (TBAF), (6S)-leucovorin, and (6S)-5-methyltetrahydrofolic acid. The maximum plasma concentration (Cmax) of TBAF was 821 +/- 97 (SE) nM, occurring at a median of 8 h; the Cmax of (6S)-leucovorin was 77 +/- 11 nM, occurring at 4 h. The TBAF concentration fell to 146 +/- 42 nM by 24 h. (6S)-5-Methyltetrahydrofolic acid accounted for 90 +/- 7% of the TBAF at the Cmax. The plasma concentration of (6R)-leucovorin, the unnatural isomer, was equal to that of TBAF. Thus, p.o. leucovorin reduced the 5-fold excess of (6R)-leucovorin over TBAF seen after i.v. doses. The relative amounts of the three major plasma species were approximately the same as in adults, even though the Cmax of each compound was lower.

Administration, Oral↗
PubMed1991

The use of 5-fluorouracil in patients following combined trabeculectomy and cataract extraction.

We studied the effect of postoperative administration of subconjunctival 5-fluorouracil in maintaining postoperative filtration following combined trabeculectomy and extracapsular cataract extraction with posterior chamber lens implantation. Three months postoperatively, the mean intraocular pressure in 15 patients who had received 5-fluorouracil was 13.1 +/- 3.2 mm Hg; in 17 control patients, it was 13.0 +/- 3.0 mm Hg (P greater than .05). The mean number of postoperative medicines in the study patients was 0.7; in the control patients, 0.8 (P greater than .05). Bleb appearance and improvement in visual acuity were similar in the two groups. This study does not support the routine use of 5-fluorouracil in patients who have undergone combined trabeculectomy and extracapsular cataract extraction.

Aged↗
PubMed1991

Genital human papillomavirus infection in men. Diagnosis and treatment with a laser and 5-fluorouracil.

One hundred twenty-eight consecutive men, sexual partners (for more than six months) of women treated for genital condylomata acuminata, were evaluated with colposcopy to assess the percentage of infected men among the couples. Ninety-three (73%) of the men were found to have a genital human papillomavirus infection on colposcopically directed biopsies. All but one patient were treated with outpatient colposcopically guided laser vaporization under local anesthesia (one patient with extensive condylomata required general anesthesia). Two weeks after laser surgery, 5% 5-fluorouracil cream, used in the genital area, was initiated on a weekly basis for two months and every other week for two more months. Patients were followed in the clinic with colposcopy performed every eight weeks for six months to evaluate the regimen's results. Thirty-seven (40%) of the 93 men had "clinically" apparent genital HPV infection, and 56 (60%) of the 93 had "subclinical" disease (as determined with colposcopy). The majority of the patients (87 of 93, or 94%) responded to one laser treatment followed by 5-fluorouracil cream and had no visible lesions at six months. Colposcopic evaluation of the male partners of infected women and laser surgery followed by topical 5-fluorouracil therapy appear to be safe and effective in controlling genital HPV infection.

Acetates↗
PubMed1990

[Fluorouracil and high-dose folinic acid in the treatment of advanced colorectal carcinoma].

Forty-five consecutive patients with advanced colorectal cancer were treated with 5-fluorouracil and high dose folinic acid. Among 43 evaluable patients there were 7 objective responses for an overall response rate of 16%. Toxicity was generally mild and rapidly reversible. Compared to those reported with 5-fluorouracil alone, these results failed to demonstrate an increase in response rate in the treatment of advanced colorectal cancer with the combination of 5-fluorouracil and folinic acid.

Adult↗
PubMed1990

[Activities of enzymes converting 5-fluorouracil to 5-fluorouridine-5' monophosphate and 5-fluorodeoxyuridine-5' monophosphate in subcultured cell lines and solid tumor tissues].

The activities of five enzymes, orotate phosphoribosyltransferase (OPRTase), uridine kinase (UR kinase), thymidine kinase (TdR kinase), uridine phosphorylase (UR Prylase) and thymidine phosphorylase (TdR Prylase), were examined in subcultured human acute leukemia cell lines (HL-60, CCRF-CEM), subcultured human solid tumor cell lines (Colo-205, HeLa-S3) and human cancerous tissues with a view to compare the activation of 5-fluorouracil in them. There was no significant difference in the activity of any enzyme between HL-60 and CCRF-CEM, Colo-205 and HeLa-S3, and human lung cancerous tissue and human colon cancerous tissue. Compared between the acute leukemia cell lines and the solid tumor cell lines, the UR kinase activity was high in both cell lines. The OPRTase and UR Prylase activities were low in the solid tumor cell lines. In the cancerous tissues, both the UR kinase and TdR kinase activities were low, but the UR Prylase and TdR Prylase activities were markedly high. The results suggest that the intracellular activation of 5-fluorouracil varies with different human cancerous cells. When the anti-cancer activity of 5-fluorouracil is tested in vitro, the difference of fluoropyrimidine metabolism in subcultured cell lines from that in the cancerous tissue should be taken in account.

Fluorouracil↗
PubMed1990

Glaucoma secondary to epithelial downgrowth and 5-fluorouracil.

Since epithelial downgrowth involves an actively proliferating intraocular tissue, it is possible that the antimetabolite 5-fluorouracil may inhibit it. We report a case of secondary glaucoma caused by epithelial downgrowth in which filtration surgery was performed with adjunctive use of subconjunctival 5-fluorouracil. On cessation of the injections, the retrocorneal membrane grew rapidly to involve the entire posterior cornea. The eye eventually became blind and painful and was enucleated. The use of 5-fluorouracil given in the usual manner appears to have been a failure.

Anterior Chamber↗
PubMed1990

[Metabolic characteristics and antitumor activity of BOF-A2, a new 5-fluorouracil derivative].

A new 5-fluorouracil (5-FU) derivative, BOF-A2 (3-[3-(6-benzoyloxy-3-cyano-2-pyridyloxycarbonyl)benzoyl]-1- ethoxymethyl- 5-fluorouracil), is consisted of EM-FU (1-ethoxymethyl-5-fluorouracil) which is specifically and gradually converted to 5-FU by the drug-metabolizing enzyme of liver microsomes and CNDP (3-cyano-2,6-dihydroxypyridine), a potent inhibitor of 5-FU degradation in the liver. When BOF-A2 was given orally, blood levels of the main metabolites, EM-FU and CNDP, were maintained for a longer time in the tumor-bearing rats, and eventually the blood 5-FU levels were maintained over 12 hours. Moreover, 5-FU levels in the tumor tissue tended to be maintained higher and longer time over 24 hrs. than those in the blood of rats. Antitumor activity of such characterized BOF-A2 was investigated with transplantable tumors in rodents and DMBA-induced breast carcinomas in rats. The ED 50 (the dose for 50% inhibition of tumor growth) value was about 15 to 25 mg/kg against the tumors tested. These result may suggest that BOF-A2 has potent antitumor activity in accordance to the long persistence of 5-FU level in the tumor tissue.

Animals↗
PubMed1990

Treatment of large lower genital tract condylomata acuminata with topical 5-fluorouracil.

Nineteen women with extensive condyloma acuminatum involvement of the lower female genital tract were treated with seven-day courses of topical 5-fluorouracil. The complete response rate was 68.4%. One patient completed only two courses; she underwent vaginal delivery after cryosurgical destruction of the remaining lesions. Her recurrent lesions in the immediate postpartum period were controlled with additional courses of topical 5-fluorouracil. Only one patient was totally unresponsive to treatment with topical 5-fluorouracil.

Administration, Topical↗
PubMed1985

[Intratumoral administration of 5-fluorouracil and bleomycin in inoperable cancer of the cardioesophageal region].

The methods and results of combined therapy (drugs+radiation+intratumoral injection of 5-fluorouracil and (chemoimmunotherapy+intratumoral injection of bleomycin) were compared with the standard procedure (chemotherapy+radiation) for treating inoperable cancer in the cardioesophageal region. The study group included 47 patients aged 32-79. Tumors were inoperable due to considerable expansion in 32 and remote metastases in 15 patients. The single dose of 5-fluorouracil injected into tumor via a fibroendoscope at the start of chemoradiation treatment ranged 750-1,000 mg (course dose of the drug-2.75-4.25 g, total focal dose of radiation -24-36 Gy). The single intratumoral dose of bleomycin injected prior to total polychemotherapy (vinblastine, ftorafur, cyclophosphamide) was 10-15 mg. In the control group receiving standard combined therapy, the total focal dose was 60-62 Gy and course dose of 5-fluorouracil -5-7 g. Objective improvement was observed in 63.6% matched by a mean survival time of 14.6 months after combined therapy given in conjunction with supporting chemoimmunotherapy. This showed an improvement on the results of standard combination therapy which were 58.3% and 9.3 months, respectively.

Adult↗