Huagongshe화공사 화학 정보 인쇄 보고서 · 연구 참고용
플루시토신
플루시토신 · 플루시토신(FLUCYTOSINE) · FLUCYTOSINE · 5-FLUOROCYTOSINE · 5-FC · ancobon · fluorocytosine · 4-amino-5-fluoropyrimidin-2(1H)-one
식별자 및 물리적 특성
| CAS No. | 2022-85-7 |
|---|---|
| 분자식 | C4H4FN3O |
| 평균 분자량 | 129.09 g/mol |
| 단동위원소 질량 | 129.03383997 g/mol |
| SMILES | Nc1[nH]c(=O)ncc1F |
| InChIKey | XRECTZIEBJDKEO-UHFFFAOYSA-N |
| PubChem CID | 3366 |
| ChEMBL | CHEMBL1463 |
| ChEBI | CHEBI:5100 |
| EC No. | 217-968-7 |
| DTXSID | DTXSID3023059 |
| 현지명 | 플루시토신 |
화학 및 물리적 성질
| XLogP | -0.9 |
|---|---|
| 극성 표면적 | 67.5 |
| 수소 결합 공여자 수 | 2 |
| 수소 결합 수용자 수 | 3 |
| 회전 가능 결합 수 | 0 |
| 무거운 원자 수 | 9 |
| 형식 전하 | 0 |
| 복잡도 | 208 |
| 의약품 | PharmaceuticalsPharmaceuticals -> Listed in ZINC15Pharmaceuticals -> Metabolite of Capecitabine, EmtricitabinePharmaceuticals -> AntibioticsPharmaceuticals -> Anti infectives for systemic use -> Antibacterials for systemic use |
| LogP(분배 계수) | -1.1 |
| 냄새 | Odorless |
| Color/Form | White crystalline solid |
| 용해도 | In water, 1.5 g/100 mL at 25 °CSlightly soluble in alcoholpractically insoluble in chloroform, ether1 g in about 12 mL 0.1 N HCL1.92e+00 g/L>19.4 [ug/mL] (The mean of the results at pH 7.4)물에 조금 녹고, 에탄올에 약간 녹습니다(96%). |
| Human Drugs | FDA approved drugs -> Active ingredientAntifungal medicines |
| Decomposition | When heated to decomposition it emits very toxic fumes of /floride ions and nitrogen oxides/. |
| 녹는점 | 295-297 °C (dec)296 °C298-300 °C (dec.) (lit.) |
| Physical Description | Solid |
| Stability/Shelf Life | Stable under recommended storage conditions. |
| Dissociation Constants | 3.26pKa1 = 3.26pKa2 = 10.71 |
| Collision Cross Section | 118.4 Ų [M+H]+ [CCS Type: TWMethod: calibrated with polyalanine and drug standards] |
| 밀도 | 1.3990 (estimate) |
| 증기압 | 0Pa at 25℃ |
| 저장 조건 | 2-8°C |
| 물리적 상태 | 결정성 분말 |
| pKa(산도 계수) | 3.26(at 25℃) |
| 색상 | 흰색에서 거의 흰색 |
| 용해도 | 1.5g/100mL(25℃) |
| Merck | 14,4125 |
| BRN | 127285 |
| BCS Class | 1 |
| 안정성 | 감광성 |
| InChI | 1S/C4H4FN3O/c5-2-1-7-4(9)8-3(2)6/h1H,(H3,6,7,8,9) |
| InChIKey | XRECTZIEBJDKEO-UHFFFAOYSA-N |
| SMILES | NC1=NC(=O)NC=C1F |
| LogP(분배 계수) | -1.36 at 22.1℃ and pH6.4-6.9 |
화학적 성질
White Crystalline Solid
안전 및 규제
| GHS 분류 | This chemical does not meet GHS hazard criteria for 5.9% (4 of 68) of reports.WarningH361 (83.8%): Suspected of damaging fertility or the unborn child [Warning Reproductive toxicity]P203, P280, P318, P405, and P501 (click each P-code to see the statement)Aggregated GHS information provided per 68 reports by companies from 12 notifications to the ECHA C&L Inventory. |
|---|---|
| 규제 정보 | Status: Active Update: 08-04-2022 https://echa.europa.eu/registration-dossier/-/registered-dossier/19073 |
| FDA 요건 | The Approved Drug Products with Therapeutic Equivalence Evaluations identifies currently marketed prescription drug products, including flucytosine, approved on the basis of safety and effectiveness by FDA under sections 505 of the Federal Food, Drug, and Cosmetic Act. |
| Toxic Combustion Products | Special hazards arising from the substance or mixture: Carbon oxides, nitrogen oxides (NOx), Hydrogen fluoride. |
| Hazard Classes and Categories | Repr. 2 (83.8%) |
| Hazardous Reactivities and Incompatibilities | Incompatible materials: Strong oxidizing agents. |
| 소화 절차 | Suitable extinguishing media: Use water spray, alcohol-resistant foam, dry chemical or carbon dioxide.Advice for firefighters: Wear self contained breathing apparatus for fire fighting if necessary. |
| 보관 조건 | Keep container tightly closed in a dry and well-ventilated place. Light sensitive. Keep in a dry place.Store at 25 °C (77 °F)excursions permitted between 15 deg - 30 °C (59 deg - 86 °F). |
| 정리 방법 | ACCIDENTAL RELEASE MEASURES: Personal precautions, protective equipment and emergency procedures: Use personal protective equipment. Avoid dust formation. Avoid breathing vapors, mist or gas. Ensure adequate ventilation. Evacuate personnel to safe areas. Avoid breathing dust. Environmental precautions: Prevent further leakage or spillage if safe to do so. Do not let product enter drains. Methods and materials for containment and cleaning up: Pick up and arrange disposal without creating dust. Sweep up and shovel. Keep in suitable, closed containers for disposal. |
| 처리 방법 | SRP: Expired or waste pharmaceuticals shall carefully take into consideration applicable DEA, EPA, and FDA regulations. It is not appropriate to dispose by flushing the pharmaceutical down the toilet or discarding to trash. If possible return the pharmaceutical to the manufacturer for proper disposal being careful to properly label and securely package the material. Alternatively, the waste pharmaceutical shall be labeled, securely packaged and transported by a state licensed medical waste contractor to dispose by burial in a licensed hazardous or toxic waste landfill or incinerator.Product: Offer surplus and non-recyclable solutions to a licensed disposal company. Contact a licensed professional waste disposal service to dispose of this material. Dissolve or mix the material with a combustible solvent and burn in a chemical incinerator equipped with an afterburner and scrubber. Contaminated packaging: Dispose of as unused product. |
| Preventive Measures | ACCIDENTAL RELEASE MEASURES: Personal precautions, protective equipment and emergency procedures: Use personal protective equipment. Avoid dust formation. Avoid breathing vapors, mist or gas. Ensure adequate ventilation. Evacuate personnel to safe areas. Avoid breathing dust. Environmental precautions: Prevent further leakage or spillage if safe to do so. Do not let product enter drains.Precautions for safe handling: Avoid contact with skin and eyes. Avoid formation of dust and aerosols. Provide appropriate exhaust ventilation at places where dust is formed. Normal measures for preventive fire protection.Appropriate engineering controls: Handle in accordance with good industrial hygiene and safety practice. Wash hands before breaks and at the end of workday.Gloves must be inspected prior to use. Use proper glove removal technique (without touching glove's outer surface) to avoid skin contact with this product. Dispose of contaminated gloves after use in accordance with applicable laws and good laboratory practices. Wash and dry hands.SRP: Local exhaust ventilation should be applied wherever there is an incidence of point source emissions or dispersion of regulated contaminants in the work area. Ventilation control of the contaminant as close to its point of generation is both the most economical and safest method to minimize personnel exposure to airborne contaminants. Ensure that the local ventilation moves the contaminant away from the worker. |
| Personal Protective Equipment (PPE) | Eye/face protection: Use equipment for eye protection tested and approved under appropriate government standards such as NIOSH (US) or EN 166(EU).Skin protection: Handle with gloves.Body Protection: Impervious clothing. The type of protective equipment must be selected according to the concentration and amount of the dangerous substance at the specific workplace.Respiratory protection: Where risk assessment shows air-purifying respirators are appropriate use a full-face particle respirator type N100 (US) or type P3 (EN 143) respirator cartridges as a backup to engineering controls. If the respirator is the sole means of protection, use a full-face supplied air respirator. Use respirators and components tested and approved under appropriate government standards such as NIOSH (US) or CEN (EU). |
| Treatment | In the management of overdosage, prompt gastric lavage or the use of an emetic is recommended. Adequate fluid intake should be maintained, by the intravenous route if necessary, since Ancobon is excreted unchanged via the renal tract. The hematologic parameters should be monitored frequentlyliver and kidney function should be carefully monitored. Should any abnormalities appear in any of these parameters, appropriate therapeutic measures should be instituted. Since hemodialysis has been shown to rapidly reduce serum concentrations in anuric patients, this method may be considered in the management of overdosage. (L1712) |
| 상호 작용 | Invasive fungal infection is a well-known cause of morbidity and mortality in immunocompromised patients. In this study we aimed to evaluate the hepatotoxicity induced by combined therapy of flucytosine and amphotericin B, at three different doses administered to mice for 14 days: 50 mg/kg flucytosine and 300 ug/kg amphotericin B100 mg/kg flucytosine and 600 ug/kg amphotericin B150 mg/kg flucytosine and 900 ug/kg amphotericin B. Liver injuries were evaluated by analysis of optic and electron microscopy samples, changes in TNF-alpha, IL-6, and NF-kappaB inflammation markers levels of expression, and evaluation of mRNA profiles. Histological and ultrastructural analysis revealed an increase in parenchymal and portal inflammation in mice and Kupffer cells activation. Combined antifungal treatment stimulated activation of an inflammatory pathway, demonstrated by a significant dose-dependent increase of TNF-alpha and IL-6 immunoreactivity, together with mRNA upregulation. Also, NF-kappaB was activated, as suggested by the high levels found in hepatic tissue and upregulation of target genes. Our results suggest that antifungal combined therapy exerts a synergistic inflammatory activation in a dose-dependent manner, through NF-kappaB pathway, which promotes an inflammatory cascade during inflammation. The use of combined antifungal therapy needs to be dose limiting due to the associated risk of liver injury, especially for those patients with hepatic dysfunction.In some in vitro studies, the combination of flucytosine and amphotericin B resulted in synergistic inhibition of strains of Cryptococcus neoformans, Candida albicans, and C. tropicalis. The suggested mechanism of this synergism is that the binding of amphotericin B to sterols in cell membranes increases the permeability of the cytoplasmic membrane, thus allowing greater penetration of flucytosine into the fungal cell. However, in a study evaluating the antifungal effects of the drugs in the presence of serum, the combination of amphotericin B and flucytosine was not additive or synergistic against C. albicans. Concomitant use of amphotericin B and flucytosine may increase the toxicity of flucytosine, possibly by increasing cellular uptake and/or by decreasing renal excretion of the drug. If flucytosine is used in conjunction with amphotericin B, especially in HIV-infected patients, serum flucytosine concentrations and blood cell counts should be carefully monitored.In in vitro studies, the combination of flucytosine and fluconazole or itraconazole was synergistic, additive, or indifferent against Cryptococcus neoformansthere was no evidence of antagonism. The combination of fluconazole and flucytosine generally did not exert a synergistic effect against C. neoformans isolates that had fluconazole MICs of 8 ug/mL or greater. Synergism also has been demonstrated when the combination of fluconazole and flucytosine was evaluated in vivo in a murine model of cryptococcal meningitis. It has been suggested that synergism between the drugs may occur because fluconazole damages the fungal cell membrane allowing greater intracellular penetration of flucytosine.Cytarabine (cytosine arabinoside) reportedly antagonizes the antifungal activity of flucytosine, possibly by competitive inhibition. Concomitant use of the drugs is not recommended. |
| Hepatotoxicity | Transient mild-to-moderate elevations in serum aminotransferase or alkaline phosphatase levels occur in up to 41% of patients treated with flucytosine. The enzyme abnormalities are usually asymptomatic and resolve with stopping flucytosine, and sometimes even with its continuation. Clinically apparent hepatotoxicity is very rare. Instances of acute liver injury and hepatic failure have been mentioned in clinical trials of flucytosine therapy, but few details were provided and no convincing case reports of acute hepatic injury with jaundice have been published. |
| 유해 작용 | Flucytosine adverse effects can be differentiated based on the organ system involved. Product-labeled adverse effects include: |
| 노출 경로 | Rapidly and virtually completely absorbed following oral administration. Bioavailability 78% to 89%. |
| 독성 요약 | IDENTIFICATION AND USE: Flucytosine is a solid. It is used as antifungal agent and antimetabolite. Flucytosine Capsules are indicated only in the treatment of serious infections caused by susceptible strains of Candida and/or Cryptococcus. HUMAN STUDIES: It is reasonable to expect that overdosage may produce pronounced manifestations of the known clinical adverse reactions. Prolonged serum concentrations in excess of 100 ug/mL may be associated with an increased incidence of toxicity, especially gastrointestinal (diarrhea, nausea, vomiting), hematologic (leukopenia, thrombocytopenia) and hepatic (hepatitis). A case of urinary crystalluria was reported in a patient during treatment with flucytosine. Flucytosine-associated diarrhea has been described in 6%-10% of patients receiving the drug. A potentially fatal ulcerating enterocolitis has been reported in 4 patients. ANIMAL STUDIES: In mice, 400 mg/kg/day of flucytosine administered on days 7 to 13 of gestation was associated with a low incidence of cleft palate that was not statistically significant. Flucytosine was not teratogenic in rabbits up to a dose of 100 mg/kg/day administered on days 6 to 18 of gestation. Flucytosine was shown to be teratogenic (vertebral fusions) in the rat at doses of 40 mg/kg/day administered on days 7 to 13 of gestation. At higher doses (700 mg/kg/day) administered on days 9 to 12 of gestation), cleft lip and palate and micrognathia were reported. The in utero treatment had no adverse effect on the fertility or reproductive performance of the offspring in mice. The mutagenic potential of flucytosine was evaluated in Ames-type studies with five different mutants of Salmonella typhimurium and no mutagenicity was detected in the presence or absence of activating enzymes. Flucytosine was nonmutagenic in three different repair assay systems.Flucytosine toxicity can present with hepatitis and gastrointestinal symptoms such as diarrhea, nausea, and vomiting. More severe symptoms, such as leukopenia and thrombocytopenia, can also develop. The adverse effects and toxicity of flucytosine are concentration-dependent and can be managed by decreasing the dosage or discontinuing the medication if complications arise. If severe toxicity does occur, the drug is manageable through hemodialysis or peritoneal dialysis, as 97% of the drug is excreted through glomerular filtration of the kidneys.Although the exact mode of action is unknown, it has been proposed that flucytosine acts directly on fungal organisms by competitive inhibition of purine and pyrimidine uptake and indirectly by intracellular metabolism to 5-fluorouracil. Flucytosine enters the fungal cell via cytosine permeasethus, flucytosine is metabolized to 5-fluorouracil within fungal organisms. The 5-fluorouracil is extensively incorporated into fungal RNA and inhibits synthesis of both DNA and RNA. The result is unbalanced growth and death of the fungal organism. It also appears to be an inhibitor of fungal thymidylate synthase. |
| Ongoing Test Status | EPA has released the Interactive Chemical Safety for Sustainability (iCSS) Dashboard. The iCSS Dashboard provides an interactive tool to explore rapid, automated (or in vitro high-throughput) chemical screening data generated by the Toxicity Forecaster (ToxCast) project and the federal Toxicity Testing in the 21st century (Tox21) collaboration. /The title compound was tested by ToxCast and/or Tox21 assays/[USEPAICSS Dashboard ApplicationAvailable from, as of March 27, 2018: http://actor.epa.gov/dashboard/] |
| Human Toxicity Excerpts | /HUMAN EXPOSURE STUDIES/ The aim of this study is to investigate whether fluorouracil (5-FU) could be responsible for bone-marrow depression occurring in fluorocytosine (5-FC) treated patients. Six 5-FC treated patients were included in this pilot study. Toxicity was monitored by means of thrombocyte and leucocyte counts. 5-FC and 5-FU serum levels were measured using a high-performance liquid chromatography (HPLC) assay that allows simultaneous determination of both compounds. The amounts of 5-FU in the 34 available serum samples remained below the limit of quantitation (< 0.05 mg/L), whereas 5-FC levels could be detected in all samples. Instead, low levels of the 5-FU catabolite alpha-fluoro-beta-alanine (FBAL) were detected in several of the investigated serum samples. In case of three patients thrombocyte counts remained within the normal range during 5-FC treatment, whereas one patient developed thrombocytopenia (50 x 10(9) thrombocytes/L) during therapy. Furthermore, one patient developed leucocytopenia (2.6 x 10(9) leucocytes/L) during 5-FC therapy, whereas the remaining five patients were suffering from leucocytosis prior to 5-FC therapy. In conclusion, we found nondetectable 5-FU serum concentrations (< 0.05 mg/L) in ICU patients treated with intravenous 5-FC, making it unlikely that 5-FC-associated toxicity results from 5-FU exposure in patients receiving intravenous 5-FC therapy. These findings may be explained by the fact that our patients received 5-FC intravenously instead of orally, therefore not allowing active conversion of 5-FC to 5-FU by the human intestinal microflora. /5-Fluorouracil//HUMAN EXPOSURE STUDIES/ A gas chromatographic-mass spectrometric method for detecting 5-fluorouracil (5-FU) in serum at concentrations as low as 10 ng/mL was used to determine to what extent 5-FU was present in the serum of patients taking oral 5-fluorocytosine (5-FC). Preliminary studies in two patients and two healthy volunteers given an initial 2-g oral dose of 5-FC demonstrated sustained serum 5-FU levels (>100 ng/mL) during the 5 hr after ingestion of drug. Pharmaceutical preparations of 5-FC used in these studies were shown to be insignificantly contaminated with 5-FU (<0.03%), suggesting in vivo conversion of 5-FC to 5-FU had occurred. Serum samples from seven patients with cryptococcal meningitis treated with amphotericin B and 5-FC were examined for 5-FU. Five of these patients had experienced hematological or other toxicity attributed to 5-FC at some time during the course of therapy. Of 41 serum samples, 20 were observed to have 5-FU levels greater than 1,000 ng/mL in the range observed with cancer chemotherapeutic doses of 5-FU known to be associated with hematological toxicity. It is concluded that conversion of 5-FC to 5-FU occurs in humans and furthermore that 5-FU may account for some of the toxicity observed with 5-FC. /5-Fluorouracil//SIGNS AND SYMPTOMS/ Bone marrow toxicity occurred in 4 of 15 patients treated with 5-fluorocytosine (5-FC) for serious fungal infections. The development of marrow toxicity appeared to be related to serum 5-FC levels of 125 ug/mL or greater. In three patients, accumulation of toxic levels of 5-FC was related to diminished renal function. One patient with acute renal failure and prolonged high levels of 5-FC developed marrow aplasia and died of bacterial sepsis. Three patients experienced leukopenia, which was readily reversed when the dosage of 5-FC was decreased and the serum concentration was lowered. With careful monitoring of serum 5-FC concentration and renal function, the dose-related toxic effects of 5-FC on the marrow can be avoided./SIGNS AND SYMPTOMS/ There is no experience with intentional overdosage. It is reasonable to expect that overdosage may produce pronounced manifestations of the known clinical adverse reactions. Prolonged serum concentrations in excess of 100 ug/mL may be associated with an increased incidence of toxicity, especially gastrointestinal (diarrhea, nausea, vomiting), hematologic (leukopenia, thrombocytopenia) and hepatic (hepatitis).For more Human Toxicity Excerpts (Complete) data for Flucytosine (11 total), please visit the HSDB record page. |
| Carcinogen Classification | No indication of carcinogenicity to humans (not listed by IARC). |
| Drug Induced Liver Injury | Drug Induced Liver Injury Rank (DILIrank 2.0)FlucytosineAmbiguous-DILI-concern3Warnings & precautionsDOI:10.1016/j.drudis.2016.02.015 |
| Non-Human Toxicity Excerpts | /LABORATORY ANIMALS: Subchronic or Prechronic Exposure/ Invasive fungal infection is a well-known cause of morbidity and mortality in immunocompromised patients. In this study we aimed to evaluate the hepatotoxicity induced by combined therapy of flucytosine and amphotericin B, at three different doses administered to mice for 14 days: 50 mg/kg flucytosine and 300 ug/kg amphotericin B100 mg/kg flucytosine and 600 ug/kg amphotericin B150 mg/kg flucytosine and 900 ug/kg amphotericin B. Liver injuries were evaluated by analysis of optic and electron microscopy samples, changes in TNF-alpha, IL-6, and NF-kappaB inflammation markers levels of expression, and evaluation of mRNA profiles. Histological and ultrastructural analysis revealed an increase in parenchymal and portal inflammation in mice and Kupffer cells activation. Combined antifungal treatment stimulated activation of an inflammatory pathway, demonstrated by a significant dose-dependent increase of TNF-alpha and IL-6 immunoreactivity, together with mRNA upregulation. Also, NF-kappaB was activated, as suggested by the high levels found in hepatic tissue and upregulation of target genes. Our results suggest that antifungal combined therapy exerts a synergistic inflammatory activation in a dose-dependent manner, through NF-kappaB pathway, which promotes an inflammatory cascade during inflammation. The use of combined antifungal therapy needs to be dose limiting due to the associated risk of liver injury, especially for those patients with hepatic dysfunction./LABORATORY ANIMALS: Developmental or Reproductive Toxicity/ In mice, 400 mg/kg/day of flucytosine (1380 mg/sq m/day or 0.236 times the human dose) administered on days 7 to 13 of gestation was associated with a low incidence of cleft palate that was not statistically significant./LABORATORY ANIMALS: Developmental or Reproductive Toxicity/ Flucytosine was not teratogenic in rabbits up to a dose of 100 mg/kg/day (1423 mg/sq m/day or 0.243 times the human dose) administered on days 6 to 18 of gestation./LABORATORY ANIMALS: Developmental or Reproductive Toxicity/ Flucytosine was shown to be teratogenic (vertebral fusions) in the rat at doses of 40 mg/kg/day (298 mg/sq m/day or 0.051 times the human dose) administered on days 7 to 13 of gestation. At higher doses (700 mg/kg/day5208 mg/sq m/day or 0.89 times the human dose administered on days 9 to 12 of gestation), cleft lip and palate and micrognathia were reported.For more Non-Human Toxicity Excerpts (Complete) data for Flucytosine (8 total), please visit the HSDB record page. |
| Populations at Special Risk | Flucytosine capsules must be given with extreme caution to patients with bone marrow depression. Patients may be more prone to depression of bone marrow function if they: 1) have a hematologic disease, 2) are being treated with radiation or drugs which depress bone marrow, or 3) have a history of treatment with such drugs or radiation. Bone marrow toxicity can be irreversible and may lead to death in immunosuppressed patients. Frequent monitoring of hepatic function and of the hematopoietic system is indicated during therapy.Flucytosine capsules must be given with extreme caution to patients with impaired renal function. Since flucytosine capsules are excreted primarily by the kidneys, renal impairment may lead to accumulation of the drug. flucytosine capsules serum concentrations should be monitored to determine the adequacy of renal excretion in such patients. Dosage adjustments should be made in patients with renal insufficiency to prevent progressive accumulation of active drug. |
| 수질 위해 등급(WGK) | 2 |
| RTECS 번호 | HA6040000 |
| 독성 | LD50 in mice (mg/kg): >2000 orally and s.c.1190 i.p.500 i.v. (Grunberg, 1963) |
| 관세 코드 | 29335990 |
| 위험 문구(R) | 40-36/37/38-63 |
| 위험 표시 | Xn,T,Xi |
| 안전 문구(S) | 22-24/25-45-36/37-36/37/39-27-26 |
| 위험 등급 | IRRITANT, LIGHT SENSITIVERepr. 2 |
| F 고인화성물질 | 10-23 |
| 위험 참고 사항 | Toxic/Light Sensitive |
| 저장 분류 | 11 - Combustible Solids |
| 유해 물질 데이터 | 2022-85-7(Hazardous Substances Data) |
용도
개요
5-Fluorocytosine (5-FC), a fluorinated pyrimidine analog, is a synthetic antimycotic prodrug that is converted by cytosine deaminase to 5-fluorouracil. 5-Fluorouracil, a widely used cytotoxic drug, is further metabolized to fluorinated ribo- and deoxyribonucleotides, resulting in the inhibition of DNA and protein synthesis, which has multiple effects including inhibition of Candida species and C. neoformans infections and cytotoxicity towards cancer cells. In combination with a retroviral replicating vector carrying a cytosine deaminase prodrug-activating gene, 5-FC has been shown to selectively eliminate CT26 and Tu-2449 tumor cells in vitro (IC50s = 4.2 and 1.5 μM, respectively) and to significantly improve survival and reduce tumor size (at a dose of 500 mg/kg) in two different syngeneic mouse glioma models.
용도
5-Fluorocytosine acts as an antidiabetic, antifungal and antimicrobial agent. It is useful for the treatment of serious infections arises due to susceptible strains of Candida or Cryptococcus neoformans and chromomycosis. Further, it is employed in studies on TMP biosynthesis.