Page last updated: 2024-11-06

floxuridine and Leucocythaemia

floxuridine has been researched along with Leucocythaemia in 21 studies

Floxuridine: An antineoplastic antimetabolite that is metabolized to fluorouracil when administered by rapid injection; when administered by slow, continuous, intra-arterial infusion, it is converted to floxuridine monophosphate. It has been used to treat hepatic metastases of gastrointestinal adenocarcinomas and for palliation in malignant neoplasms of the liver and gastrointestinal tract.
floxuridine : A pyrimidine 2'-deoxyribonucleoside compound having 5-fluorouracil as the nucleobase; used to treat hepatic metastases of gastrointestinal adenocarcinomas and for palliation in malignant neoplasms of the liver and gastrointestinal tract.

Research Excerpts

ExcerptRelevanceReference
"The inhibitory effects of combined 5-methyltetrahydrofolate (5-CH3-THF), the physiological circulating folate species, and fluoropyrimidines, 5-fluorouracil (FUra) and 5-fluoro-2'-deoxyuridine (FdUrd), on growth of human leukemia cells, CCRF-CEM, were determined as a function of time, dose, and sequence of exposure."7.67Enhancement of fluoropyrimidine cytotoxicity by 5-methyltetrahydrofolate in a human leukemia cell line, CCRF-CEM. ( Coronnello, M; Criscuoli, L; Gualtieri, M; Mazzei, T; Mini, E; Periti, P, 1985)
"5-fluorouracil was a relatively ineffective cytotoxic agent for exposure of short duration (4 h)."5.27Modulation of fluoropyrimidine cytotoxicity by methotrexate or 5-methyltetrahydrofolate in human leukemia cells in vitro. ( Coronnello, M; Criscuoli, L; Gualtieri, M; Mazzei, T; Mini, E; Periti, P, 1984)
" Here, we describe thymineless death of human myeloid leukemia U937 cells treated with the thymidylate-synthase inhibitor 5'-fluoro- 2'-deoxyuridine (FUdR)."3.72Thymidylate synthase inhibition triggers glucose-dependent apoptosis in p53-negative leukemic cells. ( López-Rivas, A; Muñoz-Pinedo, C; Robledo, G, 2004)
"A series of aromatic, serum-stable, water soluble and nontoxic amino acid phosphoramidate monoesters of 5-fluoro-2'-deoxyuridine (FUdR) and 1-beta-arabinofuranosylcytosine (Ara-C) was shown to inhibit the cellular growth of the human leukemia cell line CCRF-CEM in the presence of human prostatic acid phosphatase (hPAP)."3.71Amino acid phosphoramidate nucleosides: potential ADEPT/GDEPT substrates. ( McIntee, EJ; Wagner, CR, 2001)
"We have previously shown that pretreatment of mouse erythroleukemia (MEL) cells with the fluorinated pyrimidines 5-fluorouracil (FUra) or 5-fluorodeoxyuridine (FUdR) followed by the differentiation inducer hexamethylene bisacetamide (HMBA) greatly enhanced the magnitude of their differentiation and caused extensive cell death."3.68Enhancement of differentiation and cytotoxicity of leukemia cells by combinations of fluorinated pyrimidines and differentiation inducers: development of DNA double-strand breaks. ( Huang, Y; Scher, BM; Scher, M; Waxman, S, 1992)
"The inhibitory effects of combined 5-methyltetrahydrofolate (5-CH3-THF), the physiological circulating folate species, and fluoropyrimidines, 5-fluorouracil (FUra) and 5-fluoro-2'-deoxyuridine (FdUrd), on growth of human leukemia cells, CCRF-CEM, were determined as a function of time, dose, and sequence of exposure."3.67Enhancement of fluoropyrimidine cytotoxicity by 5-methyltetrahydrofolate in a human leukemia cell line, CCRF-CEM. ( Coronnello, M; Criscuoli, L; Gualtieri, M; Mazzei, T; Mini, E; Periti, P, 1985)
"5-fluorouracil was a relatively ineffective cytotoxic agent for exposure of short duration (4 h)."1.27Modulation of fluoropyrimidine cytotoxicity by methotrexate or 5-methyltetrahydrofolate in human leukemia cells in vitro. ( Coronnello, M; Criscuoli, L; Gualtieri, M; Mazzei, T; Mini, E; Periti, P, 1984)

Research

Studies (21)

TimeframeStudies, this research(%)All Research%
pre-199017 (80.95)18.7374
1990's1 (4.76)18.2507
2000's3 (14.29)29.6817
2010's0 (0.00)24.3611
2020's0 (0.00)2.80

Authors

AuthorsStudies
McIntee, EJ1
Wagner, CR1
BURCHENAL, JH1
HOLMBERG, EA1
FOX, JJ1
HEMPHILL, SC1
REPPERT, JA1
SILBER, R1
GABRIO, BW1
HUENNEKENS, FM1
HARTMANN, JR1
ORIGENES, ML1
MURPHY, ML1
SITARZ, A1
ERLANDSON, M1
DOWD, JE1
DIPAOLO, JA1
WATNE, AL1
FISCHER, GA2
VONESSEN, CF1
Muñoz-Pinedo, C1
Robledo, G1
López-Rivas, A1
Cieśla, J1
Fraczyk, T1
Zieliński, Z1
Sikora, J1
Rode, W1
Fernandes, DJ3
Cranford, SK3
Mini, E2
Mazzei, T2
Coronnello, M2
Criscuoli, L2
Gualtieri, M2
Periti, P2
Ross, DD1
Groth, DP1
Kinkade, JM1
Chu, MY1
Hoovis, ML1
Waxman, S1
Huang, Y1
Scher, BM1
Scher, M1
Keyomarsi, K1
Moran, RG1
Przylepa, KA1
Wenger, SL1
Modest, EJ1
Clarkson, B1
Fried, J1
Strife, A1
Sakai, Y1
Ota, K1
Okita, T1
Lee, SY1

Clinical Trials (2)

Trial Overview

TrialPhaseEnrollmentStudy TypeStart DateStatus
Phase 0 Trial of [F-18]-5-Fluoro-2'-Deoxycytidine With Tetrahydrouridine[NCT01479348]Early Phase 15 participants (Actual)Interventional2011-11-01Terminated (stopped due to Slow, insufficient accrual.)
Phase I Trial of 5-Fluoro-2'-Deoxycytidine With Tetrahydrouridine[NCT00359606]Phase 158 participants (Actual)Interventional1999-04-30Completed
[information is prepared from clinicaltrials.gov, extracted Sep-2024]

Trial Outcomes

Number of Participants With Serious and Non-Serious Adverse Events

Here is the number of participants with serious and non-serious adverse events assessed by the Common Terminology Criteria for Adverse Events (CTCAE v4.0). A non-serious adverse event is any untoward medical occurrence. A serious adverse event is an adverse event or suspected adverse reaction that results in death, a life-threatening adverse drug experience, hospitalization, disruption of the ability to conduct normal life functions, congenital anomaly/birth defect or important medical events that jeopardize the patient or subject and may require medical or surgical intervention to prevent one of the previous outcomes mentioned. (NCT01479348)
Timeframe: Date treatment consent signed to date off study, approximately 20 months and 12 days.

InterventionParticipants (Count of Participants)
1/Intravenous (IV) Tetrahydrouridine (THU)2

Frequency and Severity of Adverse Events Assessed by the Common Terminology Criteria for Adverse Events (CTCAE) v4.0

[F-18]-5-fluoro-2'-deoxycytidine (FdCyd) was administered intravenously with administration of tetrahydrouridine (THU) and the frequency and severity of adverse events was observed. A non-serious adverse event is any untoward medical occurrence. A serious adverse event is an adverse event or suspected adverse reaction that results in death, a life-threatening adverse drug experience, hospitalization, disruption of the ability to conduct normal life functions, congenital anomaly/birth defect or important medical events that jeopardize the patient or subject and may require medical or surgical intervention to prevent one of the previous outcomes mentioned. Grade 0 is normal, Grade 1 is mild, Grade 2 is moderate, Grade 3 is severe or medically significant but not immediately life-threatening, Grade 4 is life-threatening consequences, and Grade 5 is death related to adverse event. (NCT01479348)
Timeframe: Within 5 days after interventions

Interventionadverse events (Number)
Day 1 Adverse EventsDay 2, Grade 2 HypoalbuminemiaDay 2, Grade 3 AnemiaDay 3 Adverse EventsDay 4 Adverse EventsDay 5 Adverse Events
1/Intravenous (IV) Tetrahydrouridine (THU)011000

Radiation Dosimetry Estimates of 5-fluoro-2'-Deoxycytidine (FdCyd) in Humans

Radiation dosimetry was determined based on the first patients. This involved making region of interest measurements on the scan for each major organ and measuring the uptake. Using standard dosimetry software this is converted into mSv/MBq, a standard measure of dosimetry. The software is known as Organ Level INternal Dose Assessment/EXponential Modeling (OLINDA) and is commonly used to generate this kind of data. (NCT01479348)
Timeframe: 1 year

InterventionmSv/MBq (Mean)
AdrenalsBrainBreastsGallbladder wallLower large intestine wallSmall intestineStomach wallUpper large intestine wallHeart wallKidneysLiverLungsMuscleOvariesPancreasRed marrowOsteogenic cellsSkinSpleenTestesThymusThyroidUrinary bladder wallUterus
1/Intravenous (IV) Tetrahydrouridine (THU)1.838.171.034.052.522.131.902.041.105.266.021.821.161.571.631.141.718.651.691.031.128.237.961.63

Tumor to Background Ratios (TBRs) of Target Lesions at 4 Time Points After Injection

Participants were scanned by positron emission tomography (PET) and lesions were measured at 4 time points after injection. (NCT01479348)
Timeframe: 9 minutes, 32 minutes, 56 minutes and 2 hours after injection

InterventionTBR ratio (Number)
Pt 1 L. Parotid adenosquam. cell ca at 9 minPt 1 L. Parotid adenosquam. cell ca at 32 minPt 1 L. Parotid adenosquam. cell ca at 56 minPt 1 L. Parotid adenosquam. cell ca at 2 hrsPt 2 R. Parapharyngeal Spindle Cell Ca at 9 minPt 2 R. Parapharyngeal Spindle Cell Ca at 32 minPt 2 R. Parapharyngeal Spindle Cell Ca at 56 minPt 2 R. Parapharyngeal Spindle Cell Ca at 2 hrsPt 3 Non-small Cell Lung Ca at 9 minPt 3 Non-small Cell Lung Ca at 32 minPt 3 Non-small Cell Lung Ca at 56 minPt 3 Non-small Cell Lung Ca at 2 hrsPt 4 Non-small Cell Lung Ca at 9 minPt 4 Non-small Cell Lung Ca at 32 minPt 4 Non-small Cell Lung Ca at 56 minPt 4 Non-small Cell Lung Ca at 2 hrsPt 5 Hepatocellular Ca at 9 minPt 5 Hepatocellular Ca at 32 minPt 5 Hepatocellular Ca at 56 minPt 5 Hepatocellular Ca at 2 hrs
1/Intravenous (IV) Tetrahydrouridine (THU)1.41.51.51.61.91.71.71.61.41.41.51.72.42.11.62.0NANANANA

Other Studies

21 other studies available for floxuridine and Leucocythaemia

ArticleYear
Amino acid phosphoramidate nucleosides: potential ADEPT/GDEPT substrates.
    Bioorganic & medicinal chemistry letters, 2001, Nov-05, Volume: 11, Issue:21

    Topics: Acid Phosphatase; Amides; Cell Division; Enzymes; Humans; Leukemia; Nucleosides; Phosphoric Acids; P

2001
The effects of 5-fluorodeoxycytidine, 5-fluorodeoxyuridine, and related compounds on transplanted mouse leukemias.
    Cancer research, 1959, Volume: 19, Issue:5

    Topics: Animals; Antineoplastic Agents; Deoxycytidine; Floxuridine; Leukemia; Leukemia, Experimental; Mice;

1959
STUDIES ON NORMAL AND LEUKEMIC LEUKOCYTES. VI. THYMIDYLATE SYNTHETASE AND DEOXYCYTIDYLATE DEAMINASE.
    The Journal of clinical investigation, 1963, Volume: 42

    Topics: Adenosine Triphosphate; Aminohydrolases; Carbon Isotopes; Chromatography; Clinical Enzyme Tests; DCM

1963
EFFECTS OF 2'-DEOXY-5-FLUOROURIDINE (NSC-27640) AND 5-FLUOROURACIL (NSC-19893) ON CHILDHOOD LEUKEMIA.
    Cancer chemotherapy reports, 1964, Volume: 34

    Topics: Bone Marrow Examination; Child; Floxuridine; Fluorouracil; Leukemia; Leukopenia; Melena; Nausea; Tox

1964
INDIVIDUALIZED CHEMOTHERAPY BY IN VITRO DRUG SELECTION.
    Acta - Unio Internationalis Contra Cancrum, 1964, Volume: 20

    Topics: Antineoplastic Agents; Bone Neoplasms; Dactinomycin; Female; Floxuridine; Fluorouracil; Genital Neop

1964
THE COMPARISON OF RADIATION AND ANTIMETABOLITE RESPONSES OF GENETICALLY ALTERED MURINE LEUKEMIC CELLS.
    Biochemical pharmacology, 1965, Volume: 14

    Topics: Animals; Antimetabolites; Chromosomes; Floxuridine; Genetics; Idoxuridine; Leukemia; Leukemia, Exper

1965
Thymidylate synthase inhibition triggers glucose-dependent apoptosis in p53-negative leukemic cells.
    FEBS letters, 2004, Jul-16, Volume: 570, Issue:1-3

    Topics: Antimetabolites, Antineoplastic; Apoptosis; Caspases; Cell Line, Tumor; Cell Survival; Cytochromes c

2004
Altered mouse leukemia L1210 thymidylate synthase, associated with cell resistance to 5-fluoro-dUrd, is not mutated but rather reflects posttranslational modification.
    Acta biochimica Polonica, 2006, Volume: 53, Issue:1

    Topics: Animals; Antimetabolites, Antineoplastic; Cell Line, Tumor; Drug Resistance, Neoplasm; Floxuridine;

2006
A method for the determination of total, free, and 5-fluorodeoxyuridylate-bound thymidylate synthase in cell extracts.
    Analytical biochemistry, 1984, Nov-01, Volume: 142, Issue:2

    Topics: Binding Sites; Cell Line; Floxuridine; Fluorodeoxyuridylate; Humans; Leukemia; Methyltransferases; P

1984
Modulation of fluoropyrimidine cytotoxicity by methotrexate or 5-methyltetrahydrofolate in human leukemia cells in vitro.
    Chemioterapia : international journal of the Mediterranean Society of Chemotherapy, 1984, Volume: 3, Issue:6

    Topics: Cells, Cultured; Drug Synergism; Floxuridine; Fluorouracil; Humans; Leukemia; Methotrexate; Tetrahyd

1984
Effects of urinary proteins from certain leukemics upon macromolecular synthesis and enzyme levels in bone marrow cultures.
    The Journal of biological chemistry, 1975, Nov-25, Volume: 250, Issue:22

    Topics: Adenine Phosphoribosyltransferase; Amidophosphoribosyltransferase; Animals; Bone Marrow; Bone Marrow

1975
Effects of 5-fluorodeoxyuridine on cell viability and uptake of deoxycytidine and (3H)cytosine arabinoside in L5178Y cells.
    Biochemical pharmacology, 1976, Feb-01, Volume: 25, Issue:3

    Topics: Animals; Cells, Cultured; Cytarabine; Deoxycytidine; DNA; Floxuridine; Kinetics; Leukemia; Mice; RNA

1976
Enhancement of differentiation and cytotoxicity of leukemia cells by combinations of fluorinated pyrimidines and differentiation inducers: development of DNA double-strand breaks.
    Biomedicine & pharmacotherapy = Biomedecine & pharmacotherapie, 1992, Volume: 46, Issue:5-7

    Topics: Cell Differentiation; Cell Line, Transformed; Dimethyl Sulfoxide; Drug Therapy, Combination; Floxuri

1992
Dissociation of thymidylate biosynthesis from DNA biosynthesis by 5-fluoro-2'-deoxyuridine and 5,8-dideazaisofolic acid.
    Cancer research, 1986, Volume: 46, Issue:4 Pt 1

    Topics: Deoxyguanine Nucleotides; DNA; DNA Polymerase II; Dose-Response Relationship, Drug; Floxuridine; Fol

1986
Enhancement of fluoropyrimidine cytotoxicity by 5-methyltetrahydrofolate in a human leukemia cell line, CCRF-CEM.
    Chemioterapia : international journal of the Mediterranean Society of Chemotherapy, 1985, Volume: 4, Issue:6

    Topics: Cell Division; Cell Line; Drug Synergism; Floxuridine; Fluorouracil; Humans; Leukemia; Tetrahydrofol

1985
Folinic acid augmentation of the effects of fluoropyrimidines on murine and human leukemic cells.
    Cancer research, 1986, Volume: 46, Issue:10

    Topics: Animals; Cell Line; Cell Survival; Dose-Response Relationship, Drug; Drug Synergism; Floxuridine; Fl

1986
Chromosome breaks and fragile sites in leukemic bone marrow cells.
    Cancer genetics and cytogenetics, 1988, Jul-01, Volume: 33, Issue:1

    Topics: Adolescent; Aged; Bone Marrow; Caffeine; Cells, Cultured; Child; Child, Preschool; Chromosome Aberra

1988
Resistance of CCRF-CEM cloned sublines to 5-fluorodeoxyuridine associated with enhanced phosphatase activities.
    Biochemical pharmacology, 1985, Jan-01, Volume: 34, Issue:1

    Topics: Acid Phosphatase; Alkaline Phosphatase; Biological Transport; Clone Cells; Drug Resistance; Floxurid

1985
Formal discussion: future prospects in leukemia chemotherapy.
    Cancer research, 1965, Volume: 25, Issue:9

    Topics: Animals; Dactinomycin; Floxuridine; Leukemia; Melphalan; Mercaptopurine; Methotrexate; Mitomycins; N

1965
Studies of cellular proliferation in human leukemia. 3. Behavior of leukemic cells in three adults with acute leukemia given continuous infusions of 3H-thymidine for 8 or 10 days.
    Cancer, 1970, Volume: 25, Issue:6

    Topics: Acute Disease; Adult; Aged; Autoradiography; Bone Marrow; Bone Marrow Cells; Cell Division; Cell Nuc

1970
Current status of the host-mediated L5178Y system for detecting chemical mutagens.
    Environmental health perspectives, 1973, Volume: 6

    Topics: Alkylating Agents; Animals; Bromodeoxyuridine; Cell Line; Cells, Cultured; Cyclophosphamide; Ethylen

1973