Details of the Drug

General Information of Drug (ID: DMUM7HZ)

Drug Name
Fluorouracil
Synonyms
5-Fluorouracil; 51-21-8; fluorouracil; 5-FU; Fluoroplex; Adrucil; Efudex; Carac; Fluracil; Fluoroblastin; 5-fluoropyrimidine-2,4(1H,3H)-dione; Kecimeton; Timazin; Carzonal; Efudix; Arumel; Fluril; Queroplex; Fluracilum; Ulup; 5-Fluoracil; Phthoruracil; Fluro Uracil; 5-Fluoro-2,4(1H,3H)-pyrimidinedione; Ftoruracil; Fluorouracilum; Efurix; Fluri; 5 Fluorouracil; Effluderm (free base); 5-fluoro-1H-pyrimidine-2,4-dione; Fluorouracilo; Fluroblastin; Phtoruracil; 2,4-Dihydroxy-5-fluoropyrimidine; 2,4(1H,3H)-Pyrimidinedione, 5-fluoro-; Adrucil; Effluderm; Fluorouracile; Fluoruracil; Fluracedyl; Flurodex; Neofluor; Onkofluor; Ribofluor; Tetratogen; URF; Allergan Brand of Fluorouracil; Biosyn Brand of Fluorouracil; CSP Brand of Fluorouracil; Cinco FU; Dakota Brand of Fluorouracil; Dermatech Brand of Fluorouracil; Dermik Brandof Fluorouracil; Ferrer Brand of Fluorouracil; Fluoro Uracile ICN; Fluorouracil GRY; Fluorouracil Mononitrate; Fluorouracil Monopotassium Salt; Fluorouracil Monosodium Salt; Fluorouracil Potassium Salt; Fluorouracil Teva Brand; Fluorouracile Dakota; Fluorouracile [DCIT]; Fluorouracilo Ferrer Far; Gry Brand of Fluorouracil; Haemato Brand of Fluorouracil; Haemato fu; Hexal Brand of Fluorouracil; ICN Brand of Fluorouracil; Inhibits thymilidate synthetase; Medac Brand of Fluorouracil; Neocorp Brand of Fluorouracil; Onkoworks Brand of Fluorouracil; Ribosepharm Brand of Fluorouracil; Riemser Brand of Fluorouracil; Roche Brand of Fluorouracil; Teva Brand of Fluorouracil; F 6627; F0151; IN1335; U 8953; Adrucil (TN); Carac (TN); Dakota, Fluorouracile; Efudex (TN); Fluoro-Uracile ICN; Fluoro-uracile; Fluoro-uracilo; Fluoroplex (TN); Fluorouracil-GRY; Fluorouracilo [INN-Spanish]; Fluorouracilum [INN-Latin]; Haemato-fu; Ro 2-9757; U-8953; Ro-2-9757; Fluorouracil (JP15/USP/INN); Fluorouracil [USAN:INN:BAN:JAN]; 1-fluoro-1h-pyrimidine-2,4-dione; 2,4-Dioxo-5-fluoropryimidine; 2,4-Dioxo-5-fluoropyrimidine; 5 FU Lederle; 5 FU medac; 5 Fluorouracil biosyn; 5 HU Hexal; 5-FU (TN); 5-FU Lederle; 5-FU medac; 5-Faracil; 5-Fluor-2,4(1H,3H)-pyrimidindion; 5-Fluor-2,4(1H,3H)-pyrimidindion [Czech]; 5-Fluor-2,4-dihydroxypyrimidin; 5-Fluor-2,4-dihydroxypyrimidin [Czech]; 5-Fluor-2,4-pyrimidindiol; 5-Fluor-2,4-pyrimidindiol [Czech]; 5-Fluoracil [German]; 5-Fluoracyl; 5-Fluoro-2,4-pyrimidinedione; 5-Fluoropyrimidin-2,4-diol; 5-Fluoropyrimidine-2,4-dione; 5-Fluorouracil-biosyn; 5-Fluoruracil; 5-Fluoruracil [German]; 5-Ftouracyl; 5-HU Hexal; 5-fluoro uracil; 5FU
Indication
Disease Entry ICD 11 Status REF
Solid tumour/cancer 2A00-2F9Z Approved [1]
Colorectal cancer 2B91.Z Investigative [2]
Tumour 2A00-2F9Z Investigative [3]
Therapeutic Class
Immunosuppressive Agents
Drug Type
Small molecular drug
Structure
3D MOL 2D MOL
#Ro5 Violations (Lipinski): 0 Molecular Weight (mw) 130.08
Topological Polar Surface Area (xlogp) -0.9
Rotatable Bond Count (rotbonds) 0
Hydrogen Bond Donor Count (hbonddonor) 2
Hydrogen Bond Acceptor Count (hbondacc) 3
ADMET Property
Absorption
The absorption of drug is 28-100% [4]
BDDCS Class
Biopharmaceutics Drug Disposition Classification System (BDDCS) Class 1: high solubility and high permeability [5]
Clearance
The drug present in the plasma can be removed from the body at the rate of 26 mL/min/kg [6]
Elimination
5% of drug is excreted from urine in the unchanged form [5]
Half-life
The concentration or amount of drug in body reduced by one-half in 10 - 20 minutes [6]
Metabolism
The drug is metabolized via the hepatic [4]
MRTD
The Maximum Recommended Therapeutic Dose (MRTD) of drug that ensured maximising efficacy and moderate side effect is 92.25 micromolar/kg/day [7]
Unbound Fraction
The unbound fraction of drug in plasma is 0.64% [6]
Vd
Fluid volume that would be required to contain the amount of drug present in the body at the same concentration as in the plasma 0.23 L/kg [6]
Water Solubility
The ability of drug to dissolve in water is measured as 12.2 mg/mL [5]
Chemical Identifiers
Formula
C4H3FN2O2
IUPAC Name
5-fluoro-1H-pyrimidine-2,4-dione
Canonical SMILES
C1=C(C(=O)NC(=O)N1)F
InChI
InChI=1S/C4H3FN2O2/c5-2-1-6-4(9)7-3(2)8/h1H,(H2,6,7,8,9)
InChIKey
GHASVSINZRGABV-UHFFFAOYSA-N
Cross-matching ID
PubChem CID
3385
ChEBI ID
CHEBI:46345
CAS Number
51-21-8
DrugBank ID
DB00544
TTD ID
D05LEO
VARIDT ID
DR00153
INTEDE ID
DR0020
ACDINA ID
D01095

Molecular Interaction Atlas of This Drug


Drug Therapeutic Target (DTT)
DTT Name DTT ID UniProt ID MOA REF
Candida Thymidylate synthase (Candi TMP1) TTU6BFZ TYSY_CANAL Inhibitor [8], [9], [10], [11]
Dihydrothymine dehydrogenase (DPYD) TTZPS91 DPYD_HUMAN Inhibitor [12]
TERT messenger RNA (TERT mRNA) TTQY2EJ TERT_HUMAN Not Available [3]
Thymidylate synthase messenger RNA (TYMS mRNA) TTP1UKZ TYSY_HUMAN Not Available [3]

Drug Transporter (DTP)
DTP Name DTP ID UniProt ID MOA REF
Equilibrative nucleoside transporter 1 (SLC29A1) DTXD1TQ S29A1_HUMAN Substrate [13]
Multidrug resistance-associated protein 5 (ABCC5) DTYVM24 MRP5_HUMAN Substrate [14]
Organic anion transporter 2 (SLC22A7) DT0OC1Q S22A7_HUMAN Substrate [15]
Multidrug resistance-associated protein 3 (ABCC3) DTQ3ZHF MRP3_HUMAN Substrate [14]
Multidrug resistance-associated protein 2 (ABCC2) DTFI42L MRP2_HUMAN Substrate [16]
Multidrug resistance-associated protein 4 (ABCC4) DTCSGPB MRP4_HUMAN Substrate [14]
Breast cancer resistance protein (ABCG2) DTI7UX6 ABCG2_HUMAN Substrate [17]
P-glycoprotein 1 (ABCB1) DTUGYRD MDR1_HUMAN Substrate [18]

Drug-Metabolizing Enzyme (DME)
DME Name DME ID UniProt ID MOA REF
Cytochrome P450 2A6 (CYP2A6) DEJVYAZ CP2A6_HUMAN Substrate [19]
Cytochrome P450 1A2 (CYP1A2) DEJGDUW CP1A2_HUMAN Substrate [19]
Cytochrome P450 2C8 (CYP2C8) DES5XRU CP2C8_HUMAN Substrate [19]
Thymidylate synthase (TYMS) DEASG0Q TYSY_HUMAN Substrate [20]
Methylenetetrahydrofolate reductase (MTHFR) DEOXTPZ MTHR_HUMAN Substrate [20]
Thymidine phosphorylase (TYMP) DE4HCYL TYPH_HUMAN Substrate [20]
Uridine phosphorylase 1 (UPP1) DEFZWAX UPP1_HUMAN Substrate [21]
Dihydrothymine dehydrogenase (DPYD) DESOEW1 DPYD_HUMAN Substrate [22]
Uridine 5'-monophosphate synthase (UMPS) DEWJYTE UMPS_HUMAN Substrate [23]
Uracil phosphoribosyltransferase (UPRT) DE20ETR UPP_HUMAN Substrate [24]
Uridine phosphorylase 2 (UPP2) DEBQ2WU UPP2_HUMAN Substrate [21]
Amidophosphoribosyltransferase (GPAT) DEMJ7R2 PUR1_HUMAN Substrate [25]
Molecular Interaction Atlas (MIA) Jump to Detail Molecular Interaction Atlas of This Drug

Drug-Drug Interaction (DDI) Information of This Drug

Coadministration of a Drug Treating the Same Disease as Fluorouracil
DDI Drug Name DDI Drug ID Severity Mechanism Disease REF
Vinblastine DM5TVS3 Minor Decreased metabolism of Fluorouracil caused by Vinblastine mediated inhibition of CYP450 enzyme. Solid tumour/cancer [2A00-2F9Z] [143]
Coadministration of a Drug Treating the Disease Different from Fluorouracil (Comorbidity)
DDI Drug Name DDI Drug ID Severity Mechanism Comorbidity REF
Roflumilast DMPGHY8 Moderate Additive immunosuppressive effects by the combination of Fluorouracil and Roflumilast. Asthma [CA23] [144]
Ofloxacin DM0VQN3 Minor Decreased absorption of Fluorouracil due to intestinal mucosa variation caused by Ofloxacin. Bacterial infection [1A00-1C4Z] [145]
Trovafloxacin DM6AN32 Minor Decreased absorption of Fluorouracil due to intestinal mucosa variation caused by Trovafloxacin. Bacterial infection [1A00-1C4Z] [145]
Sparfloxacin DMB4HCT Minor Decreased absorption of Fluorouracil due to intestinal mucosa variation caused by Sparfloxacin. Bacterial infection [1A00-1C4Z] [145]
Gemifloxacin DMHT34O Minor Decreased absorption of Fluorouracil due to intestinal mucosa variation caused by Gemifloxacin. Bacterial infection [1A00-1C4Z] [145]
Norfloxacin DMIZ6W2 Minor Decreased absorption of Fluorouracil due to intestinal mucosa variation caused by Norfloxacin. Bacterial infection [1A00-1C4Z] [145]
ABT-492 DMJFD2I Minor Decreased absorption of Fluorouracil due to intestinal mucosa variation caused by ABT-492. Bacterial infection [1A00-1C4Z] [145]
Levofloxacin DMS60RB Minor Decreased absorption of Fluorouracil due to intestinal mucosa variation caused by Levofloxacin. Bacterial infection [1A00-1C4Z] [145]
Lomefloxacin DMVRH9C Minor Decreased absorption of Fluorouracil due to intestinal mucosa variation caused by Lomefloxacin. Bacterial infection [1A00-1C4Z] [145]
Teriflunomide DMQ2FKJ Major Additive myelosuppressive effects by the combination of Fluorouracil and Teriflunomide. Hyper-lipoproteinaemia [5C80] [146]
Denosumab DMNI0KO Moderate Additive myelosuppressive effects by the combination of Fluorouracil and Denosumab. Low bone mass disorder [FB83] [147]
Porfimer Sodium DM7ZWNY Moderate Increased risk of photosensitivity reactions by the combination of Fluorouracil and Porfimer Sodium. Lung cancer [2C25] [148]
Thalidomide DM70BU5 Major Additive thrombogenic effects by the combination of Fluorouracil and Thalidomide. Multiple myeloma [2A83] [149]
Tecfidera DM2OVDT Moderate Additive immunosuppressive effects by the combination of Fluorouracil and Tecfidera. Multiple sclerosis [8A40] [150]
Siponimod DM2R86O Major Additive immunosuppressive effects by the combination of Fluorouracil and Siponimod. Multiple sclerosis [8A40] [151]
Fingolimod DM5JVAN Major Additive immunosuppressive effects by the combination of Fluorouracil and Fingolimod. Multiple sclerosis [8A40] [152]
Ocrelizumab DMEZ2KH Moderate Additive immunosuppressive effects by the combination of Fluorouracil and Ocrelizumab. Multiple sclerosis [8A40] [153]
Ozanimod DMT6AM2 Major Additive immunosuppressive effects by the combination of Fluorouracil and Ozanimod. Multiple sclerosis [8A40] [144]
Omacetaxine mepesuccinate DMPU2WX Moderate Additive myelosuppressive effects by the combination of Fluorouracil and Omacetaxine mepesuccinate. Myeloproliferative neoplasm [2A20] [154]
Gatifloxacin DMSL679 Minor Decreased absorption of Fluorouracil due to intestinal mucosa variation caused by Gatifloxacin. Respiratory infection [CA07-CA4Z] [145]
Canakinumab DM8HLO5 Moderate Additive immunosuppressive effects by the combination of Fluorouracil and Canakinumab. Rheumatoid arthritis [FA20] [155]
Rilonacept DMGLUQS Moderate Additive immunosuppressive effects by the combination of Fluorouracil and Rilonacept. Rheumatoid arthritis [FA20] [155]
Golimumab DMHZV7X Major Additive immunosuppressive effects by the combination of Fluorouracil and Golimumab. Rheumatoid arthritis [FA20] [156]
Leflunomide DMR8ONJ Major Additive myelosuppressive effects by the combination of Fluorouracil and Leflunomide. Rheumatoid arthritis [FA20] [146]
Anthrax vaccine DM9GSWY Moderate Antagonize the effect of Fluorouracil when combined with Anthrax vaccine. Sepsis [1G40-1G41] [157]
Azathioprine DMMZSXQ Moderate Additive myelosuppressive effects by the combination of Fluorouracil and Azathioprine. Transplant rejection [NE84] [151]
Cinoxacin DM4EWNS Minor Decreased absorption of Fluorouracil due to intestinal mucosa variation caused by Cinoxacin. Urinary tract infection [GC08] [145]
Nalidixic acid DMRM0JV Minor Decreased absorption of Fluorouracil due to intestinal mucosa variation caused by Nalidixic acid. Urinary tract infection [GC08] [145]
Ganciclovir DM1MBYQ Moderate Additive myelosuppressive effects by the combination of Fluorouracil and Ganciclovir. Virus infection [1A24-1D9Z] [151]
Valganciclovir DMS2IUH Moderate Additive myelosuppressive effects by the combination of Fluorouracil and Valganciclovir. Virus infection [1A24-1D9Z] [151]
⏷ Show the Full List of 30 DDI Information of This Drug

Drug Inactive Ingredient(s) (DIG) and Formulation(s) of This Drug

DIG
DIG Name DIG ID PubChem CID Functional Classification
methylparaben E00149 7456 Antimicrobial preservative
Propylparaben sodium E00567 23679044 Antimicrobial preservative
Stearic acid E00079 5281 Emulsifying agent; Solubilizing agent; Viscosity-controlling agent; lubricant
Trolamine E00151 7618 Alkalizing agent; Emulsifying agent
Edetate disodium E00186 8759 Complexing agent
Glycerin E00026 753 Antimicrobial preservative; Emollient; Flavoring agent; Humectant; Lubricant; Plasticizing agent; Solvent; Suppository base; Tonicity agent; Viscosity-controlling agent
Hydroxypropyl cellulose E00632 Not Available Binding agent; Coating agent; Emulsifying agent; Film/Membrane-forming agent; Modified-release agent; Suspending agent; Viscosity-controlling agent
Polyethylene glycol 400 E00653 Not Available Coating agent; Diluent; Ointment base; Plasticizing agent; Solvent; Suppository base; lubricant
Polysorbate 80 E00665 Not Available Dispersing agent; Emollient; Emulsifying agent; Plasticizing agent; Solubilizing agent; Surfactant; Suspending agent
Propylene glycol E00040 1030 Antimicrobial preservative; Humectant; Plasticizing agent; Solvent
Sodium hydroxide E00234 14798 Alkalizing agent
Sorbitan monooleate E00503 9920342 Dispersing agent; Emulsifying agent; Solubilizing agent; Surfactant; Suspending agent; Vaccine adjuvant
Tromethamine E00125 6503 Alkalizing agent; Buffering agent; Emulsifying agent
Water E00035 962 Solvent
Ethylhexyl hydroxystearate E00534 5463971 Emollient
Dimethicone 350 E00706 Not Available Antifoaming agent; Emollient; Water-repelling agent
Methyl gluceth-20 E00708 62247 Emulsifying agent; Humectant
⏷ Show the Full List of 17 Pharmaceutical Excipients of This Drug
Pharmaceutical Formulation
Formulation Name Drug Dosage Dosage Form Route
Fluorouracil 0.5% cream 0.50% Cream Topical
Fluorouracil 2% solution 2% Solution Topical
Fluorouracil 1g/20ml solution 1g/20ml Solution Intravenous
Jump to Detail Pharmaceutical Formulation Page of This Drug

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155 Product Information. Arcalyst (rilonacept). Regeneron Pharmaceuticals Inc, Tarrytown, NY.
156 Product Information. Cimzia (certolizumab). UCB Pharma Inc, Smyrna, GA.
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