Drug Details
| General Information of the Drug (ID: DR3231) | ||||
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| Name |
Busulfan
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| Synonyms |
Busulfano; Busulfanum; Busulfex; Busulphan; Busulphane; Butanedioldimethanesulfonate; Buzulfan; Citosulfan; Glyzophrol; Leucosulfan; Mablin; Methanesulfonic; Mielevcin; Mielosan; Mielucin; Milecitan; Mileran; Misulban; Mitosan; Mitostan; Myeleukon; Myeloleukon; Myelosan; Myelosanum; Mylecytan; Myleran; Mylerlan; Sulfabutin; Sulphabutin; Busulfan GlaxoSmithKline Brand; Busulfan Orphan Brand; Busulfan Wellcome; Busulfan Wellcome Brand; Glaxo Wellcome Brand of Busulfan; GlaxoSmithKline Brand of Busulfan; Myleran tablets; Orphan Brand of Busulfan; Tetramethylene bis[methanesulfonate]; Tetramethylene dimethane sulfonate; Tetramethylenester kyseliny methansulfonove; Tetramethylenester kyseliny methansulfonove[Czech]; Wellcome Brand of Busulfan; AN 33501; CB 2041; GT 2041; GT 41; X 149; Acid, tetramethylene ester; Alkylating agent: crosslinks guanine residues; Busulfan [INN:JAN]; Busulfano [INN-Spanish]; Busulfanum [INN-Latin]; MYLERAN (TN); Methanesulfonic acid, tetram ethylene ester; Methanesulfonic acid, tetramethylene ester; Myleran (TN); Sulfabutin (VAN); Tetramethylene bis(methanesulfonate); Tetramethylene {bis[methanesulfonate]}; Wellcome, Busulfan; C.B. 2041; G.T. 41; Myleran, Busulfex, Busulfan; Busulfan (JP15/USP/INN); Butane-1,4-diyl dimethanesulfonate; BUSULFAN (1,4-BUTANEDIOL, DIMETHANESULFONATE); N-Butane-1,3-di(methylsulfonate); 1,4-BUTANEDIOL DIMETHANESULFONATE; 1,4-Bis(methanesulfonoxy)butane; 1,4-Bis(methanesulfonyloxy)butane; 1,4-Bis[methanesulfonoxy]butane; 1,4-Butanedi yl dimethanesulfonate; 1,4-Butanediol dimethanesulphonate; 1,4-Butanediol dimethylsulfonate; 1,4-Butanediol, dimethanesulfonate; 1,4-Butanediol, dimethanesulphonate; 1,4-Butanediyl dimethanesulfonate; 1,4-Di(methylsulfonoxy)butane; 1,4-Dimesyloxybutane; 1,4-Dimethane sulfonyl oxybutane; 1,4-Dimethanesulfonoxybutane; 1,4-Dimethanesulfonoxylbutane; 1,4-Dimethanesulfonyloxybutane; 1,4-Dimethanesulphonyloxybutane; 1,4-Dimethylsulfonoxybutane; 1,4-Dimethylsulfonyloxybutane; 1,{4-Bis[methanesulfonoxy]butane}; 4-((Methylsulfonyl)oxy)butyl methanesulfonate; 4-methylsulfonyloxybutyl methanesulfonate
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| Molecular Type |
Small molecule
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| Disease | Myelofibrosis [ICD-11: 2A22] | Approved | [1] | |
| Structure |
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Click to Download Mol2D MOL |
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| ADMET Property |
BDDCS Class
Biopharmaceutics Drug Disposition Classification System (BDDCS) Class 1: high solubility and high permeability
Bioavailability
70% of drug becomes completely available to its intended biological destination(s)
Clearance
The drug present in the plasma can be removed from the body at the rate of 2.4 mL/min/kg
Elimination
1% of drug is excreted from urine in the unchanged form
Half-life
The concentration or amount of drug in body reduced by one-half in 2.6 hours
Metabolism
The drug is metabolized via the hepatic
MRTD
The Maximum Recommended Therapeutic Dose (MRTD) of drug that ensured maximising efficacy and moderate side effect is 0.232 micromolar/kg/day
Unbound Fraction
The unbound fraction of drug in plasma is 1%
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 0.55 L/kg
Water Solubility
The ability of drug to dissolve in water is measured as 0.1 mg/mL
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| Click to Show/Hide the Molecular Information and External Link(s) of This Natural Product | ||||
| Formula |
C6H14O6S2
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| PubChem CID | ||||
| Canonical SMILES |
CS(=O)(=O)OCCCCOS(=O)(=O)C
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| InChI |
1S/C6H14O6S2/c1-13(7,8)11-5-3-4-6-12-14(2,9)10/h3-6H2,1-2H3
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| InChIKey |
COVZYZSDYWQREU-UHFFFAOYSA-N
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| CAS Number |
CAS 55-98-1
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| ChEBI ID | ||||
| TTD Drug ID | ||||
| DrugBank ID | ||||
| Combinatorial Therapeutic Effect(s) Validated Clinically or Experimentally | ||||||
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| α. A List of Natural Product(s) Able to Enhance the Efficacy of This Drug | ||||||
| Cladribine | Homo sapiens | Click to Show/Hide the Molecular Data of This NP | ||||
| Achieving Therapeutic Synergy | Click to Show/Hide | |||||
| Representative Experiment Reporting the Effect of This Combination | [2] | |||||
| Detail(s) |
Combination Info
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| In-vitro Model | J45.01 | CVCL_2530 | T acute lymphoblastic leukemia | Homo sapiens | ||
| U-937 | CVCL_0007 | Adult acute monocytic leukemia | Homo sapiens | |||
| Experimental
Result(s) |
The Clad+Gem+Bu+SAHA combination provides synergistic cytotoxicity in lymphoma cell lines. | |||||
| Curcumin | Hellenia speciosa | Click to Show/Hide the Molecular Data of This NP | ||||
| Augmenting Drug Sensitivity | Click to Show/Hide | |||||
| Representative Experiment Reporting the Effect of This Combination | [3] | |||||
| Detail(s) |
Combination Info
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| Molecule(s)
Regulation |
Down-regulation | Expression | CASP3 | Molecule Info |
Pathway MAP
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| Up-regulation | Cleavage | PARP1 | Molecule Info |
Pathway MAP
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| In-vitro Model | KG-1a | CVCL_1824 | Adult acute myeloid leukemia | Homo sapiens | ||
| HL-60 | CVCL_0002 | Adult acute myeloid leukemia | Homo sapiens | |||
| Experimental
Result(s) |
Curcumin could increase the sensitivity of leukemia stem-like KG1a cells to busulfan by downregulating the expression of survivin. | |||||
| Target and Pathway | ||||
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| Target(s) | Human Deoxyribonucleic acid (hDNA) | Molecule Info | [4] | |
