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Busulfan
drug data and news
Busulfan drug data, resources, and news articles (when available). Onconews.org provides news on cancer research. This section, which includes profiles on medicines that may or not be cancer-related is in beta form. If things run smoothly we will be releasing a new format late in the summer of 2006.
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| Generic name | Busulfan | ||
| Brand Names/Synonyms | 2041 C. B.; AN 33501; Busulfan; Busulfex; Busulphan; Busulphane; Butanedioldimethanesulfonate; Buzulfan; C.B. 2041; CB 2041; Citosulfan; G.T. 41; GT 2041; GT 41; Leucosulfan; Mablin; Mielevcin; Mielosan; Mielucin; Milecitan; Mileran; Misulban; Mitosan; Mitostan; Myeleukon; Myeloleukon; Myelosan; Myelosanum, Busulphan; Mylecytan; Myleran; Myleran Tablets; NCI-C01592; NSC 750; NSC-750; Nsc-750sulphabutin; Sulfabutin; Sulphabutin; Tetramethylene Dimethane Sulfonate; Tetramethylenester Kyseliny Methansulfonove; X 149 | ||
| Indication | For use in combination with cyclophosphamide as a conditioning regimen prior to allogeneic hematopoietic progenitor cell transplantation for chronic myelogenous leukemia. | ||
| Sponsored links | Description | Not Available | |
| Pharmacology | Busulfan is an antineoplastic in the class of alkylating agents and is used to treat various forms of cancer. Alkylating agents are so named because of their ability to add alkyl groups to many electronegative groups under conditions present in cells. They stop tumor growth by cross-linking guanine bases in DNA double-helix strands - directly attacking DNA. This makes the strands unable to uncoil and separate. As this is necessary in DNA replication, the cells can no longer divide. In addition, these drugs add methyl or other alkyl groups onto molecules where they do not belong which in turn inhibits their correct utilization by base pairing and causes a miscoding of DNA. Alkylating agents are cell cycle-nonspecific. Alkylating agents work by three different mechanisms all of which achieve the same end result - disruption of DNA function and cell death. | ||
| Mechanism Of Action | Alkylating agents work by three different mechanisms: 1) attachment of alkyl groups to DNA bases, resulting in the DNA being fragmented by repair enzymes in their attempts to replace the alkylated bases, preventing DNA synthesis and RNA transcription from the affected DNA, 2) DNA damage via the formation of cross-links (bonds between atoms in the DNA) which prevents DNA from being separated for synthesis or transcription, and 3) the induction of mispairing of the nucleotides leading to mutations. | ||
| Busulfan News (When available) |
Convention doubles expectations Feb 15, 2006 Protein Design Labs Becomes PDL BioPharma Jan 9, 2006 Recent Studies Produce Promising Results in Effectively Treating ... 11 Dec 2005 Committee for Medicinal Products for Human Use Post-authorisation ... Sep 16, 2005 THE FAMILY DOCTOR Aug 23, 2005 New Eggs From Bone Marrow? Jul 26, 2005 New oocytes from bone marrow? Jul 28, 2005 REPRODUCTIVE BIOLOGY: Controversial Study Finds an Unexpected ... Jul 28, 2005 New method of administering anti-cancer drug may be more effective ... May 19, 2005 Single-Dose Phase I Data on Velafermin (CG53135) for Prevention of ... May 18, 2005 Blood Stem Cells Save Lives of Infants with Genetic Disorder May 18, 2005 Vion Gets SPA Go-Ahead For AML Drug's Phase III Feb 10, 2005 | ||
| Dosage Forms | SOLUTION; TABLET | ||
| Drug_Category | Antineoplastic Agents; Immunosuppressive Agents; Alkylating Agents; ATC:L01AB01 | ||
| Absorption | Completely absorbed from the gastrointestinal tract. | ||
| Interactions |
Interactions for Busulfan: Itraconazole decreases busulfan clearance by up to 25%, and may produce AUCs > 1500 µM·min in some patients. Fluconazole, and the 5-HT3 antiemetics odansetron (Zofran) and granisetron (Kytril) have all been used with BUSULFEX. Phenytoin increases the clearance of busulfan by 15% or more, possibly due to the induction of glutathione-S-transferase. Since the pharmacokinetics of BUSULFEX were studied in patients treated with phenytoin, the clearance of BUSULFEX at the recommended dose may be lower and exposure (AUC) higher in patients not treated with phenytoin. Because busulfan is eliminated from the body via conjugation with glutathione, use of acetaminophen prior to (<72 hours) or concurrent with BUSULFEX may result in reduced busulfan clearance based upon the known property of acetaminophen to decrease glutathione levels in the blood and tissues. | ||
| Toxicity | Signs of overdose include allergic reaction, unusual bleeding or bruising, sudden weakness or unusual fatigue, persistent cough, congestion, or shortness of breath; flank, stomach or joint pain; pronounced nausea, vomiting, diarrhea, dizziness, confusion, or darkening of the skin, chills, fever, collapse, and loss of consciousness. | ||
| Organisms Affected | Humans and other mammals | ||
| Chemical IUPAC Name | 1,4-bis(methylsulfonyloxy)butane | ||
| Chemical Formula | C6H14O6S2 | ||
| Molecular Weight | 246.304 g/mol | ||
| Smiles String | CS(=O)(=O)OCCCCOS(=O)(=O)C | ||
| Melting Point | 287 °C | ||
| Water Solubility | 6.9E+004 mg/L | ||
| State | Solid (white crystalline powder) | ||
| LogP/Hphobicity | -0.52 | ||
| Isoelectric Point | Not Available | ||
| Biotransformation | Mainly Hepatic. Busulfan is predominantly metabolized by conjugation with glutathione, both spontaneously and by glutathione S-transferase (GST) catalysis. | ||
| Half Life | 2.5 hours | ||
| Protein Binding [%] | 32.40% | ||
| RxList Link | RXlist | ||
| Sponsored links | |||
| Drug Reference |
http://www.drugs.com/cons/Busulfan.html http://www.rxlist.com/cgi/generic2/busulfan.htm | ||
| Drug Type | Approved Drug | ||
| Accession No | APRD00664 | ||
| CAS Registry Number | 55-98-1 | ||
| KEGG Compound ID | C06862 | ||
| PubChem ID | SID:148760 | ||
| PharmGKB ID | PA448691 | ||
| SwissProt ID | Not Available | ||
| GenBank ID | Not Available | ||
| Drug ID Number [DIN] | 2240602 |
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