|
|
|
|
|
Cladribine
drug data and news
Cladribine 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.
|
| Generic name | Cladribine | ||
| Brand Names/Synonyms | 2 Chlorodeoxyadenosine; Chlorodeoxyadenosine; Cladribine; Cladribine [Usan:Ban:Inn]; Leustatin | ||
| Indication | For the treatment of active Hairy Cell Leukemia as defined by clinically significant anemia, neutropenia, thrombocytopenia or disease-related symptoms | ||
| Sponsored links | Description | Not Available | |
| Pharmacology | Cladribine is a synthetic antineoplastic agent indicated for the treatment of active Hairy Cell Leukemia as defined by clinically significant anemia, neutropenia, thrombocytopenia or disease-related symptoms. Cladribine is an antimetabolite. Cladribine's action is cell cycle-phase nonspecific; cladribine affects both dividing and resting lymphocytes. | ||
| Mechanism Of Action | Cladribine is structurally related to fludarabine and pentostatin but has a different mechanism of action. It is phosphorylated by deoxycytidine kinase to the corresponding nucleotide CdATP which accumulates and is incorporated into the DNA of cells such as lymphocytes. The phosphorylated metabolites of cladribine tend to accumulate in cells with a high ratio of deoxycytidine kinase activity to 5' nucleotidase activity (lymphocytes, monocytes ) and are converted to the active triphosphate deoxynucleotide. Intracellular accumulation of toxic deoxynucleotides selectively kills these cells, which become unable to properly repair single-strand DNA breaks, leading to disruption of cell metabolism. In addition, there is some evidence that deoxynucleotides are incorporated into the DNA of dividing cells and impair DNA synthesis. Cladribine also induces apoptosis (a form of programmed cell death in sensitive cells). Cladribine is resistant to the action of adenosine deaminase (ADA), which normally deaminates deoxyadenosine to deoxyinosine. | ||
| Cladribine News (When available) |
| ||
| Dosage Forms | SOLUTION | ||
| Drug_Category | Immunosuppressive Agents; Antineoplastic Agents; ATC:L01BB04 | ||
| Absorption | Oral bioavailability is 34-48% | ||
| Interactions |
Interactions for Cladribine: There are no known drug interactions with LEUSTATIN Injection. Caution should be exercised if LEUSTATIN Injection is administered before, after, or in conjunction with other drugs known to cause immunosuppression or myelosuppression. | ||
| Toxicity | Side effects include nausea and vomiting, lymphopenia, anemia, neutropenia and fever | ||
| Organisms Affected | Humans and other mammals | ||
| Chemical IUPAC Name | 5-(6-amino-2-chloro-purin-9-yl)-2-(hydroxymethyl)oxolan-3-ol | ||
| Chemical Formula | C10H12ClN5O3 | ||
| Molecular Weight | 285.687 g/mol | ||
| Smiles String | C1C(C(OC1N2C=NC3=C2N=C(N=C3N)Cl)CO)O | ||
| Melting Point | Not Available | ||
| Water Solubility | Not Available | ||
| State | Solid | ||
| LogP/Hphobicity | 1.57 | ||
| Isoelectric Point | Not Available | ||
| Biotransformation | Metabolized in all cells with deoxycyticine kinase activity to t-chloro-2’-deoxyadenosine-5’-triphosphate | ||
| Half Life | 5.4 hours, with a half life in leukemic cells of 23 hours | ||
| Protein Binding [%] | 20% | ||
| RxList Link | RXlist | ||
| Sponsored links | |||
| Drug Reference |
http://www.drugs.com/cons/Cladribine.html http://www.rxlist.com/cgi/generic3/cladribine.htm http://www.pharmgkb.org/views/index.jsp?objId= | ||
| Drug Type | Approved Drug | ||
| Accession No | APRD00260 | ||
| CAS Registry Number | 4291-63-8 | ||
| KEGG Compound ID | D01370 | ||
| PubChem ID | SID:163106 | ||
| PharmGKB ID | PA449027 | ||
| SwissProt ID | Not Available | ||
| GenBank ID | Not Available | ||
| Drug ID Number [DIN] | 2022117 |
|
Home | About | Cancers | Treatment | Medications Copyright onconews.org 2005. All Rights Reserved. |