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Leucovorin
drug data and news
Leucovorin 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 | Leucovorin | ||
| Brand Names/Synonyms | Acide Folinique; C03479; Calcium Citrovorum Factor; Calcium Folinate; Citrovorum Factor; Folinic Acid; Folinic Acid Calcium Salt; Folinic Acid-Sf; Folinic Acid-Sf, Calcium Salt; Folinic Acidcalcium Salt Usp27; L-Leucovorin; Leucal; Leucovorin Calcium; Leucovorin Calcium Preservative Free; Leucovorin Folinic Acid; Leucovorin [Usan]; Wellcovorin | ||
| Indication | Used to treat osteosarcoma (after high dose methotrexate therapy), to diminish the toxicity and counteract the effects of impaired methotrexate elimination and of inadvertent overdosages of folic acid antagonists, and to treat megaloblastic anemias due to folic acid deficiency. Also used in combination with 5-fluorouracil to prolong survival in the palliative treatment of patients with advanced colorectal cancer. | ||
| Sponsored links | Description | Not Available | |
| Pharmacology | Leucovorin is one of several active, chemically reduced derivatives of folic acid. It is useful as an antidote to drugs which act as folic acid antagonists. Leucovorin is a mixture of the diastereoisomers of the 5-formyl derivative of tetrahydrofolic acid (THF). The biologically active compound of the mixture is the (-)-l-isomer, known as Citrovorum factor or (-)-folinic acid. Leucovorin does not require reduction by the enzyme dihydrofolate reductase in order to participate in reactions utilizing folates as a source of “one-carbon” moieties. Administration of leucovorin can counteract the therapeutic and toxic effects of folic acid antagonists such as methotrexate, which act by inhibiting dihydrofolate reductase. Leucovorin has also been used to enhance the activity of fluorouracil. | ||
| Mechanism Of Action | As leucovorin is a derivative of folic acid, it can be used to increase levels of folic acid under conditions favoring folic acid inhibition (following treatment of folic acid antagonists such as methotrexate). Leucovorin enhances the activity of fluorouracil by stabilizing the bond of the active metabolite (5-FdUMP) to the enzyme thymidylate synthetase. | ||
| Leucovorin News (When available) |
Pro-Pharmaceuticals to Present Abstract & Poster at Mass ... Mar 2, 2006 Patients Prefer Xeloda® Over 5-FU for Colon Cancer Cancer Feb 14, 2006 ADVENTRX CoFactor Phase IIb Trial Surpasses 50% Enrollment ... Feb 14, 2006 Chemotherapy Given Directly to Liver Improves Survival for ... Feb 27, 2006 Recruitment Temporarily Suspended In An International Phase III ... Feb 20, 2006 Avastin May Cause Leukoencephalopathy Syndrome Mar 2, 2006 Recruitment Temporarily Suspended in an International Phase III ... Feb 12, 2006 CoFactor™ (5,10-methylenetetrahydrofolate) May Enhance Activity ... Feb 3, 2006 Oxaliplatin Safely Stopped with FOLFOX Regimen for Colorectal ... Feb 21, 2006 Xaliproden Reduces Occurrence Of Severe Peripheral Sensory ... Feb 23, 2006 Cancer Drug Trial on Hold Feb 13, 2006 Genentech stops colon-cancer study Feb 13, 2006 Genentech/Roche: trial delay won't choke Avastin's growth Feb 13, 2006 Study Sets Treatment Standard for Elderly With Colon Cancer Feb 10, 2006 Colon cancer chemotherapies OK for elderly Feb 10, 2006 Pro-Pharmaceuticals Announces $10 Million Financing Feb 15, 2006 Roche halts enrollment in Avastin trial Feb 13, 2006 CoFactor™ Plus 5-FU Provides Large Response in Metastatic ... Feb 1, 2006 Xaliproden May Reduce Side Effect Caused by Eloxatin® in ... Feb 6, 2006 Patients Prefer Xeloda® to 5-Flurouracil in Treatment of ... Feb 15, 2006 Xaliproden May Reduce Side Effect Caused by Eloxatin® in ... Feb 2, 2006 | ||
| Dosage Forms | LIQUID; POWDER FOR SOLUTION; SOLUTION; TABLET | ||
| Drug_Category | Hematinics; Antihypertensive Agents; Methotrexate Antidote; Unclassified Therapeutic Agents (92:00.00); | ||
| Absorption | Following oral administration, leucovorin is rapidly absorbed. The apparent bioavailability of leucovorin was 97% for 25 mg, 75% for 50 mg, and 37% for 100 mg. | ||
| Interactions |
Interactions for Leucovorin: Folic acid in large amounts may counteract the antiepileptic effect of phenobarbital, phenytoin and primidone, and increase the frequency of seizures in susceptible pediatric patients. Preliminary animal and human studies have shown that small quantities of systemically administered leucovorin enter the CSF primarily as 5-methyltetrahydro-folate and, in humans, remain 1 to 3 orders of magnitude lower than the usual methotrexate concentrations following intrathecal administration. However, high doses of leucovorin may reduce the efficacy of intrathecally administered methotrexate. Leucovorin may enhance the toxicity of 5-fluorouracil. | ||
| Toxicity | Oral, rat LD50: >8000 mg/kg. Excessive amounts of leucovorin may nullify the chemotherapeutic effect of folic acid antagonists. | ||
| Organisms Affected | Humans and other mammals | ||
| Chemical IUPAC Name | 2-[4-[(2-amino-5-formyl-4-oxo-5,6,7,8-tetrahydro-1H-pteridin-6-yl)methylamino]benzoyl]aminopentanedioicacid | ||
| Chemical Formula | C20H23N7O7 | ||
| Molecular Weight | 473.44 g/mol | ||
| Smiles String | C1C(N(C2=C(N1)NC(=NC2=O)N)C=O)CNC3=CC=C(C=C3)C(=O)NC(CCC(=O)O)C(=O)O | ||
| Melting Point | Not Available | ||
| Water Solubility | Complete | ||
| State | Solid | ||
| LogP/Hphobicity | -1.744 | ||
| Isoelectric Point | Not Available | ||
| Biotransformation | Hepatic and intestinal mucosal, the main metabolite being the active 5-methyltetrahydrofolate. Leucovorin is readily converted to another reduced folate, 5,10-methylenetetrahydrofolate, which acts to stabilize the binding of fluorodeoxyridylic acid to thymidylate synthase and thereby enhances the inhibition of this enzyme. | ||
| Half Life | 6.2 hours | ||
| Protein Binding [%] | ~15% | ||
| RxList Link | RXlist | ||
| Sponsored links | |||
| Drug Reference |
http://www.drugs.com/cons/Leucovorin.html http://www.rxlist.com/cgi/generic2/leucovorin.htm | ||
| Drug Type | Approved Drug | ||
| Accession No | APRD00698 | ||
| CAS Registry Number | 1492-18-8 | ||
| KEGG Compound ID | C12611 | ||
| PubChem ID | SID:148853 | ||
| PharmGKB ID | PA450198 | ||
| SwissProt ID | Not Available | ||
| GenBank ID | Not Available | ||
| Drug ID Number [DIN] | 2182998 |
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