Definition
The active metabolite of FOLIC ACID. Leucovorin is used principally as an antidote to FOLIC ACID ANTAGONISTS.
The active metabolite of folic acid. Leucovorin is used principally as its calcium salt as an antidote to folic acid antagonists which block the conversion of folic acid to folinic acid. [HMDB]
Description
The active metabolite of Folic acid, Pteroyl-D-glutamic acid is used principally as its calcium salt as an antidote to folic acid antagonists which block the conversion of folic acid to folinic acid. Folic acid, a water-soluble B-complex vitamin, is found in foods such as liver, kidneys, yeast, and leafy, green vegetables. Folic acid is used to diagnose folate deficiency and to treat topical sprue and megaloblastic and macrocytic anemias, hematologic complications resulting from a deficiency in folic acid. A member of the vitamin B family that stimulates the hematopoietic system. It is present in the liver and kidney and is found in mushrooms, spinach, yeast, green leaves, and grasses (poaceae). Folic acid is used in the treatment and prevention of folate deficiencies and megaloblastic anemia.
Top Gene Interactions
Related Pathways
General Information
- Metabolism: 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
- Uses/Sources: For the treatment of osteosarcoma (after high dose methotrexate therapy). Used 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. Used in cancer chemotherapy involving the drug methotrexate.
- Health Effects: Should not be administered intrathecally as this may produce severe adverse effects or even death when administered. [Wikipedia]. Allergic sensitization (<1%), including anaphylactoid reactions
- Symptoms: Excessive amounts of leucovorin may nullify the chemotherapeutic effect of folic acid antagonists.
- Route of Exposure: 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.
Toxicity
- Carcinogenicity: No indication of carcinogenicity to humans (not listed by IARC).
- Toxicity: LD50: >8000 mg/kg (oral, rats).
Leucovorin Interacts with Diseases
| Disease | Inference Score | References/Inference Genes |
| Colorectal cancer | 29.01 |
References/Inference Genes
|
| Stomach Neoplasms | 28.07 | |
| Colonic neoplasm | 26.51 |
References/Inference Genes
|
| Reperfusion Injury | 13.26 | |
| Esophageal squamous cell carcinoma | 12.45 | |
| Lipoid congenital adrenal hyperplasia | 11.51 |
|
| Breast carcinoma | 11.06 | |
| Calcinosis | 10.83 |
|
| Uterine Cervical Neoplasms | 10.55 |
References/Inference Genes
|
| Hepatocellular carcinoma | 10.37 | |
| Infertility, Female | 10.27 |
|
| Nervous System Diseases | 10.22 | |
| Chronic lymphocytic leukemia | 10.12 |
References/Inference Genes
|
| Lung Neoplasms | 9.99 | |
| Stroke | 9.24 | |
| Urinary Bladder Neoplasms | 9.17 | |
| Brain Ischemia | 9.16 | |
| Prostatic Neoplasms | 9.08 | |
| Diabetic Angiopathies | 9.02 |
|
| Cleft lip | 8.94 |
|