Folinic acid (BioDeep_00000017460)

描述信息

(6S)-5-formyltetrahydrofolic acid is the pharmacologically active (6S)-stereoisomer of 5-formyltetrahydrofolic acid. It has a role as an antineoplastic agent and a metabolite. It is a conjugate acid of a (6S)-5-formyltetrahydrofolate(2-).
Levoleucovorin is the enantiomerically active form of Folinic Acid (also known as 5-formyl tetrahydrofolic acid or leucovorin). Commercially available leucovorin is composed of a 1:1 racemic mixture of the dextrorotary and levorotary isomers, while levoleucovorin contains only the pharmacologically active levo-isomer. In vitro, the levo-isomer has been shown to be rapidly converted to the biologically available methyl-tetrahydrofolate form while the dextro form is slowly excreted by the kidneys. Despite this difference in activity, the two commercially available forms have been shown to be pharmacokinetically identical and may be used interchangeably with limited differences in efficacy or side effects (Kovoor et al, 2009). As folate analogs, levoleucovorin and leucovorin are both used to counteract the toxic effects of folic acid antagonists, such as methotrexate, which act by inhibiting the enzyme dihydrofolate reductase (DHFR). They are indicated for use as rescue therapy following use of high-dose methotrexate in the treatment of osteosarcoma or for diminishing the toxicity associated with inadvertent overdosage of folic acid antagonists. Levoleucovorin, as the product Fusilev (FDA), has an additional indication for use in combination chemotherapy with 5-fluorouracil in the palliative treatment of patients with advanced metastatic colorectal cancer. Folic acid is an essential B vitamin required by the body for the synthesis of purines, pyrimidines, and methionine before incorporation into DNA or protein. However, in order to function in this role, it must first be reduced by the enzyme dihydrofolate reductase (DHFR) into the cofactors dihydrofolate (DHF) and tetrahydrofolate (THF). This important pathway, which is required for de novo synthesis of nucleic acids and amino acids, is disrupted when high-dose methotrexate is used for cancer therapy. As methotrexate functions as a DHFR inhibitor to prevent DNA synthesis in rapidly dividing cells, it also prevents the formation of DHF and THF. This results in a deficiency of coenzymes and a resultant buildup of toxic substances that are responsible for numerous adverse side effects of methotrexate therapy. As levoleucovorin and leucovorin are analogs of tetrahydrofolate (THF), they are able to bypass DHFR reduction and act as a cellular replacement for the co-factor THF, thereby preventing these toxic side effects.
Levoleucovorin is a Folate Analog.
Levoleucovorin is a natural product found in Homo sapiens with data available.
Levoleucovorin is the active l-isomer of the racemic mixture of the 5-formyl derivative of tetrahydrofolic acid. Metabolically active, l-leucovorin, also known levoleucovorin, does not require bioactivation by dihydrofolate reductase, an enzyme inhibited by folic acid antagonists. This agent may enhance the effects of fluoropyrimidines by stabilizing their binding to the enzyme thymidylate synthase. (NCI04)
5-Formyltetrahydrofolic acid is a metabolite found in or produced by Saccharomyces cerevisiae.
A folate analog consisting of the pharmacologically active isomer of LEUCOVORIN.
See also: Levoleucovorin Calcium (active moiety of); Levoleucovorin disodium (active moiety of).
Folinic acid (CAS: 58-05-9), also known as leucovorin, is a medication used to decrease the toxic effects of methotrexate (a chemotherapy agent and immune system suppressant) and pyrimethamine (Wikipedia). Folinic acid is 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.
D020011 - Protective Agents > D000931 - Antidotes
C2140 - Adjuvant > C2078 - Folic Acid Derivative
Folinic acid (Leucovorin) is a biological folic acid and is generally administered along with Methotrexate (MTX) (HY-14519) as a rescue agent to decrease MTX-induced toxicity[1].
Folinic acid (Leucovorin) is a biological folic acid and is generally administered along with Methotrexate (MTX) (HY-14519) as a rescue agent to decrease MTX-induced toxicity[1].

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