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levoleucovorin
- Development stage
- Approved
- Lead developer
- Assertio
- Modality
- Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules, Metabolically Activated Prodrugs → Prodrugs/Conditional Activator Small Molecules → Small Molecules
- Administration
- Intravenous
01
Overview
Levoleucovorin is the pharmacologically active levo-isomer of leucovorin (folinic acid), a chemically reduced derivative of folic acid. It is used as a rescue agent after high-dose methotrexate therapy in osteosarcoma to reduce toxic effects and as an antidote for overdoses or impaired elimination of methotrexate and other folic acid antagonists. Levoleucovorin is also used in combination with fluorouracil for the palliative treatment of advanced metastatic colorectal cancer. Its mechanism involves bypassing dihydrofolate reductase inhibition by providing a source of tetrahydrofolate, thereby allowing DNA synthesis to continue even when methotrexate or similar drugs are present[1][2][4][5].
- Brand names
- FusilevKhapzory
- Other names
- L-leucovorin(6S)-leucovorinfolinic acid levo-isomer
02
Targets
DHFR (Dihydrofolate reductase)Reduced folate-dependent enzymes
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