Stereochemistry | EPIMERIC |
Molecular Formula | C20H23N7O7 |
Molecular Weight | 473.4393 |
Optical Activity | UNSPECIFIED |
Defined Stereocenters | 1 / 2 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
NC1=NC(=O)C2=C(NCC(CNC3=CC=C(C=C3)C(=O)N[C@@H](CCC(O)=O)C(O)=O)N2C=O)N1
InChI
InChIKey=VVIAGPKUTFNRDU-ABLWVSNPSA-N
InChI=1S/C20H23N7O7/c21-20-25-16-15(18(32)26-20)27(9-28)12(8-23-16)7-22-11-3-1-10(2-4-11)17(31)24-13(19(33)34)5-6-14(29)30/h1-4,9,12-13,22H,5-8H2,(H,24,31)(H,29,30)(H,33,34)(H4,21,23,25,26,32)/t12?,13-/m0/s1
Leucovorin is a compound similar to folic acid, which is a necessary vitamin. It has been around and in use for many decades. Leucovorin is a medication frequently used in combination with the chemotherapy drugs fluoruracil and methotrexate. Leucovorin is not a chemotherapy drug itself, however it is used in addition to these chemotherapy drugs to enhance anticancer effects (with fluorouracil) or to help prevent or lessen side effects (with methotrexate). Leucovorin is also used by itself to treat certain anemia problems when folic acid deficiency is present.
CNS Activity
Originator
Approval Year
AUC
Doses
AEs
Overview
CYP3A4 | CYP2C9 | CYP2D6 | hERG |
---|---|---|---|
OverviewOther
Other Inhibitor | Other Substrate | Other Inducer |
---|---|---|
Drug as perpetrator
Drug as victim
Sourcing
PubMed
Sample Use Guides
200 mg/m2 or 20 mg/m2 in Advanced Colorectal Cancer, 10 mg/m2 in Leucovorin Rescue After High-Dose Methotrexate Therapy and up to 1 mg daily in Megaloblastic Anemia Due to Folic Acid Deficiency.
Route of Administration:
Intravenous
RPMI 1788 cells revealed a high intrinsic resistance to methotrexate (MTX). The cytotoxic effect of high concentrations of MTX (10 -5 M) was reversed by relatively low (10 -6 M) concentrations of simultaneously added leucovorin (LV). The enhancement of cell survival was less marked when LV application was delayed for 12 h.