Overview

NCI Definition [1]:
A derivative of folic acid with chemoprotectant, antidote and synergistic activity. Leucovorin does not require metabolism by dihydrofolate reductase, the molecular target of folate antagonist-type chemotherapeutic drugs, and is converted to a tetrahydrofolate, which is the necessary folate for purine and pyrimidine synthesis. As this agent allows for some purine/pyrimidine synthesis to occur, the toxic effects of folic acid antagonist-type chemotherapeutic drugs are counteracted while still permitting the antitumor activity of the folic acid antagonist through dihydrofolate reductase inhibition. This agent also potentiates the effects of 5-fluorouracil and its derivatives by stabilizing the binding of 5-fluorouracil's converted form fluorodeoxyuridylic acid to its target enzyme thymidylate synthase, thus prolonging drug activity.

Leucovorin has been investigated in 89 clinical trials, of which 75 are open and 14 are closed. Of the trials investigating leucovorin, 2 are early phase 1 (2 open), 14 are phase 1 (8 open), 15 are phase 1/phase 2 (12 open), 32 are phase 2 (28 open), 2 are phase 2/phase 3 (2 open), 22 are phase 3 (21 open), 1 is phase 4 (1 open), and 1 is no phase specified (1 open).

ERBB2 Amplification, Deficient DNA Mismatch Repair (dMMR), and HER2 Deficient Expression are the most frequent biomarker inclusion criteria for leucovorin clinical trials.

Pancreatic adenocarcinoma, adenocarcinoma of the gastroesophageal junction, and colorectal carcinoma are the most common diseases being investigated in leucovorin clinical trials [2].

Top Biomarker Inclusion Criteria for Open Clinical Trials Investigating Leucovorin
Top Biomarker Inclusion Criteria for Closed Clinical Trials Investigating Leucovorin
This graph displays the 20 most frequently occurring biomarkers curated on clinical trials investigating leucovorin and the cancer types associated with these biomarkers. These numbers are derived from a set of 5,956 clinical trials for which biomarker status defines treatment.

Drug Details

Synonyms [2]:
folinic acid sf, leucovorin, citrovorum factor, folinic acid, leucovorin [chemical/ingredient], 5-formyl-5,6,7,8-tetrahydrofolic acid, 5-formyl-5,6,7,8-tetrahydropteroyl-l-glutamic acid, n5-formyl-5,6,7,8-tetrahydrofolic acid, (5-formyl-5,6,7,8-tetrahydropteroyl)glutamate, dihydrofolic acid, folinic acid product, 5-formyltetrahydrofolic acid, folinic acid (product), 5-formyl-5,6,7,8-tetrahydropteroyl-l-glutamic acid, 5-formyl-5,6,7,8-tetrahydrofolic acid, folinate, leukovorum, acid, folinic, l(-)-5-formyl-5,6,7,8-tetrahydrofolic acid, folinic acid, folinic acid (substance), 5 formyltetrahydropteroylglutamate, 5-formyltetrahydropteroylglutamate, n5-formyltetrahydrofolic acid, dihydrofolic acid (substance), folinic acid-sf, 5-formyl tetrahydrofolate, leucovorin, leucovorinum, 5 formyltetrahydrofolate, citrovorum, n(5)-formyltetrahydrofolate, n-(5-formyl-5,6,7,8-tetrahydropteroyl)-l-glutamic acid, leucovorin®, folinic acid, acide folinique, 5-formyl tetrahydrofolate preparation, leukovorin, formyltetrahydrofolate n 05, 5-formyltetrahydrofolate, l-glutamic acid, n-(4-(((2-amino-5-formyl-1,4,5,6,7,8-hexahydro-4-oxo-6-pteridinyl)methyl)amino)benzoyl)-
NCIT ID [1]:
C71631
SNOMED ID [1]:
F-BB001

References

1. National Cancer Institute. NCI Thesaurus Version 18.11d. https://ncit.nci.nih.gov/ncitbrowser/. [2018-07-30] [2018-08-02].

2. All assertions and clinical trial landscape data are curated from primary sources. You can read more about the curation process here.