Overview

Generic Name(s):
letrozole
Trade Name(s):
Femara
NCI Definition [1]:
A nonsteroidal inhibitor of estrogen synthesis with antineoplastic activity. As a third-generation aromatase inhibitor, letrozole selectively and reversibly inhibits aromatase, which may result in growth inhibition of estrogen-dependent breast cancer cells. Aromatase, a cytochrome P-450 enzyme localized to the endoplasmic reticulum of the cell and found in many tissues including those of the premenopausal ovary, liver, and breast, catalyzes the aromatization of androstenedione and testosterone into estrone and estradiol, the final step in estrogen biosynthesis.

Biomarker-Directed Therapies

Letrozole has been investigated in 108 clinical trials, of which 81 are open and 27 are closed. Of the trials investigating letrozole, 6 are early phase 1 (4 open), 18 are phase 1 (15 open), 11 are phase 1/phase 2 (11 open), 53 are phase 2 (36 open), 4 are phase 2/phase 3 (3 open), 12 are phase 3 (10 open), 1 is phase 4 (0 open), and 3 are no phase specified (2 open).

ER Positive, HER2 Deficient Expression, and HER2 Negative are the most frequent biomarker inclusion criteria for letrozole clinical trials.

Breast carcinoma, invasive breast carcinoma, and breast adenocarcinoma are the most common diseases being investigated in letrozole clinical trials [2].

Top Biomarker Inclusion Criteria for Open Clinical Trials Investigating Letrozole
Top Biomarker Inclusion Criteria for Closed Clinical Trials Investigating Letrozole
This graph displays the 20 most frequently occurring biomarkers curated on clinical trials investigating letrozole 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]:
Femara, letrozole, ltz, letrozol, cgs-20267, 4,4'-(1h-1,2,4-triazol-1-yl-methylene)-bis(benzonitrile), letrozole (substance), femara®, 719345, benzonitrile, 4,4'-(1h-1,2,4-triazol-1-ylmethylene)bis-, 112809-51-5, letrozole (product), fémara, cgs 20267, 4,4'-(1h-1,2,4triazol-1-ylmethylene)dibenzonitrile, novartis brand of letrozole, letrozole [chemical/ingredient], letrozole
Drug Categories [2]:
Aromatase inhibitors
Drug Target(s) [2]:
CYP19A1
NCIT ID [1]:
C1527
SNOMED ID [1]:
F-61B25

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.