Letrozole

Letrozole, sold under the brand name Femara among others, is an aromatase inhibitor medication that is used in the treatment of breast cancer.

Letrozole
Clinical data
Trade namesFemara, others
AHFS/Drugs.comMonograph
MedlinePlusa698004
License data
Routes of
administration
By mouth
Drug classAromatase inhibitor; Antiestrogen
ATC code
Legal status
Legal status
Pharmacokinetic data
Bioavailability99.9%
Protein binding60%, mainly to albumin
Metabolismpharmacologically-inactive metabolites Bis(4-cyanophenyl)methanol and 4,4'-dicyanobenzophenone.
Elimination half-life2 days
ExcretionKidney
Identifiers
  • 4,4'-((1H-1,2,4-triazol-1-yl)methylene)dibenzonitrile
CAS Number
PubChem CID
IUPHAR/BPS
DrugBank
ChemSpider
UNII
KEGG
ChEBI
ChEMBL
CompTox Dashboard (EPA)
ECHA InfoCard100.200.357
Chemical and physical data
FormulaC17H11N5
Molar mass285.310 g·mol−1
3D model (JSmol)
  • N#Cc1ccc(cc1)C(c2ccc(C#N)cc2)n3ncnc3
  • InChI=1S/C17H11N5/c18-9-13-1-5-15(6-2-13)17(22-12-20-11-21-22)16-7-3-14(10-19)4-8-16/h1-8,11-12,17H Y
  • Key:HPJKCIUCZWXJDR-UHFFFAOYSA-N Y
  (verify)

It was patented in 1986 and approved for medical use in 1996. In 2020, it was the 257th most commonly prescribed medication in the United States, with more than 1 million prescriptions. It is on the World Health Organization's List of Essential Medicines.

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