Drug intelligence / Profile preview

letrozole + capecitabine

Development stage
Unknown
Lead developer
Novartis
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules, Metabolically Activated Prodrugs → Prodrugs/Conditional Activator Small Molecules → Small Molecules, Nucleic Acid-Directed Small Molecules → Small Molecules
Administration
Oral
01

Overview

Letrozole + capecitabine is an oral combination regimen used primarily in the treatment of hormone receptor-positive, HER2-negative metastatic breast cancer. Letrozole is a nonsteroidal aromatase inhibitor that suppresses estrogen synthesis by inhibiting the aromatase enzyme, thereby reducing tumor growth in estrogen-dependent cancers. Capecitabine is a prodrug of 5-fluorouracil (5-FU), an antimetabolite that interferes with DNA synthesis and induces cytotoxicity in rapidly dividing cells. The combination leverages both endocrine therapy (letrozole) and chemotherapy (capecitabine), aiming to improve progression-free survival and response rates compared to monotherapy, especially where CDK4/6 inhibitors are unavailable or unsuitable. Clinical studies have shown this regimen has an acceptable safety profile consistent with known toxicities of each agent[1][2][7].

Other names
XELIA
02

Targets

TS (Thymidylate synthase)CYP19A1 (Aromatase)

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