Drug intelligence / Profile preview

letrozole + cyclophosphamide

Development stage
Unknown
Lead developer
Novartis
Modality
DNA Intercalators/Alkylators → Nucleic Acid-Directed Small Molecules → Small Molecules
Administration
Oral, Intravenous
01

Overview

Letrozole + cyclophosphamide is a combination therapy consisting of letrozole, an aromatase inhibitor, and cyclophosphamide, an alkylating agent. This regimen is primarily investigated and used in the treatment of hormone receptor-positive breast cancer, particularly in postmenopausal women. Letrozole works by inhibiting the enzyme aromatase, thereby reducing estrogen production and limiting the growth stimulus for estrogen-dependent tumors. Cyclophosphamide acts as a cytotoxic agent that crosslinks DNA strands, leading to apoptosis of rapidly dividing cells. When administered together—often with metronomic (low-dose continuous) scheduling—this combination has demonstrated synergistic effects on tumor cell cytotoxicity and apoptosis beyond what either drug achieves alone. The regimen has shown promising results as neoadjuvant or primary systemic therapy in elderly patients with breast cancer[1][2][3][6].

Other names
metronomic cyclophosphamide + letrozoleoral cyclophosphamide + letrozole
02

Targets

DNACYP19A1 (Aromatase)

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