Drug intelligence / Profile preview

zoledronic acid + letrozole

Development stage
Phase 3
Lead developer
Novartis
Modality
Small Molecules
Administration
Intravenous, Oral
01

Overview

Zoledronic acid + letrozole is a combination therapy used primarily in the treatment of hormone receptor-positive breast cancer in postmenopausal women. Zoledronic acid is a bisphosphonate that inhibits osteoclast-mediated bone resorption by binding to bone hydroxyapatite and inhibiting farnesyl pyrophosphate synthase in the mevalonate pathway. Letrozole is an aromatase inhibitor that blocks estrogen synthesis by inhibiting the aromatase enzyme, thereby reducing estrogen levels and limiting growth stimulation of hormone-sensitive breast cancer cells. The combination has been shown to improve disease-free survival and reduce recurrence risk compared to some other regimens, with additive or synergistic effects on tumor cell apoptosis and prevention of osteoporosis associated with aromatase inhibitor therapy[1][2][3][5][6].

Other names
zoledronic acid + letrozole
02

Targets

CYP19A1 (Aromatase)FDPS (Farnesyl pyrophosphate synthase)

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