Drug intelligence / Profile preview

anastrozole + everolimus

Development stage
Phase 3
Lead developer
AstraZeneca
Modality
Small Molecules
Administration
Oral
01

Overview

Combination of anastrozole and everolimus is a therapeutic regimen combining two drugs with complementary mechanisms to treat hormone receptor-positive cancers, primarily breast cancer. Anastrozole is an aromatase inhibitor that reduces estrogen production by inhibiting the aromatase enzyme, thereby lowering estrogen levels which fuel certain breast cancers. Everolimus is an mTOR (mammalian target of rapamycin) inhibitor that blocks the PI3K/AKT/mTOR signaling pathway involved in cell growth and proliferation. This combination aims to overcome resistance to hormone therapy by targeting both estrogen production and downstream signaling pathways promoting tumor growth. The combination has been studied in heavily pretreated patients with ER and/or PR-positive metastatic breast, ovarian, and endometrial cancers. It was found to be well tolerated at full approved doses (anastrozole 1 mg daily; everolimus 10 mg daily) with clinical activity including stable disease ≥6 months, partial responses, and complete responses observed especially in patients harboring molecular alterations in the PI3K/AKT/mTOR pathway such as PIK3CA mutations or PTEN loss[1].

02

Targets

CYP19A1 (Aromatase)Mechanistic target of rapamycin complex 1

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