Drug intelligence / Profile preview

sacituzumab govitecan + anastrozole + exemestane

Development stage
Unknown
Lead developer
Gilead Sciences
Modality
Small Molecules, Cytotoxic ADCs → Antibody-Drug Conjugates (ADCs) → Antibody Conjugates → Antibody-Based Therapeutics
Administration
Intravenous, Oral
01

Overview

This combination therapy consists of the trophoblast cell-surface antigen 2 (Trop-2)-directed antibody-drug conjugate (ADC) sacituzumab govitecan and the aromatase inhibitors anastrozole or exemestane. It is being evaluated by Hunan Cancer Hospital in the Phase Ib/II SoGreat trial for patients with hormone receptor-positive (HR+), HER2-negative metastatic breast cancer who have progressed on CDK4/6 inhibitors. Sacituzumab govitecan delivers the topoisomerase I inhibitor payload SN-38 directly to Trop-2-expressing cancer cells, while anastrozole and exemestane inhibit the enzyme aromatase, thereby reducing systemic estrogen levels and slowing the growth of hormone-sensitive tumors. The combination aims to overcome resistance to endocrine therapy by simultaneously targeting Trop-2 and the estrogen signaling pathway.

Other names
Sacituzumab Govitecan + Endocrine TherapySacituzumab Govitecan + Aromatase Inhibitors
02

Targets

TOP1 (DNA Topoisomerase I)CYP19A1 (Aromatase)TACSTD2 (Tumor-associated calcium signal transducer 2)

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