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enzalutamide + fulvestrant

Development stage: Unknown
Lead developer: Pfizer
Modality: Small Molecules
Administration: Intramuscular, Oral

Overview

A combination therapy consisting of enzalutamide, an androgen receptor (AR) antagonist, and fulvestrant, a selective estrogen receptor degrader (SERD). This combination targets both hormonal pathways that may contribute to breast cancer progression by blocking androgen receptor signaling and inhibiting estrogen receptor dimerization and translocation into the nucleus while promoting proteasomal degradation of estrogen receptors. It has been investigated primarily for hormone receptor-positive breast cancer and has shown potential in overcoming resistance mechanisms to single-agent therapies.

Brand names: Xtandi + Faslodex
Other names: Enzalutamide and FulvestrantEnzalutamide plus Fulvestrant

Targets

ESR2 (ERβ)AR (Adrenergic receptors)ESR1 (ERα)

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