Drug intelligence / Profile preview

zb716

Development stage
Phase 2
Lead developer
EnhancedBio
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules
Administration
Oral
01

Overview

ZB716 is a synthetic steroidal selective estrogen receptor degrader (SERD), structurally analogous to fulvestrant but modified with a boronic acid group at the C3 position. Unlike fulvestrant—which requires intramuscular injection—ZB716 is orally bioavailable and demonstrates superior systemic exposure and tumor tissue penetration in preclinical models. It binds to the estrogen receptor alpha (ERα), induces its degradation, and blocks ER-mediated signaling pathways that drive the growth of ER-positive breast cancer cells. Preclinical studies show that ZB716 effectively inhibits tumor growth in both cell line-derived and patient-derived xenograft models of endocrine-resistant breast cancer. The drug is under development primarily for the treatment of ER-positive metastatic breast cancer[1][2][3][4][5][6][7].

Brand names
Borestrant
Other names
fulvestrant-3-boronic acidfulvestrant3-boronic acidfulvestrant 3-boronic acidfulvestrant-3-boronoatefulvestrant3-boronoatefulvestrant 3-boronoateB-((7alpha,17beta)-17-Hydroxy-7-(9-((4,4,5,5,5-pentafluoropentyl)sulfinyl)nonyl)estra-1,3,5(10)-trien-3-yl)boronic acid
02

Targets

ESR1 (ERα)

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