2. Academic Validation
  3. Fulvestrant-3 Boronic Acid (ZB716): An Orally Bioavailable Selective Estrogen Receptor Downregulator (SERD)

Fulvestrant-3 Boronic Acid (ZB716): An Orally Bioavailable Selective Estrogen Receptor Downregulator (SERD)

  • J Med Chem. 2016 Sep 8;59(17):8134-40. doi: 10.1021/acs.jmedchem.6b00753.
Jiawang Liu 1,  Shilong Zheng 1,  Victoria L Akerstrom 2,  Chester Yuan 3,  Youning Ma 3,  Qiu Zhong 1,  Changde Zhang 1,  Qiang Zhang 1,  Shanchun Guo 1,  Peng Ma 4,  Elena V Skripnikova 4,  Melyssa R Bratton 4,  Antonio Pannuti 2,  Lucio Miele 2,  Thomas E Wiese 4,  Guangdi Wang 1
Affiliations

Affiliations

  • 1 RCMI Cancer Research Center, Xavier University of Louisiana , New Orleans, Louisiana 70125, United States.
  • 2 Stanley S. Scott Cancer Center, Louisiana State University Health Sciences Center , New Orleans, Louisiana 70112, United States.
  • 3 Xiamen Medichance Laboratory , Xiamen 361022, China.
  • 4 College of Pharmacy, Xavier University of Louisiana , New Orleans, Louisiana 70125, United States.
PMID: 27529700 DOI: 10.1021/acs.jmedchem.6b00753
Abstract

Orally bioavailable SERDs may offer greater systemic drug exposure, improved clinical efficacy, and more durable treatment outcome for patients with ER-positive endocrine-resistant breast Cancer. We report the design and synthesis of a boronic acid modified fulvestrant (5, ZB716), which binds to ERα competitively (IC50 = 4.1 nM) and effectively downregulates ERα in both tamoxifen-sensitive and tamoxifen-resistant breast Cancer cells. Furthermore, It has superior oral bioavailability (AUC = 2547.1 ng·h/mL) in mice, indicating its promising clinical utility as an oral SERD.

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