Pharmacokinetic and pharmacodynamic analysis of fulvestrant in preclinical models of breast cancer to assess the importance of its estrogen receptor-α degrader activity in antitumor efficacy

• Published in: Breast cancer research and treatment Vol. 179; no. 1; pp. 67 - 77
• Main Authors: Wardell, Suzanne E., Yllanes, Alexander P., Chao, Christina A., Bae, Yeeun, Andreano, Kaitlyn J., Desautels, Taylor K., Heetderks, Kendall A., Blitzer, Jeremy T., Norris, John D., McDonnell, Donald P.
• Format: Journal Article
• Language: English
• Published: New York Springer US 01.01.2020; Springer Nature B.V
• Subjects: 1-Phosphatidylinositol 3-kinase; Administration, Oral; Animal models; Animals; Antineoplastic Agents, Hormonal - administration & dosage; Antineoplastic Agents, Hormonal - pharmacokinetics; Antitumor activity; Breast cancer; Breast Neoplasms - drug therapy; Cancer research; Dose-Response Relationship, Drug; Endocrine therapy; Estrogen Receptor alpha - antagonists & inhibitors; Estrogen Receptor Antagonists - administration & dosage; Estrogen Receptor Antagonists - pharmacokinetics; Estrogen receptors; Female; Fulvestrant; Fulvestrant - administration & dosage; Fulvestrant - pharmacokinetics; Medicine; Medicine & Public Health; Menopause; Metastases; Mice; Oncology; Pharmacodynamics; Pharmacokinetics; Preclinical Study; Tumors; Xenograft Model Antitumor Assays; Xenografts; Endocrine resistant breast cancer; Selective estrogen receptor downregulator; Fulvestrant

Purpose Fulvestrant is a selective estrogen receptor downregulator (SERD) that is approved for first- or second-line use as a single agent or in combination with cyclin dependent kinase or phosphatidylinositol 3-kinase inhibitors for the treatment of metastatic breast cancer. Fulvestrant exhibits ex...