Fulvestrant: pharmacokinetics and pharmacology.
Fulvestrant is a new type of oestrogen receptor (ER) antagonist with no agonist activity and a novel pharmacological profile. Fulvestrant has been shown to significantly reduce cellular levels of the ER and progesterone receptor in both preclinical studies and in clinical trials of postmenopausal women with primary breast cancer. This paper reviews the pharmacokinetics and metabolism of fulvestrant, which support the rationale for drug delivery as a single, once-monthly intramuscular injection, and show that this agent has minimal potential to be the subject, or cause, of significant cytochrome p450-mediated drug interactions.
Robertson
J F R
JF
Unit of Surgery, City Hospital, Nottingham NG5 1PB, UK. john.robertson@nottingham.ac.uk
Harrison
M
M
D000818:Animals; D001943:Breast Neoplasms / Q000188:drug therapy; D002986:Clinical Trials as Topic; D004958:Estradiol / Q000031:analogs & derivatives* / Q000493:pharmacokinetics* / Q000494:pharmacology*; D004965:Estrogen Antagonists / Q000493:pharmacokinetics* / Q000494:pharmacology*; D020847:Estrogen Receptor Modulators / Q000493:pharmacokinetics / Q000494:pharmacology; D005260:Female; D000077267:Fulvestrant; D006801:Humans
D004965:Estrogen Antagonists; D020847:Estrogen Receptor Modulators; D000077267:Fulvestrant; D004958:Estradiol