Fulvestrant

hormone · endocrine · reproductive · Intramuscular

Fulvestrant, a hormone. Pure estrogen receptor antagonist + degrader — binds ER, blocks dimerization and DNA binding, marks ER for… Intramuscular half-life 50 d.

Pure estrogen receptor antagonist + degrader — binds ER, blocks dimerization and DNA binding, marks ER for proteasomal degradation. IM depot for advanced ER-positive breast cancer. No agonist activity (unlike tamoxifen) → no endometrial-cancer risk.

Pharmacokinetics

• Intramuscular — t½ 50.0 d · F 100% · ka 0.000589 h⁻¹ · Vd 200 L

Sources: PMID:12867220, PMID:15170367, PMID:12672240