Raloxifene

Category: pharmacological

Aliases: Evista, keoxifene

Pharmacological Mechanism

A benzothiophene selective estrogen receptor modulator (SERM): an estrogen-receptor antagonist in breast and uterine tissue but an agonist in bone, where it reduces osteoclastic resorption and preserves bone mineral density. Approved for postmenopausal osteoporosis and breast-cancer-risk reduction; used off-label in PCT as an estrogen-antagonist alternative to aromatase inhibitors.

Half-Life (t½)

PO: 32.5h

Dosing Guidelines

• PO: Typical 60 (Range: 30–120)

Target Organ Systems

• endocrine
• reproductive
• musculoskeletal

Notes

PubChem CID 5035 (free base). PK: Snyder 2000 (PMID:11006795) verbatim "the elimination half-life averages 32.5 hours." Occupancy SKIP — only verbatim value is an antagonist IC50 (1 nM, Fitzpatrick 1999 PMID:10465261), incompatible with the agonist model (see AUTHORING_GAPS).

Chemical Identifiers

• PubChem CID: 5035
• Formula: C28H27NO4S
• Molecular weight: 473.6 g/mol
• InChIKey: GZUITABIAKMVPG-UHFFFAOYSA-N
• SMILES: C1CCN(CC1)CCOC2=CC=C(C=C2)C(=O)C3=C(SC4=C3C=CC(=C4)O)C5=CC=C(C=C5)O

References

• PMID 11006795