Bexirestrant

Bexirestrant is an orally active ER-α degrader. Bexirestrant can be used for the research of antiestrogen, antineoplastic[1][2].

Signaling Pathways >> Others >> Estrogen Receptor/ERR

Research Areas >> Cancer

Bexirestrant (compound Formula Ia) inhibits the growth of wild type (WT), Y537S and D538G mutated MCF-7 cells with IC50s of 0.3. 6.0, 2.2 nM, respectively[1]. Bexirestrant induces the ER-α degradation in WT, Y537S and D538G mutated MCF-7 cells with IC50s of 0.3. 19.6, 12.7 nM, respectively[1]. Bexirestrant shows 16.3% ER-α remaining in WT MCF-7 cells at concentration of 1 nM[1].

Bexirestrant (50mg/kg; p.o.; 28 days) shows a good efficacy in an MCF-Y537S xenograft[1].Pharmacokinetic parameters in rat at 50 mg/kg p.o. dose[1]： Tmax (h) Cmax (ng/mL) AUClast (hr× ng/mL) AUCinf_obs (hr×ng/mL) T1/2 (h) 4.00 343 7582 9804 26 Animal Model: Female athymic nude mice harboring subcutaneous MCF7-Y537S xenograft[1] Dosage: 50mg/kg Administration: p.o. for 28 days Result: Showed 56% tumor growth inhibition compared to vehicle group after 28 days.

[1]. Ranjan Kumar Pal, et al, Selective estrogen receptor degrader. WO2021014386 A1.

[2]. WHO Drug Information, Vol. 35, No. 4, 2021. Geneva: World Health Organization; 2022.