Rintodestrant

Rintodestrant (G1T48) is an orally active, non-steroidal and selective estrogen receptor degrader. Rintodestrant (G1T48) is also a CDK4/6 inhibitor[1].

Signaling Pathways >> Others >> Estrogen Receptor/ERR

Research Areas >> Cancer

Signaling Pathways >> Cell Cycle/DNA Damage >> CDK

Rintodestrant (G1T48) is a potent and efficacious inhibitor of estrogen-mediated transcription and proliferation in ER-positive breast cancer cells, similar to the pure antiestrogen fulvestrant[1]. Rintodestrant (G1T48) selectively inhibits the growth of ER-positive, but not ER-negative, breast cancer cells[1]. Cell Viability Assay[1] Cell Line: MCF7 cells. Concentration: 1 pM-1 μM. Incubation Time: 18 h. Result: Downregulates the estrogen receptor in breast cancer cells. Significantly inhibited estrogen-mediated growth of MCF7 cells demonstrating approximately threefold higher potency when compared to Fulvestrant. Does not impact apoptosis in MCF7 breast cancer cells.

Rintodestrant (G1T48, 30 or 100 mg/kg) inhibits estrogen signaling in endocrine-resistant breast cancer models[1]. Animal Model: MCF7 xenograft tumors[1]. Dosage: 30 or 100 mg/kg. Administration: P.O. daily for 28 days. Result: Demonstrated dose-dependent inhibition of TamR tumor growth.

[1]. Kaitlyn J Andreano, et al. G1T48, an oral selective estrogen receptor degrader, and the CDK4/6 inhibitor lerociclib inhibit tumor growth in animal models of endocrine-resistant breast cancer. Breast Cancer Res Treat. 2020 Apr;180(3):635-646.