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rintodestrant
- Development stage
- Phase 1
- Lead developer
- G1 Therapeutics
- Modality
- Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules, Allosteric Modulators → Classical Binding Small Molecules → Small Molecules
- Administration
- Oral
01
Overview
Rintodestrant is an orally available, non-steroidal small molecule selective estrogen receptor degrader (SERD) developed by G1 Therapeutics. It competitively binds to the estrogen receptor alpha (ERα/ESR1), induces a conformational change that promotes ERα degradation and downregulation, thereby blocking ER-mediated signaling. This mechanism inhibits the growth and survival of ER-positive breast cancer cells, including those resistant to other endocrine therapies. Rintodestrant was evaluated as monotherapy and in combination with palbociclib in patients with advanced or metastatic ER+/HER2– breast cancer[1][2][3][4][6].
- Other names
- rintodestrantG1T-48G-1T-48G 1T-48XR5-28XR-5-28XR 5-28
02
Targets
ESR1 (ERα)
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