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elacestrant + onapristone
- Development stage
- Unknown
- Lead developer
- Context Therapeutics
- Modality
- Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules, Molecular Glues → Targeted Protein Degraders (TPDs) → Small Molecules
- Administration
- Oral
01
Overview
Elacestrant + onapristone is an investigational oral combination therapy for advanced or metastatic breast cancer that is estrogen receptor-positive (ER+), progesterone receptor-positive (PR+), and HER2-negative. Elacestrant is a selective estrogen receptor degrader (SERD) that binds to and promotes degradation of the estrogen receptor, thereby inhibiting estrogen-driven tumor growth. Onapristone is a type I antiprogestin that blocks the progesterone receptor by preventing its dimerization and ligand-induced phosphorylation. The rationale for combining these agents is to simultaneously target both hormone receptors implicated in breast cancer progression and endocrine resistance. This combination has been evaluated in phase 1b/2 clinical trials for patients who have progressed after prior endocrine therapy with CDK4/6 inhibitors[1][3][6].
- Brand names
- Orserdu (elacestrant)ONA-XR (onapristone)
- Other names
- elacestrant + onapristone combination
02
Targets
ESR1 (ERα)PR (Progesterone receptor)
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