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onapristone extended release
- Development stage
- Discontinued
- Lead developer
- Context Therapeutics
- Modality
- Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules, Covalent Small Molecules → Small Molecules, Nucleic Acid-Directed Small Molecules → Small Molecules
- Administration
- Oral
01
Overview
Onapristone extended release is an orally bioavailable extended-release formulation of onapristone, a potent and selective antagonist of the progesterone receptor (PR). It is classified as an antineoplastic agent and antiprogestogen. The drug was developed to treat PR-positive cancers such as breast cancer (including HER2-negative), endometrial cancer, ovarian cancer, peritoneal cancer, prostate cancer, and uterine cancer. Onapristone works by inhibiting progesterone receptor binding to chromatin in tumor cells—thereby blocking both ligand-dependent and ligand-independent PR activity—downregulating cancer stem cell mobilization and blocking immune evasion. The extended-release formulation was designed to reduce peak serum concentrations in order to mitigate hepatotoxicity observed with earlier formulations[1][2][5][6][7].
- Brand names
- ONA-XR
- Other names
- ApristorOnapristone - Arno Therapeutics
02
Targets
PR (Progesterone receptor)
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