onapristone
Onapristone is a synthetic and steroidal antiprogestogen with additional antiglucocorticoid activity which was developed by Schering and described in 1984 but was never marketed. It is a silent antagonist of the progesterone receptor (PR), in contrast to the related antiprogestogen mifepristone. Moreover, compared to mifepristone, onapristone has reduced antiglucocorticoid activity, shows little antiandrogenic activity, and has 10- to 30-fold greater potency as an antiprogestogen. The medication was under development for clinical use, for instance in the treatment of breast cancer and as an endometrial contraceptive, but was discontinued during phase III clinical trials in 1995 due to findings that liver function abnormalities developed in a majority patients. — Wikipedia
Clinical trial activity
9 trials · 8 clinical orgs · 0 marketing orgs
Earliest trial started Jan 1, 2014 (NCT02052128)
Timeline
Indications
Mechanism of action
- Progesterone receptorANTAGONIST
PGR antagonist
Chemistry & pharmacology
SMILES
CN(C)c1ccc([C@H]2C[C@]3(C)[C@@H](CC[C@]3(O)CCCO)[C@@H]3CCC4=CC(=O)CCC4=C32)cc1- Mol. weight
- 449.64 g/mol
- Lipinski Ro5
- 1 violation(s)
- Rule of 3
- No
- Chirality
- Single Stereoisomer
- Inorganic
- No
- Polymer
- No
Oral
No
Parenteral
No
Topical
No
Sources
- WikipediaOnapristone ↗
- ChEMBLCHEMBL1908373 ↗
Also known as
- 11 beta-(4-dimethylaminophenyl)-17 alpha-hydroxy-17 beta-(3-hydroxypropyl)-13 alpha-methyl-4,9-gonadien-3-one
- estra-4,9-dien-3-one, 11-(4-(dimethylamino)phenyl)-17-hydroxy-17-(3-hydroxypropyl)-, (11beta,13alpha,17alpha)-
- onapristone
- onapristone
- onapristone
- onapristone
- onapristone
- zk 299
- zk-299
- zk-299
- zk-299
- zk 98299
- zk 98.299
- zk-98299
- zk-98299
- zk-98299
Clinical trials
| NCT ID | Phase | Start date | Sponsor(s) |
|---|---|---|---|
| NCT06938711 | Phase 1/Phase 2 (Phase 2) | Jun 30, 2023 | Context Therapeutics |
| NCT05618613 | Phase 1/Phase 2 (Phase 2) | Nov 22, 2022 | Context Therapeutics |
| NCT04738292 | Phase 2 | Oct 5, 2021 | Context Therapeutics, Medical College of Wisconsin, University of Wisconsin |
| NCT04872608 | Phase 1 | Sep 9, 2021 | Context Therapeutics, Memorial Sloan-Kettering Cancer Center |
| NCT04719273 | Phase 2 | Jan 28, 2021 | Thomas Jefferson University |
| NCT04142892 | Early Phase 1 (Phase 1) | Nov 24, 2019 | SOLTI Breast Cancer Research Group |
| NCT03909152 | Phase 2 | May 2, 2019 | Context Therapeutics, Memorial Sloan-Kettering Cancer Center |
| NCT02049190 | Phase 1/Phase 2 (Phase 2) | Feb 1, 2014 | Arno Therapeutics |
| NCT02052128 | Phase 1/Phase 2 (Phase 2) | Jan 1, 2014 | Arno Therapeutics, Curie Institute |
Organizations
Research & Development (8)
| Organization | Org type | Trials | As lead sponsor | Phases | Earliest year |
|---|---|---|---|---|---|
| Context Therapeutics | For profit | 5 | 2 | 2 | 2019 |
| Arno Therapeutics | For profit | 2 | 2 | 1 | 2014 |
| Memorial Sloan-Kettering Cancer Center | Academic/Hospital | 2 | 2 | 2 | 2019 |
| Curie Institute | Academic/Hospital | 1 | 0 | 1 | 2014 |
| Medical College of Wisconsin | Academic/Hospital | 1 | 0 | 1 | 2021 |
| SOLTI Breast Cancer Research Group | Academic/Hospital | 1 | 1 | 1 | 2019 |
| Thomas Jefferson University | Academic/Hospital | 1 | 1 | 1 | 2021 |
| University of Wisconsin | Academic/Hospital | 1 | 1 | 1 | 2021 |