cortisone acetate
Trade name: cortone
Approved
Jun 13, 1950
Cortisone is a hormone that is FDA approved for the treatment of primary and secondary adrenocortical deficiency, rheumatic disorders, psoriasis, exfoliative dermatitis, bronchial asthma, allergic conjunctivitis, hemolytic anemia, enteritis, tuberculosis, trichnosis. Cortisone acetate binds to the cytosolic glucocorticoid receptor. After binding the receptor, the newly formed receptor-ligand complex translocates itself into the cell nucleus, where it binds to many glucocorticoid response elements (GRE) in the promoter region of the target genes. The DNA bound receptor then interacts with basic transcription factors, causing the increase in expression of specific target genes. Common adverse reactions include convulsions, increased intracranial pressure with papilledema, vertigo, headache, psychic disturbances, hirsuitism, glaucoma, exophthalmos. Aminoglutethimide may lead to a loss of corticosteroid-induced adrenal suppression. Co-administration of corticosteroids and warfarin usually results in inhibition of response to warfarin, although there have been some conflicting reports. Cortisone is a natural steroid hormone. Its sulfate analog has been detected in in umbilical vein blood fetus plasma between 19 and 32 weeks of gestation with a significant increase at 29-30 weeks and in amniotic fluid. Base on the experiments with rats it was suggested that cortisone sulfate in mammals could be hydrolyzed enzymatically liberating sulfate ions from cortisone. Cortisone sulfate has been proposed for use as one of the glycosaminoglycan compound materials in a cartilage prosthesis and biological nasal bridge implant manufacture as well as auxiliary agent in powder aerosol composition for use in baby powder, dry shampoo, water-eczema remedy and antiperspirant. — NCATS
Clinical trial activity
16 trials · 29 clinical orgs · 17 marketing orgs
Earliest trial started Jan 1, 2000 (NCT03558971)
Timeline
1950s
- Jun 13, 1950
Merck — Earliest FDA Approval
- Jun 13, 1950
Merck — NDA Organization
- Jun 13, 1950
Merck — NDA Secondary Org
- Nov 2, 1951
Pharmacia & Upjohn — NDA Secondary Org
- Jan 14, 1952
Panray Corp. — NDA Secondary Org
1970s
- Jan 3, 1972
Teva — Marketing Organization
- Jun 13, 1972
Hikma — Marketing Organization
- Jun 20, 1973
Whiteworth Towne Paulsen — Marketing Organization
- Aug 31, 1973
Barr Laboratories — Marketing Organization
- Oct 17, 1974
Chartwell Pharmaceuticals — Marketing Organization
- Oct 17, 1974
Lannett Company, Inc. — Marketing Organization
- Jan 22, 1975
Everylife Foundation for Rare Diseases — Marketing Organization
- Feb 23, 1977
Impax Laboratories — Marketing Organization
- Mar 7, 1978
Watson Pharmaceuticals — Marketing Organization
2000s
- Sep 17, 2001
Impax Laboratories — NDA Secondary Org
- Jan 1, 2005
Earliest Phase 1 Sponsor(trial)
Indications
Approved for
Studied for
- Adrenal Hyperplasia, Congenital · Phase 4
- Angioedema · Phase 2
- Diabetes Mellitus, Type 2 · Phase 1
- Hip Injuries · Phase 4
- Low Back Pain · Phase 3
- Obesity · Phase 1
- Osteoarthritis · Phase 2/Phase 3
- Osteoarthritis, Knee · Phase 1
- Out-of-Hospital Cardiac Arrest · Phase 2
- Post-Cardiac Arrest Syndrome · Phase 2
- Rheumatic Diseases · Phase 4
- Rotator Cuff Injuries · Phase 1
Mechanism of action
- Glucocorticoid receptorANTAGONIST
NR3C1 antagonist
Approval history
- approvedPriority reviewJun 13, 1950
Chemistry & pharmacology
SMILES
C[C@]12CC(=O)[C@H]3[C@@H](CCC4=CC(=O)CC[C@]34C)[C@@H]1CC[C@]2(O)C(=O)CO- Mol. weight
- 360.444 g/mol
- Lipinski Ro5
- Pass
- Rule of 3
- No
- Chirality
- Single Stereoisomer
- Inorganic
- No
- Polymer
- No
- Availability
- Discontinued
Oral
No
Parenteral
No
Topical
No
Sources
- WikipediaCortisone acetate ↗
- NCATSV27W9254FZ ↗
- ChEMBLCHEMBL1650 ↗
- ChEMBLCHEMBL1499 ↗
- ChEMBLCHEMBL111861 ↗
Also known as
- adrenalex
- cortelan
- cortelan
- cortisone
- cortisone
- cortisone
- cortisone
- cortisone acetate
- cortisone acetate
- cortisone acetate
- cortisone acetate
- cortisone acetate
- cortisone acetate
- cortisone acetate
- cortisone acetate
- cortisone acetate
- cortisone acetate
- cortistab
- cortistab
- cortisyl
- cortisyl
- cortisyl
- cortone
- cortone
- cortone
- cortone acetate
- cortone acetate
- irisone acetate
Clinical trials
| NCT ID | Phase | Start date | Sponsor(s) |
|---|---|---|---|
| NCT05409027 | Phase 1 | Aug 5, 2021 | Sparrow Pharmaceuticals |
| NCT04921189 | Phase 2 | Jun 4, 2021 | Catholic University of Korea, Chung-Ang University, Ewha Womans University, Hanil General Hospital, Hanyang University, Sungkyunkwan University, University of Ulsan, Wonju Christian Hospital |
| NCT03951480 | N/A | Jun 30, 2019 | Centre Hospitalier Departemental Vendee |
| NCT02918136 | Phase 1 | Dec 1, 2016 | InGeneron, Inc., Sanford Health |
| NCT03760835 | Phase 4 | Aug 11, 2016 | University of Naples Frederico II |
| NCT02196155 | N/A | Jul 1, 2016 | Luzerner Kantonsspital, University of Bern |
| NCT03580148 | Phase 2/Phase 3 (Phase 3) | Oct 8, 2015 | University of Toronto |
| NCT02855866 | N/A | Sep 1, 2013 | University of Burgundy |
| NCT03195933 | N/A | Jul 31, 2013 | Brain & Behavior Research Foundation, National Institute of Mental Health (NIMH), University of Wisconsin |
| NCT01771328 | Phase 2 | Feb 1, 2013 | University of Bergen |
| NCT02639039 | Phase 4 | Feb 1, 2013 | Scott and White Healthcare |
| NCT01447160 | Phase 3 | Oct 1, 2011 | Federal University of Sao Paulo, University of Sao Paulo |
| NCT01154361 | Phase 2 | Jun 29, 2010 | Technical University of Munich |
| NCT00951236 | N/A | May 1, 2009 | Thomas Jefferson University |
| NCT00279903 | Phase 1 | Nov 1, 2005 | Mayo Clinic |
| NCT03558971 | Phase 4 | Jan 1, 2000 | Helen Foundation, University of North Dakota |
Organizations
Research & Development (29)
| Organization | Org type | Trials | As lead sponsor | Phases | Earliest year |
|---|---|---|---|---|---|
| Brain & Behavior Research Foundation | Academic/Hospital | 1 | 0 | 1 | 2013 |
| Catholic University of Korea | Academic/Hospital | 1 | 0 | 1 | 2021 |
| Centre Hospitalier Departemental Vendee | Academic/Hospital | 1 | 1 | 1 | 2019 |
| Chung-Ang University | Academic/Hospital | 1 | 0 | 1 | 2021 |
| Ewha Womans University | Academic/Hospital | 1 | 0 | 1 | 2021 |
| Federal University of Sao Paulo | Academic/Hospital | 1 | 0 | 1 | 2011 |
| Hanil General Hospital | Academic/Hospital | 1 | 0 | 1 | 2021 |
| Hanyang University | Academic/Hospital | 1 | 0 | 1 | 2021 |
| Helen Foundation | Academic/Hospital | 1 | 1 | 1 | 2000 |
| InGeneron, Inc. | For profit | 1 | 1 | 1 | 2016 |
| Luzerner Kantonsspital | Academic/Hospital | 1 | 0 | 1 | 2016 |
| Mayo Clinic | Academic/Hospital | 1 | 1 | 1 | 2005 |
| National Institute of Mental Health (NIMH) | Government | 1 | 0 | 1 | 2013 |
| Sanford Health | Academic/Hospital | 1 | 0 | 1 | 2016 |
| Scott and White Healthcare | Academic/Hospital | 1 | 1 | 1 | 2013 |
| Sparrow Pharmaceuticals | For profit | 1 | 1 | 1 | 2021 |
| Sungkyunkwan University | Academic/Hospital | 1 | 0 | 1 | 2021 |
| Technical University of Munich | Academic/Hospital | 1 | 1 | 1 | 2010 |
| Thomas Jefferson University | Academic/Hospital | 1 | 1 | 1 | 2009 |
| University of Bergen | Academic/Hospital | 1 | 1 | 1 | 2013 |
Marketing (19)
| Organization | Org type | Relationship | Date |
|---|---|---|---|
| Barr Laboratories | For profit | MKTG | Aug 31, 1973 |
| Chartwell Pharmaceuticals | For profit | MKTG | Oct 17, 1974 |
| Elkins Sinn | For profit | MKTG | — |
| Everylife Foundation for Rare Diseases | Academic/Hospital | MKTG | Jan 22, 1975 |
| Heather Pharma | For profit | MKTG | — |
| Hikma | For profit | MKTG | Jun 13, 1972 |
| Impax Laboratories | For profit | MKTG | Feb 23, 1977 |
| Impax Laboratories | For profit | NDA2 | Sep 17, 2001 |
| Inwood Laboratories | For profit | MKTG | — |
| Lannett Company, Inc. | For profit | MKTG | Oct 17, 1974 |
| Merck | For profit | NDA | Jun 13, 1950 |
| Merck | For profit | NDA2 | Jun 13, 1950 |
| Panray Corp. | For profit | NDA2 | Jan 14, 1952 |
| Pharmacia & Upjohn | For profit | NDA2 | Nov 2, 1951 |
| Puracap Pharmaceutical | For profit | MKTG | — |
| Teva | For profit | MKTG | Jan 3, 1972 |
| Vitarine | For profit | MKTG | — |
| Watson Pharmaceuticals | For profit | MKTG | Mar 7, 1978 |
| Whiteworth Towne Paulsen | For profit | MKTG | Jun 20, 1973 |