cabergoline
Trade name: dostinex
Small moleculeapproved
Approved
Dec 23, 1996
Cabergoline is a long-acting dopamine receptor agonist with a high affinity for D2 receptors. Results of in vitro studies demonstrate that cabergoline exerts a direct inhibitory effect on the secretion of prolactin by rat pituitary lactotrophs. It is FDA approved for the treatment of hyperprolactinemic disorders, either idiopathic or due to pituitary adenomas. Common adverse reactions include constipation, nausea, dizziness, headache and fatigue. Cabergoline should not be administered concurrently with D-antagonists, such as phenothiazines, butyrophenones, thioxanthenes, or metoclopramide. — NCATS
Clinical trial activity
71 trials · 69 clinical orgs · 10 marketing orgs
Phase 1
10
Phase 2
28
Phase 3
17
Phase 4
14
Earliest trial started Jun 1, 2001 (NCT00033111)
Timeline
1990s
- Dec 23, 1996
Pharmacia & Upjohn — Earliest FDA Approval
- Dec 23, 1996
Pfizer — Marketing Organization
- Dec 23, 1996
Pharmacia & Upjohn — NDA Organization
- Dec 23, 1996
Pfizer — NDA Secondary Org
2000s
- Jan 1, 2001
Par Pharmaceuticals — Earliest Phase 1 Sponsor(trial)
- Jan 1, 2001
Earliest Phase 2 Sponsor(trial)
- Jan 1, 2002
- Dec 29, 2005
Par Pharmaceuticals — Marketing Organization
- Dec 29, 2005
Strides Pharma Science — Marketing Organization
- Mar 7, 2007
Teva — Marketing Organization
- Jul 3, 2007
Impax Laboratories — Marketing Organization
- Apr 21, 2008
Actavis — Marketing Organization
2010s
- Mar 8, 2013
Apotex — Marketing Organization
- Dec 2, 2013
Mylan — Marketing Organization
- Aug 1, 2018
Ingenus Pharmaceuticals — Marketing Organization
Indications
Approved for
Studied for
- Abortion, Induced · Phase 4
- Acromegaly · Phase 4
- ACTH-Secreting Pituitary Adenoma · Phase 3
- Adenoma · Phase 3
- Atrial Fibrillation · Phase 4
- Body Weight · Phase 1/Phase 2
- Breast Neoplasms · Early Phase 1
- Cocaine-Related Disorders · Phase 2
- Cushing Syndrome · Phase 2
- Diabetes Mellitus · Phase 3
- Drug-Related Side Effects and Adverse Reactions · Phase 4
- Drugs, Generic · Phase 1
- Dry Eye Syndromes · Early Phase 1
- Endometriosis · Phase 2
- Fertilization in Vitro · Phase 4
- Genital Diseases, Female · Phase 2
- Health Education · Phase 1
- Hyperprolactinemia · Phase 1
- Infertility · Phase 2/Phase 3
- Infertility, Female · Phase 4
- Ischemia · Phase 4
- Lactation Disorders · Phase 4
- Magnetic Resonance Imaging · Phase 4
- Migraine Disorders · Phase 2
- Obesity · Phase 1/Phase 2
- Ovarian Diseases · Phase 3
- Ovarian Hyperstimulation Syndrome · Phase 3
- Parkinson Disease · Phase 4
- Pituitary ACTH Hypersecretion · Phase 3
- Pituitary Neoplasms · Phase 4
- Polycystic Ovary Syndrome · Phase 2
- Prolactinoma · Phase 4
- Reproductive Health · Phase 2
- Restless Legs Syndrome · Phase 3
- Scleroderma, Diffuse · Phase 3
- Substance-Related Disorders · Phase 2
- Tachycardia, Ventricular · Phase 4
Mechanism of action
- Dopamine D2 receptorAGONIST
DRD2 agonist
Long acting
Approval history
- approvedDec 23, 1996
Chemistry & pharmacology
Loading structure…
SMILES
CCNC(=O)N(CCCN(C)C)C(=O)[C@@H]1C[C@H]2[C@@H](CC3=CNC4=C3C2=CC=C4)N(CC=C)C1- Mol. weight
- 451.6043 g/mol
- Lipinski Ro5
- Pass
- Rule of 3
- No
- Chirality
- Single Stereoisomer
- Inorganic
- No
- Polymer
- No
- Delivery
- Oral
- Availability
- Prescription Only
Oral
Yes
Parenteral
No
Topical
No
Sources
- WikipediaCabergoline ↗
- NCATSLL60K9J05T ↗
- ChEMBLCHEMBL1201087 ↗
Also known as
- 1-((6-allylergolin-8beta-yl)carbonyl)-1-(3-(dimethylamino)propyl)-3-ethylurea
- 1-((6-allylergolin-8beta-yl)carbonyl)-1-(3-(dimethylamino)propyl)-3-ethylurea
- 1-((6-allylergolin-8beta-yl)carbonyl)-1-(3-(dimethylamino)propyl)-3-ethylurea
- 1-[(6-allylergoline-8beta-yl)carbonyl]-1-[3-(dimethylamino)propyl]-3-ethylurea
- 1-[(6-allylergoline-8beta-yl)carbonyl]-1-[3-(dimethylamino)propyl]-3-ethylurea
- 1-ethyl-2-(3'-dimethylaminopropyl)-3-(6'-allylergoline-8'-beta-carbonyl)urea diphosphate
- 1-ethyl-3-(3'-dimethylamionpropyl)-2-(6'-allylergoline-8'beta-carbonyl)urea
- 1-ethyl-3-(3'-dimethylamionpropyl)-2-(6'-allylergoline-8'beta-carbonyl)urea
- (8beta)-n-[3-(dimethylamino)propyl]-n-[(ethylamino)carbonyl]-6-(2-propenyl)-ergoline-8-carboxamide
- (8beta)-n-[3-(dimethylamino)propyl]-n-[(ethylamino)carbonyl]-6-(2-propenyl)-ergoline-8-carboxamide
- (8r)-6-allyl-n-[3-(dimethylamino)propyl]-n-(ethylcarbamoyl)ergoline-8-carboxamide
- (8r)-6-allyl-n-[3-(dimethylamino)propyl]-n-(ethylcarbamoyl)ergoline-8-carboxamide
- cabaser
- cabaser
- cabaser
- cabaser
- cabaseril
- cabaseril
- cabergolina
- cabergolina
- cabergoline
- cabergoline
- cabergoline
- cabergoline
- cabergoline
- cabergoline
- cabergoline
- cabergoline
- cabergoline
- cabergoline
- cabergoline
- cabergoline diphosphate
- cabergolinum
- cabergolinum
- dostinex
- dostinex
- dostinex
- dostinex
- dostinex
- dostinex
- fce 21336
- fce-21336
- fce-21336
- fce-21336
- galastop
- galastop
Clinical trials
| NCT ID | Phase | Start date | Sponsor(s) |
|---|---|---|---|
| NCT07072910 | Phase 2 | Nov 12, 2025 | Aarhus University |
| NCT07045935 | Phase 4 | Sep 16, 2025 | University of Basel |
| NCT06909123 | Phase 2 | Jul 31, 2025 | Stanford University |
| NCT07008417 | Phase 1 | Jun 30, 2025 | GeneScience Pharmaceuticals Co., Ltd. |
| NCT07043322 | Phase 2 | Jun 30, 2025 | Tanta University |
| NCT07255911 | N/A | Feb 7, 2025 | Bangladesh Medical University |
| NCT07034859 | Phase 4 | May 20, 2024 | National Taiwan University |
| NCT06792903 | Early Phase 1 (Phase 1) | Apr 23, 2024 | Fudan University |
| NCT06029673 | Phase 2 | Jan 31, 2024 | Stanford University |
| NCT07037472 | N/A | Jan 1, 2024 | Chinese Academy of Medical Sciences |
| NCT06123026 | Phase 4 | Dec 31, 2023 | Northwestern University |
| NCT05981742 | Phase 2 | Sep 21, 2022 | Al-Mustafa University College, University of Baghdad |
| NCT05525611 | N/A | Sep 5, 2022 | Aarhus University |
| NCT05024422 | N/A | Oct 31, 2021 | Emek Medical Center |
| NCT04701333 | Phase 2 | Feb 18, 2021 | Stanford University |
| NCT06560814 | Phase 2 | Jul 1, 2020 | Bangladesh Medical University |
| NCT03928288 | Phase 2 | Sep 30, 2019 | Harvard University |
| NCT04096027 | Phase 4 | Sep 23, 2019 | Fertility Center of Las Vegas |
| NCT04037111 | N/A | Jul 23, 2019 | Xidian University, Xijing Hospital |
| NCT04107480 | Phase 4 | Jun 21, 2019 | Leiden University |
Showing 20 of 71 trials
Page 1 / 4
Organizations
Research & Development (69)
| Organization | Org type | Trials | As lead sponsor | Phases | Earliest year |
|---|---|---|---|---|---|
| Pfizer | For profit | 5 | 3 | 3 | 2002 |
| Chinese Academy of Medical Sciences | Academic/Hospital | 4 | 1 | 1 | 2018 |
| Fudan University | Academic/Hospital | 4 | 1 | 2 | 2018 |
| Assiut University | Academic/Hospital | 3 | 3 | 3 | 2015 |
| Benha University | Academic/Hospital | 3 | 3 | 1 | 2014 |
| Cairo University | Academic/Hospital | 3 | 3 | 2 | 2014 |
| Capital Medical University | Academic/Hospital | 3 | 0 | 1 | 2018 |
| China Medical University | Academic/Hospital | 3 | 0 | 1 | 2018 |
| Fujian Medical University | Academic/Hospital | 3 | 0 | 1 | 2018 |
| Jiao Tong University | Academic/Hospital | 3 | 3 | 1 | 2018 |
| Novartis | For profit | 3 | 3 | 2 | 2006 |
| People's Liberation Army of China | Government | 3 | 0 | 1 | 2018 |
| Stanford University | Academic/Hospital | 3 | 3 | 1 | 2021 |
| Wenzhou Medical University | Academic/Hospital | 3 | 0 | 1 | 2018 |
| Aarhus University | Academic/Hospital | 2 | 2 | 2 | 2022 |
| Aljazeera Hospital | Academic/Hospital | 2 | 2 | 1 | 2013 |
| Bangladesh Medical University | Academic/Hospital | 2 | 2 | 2 | 2020 |
| Biosense Webster, Inc. | For profit | 2 | 2 | 1 | 2012 |
| Federal University of Sao Paulo | Academic/Hospital | 2 | 2 | 2 | 2010 |
| Harvard University | Academic/Hospital | 2 | 2 | 1 | 2016 |
69 organizations
Page 1 / 4
Marketing (12)
| Organization | Org type | Relationship | Date |
|---|---|---|---|
| Actavis | For profit | MKTG | Apr 21, 2008 |
| Apotex | For profit | MKTG | Mar 8, 2013 |
| Impax Laboratories | For profit | MKTG | Jul 3, 2007 |
| Ingenus Pharmaceuticals | For profit | MKTG | Aug 1, 2018 |
| Mylan | For profit | MKTG | Dec 2, 2013 |
| Mylan | For profit | SYN | Dec 2, 2013 |
| Par Pharmaceuticals | For profit | MKTG | Dec 29, 2005 |
| Pfizer | For profit | MKTG | Dec 23, 1996 |
| Pfizer | For profit | NDA2 | Dec 23, 1996 |
| Pharmacia & Upjohn | For profit | NDA | Dec 23, 1996 |
| Strides Pharma Science | For profit | MKTG | Dec 29, 2005 |
| Teva | For profit | MKTG | Mar 7, 2007 |