anagrelide
Trade name: agrylin
Approved
Mar 14, 1997
Anagrelide is an orally active quinazinolone derivative that was originally developed as an antiplatelet drug. The drug inhibits cyclic nucleotide phosphodiesterase III (PDEIII) and phopholipase A2, which is thought to cause the side effects of vasodilation, positive inotropism, reduced platelet aggregation. However, significant inhibition of platelet aggregation is observed only at doses of anagrelide higher than those required to reduce platelet count. It is indicated for the treatment of patients with thrombocythemia, secondary to myeloproliferative disorders. Commonly reported side effects of anagrelide include: abdominal pain, dizziness, headache, nausea, and palpitations. Other side effects include: back pain, fever, tachycardia, vomiting, and anorexia. There is a single case report, which suggests that sucralfate may interfere with anagrelide absorption. Anagrelide is an inhibitor of cyclic AMP PDE III. The effects of medicinal products with similar properties such as inotropes milrinone, enoximone, amrinone, olprinone and cilostazol may be exacerbated by anagrelide. — NCATS
Clinical trial activity
15 trials · 13 clinical orgs · 13 marketing orgs
Earliest trial started Sep 1, 2002 (NCT01065038)
Timeline
1980s
- Jan 27, 1988
Orphan Drug Designation
1990s
2000s
- Jan 1, 2002
Earliest Phase 3 Sponsor(trial)
- Jan 1, 2003
- Apr 18, 2005
Barr Laboratories — Marketing Organization
- Apr 18, 2005
Impax Laboratories — Marketing Organization
- Apr 18, 2005
Teva — Marketing Organization
- Apr 18, 2005
Mylan — Marketing Organization
- Apr 18, 2005
Roxane Laboratories — Marketing Organization
- Apr 18, 2005
Upsher-Smith Laboratories — Marketing Organization
- Apr 18, 2005
Watson Pharmaceuticals — Marketing Organization
- Apr 18, 2005
Chartwell Pharmaceuticals — Marketing Organization
- Apr 18, 2005
Boehringer Ingelheim — Marketing Organization
- Jan 1, 2006
- Jun 27, 2006
Rising Pharmaceuticals — Marketing Organization
2010s
- Jun 30, 2017
Torrent Pharmaceuticals Limited — Marketing Organization
Indications
Approved for
Mechanism of action
Approval history
- approvedPriority reviewMar 14, 1997
Chemistry & pharmacology
SMILES
O=C1CN2Cc3c(ccc(Cl)c3Cl)N=C2N1- Mol. weight
- 256.09 g/mol
- Lipinski Ro5
- Pass
- Rule of 3
- Yes
- Chirality
- Achiral Molecule
- Inorganic
- No
- Polymer
- No
- Delivery
- Oral
- Availability
- Prescription Only
Oral
Yes
Parenteral
No
Topical
No
Sources
- ChEMBLCHEMBL760 ↗
- WikipediaAnagrelide ↗
- NCATSK9X45X0051 ↗
- ChEMBLCHEMBL1200759 ↗
Also known as
- 6,7-dichloro-1,5-dihydroimidazo(2,1-b)quinazolin-2(3h)-one hydrochloride
- agrelin
- agrelin
- agrelin
- agrylin
- agrylin
- agrylin
- agrylin
- agrylin
- anagrelida
- anagrelida
- anagrelide
- anagrelide
- anagrelide
- anagrelide
- anagrelide
- anagrelide
- anagrelide
- anagrelide
- anagrelide
- anagrelide
- anagrelide
- anagrelide hcl
- anagrelide hcl
- anagrelide hcl
- anagrelide hydrochloride
- anagrelide hydrochloride
- anagrelide hydrochloride
- anagrelide hydrochloride
- anagrelide hydrochloride
- anagrelide hydrochloride
- anagrelide hydrochloride hydrate
- anagrelide hydrochloride monohydrate
- anagrelidum
- anagrelidum
- bl 4162a
- bl-4162a
- bl-4162a
- imidazo(2,1-b)quinazolin-2(3h)-one, 6,7-dichloro-1,5-dihydro-, monohydrochloride
- spd422
- thromboreductin
- thromboreductin
- xagrid
- xagrid
- xagrid
Clinical trials
| NCT ID | Phase | Start date | Sponsor(s) |
|---|---|---|---|
| NCT03866434 | Phase 1 | Feb 26, 2019 | Shire |
| NCT03232177 | Phase 4 | Jun 5, 2017 | Yuhan Pharmaceutical Company |
| NCT03123588 | Phase 2 | Apr 20, 2017 | Incyte |
| NCT02962388 | Phase 2/Phase 3 (Phase 3) | Jan 1, 2017 | French Innovative Leukemia Organisation, Novartis |
| NCT02125318 | Phase 2 | May 1, 2014 | Galena Biopharma, Inc. |
| NCT02076815 | Phase 3 | Feb 1, 2014 | AOP Orphan Pharmaceuticals AG, Medical University of Vienna |
| NCT01552928 | Phase 1 | Mar 1, 2012 | Biotrial, Shire |
| NCT01467661 | Phase 3 | Nov 1, 2011 | Osaka University, Shire |
| NCT01230775 | Phase 3 | Dec 1, 2010 | AOP Orphan Pharmaceuticals AG |
| NCT01214915 | Phase 3 | Nov 1, 2010 | Osaka University, Shire |
| NCT00413634 | Phase 2 | Aug 1, 2006 | Shire |
| NCT00202644 | Phase 4 | Jan 1, 2006 | Institute for Haematology of Clinical Centre of Serbia, Shire |
| NCT00648765 | Phase 1 | Jan 1, 2003 | Mylan, PRACS |
| NCT00648024 | Phase 1 | Jan 1, 2003 | Mylan, PRACS |
| NCT01065038 | Phase 3 | Sep 1, 2002 | AOP Orphan Pharmaceuticals AG |
Organizations
Research & Development (13)
| Organization | Org type | Trials | As lead sponsor | Phases | Earliest year |
|---|---|---|---|---|---|
| Shire | For profit | 6 | 6 | 4 | 2006 |
| AOP Orphan Pharmaceuticals AG | For profit | 3 | 3 | 1 | 2002 |
| Mylan | For profit | 2 | 2 | 1 | 2003 |
| Osaka University | Academic/Hospital | 2 | 0 | 1 | 2010 |
| PRACS | For profit | 2 | 0 | 1 | 2003 |
| Biotrial | For profit | 1 | 0 | 1 | 2012 |
| French Innovative Leukemia Organisation | Academic/Hospital | 1 | 1 | 1 | 2017 |
| Galena Biopharma, Inc. | For profit | 1 | 1 | 1 | 2014 |
| Incyte | For profit | 1 | 1 | 1 | 2017 |
| Institute for Haematology of Clinical Centre of Serbia | Academic/Hospital | 1 | 0 | 1 | 2006 |
| Medical University of Vienna | Academic/Hospital | 1 | 0 | 1 | 2014 |
| Novartis | For profit | 1 | 0 | 1 | 2017 |
| Yuhan Pharmaceutical Company | For profit | 1 | 1 | 1 | 2017 |
Marketing (16)
| Organization | Org type | Relationship | Date |
|---|---|---|---|
| Barr Laboratories | For profit | MKTG | Apr 18, 2005 |
| Boehringer Ingelheim | For profit | MKTG | Apr 18, 2005 |
| Chartwell Pharmaceuticals | For profit | MKTG | Apr 18, 2005 |
| Impax Laboratories | For profit | MKTG | Apr 18, 2005 |
| Mylan | For profit | MKTG | Apr 18, 2005 |
| Mylan | For profit | SYN | Apr 18, 2005 |
| Rising Pharmaceuticals | For profit | MKTG | Jun 27, 2006 |
| Roxane Laboratories | For profit | MKTG | Apr 18, 2005 |
| Shire | For profit | NDA | Mar 14, 1997 |
| Shire | For profit | NDA2 | Mar 14, 1997 |
| Takeda | For profit | MKTG | Mar 14, 1997 |
| Takeda | For profit | NDA2 | Mar 14, 1997 |
| Teva | For profit | MKTG | Apr 18, 2005 |
| Torrent Pharmaceuticals Limited | For profit | MKTG | Jun 30, 2017 |
| Upsher-Smith Laboratories | For profit | MKTG | Apr 18, 2005 |
| Watson Pharmaceuticals | For profit | MKTG | Apr 18, 2005 |