anagrelide

Trade name: agrylin

Small moleculeapprovedOrphan Drug FDA

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

Phase 1
4
Phase 2
8
Phase 3
6
Phase 4
2

Earliest trial started Sep 1, 2002 (NCT01065038)

Timeline

1980s

  1. Jan 27, 1988

    Orphan Drug Designation

1990s

  1. Mar 14, 1997

    Shire — Earliest FDA Approval

  2. Mar 14, 1997

    Shire — NDA Organization

  3. Mar 14, 1997

    Shire — NDA Secondary Org

  4. Mar 14, 1997

    Takeda — Marketing Organization

  5. Mar 14, 1997

    Takeda — NDA Secondary Org

2000s

  1. Jan 1, 2002

    Earliest Phase 3 Sponsor(trial)

  2. Jan 1, 2003

    Mylan — Earliest Phase 1 Sponsor(trial)

  3. Apr 18, 2005

    Barr Laboratories — Marketing Organization

  4. Apr 18, 2005

    Impax Laboratories — Marketing Organization

  5. Apr 18, 2005

    Teva — Marketing Organization

  6. Apr 18, 2005

    Mylan — Marketing Organization

  7. Apr 18, 2005

    Roxane Laboratories — Marketing Organization

  8. Apr 18, 2005

    Upsher-Smith Laboratories — Marketing Organization

  9. Apr 18, 2005

    Watson Pharmaceuticals — Marketing Organization

  10. Apr 18, 2005

    Chartwell Pharmaceuticals — Marketing Organization

  11. Apr 18, 2005

    Boehringer Ingelheim — Marketing Organization

  12. Jan 1, 2006

    Shire — Earliest Phase 2 Sponsor(trial)

  13. Jun 27, 2006

    Rising Pharmaceuticals — Marketing Organization

2010s

  1. Jun 30, 2017

    Torrent Pharmaceuticals Limited — Marketing Organization

Indications

Mechanism of action

Approval history

  • approvedPriority reviewMar 14, 1997

Chemistry & pharmacology

Loading structure…

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

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 IDPhaseStart dateSponsor(s)
NCT03866434Phase 1Feb 26, 2019Shire
NCT03232177Phase 4Jun 5, 2017Yuhan Pharmaceutical Company
NCT03123588Phase 2Apr 20, 2017Incyte
NCT02962388Phase 2/Phase 3 (Phase 3)Jan 1, 2017French Innovative Leukemia Organisation, Novartis
NCT02125318Phase 2May 1, 2014Galena Biopharma, Inc.
NCT02076815Phase 3Feb 1, 2014AOP Orphan Pharmaceuticals AG, Medical University of Vienna
NCT01552928Phase 1Mar 1, 2012Biotrial, Shire
NCT01467661Phase 3Nov 1, 2011Osaka University, Shire
NCT01230775Phase 3Dec 1, 2010AOP Orphan Pharmaceuticals AG
NCT01214915Phase 3Nov 1, 2010Osaka University, Shire
NCT00413634Phase 2Aug 1, 2006Shire
NCT00202644Phase 4Jan 1, 2006Institute for Haematology of Clinical Centre of Serbia, Shire
NCT00648765Phase 1Jan 1, 2003Mylan, PRACS
NCT00648024Phase 1Jan 1, 2003Mylan, PRACS
NCT01065038Phase 3Sep 1, 2002AOP Orphan Pharmaceuticals AG
Showing 15 of 15 trials
Page 1 / 1

Organizations

Research & Development (13)

OrganizationOrg typeTrialsAs lead sponsorPhasesEarliest year
ShireFor profit6642006
AOP Orphan Pharmaceuticals AGFor profit3312002
MylanFor profit2212003
Osaka UniversityAcademic/Hospital2012010
PRACSFor profit2012003
BiotrialFor profit1012012
French Innovative Leukemia OrganisationAcademic/Hospital1112017
Galena Biopharma, Inc.For profit1112014
IncyteFor profit1112017
Institute for Haematology of Clinical Centre of SerbiaAcademic/Hospital1012006
Medical University of ViennaAcademic/Hospital1012014
NovartisFor profit1012017
Yuhan Pharmaceutical CompanyFor profit1112017
13 organizations
Page 1 / 1

Marketing (16)

OrganizationOrg typeRelationshipDate
Barr LaboratoriesFor profitMKTGApr 18, 2005
Boehringer IngelheimFor profitMKTGApr 18, 2005
Chartwell PharmaceuticalsFor profitMKTGApr 18, 2005
Impax LaboratoriesFor profitMKTGApr 18, 2005
MylanFor profitMKTGApr 18, 2005
MylanFor profitSYNApr 18, 2005
Rising PharmaceuticalsFor profitMKTGJun 27, 2006
Roxane LaboratoriesFor profitMKTGApr 18, 2005
ShireFor profitNDAMar 14, 1997
ShireFor profitNDA2Mar 14, 1997
TakedaFor profitMKTGMar 14, 1997
TakedaFor profitNDA2Mar 14, 1997
TevaFor profitMKTGApr 18, 2005
Torrent Pharmaceuticals LimitedFor profitMKTGJun 30, 2017
Upsher-Smith LaboratoriesFor profitMKTGApr 18, 2005
Watson PharmaceuticalsFor profitMKTGApr 18, 2005