Anagrelide

Title: Anagrelide
CAS Registry Number: 68475-42-3
CAS Name: 6,7-Dichloro-1,5-dihydroimidazo[2,1-b]quinazolin-2(3H)-one
Additional Names: 6,7-dichloro-1,2,3,5-tetrahydroimidazo[2,1-b]quinazolin-2-one
Molecular Formula: C10H7Cl2N3O
Molecular Weight: 256.09
Percent Composition: C 46.90%, H 2.76%, Cl 27.69%, N 16.41%, O 6.25%
Literature References: Phosphodiesterase inhibitor with antiplatelet activity. Prepn: W. N. Beverung, A. Partyka, US 3932407; US RE 31617; T. A. Jenks et al., US 4146718 (1976, 1984, 1979 all to Bristol-Myers); H. Yamaguchi, F. Ishikawa, J. Heterocycl. Chem. 18, 67 (1981). Antithrombotic and platelet aggregation inhibiting properties: J. S. Fleming, J. P. Buyniski, Thromb. Res. 15, 373 (1979). Mode of action studies: S. S. Tang, M. M. Frojmovic, J. Lab. Clin. Med. 95, 241 (1980); S. Seiler et al., J. Pharmacol. Exp. Ther. 243, 767 (1987). GC-MS determn in human plasma: E. H. Kerns et al., J. Chromatogr. 416, 357 (1987). Clinical reduction of platelet counts: W. A. Andes et al., Thromb. Haemostasis 52, 325 (1984). Clinical trials to control thrombocytosis in chronic myeloproliferative diseases: M. N. Silverstein et al., N. Engl. J. Med. 318, 1292 (1988); Anagrelide Study Group, Am. J. Med. 92, 69 (1992). Review of pharmacology and clinical experience: P. E. Petrides, Expert Opin. Pharmacother. 5, 1781-1798 (2004).
Derivative Type: Hydrochloride monohydrate
CAS Registry Number: 58579-51-4
Manufacturers' Codes: BL-4162A; BMY-26538-01
Trademarks: Agrylin (Shire); Thromboreductin (AOP Orphan Pharm.); Xagrid (Shire)
Molecular Formula: C10H7Cl2N3O.HCl.H2O
Molecular Weight: 310.56
Percent Composition: C 38.67%, H 3.25%, Cl 34.25%, N 13.53%, O 10.30%
Properties: Off-white powder. Very slightly sol in water; sparingly sol in DMSO, DMF. Also prepd as the hemihydrate; crystals from ethanolic HCl, mp >280°.
Melting point: mp >280°
Therap-Cat: Antithrombocythemic.
Keywords: Antithrombocythemic.
Anagyrine Anandamide Anatoxins Anazolene Sodium Ancitabine

Anagrelide
Anagrelide2DACS.svg
Systematic (IUPAC) name
6,7-dichloro-1,5-dihydroimidazo
(2,1-b)quinazolin-2(3H)-one
Clinical data
Trade names Agrylin
AHFS/Drugs.com monograph
MedlinePlus a601020
Pregnancy cat. B3 (AU) C (US)
Legal status Prescription Only (S4) (AU) -only (CA) POM (UK) -only (US)
Routes Oral
Pharmacokinetic data
Metabolism Hepatic, partially through CYP1A2
Half-life 1.3 hours
Excretion Urine (<1%)
Identifiers
CAS number 68475-42-3 YesY
ATC code L01XX35
PubChem CID 2182
DrugBank DB00261
ChemSpider 2097 YesY
UNII K9X45X0051 YesY
KEGG D07455 YesY
ChEBI CHEBI:142290 YesY
ChEMBL CHEMBL760 YesY
Chemical data
Formula C10H7Cl2N3O 
Mol. mass 256.088 g/mol
 YesY (what is this?)  (verify)

Anagrelide (Agrylin/Xagrid, Shire) is a drug used for the treatment of essential thrombocytosis (ET; essential thrombocythemia), or overproduction of blood platelets. It also has been used in the treatment of chronic myeloid leukemia.[1]