Anagrelide

drugbox
IUPAC_name = 6,7-dichloro-1,5-dihydroimidazo
(2,1-b)quinazolin-2(3"H")-one

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CAS_number = 68475-42-3
ATC_prefix = L01
ATC_suffix = XX35
PubChem = 2182
ChemSpiderID = 2097
DrugBank = APRD00798
C = 10 | H = 7 | Cl = 2 | N = 3 | O = 1
molecular_weight = 256.088 g/mol
bioavailability =
protein_bound =
metabolism =
elimination_half-life = 1.3 hours
excretion =
pregnancy_category =
legal_status = Rx-only
routes_of_administration = Oral

Anagrelide (Agrylin/Xagrid, Shire) is a drug used for the treatment of essential thrombocytosis (ET; essential thrombocythemia). It also has been used in the treatment of chronic myeloid leukemia. cite journal |author=Voglová J, Maisnar V, Beránek M, Chrobák L |title= [Combination of imatinib and anagrelide in treatment of chronic myeloid leukemia in blastic phase] |language=Czech |journal=Vnitr̆ní lékar̆ství |volume=52 |issue=9 |pages=819–22 |year=2006 |pmid=17091608 |doi=]

Mechanism

It works by inhibiting the maturation of megakaryocytes into platelets.cite journal |author=Petrides PE |title=Anagrelide: what was new in 2004 and 2005? |journal=Semin. Thromb. Hemost. |volume=32 |issue=4 Pt 2 |pages=399–408 |year=2006 |pmid=16810615 |doi=10.1055/s-2006-942760] The exact mechanism of action is unclear, although it is known to be a potent (IC₅₀ = 36nM) inhibitor of phosphodiesterase-III.

Uses

According to a 2005 Medical Research Council randomized trial, the combination of hydroxyurea with aspirin is superior to the combination of anagrelide and aspirin for the initial management of ET. The hydroxyurea arm had a lower likelihood of myelofibrosis, arterial thrombosis, and bleeding, but it had a slightly higher rate of venous thrombosis. [Harrison CN, Campbell PJ, Buck G, Wheatley K, East CL, Bareford D, Wilkins BS, van der Walt JD, Reilly JT, Grigg AP, Revell P, Woodcock BE, Green AR; United Kingdom Medical Research Council Primary Thrombocythemia 1 Study. Hydroxyurea compared with anagrelide in high-risk essential thrombocythemia. "N Engl J Med" 2005;353:33-45. PMID 16000354.]

ide-effects

Common side effects are headache, diarrhea, unusual weakness/fatigue, hair loss, nausea and dizziness.

Less common side effects include: congestive heart failure, myocardial infarction, cardiomyopathy, cardiomegaly, complete heart block, atrial fibrillation, cerebrovascular accident, pericarditis, pulmonary infiltrates, pulmonary fibrosis, pulmonary hypertension, pancreatitis, gastric/duodenal ulceration, renal impairment/failure and seizure.

References