Peringatan Keamanan

The oral LD50 of anagrelide as reported in rats and mice is >1500mg/kg and >2500mg/kg, respectively.L14243 Symptoms of overdose may include hypotension, sinus tachycardia, and vomiting. As the therapeutic effect of anagrelide (i.e. platelet reduction) is dose-related, significant thrombocytopenia is expected in instances of overdose.L14153 Treatment of overdose should involve careful monitoring of platelet counts and complications such as bleeding.L14153 Employ symptomatic and supportive measures if clinically indicated.

Anagrelide

DB00261

small molecule approved

Deskripsi

Anagrelide is a platelet-reducing agent used to lower dangerously elevated platelet levels (i.e. to treat thrombocythemia) in patients with myeloproliferative neoplasms.L14153 It is an oral imidazoquinazoline that was first approved for use in the US in 1997.A214274 It appears to carry a better response rate than other thrombocythemia treatments (e.g. busulfan, hydroxyurea) and may be better tolerated.A214274

Struktur Molekul 2D

Berat 256.088
Wujud solid

Peta Jejaring Molekuler
Legenda: Obat • Target • Gen • Enzim • (Panah → menunjukkan arah efek / relasi) • Transporter • Carrier

Profil Farmakokinetik

Waktu Paruh (Half-Life) The t<sub>1/2</sub> of anagrelide and its active metabolite, 3-hydroxy anagrelide, are approximately 1.5 hours and 2.5 hours, respectively.[L14153]
Volume Distribusi -
Klirens (Clearance) -

Absorpsi

Following oral administration, the bioavailability of anagrelide is approximately 70%.L14153 Given on an empty stomach, the Cmax is reached within 1 hour (Tmax) of administration. Co-administration with food slightly lowers the Cmax and increases the AUC, but not to a clinically significant extent.L14153

Metabolisme

Anagrelide is extensively metabolized, primarily in the liver by cytochrome P450 1A2 (CYP1A2), into two major metabolites: 6,7-dichloro-3-hydroxy-1,5 dihydro-imidazo2,1-bquinazolin-2-one (3-hydroxy anagrelide) and 2-amino-5,6-dichloro-3,4,-dihydroquinazoline (RL603). The 3-hydroxy metabolite is considered pharmacologically active and carries a similar potency and efficacy in regards to its platelet-lowering effects, but inhibits PDE3 with a potency 40x greater than that of the parent drug.L14153

Rute Eliminasi

Following metabolism, urinary excretion of metabolites appears to be the primary means of anagrelide elimination. Less than 1% of an administered dose is recovered in the urine as unchanged parent drug, while approximately 3% and 16-20% of the administered dose is recovered as 3-hydroxy anagrelide and RL603, respectively.L14153

Interaksi Makanan

1 Data
  • 1. Take with or without food. Co-administration with food slightly alters pharmacokinetics, but not to a clinically significant extent.

Interaksi Obat

1182 Data
Tizanidine The serum concentration of Tizanidine can be increased when it is combined with Anagrelide.
Apixaban The risk or severity of adverse effects can be increased when Anagrelide is combined with Apixaban.
Dasatinib Dasatinib may increase the anticoagulant activities of Anagrelide.
Ursodeoxycholic acid The risk or severity of adverse effects can be increased when Anagrelide is combined with Ursodeoxycholic acid.
Glycochenodeoxycholic Acid The risk or severity of adverse effects can be increased when Anagrelide is combined with Glycochenodeoxycholic Acid.
Cholic Acid The risk or severity of adverse effects can be increased when Anagrelide is combined with Cholic Acid.
Glycocholic acid The risk or severity of adverse effects can be increased when Anagrelide is combined with Glycocholic acid.
Deoxycholic acid The risk or severity of adverse effects can be increased when Anagrelide is combined with Deoxycholic acid.
Taurocholic acid The risk or severity of adverse effects can be increased when Anagrelide is combined with Taurocholic acid.
Chenodeoxycholic acid The risk or severity of adverse effects can be increased when Anagrelide is combined with Chenodeoxycholic acid.
Taurochenodeoxycholic acid The risk or severity of adverse effects can be increased when Anagrelide is combined with Taurochenodeoxycholic acid.
Tauroursodeoxycholic acid The risk or severity of adverse effects can be increased when Anagrelide is combined with Tauroursodeoxycholic acid.
Bamet-UD2 The risk or severity of adverse effects can be increased when Anagrelide is combined with Bamet-UD2.
Dehydrocholic acid The risk or severity of adverse effects can be increased when Anagrelide is combined with Dehydrocholic acid.
Hyodeoxycholic Acid The risk or severity of adverse effects can be increased when Anagrelide is combined with Hyodeoxycholic Acid.
Glucosamine Glucosamine may increase the antiplatelet activities of Anagrelide.
Ibritumomab tiuxetan The risk or severity of adverse effects can be increased when Anagrelide is combined with Ibritumomab tiuxetan.
Ibrutinib The risk or severity of adverse effects can be increased when Ibrutinib is combined with Anagrelide.
Obinutuzumab The risk or severity of adverse effects can be increased when Anagrelide is combined with Obinutuzumab.
Pentoxifylline Pentoxifylline may increase the antiplatelet activities of Anagrelide.
Rivaroxaban Anagrelide may increase the anticoagulant activities of Rivaroxaban.
Tipranavir Tipranavir may increase the antiplatelet activities of Anagrelide.
Urokinase Anagrelide may increase the anticoagulant activities of Urokinase.
Vitamin E Vitamin E may increase the antiplatelet activities of Anagrelide.
Deferasirox The serum concentration of Anagrelide can be increased when it is combined with Deferasirox.
Peginterferon alfa-2b The serum concentration of Anagrelide can be increased when it is combined with Peginterferon alfa-2b.
Leflunomide The serum concentration of Anagrelide can be decreased when it is combined with Leflunomide.
Teriflunomide The serum concentration of Anagrelide can be decreased when it is combined with Teriflunomide.
Milrinone The risk or severity of congestive heart failure, bleeding, hypotension, and Tachycardia can be increased when Milrinone is combined with Anagrelide.
Cilostazol The risk or severity of congestive heart failure, bleeding, hypotension, and Tachycardia can be increased when Anagrelide is combined with Cilostazol.
Amrinone The risk or severity of congestive heart failure, bleeding, hypotension, and Tachycardia can be increased when Anagrelide is combined with Amrinone.
Enoximone The risk or severity of congestive heart failure, bleeding, hypotension, and Tachycardia can be increased when Anagrelide is combined with Enoximone.
Zolmitriptan The metabolism of Zolmitriptan can be decreased when combined with Anagrelide.
Riociguat Anagrelide may increase the hypotensive activities of Riociguat.
Pentosan polysulfate The risk or severity of adverse effects can be increased when Pentosan polysulfate is combined with Anagrelide.
Abiraterone The serum concentration of Anagrelide can be increased when it is combined with Abiraterone.
Limaprost Limaprost may increase the antiplatelet activities of Anagrelide.
Omega-3 fatty acids Omega-3 fatty acids may increase the antiplatelet activities of Anagrelide.
Tositumomab The risk or severity of adverse effects can be increased when Anagrelide is combined with Tositumomab.
Cyproterone acetate The metabolism of Anagrelide can be increased when combined with Cyproterone acetate.
Abciximab The risk or severity of bleeding can be increased when Anagrelide is combined with Abciximab.
Lepirudin The risk or severity of bleeding can be increased when Anagrelide is combined with Lepirudin.
Bivalirudin The risk or severity of bleeding can be increased when Anagrelide is combined with Bivalirudin.
Alteplase The risk or severity of bleeding can be increased when Anagrelide is combined with Alteplase.
Reteplase The risk or severity of bleeding can be increased when Anagrelide is combined with Reteplase.
Anistreplase The risk or severity of bleeding can be increased when Anagrelide is combined with Anistreplase.
Tenecteplase The risk or severity of bleeding can be increased when Anagrelide is combined with Tenecteplase.
Drotrecogin alfa The risk or severity of bleeding can be increased when Anagrelide is combined with Drotrecogin alfa.
Streptokinase The risk or severity of bleeding can be increased when Anagrelide is combined with Streptokinase.
Dicoumarol The risk or severity of bleeding can be increased when Anagrelide is combined with Dicoumarol.
Argatroban The risk or severity of bleeding can be increased when Anagrelide is combined with Argatroban.
Ardeparin The risk or severity of bleeding can be increased when Anagrelide is combined with Ardeparin.
Phenindione The risk or severity of bleeding can be increased when Anagrelide is combined with Phenindione.
Fondaparinux The risk or severity of bleeding can be increased when Anagrelide is combined with Fondaparinux.
Warfarin The risk or severity of bleeding can be increased when Anagrelide is combined with Warfarin.
Phenprocoumon The risk or severity of bleeding can be increased when Anagrelide is combined with Phenprocoumon.
Dipyridamole The risk or severity of bleeding can be increased when Anagrelide is combined with Dipyridamole.
Heparin The risk or severity of bleeding can be increased when Anagrelide is combined with Heparin.
Enoxaparin The risk or severity of bleeding can be increased when Anagrelide is combined with Enoxaparin.
Epoprostenol The risk or severity of bleeding can be increased when Anagrelide is combined with Epoprostenol.
Acenocoumarol The risk or severity of bleeding can be increased when Anagrelide is combined with Acenocoumarol.
4-hydroxycoumarin The risk or severity of bleeding can be increased when Anagrelide is combined with 4-hydroxycoumarin.
Coumarin The risk or severity of bleeding can be increased when Anagrelide is combined with Coumarin.
Ximelagatran The risk or severity of bleeding can be increased when Anagrelide is combined with Ximelagatran.
Desmoteplase The risk or severity of bleeding can be increased when Anagrelide is combined with Desmoteplase.
Defibrotide The risk or severity of bleeding can be increased when Anagrelide is combined with Defibrotide.
Ancrod The risk or severity of bleeding can be increased when Anagrelide is combined with Ancrod.
Beraprost The risk or severity of bleeding can be increased when Anagrelide is combined with Beraprost.
Prasugrel The risk or severity of bleeding can be increased when Anagrelide is combined with Prasugrel.
Sulodexide The risk or severity of bleeding can be increased when Anagrelide is combined with Sulodexide.
Semuloparin The risk or severity of bleeding can be increased when Anagrelide is combined with Semuloparin.
Idraparinux The risk or severity of bleeding can be increased when Anagrelide is combined with Idraparinux.
Cangrelor The risk or severity of bleeding can be increased when Anagrelide is combined with Cangrelor.
Astaxanthin The risk or severity of bleeding can be increased when Anagrelide is combined with Astaxanthin.
Otamixaban The risk or severity of bleeding can be increased when Anagrelide is combined with Otamixaban.
Amediplase The risk or severity of bleeding can be increased when Anagrelide is combined with Amediplase.
Danaparoid The risk or severity of bleeding can be increased when Anagrelide is combined with Danaparoid.
Dalteparin The risk or severity of bleeding can be increased when Anagrelide is combined with Dalteparin.
Tinzaparin The risk or severity of bleeding can be increased when Anagrelide is combined with Tinzaparin.
(R)-warfarin The risk or severity of bleeding can be increased when Anagrelide is combined with (R)-warfarin.
Ethyl biscoumacetate The risk or severity of bleeding can be increased when Anagrelide is combined with Ethyl biscoumacetate.
Nadroparin The risk or severity of bleeding can be increased when Anagrelide is combined with Nadroparin.
Triflusal The risk or severity of bleeding can be increased when Anagrelide is combined with Triflusal.
Ticagrelor The risk or severity of bleeding can be increased when Anagrelide is combined with Ticagrelor.
Ditazole The risk or severity of bleeding can be increased when Anagrelide is combined with Ditazole.
Sodium citrate The risk or severity of bleeding can be increased when Anagrelide is combined with Sodium citrate.
Dextran The risk or severity of bleeding can be increased when Anagrelide is combined with Dextran.
Bemiparin The risk or severity of bleeding can be increased when Anagrelide is combined with Bemiparin.
Parnaparin The risk or severity of bleeding can be increased when Anagrelide is combined with Parnaparin.
Desirudin The risk or severity of bleeding can be increased when Anagrelide is combined with Desirudin.
Antithrombin Alfa The risk or severity of bleeding can be increased when Anagrelide is combined with Antithrombin Alfa.
Protein C The risk or severity of bleeding can be increased when Anagrelide is combined with Protein C.
Antithrombin III human The risk or severity of bleeding can be increased when Anagrelide is combined with Antithrombin III human.
Letaxaban The risk or severity of bleeding can be increased when Anagrelide is combined with Letaxaban.
Darexaban The risk or severity of bleeding can be increased when Anagrelide is combined with Darexaban.
Betrixaban The risk or severity of bleeding can be increased when Anagrelide is combined with Betrixaban.
Nafamostat The risk or severity of bleeding can be increased when Anagrelide is combined with Nafamostat.
Monteplase The risk or severity of bleeding can be increased when Anagrelide is combined with Monteplase.
Gabexate The risk or severity of bleeding can be increased when Anagrelide is combined with Gabexate.
Fluindione The risk or severity of bleeding can be increased when Anagrelide is combined with Fluindione.

Target Protein

cGMP-inhibited 3',5'-cyclic phosphodiesterase 3A PDE3A

Referensi & Sumber

Synthesis reference: Warren Neil Beverung, Jr., Anthony Partyka, "Optionally substituted 1,2,3,5-tetrahydroimidezo(2,1-b)-quinazolin-2-ones and 6(H)-1,2,3,4-tetrahydropyimido(2,1-b)quinazolin-2-ones." U.S. Patent US3932407A, issued January 1976.
Artikel (PubMed)
  • PMID: 17091608
    Voglova J, Maisnar V, Beranek M, Chrobak L: Combination of imatinib and anagrelide in treatment of chronic myeloid leukemia in blastic phase. Vnitr Lek. 2006 Sep;52(9):819-22.
  • PMID: 16810615
    Petrides PE: Anagrelide: what was new in 2004 and 2005? Semin Thromb Hemost. 2006 Jun;32(4 Pt 2):399-408.
  • PMID: 16000354
    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: Hydroxyurea compared with anagrelide in high-risk essential thrombocythemia. N Engl J Med. 2005 Jul 7;353(1):33-45.
  • PMID: 31598394
    An R, Liu J, He J, Wang F, Zhang Q, Yu Q: PDE3A inhibitor anagrelide activates death signaling pathway genes and synergizes with cell death-inducing cytokines to selectively inhibit cancer cell growth. Am J Cancer Res. 2019 Sep 1;9(9):1905-1921. eCollection 2019.
  • PMID: 30530703
    Pulkka OP, Gebreyohannes YK, Wozniak A, Mpindi JP, Tynninen O, Icay K, Cervera A, Keskitalo S, Murumagi A, Kulesskiy E, Laaksonen M, Wennerberg K, Varjosalo M, Laakkonen P, Lehtonen R, Hautaniemi S, Kallioniemi O, Schoffski P, Sihto H, Joensuu H: Anagrelide for Gastrointestinal Stromal Tumor. Clin Cancer Res. 2019 Mar 1;25(5):1676-1687. doi: 10.1158/1078-0432.CCR-18-0815. Epub 2018 Dec 7.
  • PMID: 25604267
    Espasandin YR, Glembotsky AC, Grodzielski M, Lev PR, Goette NP, Molinas FC, Marta RF, Heller PG: Anagrelide platelet-lowering effect is due to inhibition of both megakaryocyte maturation and proplatelet formation: insight into potential mechanisms. J Thromb Haemost. 2015 Apr;13(4):631-42. doi: 10.1111/jth.12850. Epub 2015 Feb 18.
  • PMID: 30919941
    Gisslinger H, Buxhofer-Ausch V, Hodisch J, Radinoff A, Karyagina E, Kyrcz-Krzemien S, Abdulkadyrov K, Gerbutavicius R, Melikyan A, Burgstaller S, Hus M, Kloczko J, Yablokova V, Tzvetkov N, Calbecka M, Shneyder T, Warzocha K, Jurgutis M, Kaplanov K, Jilma B, Schoergenhofer C, Klade C: A phase III randomized, multicentre, double blind, active controlled trial to compare the efficacy and safety of two different anagrelide formulations in patients with essential thrombocythaemia - the TEAM-ET 2.0 trial. Br J Haematol. 2019 May;185(4):691-700. doi: 10.1111/bjh.15824. Epub 2019 Mar 28.
  • PMID: 15531452
    Mazzucconi MG, Redi R, Bernasconi S, Bizzoni L, Dragoni F, Latagliata R, Santoro C, Mandelli F: A long-term study of young patients with essential thrombocythemia treated with anagrelide. Haematologica. 2004 Nov;89(11):1306-13.

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