General Information of Drug (ID: DMSQ8MD)

Drug Name
Anagrelide Drug Info
Synonyms
Anagrelida; Anagrelidum; BL 416201; Agrylin (TN); Anagrelida [INN-Spanish]; Anagrelide [BAN:INN]; Anagrelide [INN:BAN]; Anagrelidum [INN-Latin]; Xagrid (TN); Anagrelide (INN/BAN); 6,7-Dichlor-1,5-dihydroimidazo(2,1-b)chinazolin-2(3H)-on; 6,7-Dichloro-1,5-dihydroimidazo(2,1-b)quinazolin-2(3H)-one; 6,7-dichloro-1,5-dihydroimidazo[2,1-]quinazolin-2(3H)-one; 6,7-dichloro-5,10-dihydro-3H-imidazo[2,1-b]quinazolin-2-one
Indication
Disease Entry ICD 11 Status REF
Thrombocythemia 3B63 Approved [1]
Essential thrombocythemia 3B63.1Z Phase 2 [2]
Therapeutic Class
Antithrombotic Agents
Cross-matching ID
PubChem CID
135409400
ChEBI ID
CHEBI:142290
CAS Number
CAS 68475-42-3
TTD Drug ID
DMSQ8MD
INTEDE Drug ID
DR0112
ACDINA Drug ID
D00038

Molecule-Related Drug Atlas

Molecule-Related Drug Atlas
Molecule Type:
DTT
DME
DOT
Drug Status:
Approved Drug(s)
Clinical Trial Drug(s)
Discontinued Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Cilostazol DMZMSCT Intermittent claudication BD40.00 Approved [6]
Aminophylline DML2NIB Bronchial asthma CA23 Approved [7]
Enoximone DMQVZJD Congestive heart failure BD10 Approved [8]
VESNARINONE DMBKX3C Cardiac failure BD10-BD13 Approved [9]
BEMORADAN DMUL6GY Heart failure BD10-BD13 Phase 2 [10]
CI-930 DMADPQX N. A. N. A. Discontinued in Phase 2 [11]
EMD-53998 DMVS8IE Cardiovascular disease BA00-BE2Z Discontinued in Phase 1 [10]
IMAZODAN DMWTFO3 N. A. N. A. Terminated [12]
LAS-31180 DMW2K1L Heart failure BD10-BD13 Terminated [13]
BMY-20844 DMDPJ8M N. A. N. A. Terminated [14]
⏷ Show the Full List of 10 Drug(s)
Drug(s) Metabolized By Cytochrome P450 1A2 (CYP1A2)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Fluorouracil DMUM7HZ Adenocarcinoma 2D40 Approved [15]
Dinoprostone DMTYOPD Medical abortion JA00.1Z Approved [16]
Tamoxifen DMLB0EZ Breast cancer 2C60-2C65 Approved [17]
Estradiol DMUNTE3 Acne vulgaris ED80 Approved [18]
Acetaminophen DMUIE76 Allergic rhinitis CA08.0 Approved [19]
Imatinib DM7RJXL Acute lymphoblastic leukaemia 2A85 Approved [20]
Etoposide DMNH3PG Acute myelogenous leukaemia 2A41 Approved [21]
Oxaliplatin DMQNWRD Adenocarcinoma 2D40 Approved [22]
Verapamil DMA7PEW Angina pectoris BA40 Approved [23]
Diclofenac DMPIHLS Chronic renal failure GB61.Z Approved [24]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Hydroxyurea DMOQVU9 Chronic myelogenous leukaemia 2A20.0 Approved [5]
Hydrogen peroxide DM1NG5W Infectious disease 1A00-CA43.1 Approved [25]
Quercetin DM3NC4M Obesity 5B81 Approved [26]
Arsenic trioxide DM61TA4 Acute lymphoblastic leukaemia 2A85 Approved [27]
Testosterone DM7HUNW Hot flushes GA30 Approved [28]
Nilotinib DM7HXWT Chronic myelogenous leukaemia 2A20.0 Approved [29]
Calcitriol DM8ZVJ7 Congenital alopecia LC30 Approved [28]
Valproate DMCFE9I Epilepsy 8A60-8A68 Approved [30]
Capsaicin DMGMF6V Back pain ME84.Z Approved [31]
Dasatinib DMJV2EK Blast phase chronic myelogenous leukemia, BCR-ABL1 positive Approved [32]
⏷ Show the Full List of 10 Drug(s)

Molecular Interaction Atlas of This Drug

Molecular Interaction Atlas

Drug Therapeutic Target (DTT)
DTT Name DTT ID UniProt ID MOA REF
Phosphodiesterase 3A (PDE3A) TT06AWU PDE3A_HUMAN Inhibitor [3]

Drug-Metabolizing Enzyme (DME)
DME Name DME ID UniProt ID MOA REF
Cytochrome P450 1A2 (CYP1A2) Main DME DEJGDUW CP1A2_HUMAN Substrate [4]

Drug Off-Target (DOT)
DOT Name DOT ID UniProt ID Interaction REF
Tyrosine-protein kinase ABL1 (ABL1) OT09YVXH ABL1_HUMAN Drug Response [5]

References

1 URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7114).
2 Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
3 Hydroxyurea compared with anagrelide in high-risk essential thrombocythemia. N Engl J Med. 2005 Jul 7;353(1):33-45.
4 Open-label, dose-titration and continuation study to assess efficacy, safety, and pharmacokinetics of anagrelide in treatment-nae Japanese patients with essential thrombocythemia. Int J Hematol. 2013 Mar;97(3):360-8.
5 ADReCS-Target: target profiles for aiding drug safety research and application. Nucleic Acids Res. 2018 Jan 4;46(D1):D911-D917. doi: 10.1093/nar/gkx899.
6 A new generation of phosphodiesterase inhibitors: multiple molecular forms of phosphodiesterase and the potential for drug selectivity. J Med Chem. 1985 May;28(5):537-45.
7 Topical fat reduction from the waist. Diabetes Obes Metab. 2007 May;9(3):300-3.
8 Inhibitors of cyclic AMP phosphodiesterase. 2. Structural variations of N-cyclohexyl-N-methyl-4-[(1,2,3,5-tetrahydro- 2-oxoimidazo[2,1-b]quinazolin... J Med Chem. 1987 Feb;30(2):303-18.
9 Design, synthesis and biological evaluation of 6-(benzyloxy)-4-methylquinolin-2(1H)-one derivatives as PDE3 inhibitors. Bioorg Med Chem. 2010 Jan 15;18(2):855-62.
10 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
11 Cardiotonic agents. 9. Synthesis and biological evaluation of a series of (E)-4,5-dihydro-6-[2-[4-(1H-imidazol-1-yl)phenyl]ethenyl]-3 (2H)-pyridazi... J Med Chem. 1989 Feb;32(2):342-50.
12 3,4-Dihydroquinolin-2(1H)-ones as combined inhibitors of thromboxane A2 synthase and cAMP phosphodiesterase. J Med Chem. 1992 Feb 21;35(4):620-8.
13 Pharmacological profile of LAS 31180, a new inotropic/vasodilator quinolone derivative. Arzneimittelforschung. 2000 Nov;50(11):980-6.
14 Inhibitors of blood platelet cAMP phosphodiesterase. 3. 1,3-Dihydro-2H-imidazo[4,5-b]quinolin-2-one derivatives with enhanced aqueous solubility. J Med Chem. 1992 Jul 10;35(14):2688-96.
15 Roles of cytochromes P450 1A2, 2A6, and 2C8 in 5-fluorouracil formation from tegafur, an anticancer prodrug, in human liver microsomes. Drug Metab Dispos. 2000 Dec;28(12):1457-63.
16 Effects of polyunsaturated fatty acids on prostaglandin synthesis and cyclooxygenase-mediated DNA adduct formation by heterocyclic aromatic amines in human adenocarcinoma colon cells. Mol Carcinog. 2004 Jul;40(3):180-8.
17 Endoxifen and other metabolites of tamoxifen inhibit human hydroxysteroid sulfotransferase 2A1 (hSULT2A1). Drug Metab Dispos. 2014 Nov;42(11):1843-50.
18 Cytochrome P450 1A2 (CYP1A2) activity and risk factors for breast cancer: a cross-sectional study. Breast Cancer Res. 2004;6(4):R352-65.
19 PharmGKB summary: pathways of acetaminophen metabolism at the therapeutic versus toxic doses. Pharmacogenet Genomics. 2015 Aug;25(8):416-26.
20 The effect of apigenin on pharmacokinetics of imatinib and its metabolite N-desmethyl imatinib in rats. Biomed Res Int. 2013;2013:789184.
21 Effects of morin on the pharmacokinetics of etoposide in rats. Biopharm Drug Dispos. 2007 Apr;28(3):151-6.
22 The influence of metabolic gene polymorphisms on urinary 1-hydroxypyrene concentrations in Chinese coke oven workers. Sci Total Environ. 2007 Aug 1;381(1-3):38-46.
23 Identification of P450 enzymes involved in metabolism of verapamil in humans. Naunyn Schmiedebergs Arch Pharmacol. 1993 Sep;348(3):332-7.
24 Metabolism and metabolic inhibition of xanthotoxol in human liver microsomes. Evid Based Complement Alternat Med. 2016;2016:5416509.
25 Acetaldehyde inhibits PPARgamma via H2O2-mediated c-Abl activation in human hepatic stellate cells. Gastroenterology. 2006 Oct;131(4):1235-52. doi: 10.1053/j.gastro.2006.08.009.
26 Quantitative proteomic analysis of HepG2 cells treated with quercetin suggests IQGAP1 involved in quercetin-induced regulation of cell proliferation and migration. OMICS. 2009 Apr;13(2):93-103. doi: 10.1089/omi.2008.0075.
27 Essential role of cell cycle regulatory genes p21 and p27 expression in inhibition of breast cancer cells by arsenic trioxide. Med Oncol. 2011 Dec;28(4):1225-54.
28 Effects of 1alpha,25 dihydroxyvitamin D3 and testosterone on miRNA and mRNA expression in LNCaP cells. Mol Cancer. 2011 May 18;10:58.
29 Endoplasmic reticulum stress-mediated apoptosis in imatinib-resistant leukemic K562-r cells triggered by AMN107 combined with arsenic trioxide. Exp Biol Med (Maywood). 2013 Aug 1;238(8):932-42. doi: 10.1177/1535370213492689. Epub 2013 Jul 24.
30 Gene Expression Regulation and Pathway Analysis After Valproic Acid and Carbamazepine Exposure in a Human Embryonic Stem Cell-Based Neurodevelopmental Toxicity Assay. Toxicol Sci. 2015 Aug;146(2):311-20. doi: 10.1093/toxsci/kfv094. Epub 2015 May 15.
31 Triggering of transient receptor potential vanilloid type 1 (TRPV1) by capsaicin induces Fas/CD95-mediated apoptosis of urothelial cancer cells in an ATM-dependent manner. Carcinogenesis. 2009 Aug;30(8):1320-9. doi: 10.1093/carcin/bgp138. Epub 2009 Jun 5.
32 Combined BCR-ABL inhibition with lentiviral-delivered shRNA and dasatinib augments induction of apoptosis in Philadelphia-positive cells. Exp Hematol. 2009 Feb;37(2):206-14. doi: 10.1016/j.exphem.2008.10.013. Epub 2008 Dec 18.