Details of the Active Pharmaceutical Ingredient (API)

General Information of API (ID: D00038)
Name
Anagrelide
Synonyms    Click to Show/Hide the Synonyms of This API
68475-42-3; Anagrelida; Xagrid; Anagrelidum; 6,7-Dichloro-5,10-dihydroimidazo[2,1-b]quinazolin-2(3H)-one; Agrylin; 6,7-dichloro-5,10-dihydro-3H-imidazo[2,1-b]quinazolin-2-one; UNII-K9X45X0051; CHEMBL760; 6,7-Dichloro-1,5-dihydroimidazo(2,1-b)quinazolin-2(3H)-one; CHEBI:142290; Imidazo[2,1-b]quinazolin-2(3H)-one, 6,7-dichloro-1,5-dihydro-; K9X45X0051; Anagrelide [INN:BAN]; Anagrelidum [INN-Latin]; Anagrelida [INN-Spanish]; 6,7-Dichloro-1,5-dihydroimidazo[2,1-b]quinazolin-2(3H)-one; Imidazo(2,1-b)quinazolin-2(3H)-one, 6,7-dichloro-1,5-dihydro-; C10H7Cl2N3O; HSDB 7325; BL 416201; Anagrelide (INN/BAN); BRN 0619582; 6,7-dichloro-1,5-dihydroimidazo[2,1-b]quinazolin-2[3H]-one; 6,7-Dichlor-1,5-dihydroimidazo(2,1-b)chinazolin-2(3H)-on; SCHEMBL9411; BIDD:GT0711; GTPL7114; 6,7-dichloro-1,5-dihydroimidazo[2,1-]quinazolin-2(3H)-one; 6,7-dichloro-3,5-dihydroimidazo[2,1-b]quinazolin-2(1H)-one; HMS2089D21; HMS3715J06; HMS3742K13; BCP21314; ZINC3871541; BDBM50000334; KM1204; MFCD00866794; AKOS015899342; AKOS016340524; AC-3401; CCG-221242; DB00261; KS-5176; NCGC00161408-02; NCGC00161408-08; NCGC00247665-01; AS-14157; SBI-0206823.P001; AB0014050; DB-055153; FT-0602855; FT-0630776; D07455; AB00698496-05; AB00698496-07; AB00698496_08; AB01566808_01; 475A423; Q408163; 6,7-dichloro-3H,5H-imidazo[2,1-b]quinazolin-2-ol; BRD-K62200014-003-05-5; BRD-K62200014-003-08-9; 6,7-Dichloro-1,5-dihydro-imidazo[2,1-b]quinazolin-2-one; 6,7-dichloro-1h,5h-imidazo[2,1-b]quinazoline-2(3h)-one; 6,7-dichloro-1, 5-dihydroimidazo[2,1-b]quinazolin-2[3H]-one; 6,7-Dichloro-1,5-dihydroimidazo[2,1-b]-quinazolin-2(3H)-one; 6,7-dichloro-1,5dihydroimidazo[2,1-b]quinazolin-2[3H]-one; 6,7-dichloro-1H,2H,3H,5H-imidazolidino[2,1-b]quinazolin-2-one; Imidazo[2,1-b]quinazolin-2(3H)-one,6,7-dichloro-1,5-dihydro-; 6,7-Dichloro-1,5-dihydro-imidazo[2,1-b]quinazolin-2-one(anagrelide); 6,7-Dichloro-1,5-dihydro-imidazo[2,1-b]quinazolin-2-one(BL-4162A)
Clinical Status
Approved
Disease Indication Thrombocytosis ICD-11: 3B63 [1]
PubChem CID
135409400
Formula
C10H7Cl2N3O
Canonical SMILES
C1C2=C(C=CC(=C2Cl)Cl)N=C3N1CC(=O)N3
InChI
1S/C10H7Cl2N3O/c11-6-1-2-7-5(9(6)12)3-15-4-8(16)14-10(15)13-7/h1-2H,3-4H2,(H,13,14,16)
InChIKey
OTBXOEAOVRKTNQ-UHFFFAOYSA-N
   Click to Show/Hide the Molecular Data (Structure/Property) of This API
Structure
<iframe style="width: 300px; height: 300px;" frameborder="0" src="https://embed.molview.org/v1/?mode=balls&cid=135409400"></iframe>
3D MOL 2D MOL
Physicochemical Properties Molecular Weight 256.079 Topological Polar Surface Area 44.7
XlogP 1.6 Complexity 360
Heavy Atom Count 16 Rotatable Bond Count 0
Hydrogen Bond Donor Count 1 Hydrogen Bond Acceptor Count 2
Full List of Drug Formulations (DFMs) Containing This API
          Anagrelide 0.5 mg capsule Click to Show/Hide the Full List of Formulation(s):          6 Formulation(s)
             Drug Formulation 1 DFM Info click to show the detail info of this DFM
                   All DIGs    Click to Show/Hide the Full List of DIGs in This DFM
Anhydrous lactose; Sodium lauryl sulfate; D&c yellow no. 10; Fd&c red no. 40; Fd&c blue no. 1; Fd&c blue no. 2; Magnesium stearate; Ferrosoferric oxide; Propylene glycol; Titanium dioxide; Crospovidone; Povidone; Cellulose, microcrystalline; Gelatin; Shellac
                   Dosage Form Oral Capsule
                   Company Mylan Pharamceuticals
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Allura red AC dye DIG Info Solute carrier SLCO2B1 (Ki = 4.7 uM) [2]
FD&C blue no. 1 DIG Info Solute carrier SLCO2B1 (Ki = 13 uM) [3]
Sodium lauryl sulfate DIG Info Solute carrier SLCO2B1 (Ki = 1.98 uM) [3]
FD&C blue no. 2 DIG Info Adenosine receptor A3 (IC50 = 1 uM) [2]
Quinoline yellow WS DIG Info Estrogen receptor alpha (IC50 = 18 uM) [2]
Allura red AC dye DIG Info Solute carrier SLCO2B1 (Ki = 2.59 uM) [3]
Propylene glycol DIG Info Albendazole monooxygenase (Inhibition ratio < 20 %) [4]
Povidone DIG Info Cholesterol 25-hydroxylase (IC50 = 78.3 uM) [5]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [6]
Crospovidone DIG Info Albendazole monooxygenase (Protein expression downregulation) [6]
             Drug Formulation 2 DFM Info click to show the detail info of this DFM
                   All DIGs    Click to Show/Hide the Full List of DIGs in This DFM
Anhydrous lactose; Lactose monohydrate; D&c yellow no. 10; Fd&c red no. 40; Fd&c blue no. 1; Fd&c blue no. 2; Indigotindisulfonate sodium; Magnesium stearate; Ferrosoferric oxide; Propylene glycol; Titanium dioxide; Crospovidone; Povidone k30; Aluminum oxide; Cellulose, microcrystalline; Gelatin; Shellac
                   Dosage Form Oral Capsule
                   Company Avera McKennan Hospital; Carilion Materials Management
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Allura red AC dye DIG Info Solute carrier SLCO2B1 (Ki = 4.7 uM) [2]
FD&C blue no. 1 DIG Info Solute carrier SLCO2B1 (Ki = 13 uM) [3]
FD&C blue no. 2 DIG Info Adenosine receptor A3 (IC50 = 1 uM) [2]
Quinoline yellow WS DIG Info Estrogen receptor alpha (IC50 = 18 uM) [2]
Allura red AC dye DIG Info Solute carrier SLCO2B1 (Ki = 2.59 uM) [3]
Propylene glycol DIG Info Albendazole monooxygenase (Inhibition ratio < 20 %) [4]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [6]
Crospovidone DIG Info Albendazole monooxygenase (Protein expression downregulation) [6]
             Drug Formulation 3 DFM Info click to show the detail info of this DFM
                   All DIGs    Click to Show/Hide the Full List of DIGs in This DFM
Anhydrous lactose; Lactose monohydrate; D&c yellow no. 10; Fd&c red no. 40; Fd&c blue no. 1; Fd&c blue no. 2; Magnesium stearate; Ferrosoferric oxide; Propylene glycol; Titanium dioxide; Crospovidone; Povidone; Aluminum oxide; Cellulose, microcrystalline; Gelatin
                   Dosage Form Oral Capsule
                   Company Physicians Total Care
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Allura red AC dye DIG Info Solute carrier SLCO2B1 (Ki = 4.7 uM) [2]
FD&C blue no. 1 DIG Info Solute carrier SLCO2B1 (Ki = 13 uM) [3]
FD&C blue no. 2 DIG Info Adenosine receptor A3 (IC50 = 1 uM) [2]
Quinoline yellow WS DIG Info Estrogen receptor alpha (IC50 = 18 uM) [2]
Allura red AC dye DIG Info Solute carrier SLCO2B1 (Ki = 2.59 uM) [3]
Propylene glycol DIG Info Albendazole monooxygenase (Inhibition ratio < 20 %) [4]
Povidone DIG Info Cholesterol 25-hydroxylase (IC50 = 78.3 uM) [5]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [6]
Crospovidone DIG Info Albendazole monooxygenase (Protein expression downregulation) [6]
             Drug Formulation 4 DFM Info click to show the detail info of this DFM
                   All DIGs    Click to Show/Hide the Full List of DIGs in This DFM
Anhydrous lactose; Lactose monohydrate; D&c yellow no. 10; Fd&c red no. 40; Fd&c blue no. 1; Fd&c blue no. 2; Indigotindisulfonate sodium; Magnesium stearate; Ferrosoferric oxide; Propylene glycol; Titanium dioxide; Povidone k30; Cellulose, microcrystalline; Crospovidone (15 mpa.s at 5%); Gelatin; Shellac
                   Dosage Form Oral Capsule
                   Company Teva Pharmaceuticals
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Allura red AC dye DIG Info Solute carrier SLCO2B1 (Ki = 4.7 uM) [2]
FD&C blue no. 1 DIG Info Solute carrier SLCO2B1 (Ki = 13 uM) [3]
FD&C blue no. 2 DIG Info Adenosine receptor A3 (IC50 = 1 uM) [2]
Quinoline yellow WS DIG Info Estrogen receptor alpha (IC50 = 18 uM) [2]
Allura red AC dye DIG Info Solute carrier SLCO2B1 (Ki = 2.59 uM) [3]
Propylene glycol DIG Info Albendazole monooxygenase (Inhibition ratio < 20 %) [4]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [6]
             Drug Formulation 5 DFM Info click to show the detail info of this DFM
                   All DIGs    Click to Show/Hide the Full List of DIGs in This DFM
Lactose monohydrate; Magnesium stearate; Ferrosoferric oxide; Potassium hydroxide; Propylene glycol; Titanium dioxide; Croscarmellose sodium; Cellulose, microcrystalline; Gelatin; Hydroxypropyl cellulose (type h); Shellac
                   Dosage Form Oral Capsule
                   Company Torrent Pharmaceuticals
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Propylene glycol DIG Info Albendazole monooxygenase (Inhibition ratio < 20 %) [4]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [6]
Carmellose sodium DIG Info Albendazole monooxygenase (Protein expression upregulation) [6]
             Drug Formulation 6 DFM Info click to show the detail info of this DFM
                   All DIGs    Click to Show/Hide the Full List of DIGs in This DFM
Anhydrous lactose; Lactose monohydrate; Magnesium stearate; Povidone k30; Crospovidone, unspecified; Microcrystalline cellulose
                   Dosage Form Oral Capsule
                   Company Shire
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [6]
          Anagrelide 1 mg capsule Click to Show/Hide the Full List of Formulation(s):          3 Formulation(s)
             Drug Formulation 1 DFM Info click to show the detail info of this DFM
                   All DIGs    Click to Show/Hide the Full List of DIGs in This DFM
Anhydrous lactose; Sodium lauryl sulfate; D&c yellow no. 10; Fd&c red no. 40; Fd&c blue no. 1; Fd&c blue no. 2; Magnesium stearate; Ferrosoferric oxide; Propylene glycol; Titanium dioxide; Crospovidone; Povidone; Cellulose, microcrystalline; Gelatin; Shellac
                   Dosage Form Oral Capsule
                   Company Mylan Pharamceuticals
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Allura red AC dye DIG Info Solute carrier SLCO2B1 (Ki = 4.7 uM) [2]
FD&C blue no. 1 DIG Info Solute carrier SLCO2B1 (Ki = 13 uM) [3]
Sodium lauryl sulfate DIG Info Solute carrier SLCO2B1 (Ki = 1.98 uM) [3]
FD&C blue no. 2 DIG Info Adenosine receptor A3 (IC50 = 1 uM) [2]
Quinoline yellow WS DIG Info Estrogen receptor alpha (IC50 = 18 uM) [2]
Allura red AC dye DIG Info Solute carrier SLCO2B1 (Ki = 2.59 uM) [3]
Propylene glycol DIG Info Albendazole monooxygenase (Inhibition ratio < 20 %) [4]
Povidone DIG Info Cholesterol 25-hydroxylase (IC50 = 78.3 uM) [5]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [6]
Crospovidone DIG Info Albendazole monooxygenase (Protein expression downregulation) [6]
             Drug Formulation 2 DFM Info click to show the detail info of this DFM
                   All DIGs    Click to Show/Hide the Full List of DIGs in This DFM
Anhydrous lactose; Lactose monohydrate; D&c yellow no. 10; Fd&c red no. 40; Fd&c blue no. 1; Fd&c blue no. 2; Indigotindisulfonate sodium; Magnesium stearate; Ferrosoferric oxide; Propylene glycol; Titanium dioxide; Povidone k30; Cellulose, microcrystalline; Crospovidone (15 mpa.s at 5%); Gelatin; Shellac
                   Dosage Form Oral Capsule
                   Company Teva Pharmaceuticals
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Allura red AC dye DIG Info Solute carrier SLCO2B1 (Ki = 4.7 uM) [2]
FD&C blue no. 1 DIG Info Solute carrier SLCO2B1 (Ki = 13 uM) [3]
FD&C blue no. 2 DIG Info Adenosine receptor A3 (IC50 = 1 uM) [2]
Quinoline yellow WS DIG Info Estrogen receptor alpha (IC50 = 18 uM) [2]
Allura red AC dye DIG Info Solute carrier SLCO2B1 (Ki = 2.59 uM) [3]
Propylene glycol DIG Info Albendazole monooxygenase (Inhibition ratio < 20 %) [4]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [6]
             Drug Formulation 3 DFM Info click to show the detail info of this DFM
                   All DIGs    Click to Show/Hide the Full List of DIGs in This DFM
Lactose monohydrate; Magnesium stearate; Ferrosoferric oxide; Potassium hydroxide; Propylene glycol; Titanium dioxide; Croscarmellose sodium; Cellulose, microcrystalline; Gelatin; Hydroxypropyl cellulose (type h); Shellac
                   Dosage Form Oral Capsule
                   Company Torrent Pharmaceuticals
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Propylene glycol DIG Info Albendazole monooxygenase (Inhibition ratio < 20 %) [4]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [6]
Carmellose sodium DIG Info Albendazole monooxygenase (Protein expression upregulation) [6]
References
1 FDA label for approved anagrelide from the official website of the U.S. Food and Drug Administration.
2 The activities of drug inactive ingredients on biological targets. Science. 2020 Jul 24;369(6502):403-413.
3 Bacterial metabolism rescues the inhibition of intestinal drug absorption by food and drug additives. Proc Natl Acad Sci U S A. 2020 Jul 7;117(27):16009-16018.
4 Pharmaceutical excipients inhibit cytochrome P450 activity in cell free systems and after systemic administration. Eur J Pharm Biopharm. 2008 Sep;70(1):279-88.
5 Mediation of in vitro cytochrome p450 activity by common pharmaceutical excipients. Mol Pharm. 2013 Jul 1;10(7):2739-48.
6 Effects of commonly used excipients on the expression of CYP3A4 in colon and liver cells. Pharm Res. 2010 Aug;27(8):1703-12.

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