Details of the Active Pharmaceutical Ingredient (API)

General Information of API (ID: D00444)
Name
Molindone
Synonyms    Click to Show/Hide the Synonyms of This API
MOLINDONE; 7416-34-4; (+-)-Molindone; Molindonum [INN-Latin]; Molindona [INN-Spanish]; 3-ethyl-2-methyl-5-(morpholin-4-ylmethyl)-1,5,6,7-tetrahydroindol-4-one; CHEMBL460; 3-Ethyl-6,7-dihydro-2-methyl-5-(morpholinomethyl)indol-4(5H)-one; Indol-4(5H)-one, 3-ethyl-6,7-dihydro-2-methyl-5-(morpholinomethyl)-; 3-ethyl-2-methyl-5-(morpholin-4-ylmethyl)-4,5,6,7-tetrahydro-1H-indol-4-one; CHEBI:6965; Molindona; Molindonum; Molindone [INN:BAN]; Molindone (INN); (+/-)-Molindone; HSDB 3131; 3-Ethyl-1,5,6,7-tetrahydro-2-methyl-5-(4-morpholinylmethyl)-4H-indol-4-one; 4H-Indol-4-one, 3-ethyl-1,5,6,7-tetrahydro-2-methyl-5-(4-morpholinylmethyl)-; PubChem21442; Prestwick0_001035; Prestwick1_001035; Prestwick2_001035; Prestwick3_001035; Oprea1_038890; BSPBio_001249; GTPL207; SCHEMBL149233; SPBio_003100; BPBio1_001374; DTXSID9023332; BDBM50130290; AKOS015899067; AC-7052; DB01618; MCULE-4631580563; NE48467; SDCCGSBI-0633741.P001; 3-ethyl-2-methyl-5-(morpholin-4-ylmethyl)-1,5,6,7-tetrahydro-4H-indol-4-one; NCGC00162218-01; NCGC00162218-02; NCGC00162218-03; NCGC00162218-11; AB00514709; EN300-51101; C07230; D08226; AB00514709_07; 416M344; L001248; Q593166; BRD-A65280694-003-03-8; Z802671522; 3-ethyl-2-methyl-5-(morpholinomethyl)-1,5,6,7-tetrahydro-4H-indol-4-one; 3-Ethyl-2-methyl-5-morpholin-4-ylmethyl-1,5,6,7-tetrahydro-indol-4-one; 3-ethyl-2-methyl-5-[(morpholin-4-yl)methyl]-4,5,6,7-tetrahydro-1H-indol-4-one; 3-Ethyl-2-methyl-5-morpholin-4-ylmethyl-1,5,6,7-tetrahydro-indol-4-one ( Molindone); 3-Ethyl-2-methyl-6-(4-morpholinylmethyl)-1,5,6,7-tetrahydro-4H-indol-4-one #; Molindone/3-Ethyl-2-methyl-5-(morpholin-4-ylmethyl)-1,5,6,7-tetrahydroindol-4-one
Clinical Status
Approved
Disease Indication Schizophrenia ICD-11: 6A20 [1]
PubChem CID
23897
Formula
C16H24N2O2
Canonical SMILES
CCC1=C(NC2=C1C(=O)C(CC2)CN3CCOCC3)C
InChI
1S/C16H24N2O2/c1-3-13-11(2)17-14-5-4-12(16(19)15(13)14)10-18-6-8-20-9-7-18/h12,17H,3-10H2,1-2H3
InChIKey
KLPWJLBORRMFGK-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=23897"></iframe>
3D MOL 2D MOL
Physicochemical Properties Molecular Weight 276.37 Topological Polar Surface Area 45.3
XlogP 1.7 Complexity 354
Heavy Atom Count 20 Rotatable Bond Count 3
Hydrogen Bond Donor Count 1 Hydrogen Bond Acceptor Count 3
Full List of Drug Formulations (DFMs) Containing This API
          Molindone 25 mg tablet Click to Show/Hide the Full List of Formulation(s):          1 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
Lactose monohydrate; D&c yellow no. 10; Fd&c blue no. 2; Fd&c yellow no. 6; Magnesium stearate; Calcium sulfate; Povidone; Silicon dioxide; Alginic acid; Cellulose, microcrystalline; Sodium starch glycolate type a potato
                   Dosage Form Oral Tablet
                   Company CorePharma
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Sunset yellow FCF DIG Info Solute carrier SLCO2B1 (Ki = 68.4 uM) [2]
FD&C blue no. 2 DIG Info Adenosine receptor A3 (IC50 = 1 uM) [3]
Quinoline yellow WS DIG Info Estrogen receptor alpha (IC50 = 18 uM) [3]
Povidone DIG Info Cholesterol 25-hydroxylase (IC50 = 78.3 uM) [4]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [5]
Silicon dioxide DIG Info Albendazole monooxygenase (Protein expression downregulation) [5]
          Molindone 10 mg tablet Click to Show/Hide the Full List of Formulation(s):          1 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
Lactose monohydrate; Fd&c blue no. 2; Magnesium stearate; Calcium sulfate; Povidone; Silicon dioxide; Alginic acid; Cellulose, microcrystalline; Sodium starch glycolate type a potato
                   Dosage Form Oral Tablet
                   Company CorePharma
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
FD&C blue no. 2 DIG Info Adenosine receptor A3 (IC50 = 1 uM) [3]
Povidone DIG Info Cholesterol 25-hydroxylase (IC50 = 78.3 uM) [4]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [5]
Silicon dioxide DIG Info Albendazole monooxygenase (Protein expression downregulation) [5]
          Molindone 5 mg tablet Click to Show/Hide the Full List of Formulation(s):          1 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
Lactose monohydrate; Fd&c yellow no. 6; Magnesium stearate; Calcium sulfate; Povidone; Silicon dioxide; Alginic acid; Cellulose, microcrystalline; Sodium starch glycolate type a potato
                   Dosage Form Oral Tablet
                   Company CorePharma
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Sunset yellow FCF DIG Info Solute carrier SLCO2B1 (Ki = 68.4 uM) [2]
Povidone DIG Info Cholesterol 25-hydroxylase (IC50 = 78.3 uM) [4]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [5]
Silicon dioxide DIG Info Albendazole monooxygenase (Protein expression downregulation) [5]
          Molindone Hydrochloride 25mg tablet Click to Show/Hide the Full List of Formulation(s):          1 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
Calcium Sulfate; Lactose; Magnesium Stearate; Microcrystalline Cellulose; Povidone; Alginic Acid; Colloidal Silicon Dioxide; D&C Yellow 10; Fd&C Blue 2; Fd&C Yellow 6
                   Dosage Form Tablet
                   Company Endo Pharms
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Sunset yellow FCF DIG Info Solute carrier SLCO2B1 (Ki = 68.4 uM) [2]
FD&C blue no. 2 DIG Info Adenosine receptor A3 (IC50 = 1 uM) [3]
Quinoline yellow WS DIG Info Estrogen receptor alpha (IC50 = 18 uM) [3]
Povidone DIG Info Cholesterol 25-hydroxylase (IC50 = 78.3 uM) [4]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [5]
          Molindone Hydrochloride 10mg tablet Click to Show/Hide the Full List of Formulation(s):          1 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
Calcium Sulfate; Lactose; Magnesium Stearate; Microcrystalline Cellulose; Povidone; Alginic Acid; Colloidal Silicon Dioxide; Fd&C Blue 2; Fd&C Red 40
                   Dosage Form Tablet
                   Company Endo Pharms
                   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) [3]
FD&C blue no. 2 DIG Info Adenosine receptor A3 (IC50 = 1 uM) [3]
Allura red AC dye DIG Info Solute carrier SLCO2B1 (Ki = 2.59 uM) [2]
Povidone DIG Info Cholesterol 25-hydroxylase (IC50 = 78.3 uM) [4]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [5]
          Molindone Hydrochloride 5mg tablet Click to Show/Hide the Full List of Formulation(s):          1 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
Calcium Sulfate; Lactose; Magnesium Stearate; Microcrystalline Cellulose; Povidone; Alginic Acid; Colloidal Silicon Dioxide; Fd&C Yellow 6
                   Dosage Form Tablet
                   Company Endo Pharms
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Sunset yellow FCF DIG Info Solute carrier SLCO2B1 (Ki = 68.4 uM) [2]
Povidone DIG Info Cholesterol 25-hydroxylase (IC50 = 78.3 uM) [4]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [5]
          Molindone Hydrochloride 50mg tablet Click to Show/Hide the Full List of Formulation(s):          1 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
Calcium Sulfate; Lactose; Magnesium Stearate; Microcrystalline Cellulose; Povidone; Fd&C Blue 2; Sodium Starch Glycolate
                   Dosage Form Tablet
                   Company Endo Pharms
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
FD&C blue no. 2 DIG Info Adenosine receptor A3 (IC50 = 1 uM) [3]
Povidone DIG Info Cholesterol 25-hydroxylase (IC50 = 78.3 uM) [4]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [5]
References
1 FDA label for approved molindone from the official website of the U.S. Food and Drug Administration.
2 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.
3 The activities of drug inactive ingredients on biological targets. Science. 2020 Jul 24;369(6502):403-413.
4 Mediation of in vitro cytochrome p450 activity by common pharmaceutical excipients. Mol Pharm. 2013 Jul 1;10(7):2739-48.
5 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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