Details of the Active Pharmaceutical Ingredient (API)

General Information of API (ID: D00100)
Name
Cariprazine
Synonyms    Click to Show/Hide the Synonyms of This API
Cariprazine; 839712-12-8; RGH-188; RGH 188; Cariprazine(RGH188); UNII-F6RJL8B278; 3-[4-[2-[4-(2,3-dichlorophenyl)piperazin-1-yl]ethyl]cyclohexyl]-1,1-dimethylurea; MP-214; F6RJL8B278; CHEMBL3085826; Urea, N'-[trans-4-[2-[4-(2,3-dichlorophenyl)-1-piperazinyl]ethyl]cyclohexyl]-N,N -diMethyl-; Cariprazine [USAN:INN]; Reagila; cis-Cariprazine; trans-Cariprazine; MP 214; RGH-188; Cariprazine; Cariprazine (USAN/INN); Cariprazine (RGH-188); C21H32Cl2N4O; SCHEMBL184342; SCHEMBL184343; GTPL7671; SCHEMBL7861573; CHEMBL2028019; CHEBI:90933; HSDB 8310; DTXSID80232867; GED-129; BDBM263449; BCP14691; RGH-188;MP-214; 3526AH; BDBM50382290; BDBM50443094; BDBM50443101; ZINC38309313; ZINC100153731; ZINC100907004; CS-1569; DB06016; EX-A1644-1; SB16839; NCGC00379014-01; NCGC00379014-02; NCGC00379014-03; AK175991; AS-74411; HY-14763; US9550741, RGH-188; FT-0664381; D09997; Q2938837; RGH-188; RGH188; RGH 188; MP-214; MP 214; MP214; 3,3-dimethyl-1-[(1r,4r)-4-{2-[4-(2,3-dichlorophenyl)piperazin-1-yl]ethyl}cyclohexyl]urea; 3-((1r,4r)-4-(2-(4-(2,3-dichlorophenyl)piperazin-1-yl)ethyl)cyclohexyl)-1,1-dimethylurea; 3-(cis-4-(2-(4-(2,3-Dichlorophenyl)piperazin-1-yl)ethyl)-cyclohexyl)-1,1-dimethylurea; 3-(trans-4-(2-(4-(2,3-Dichlorophenyl)piperazin-1-yl)ethyl)-cyclohexyl)-1,1-dimethylurea; N'-(trans-4-{2-[4-(2,3-dichlorophenyl)piperazin-1-yl]ethyl}cyclohexyl)-N,N-dimethylurea; trans-N-[4-[2-[4-(2,3-di-chlorophenyl)piperazin-1-yl]ethyl]cyclohexyl]-N',N'-dimethylurea; Trans-1-{4-[2-[4-(2,3-dichlorophenyl)-piperazin-1-yl]-ethyl]-cyclohexyl}-3,3-dimethyl-urea; trans-N-{4-[2-[4-(2,3-dichlorophenyl)piperazine-1-yl]ethyl]cyclohexyl}-N',N'-dimethylurea hydrochloride; Urea, N'-(trans-4-(2-(4-(2,3-dichlorophenyl)-1-piperazinyl)ethyl)cyclohexyl)-N,N-dimethyl-
Clinical Status
Approved
Disease Indication Bipolar disorder ICD-11: 6A60 [1]
PubChem CID
11154555
Formula
C21H32Cl2N4O
Canonical SMILES
CN(C)C(=O)NC1CCC(CC1)CCN2CCN(CC2)C3=C(C(=CC=C3)Cl)Cl
InChI
1S/C21H32Cl2N4O/c1-25(2)21(28)24-17-8-6-16(7-9-17)10-11-26-12-14-27(15-13-26)19-5-3-4-18(22)20(19)23/h3-5,16-17H,6-15H2,1-2H3,(H,24,28)
InChIKey
KPWSJANDNDDRMB-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=11154555"></iframe>
3D MOL 2D MOL
Physicochemical Properties Molecular Weight 427.4 Topological Polar Surface Area 38.8
XlogP 4.3 Complexity 491
Heavy Atom Count 28 Rotatable Bond Count 5
Hydrogen Bond Donor Count 1 Hydrogen Bond Acceptor Count 3
Full List of Drug Formulations (DFMs) Containing This API
          Cariprazine 3 mg capsule 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
Fd&c red no. 40; Fd&c blue no. 1; Magnesium stearate; Ferric oxide yellow; Ferrosoferric oxide; Titanium dioxide; Gelatin; Shellac; Starch, corn
                   Dosage Form Oral Capsule
                   Company Allergan
                   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]
Allura red AC dye DIG Info Solute carrier SLCO2B1 (Ki = 2.59 uM) [3]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [4]
          Cariprazine 4.5 mg capsule 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
Fd&c red no. 40; Fd&c blue no. 1; Magnesium stearate; Ferric oxide yellow; Titanium dioxide; Gelatin; Shellac; Starch, corn
                   Dosage Form Oral Capsule
                   Company Allergan
                   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]
Allura red AC dye DIG Info Solute carrier SLCO2B1 (Ki = 2.59 uM) [3]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [4]
          Cariprazine 6 mg capsule 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
Fd&c blue no. 1; Magnesium stearate; Ferrosoferric oxide; Titanium dioxide; Fd&c red no. 3; Gelatin; Shellac; Starch, corn
                   Dosage Form Oral Capsule
                   Company Allergan
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
FD&C blue no. 1 DIG Info Solute carrier SLCO2B1 (Ki = 13 uM) [3]
FD&C red no. 3 DIG Info Phosphodiesterase 3A (IC50 = 0.092 uM) [2]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [4]
          Cariprazine Hydrochloride eq 3mg base capsule 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
Gelatin; Magnesium Stearate; Pregelatinized Starch; Shellac; Titanium Dioxide; Black Iron Oxide; Fd&C Blue 1; Fd&C Red 40; Yellow Iron Oxide
                   Dosage Form Capsule
                   Company Allergan
                   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]
Allura red AC dye DIG Info Solute carrier SLCO2B1 (Ki = 2.59 uM) [3]
Gelatin DIG Info Mephenytoin 4-hydroxylase (EC50 = 20.5 uM) [5]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [4]
Pregelatinized starch DIG Info Multidrug resistance protein 1 (Protein expression downregulation) [4]
          Cariprazine Hydrochloride eq 6mg base capsule 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
Gelatin; Magnesium Stearate; Pregelatinized Starch; Shellac; Titanium Dioxide; Black Iron Oxide; Fd&C Blue 1; Fd&C Red 3
                   Dosage Form Capsule
                   Company Allergan
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
FD&C blue no. 1 DIG Info Solute carrier SLCO2B1 (Ki = 13 uM) [3]
Erythrosine sodium anhydrous DIG Info Multidrug resistance protein 3 (IC50 = 133000 nM) [6]
Gelatin DIG Info Mephenytoin 4-hydroxylase (EC50 = 20.5 uM) [5]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [4]
Pregelatinized starch DIG Info Multidrug resistance protein 1 (Protein expression downregulation) [4]
          Cariprazine Hydrochloride eq 4.5mg base capsule 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
Gelatin; Magnesium Stearate; Pregelatinized Starch; Shellac; Titanium Dioxide; Fd&C Blue 1; Fd&C Red 40; Yellow Iron Oxide
                   Dosage Form Capsule
                   Company Allergan
                   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]
Allura red AC dye DIG Info Solute carrier SLCO2B1 (Ki = 2.59 uM) [3]
Gelatin DIG Info Mephenytoin 4-hydroxylase (EC50 = 20.5 uM) [5]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [4]
Pregelatinized starch DIG Info Multidrug resistance protein 1 (Protein expression downregulation) [4]
          Cariprazine Hydrochloride eq 1.5mg base capsule 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
Gelatin; Magnesium Stearate; Pregelatinized Starch; Shellac; Titanium Dioxide; Black Iron Oxide
                   Dosage Form Capsule
                   Company Allergan
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Gelatin DIG Info Mephenytoin 4-hydroxylase (EC50 = 20.5 uM) [5]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [4]
Pregelatinized starch DIG Info Multidrug resistance protein 1 (Protein expression downregulation) [4]
          Cariprazine 1.5 mg capsule 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
Magnesium stearate; Ferrosoferric oxide; Titanium dioxide; Gelatin; Shellac; Starch, corn
                   Dosage Form Oral Capsule
                   Company Allergan
                   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) [4]
References
1 FDA label for approved cariprazine 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 Effects of commonly used excipients on the expression of CYP3A4 in colon and liver cells. Pharm Res. 2010 Aug;27(8):1703-12.
5 Mediation of in vitro cytochrome p450 activity by common pharmaceutical excipients. Mol Pharm. 2013 Jul 1;10(7):2739-48.
6 A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development. Toxicol Sci. 2013 Nov; 136(1):216-41.

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