Details of the Active Pharmaceutical Ingredient (API)

General Information of API (ID: D00465)
Name
Nicardipine
Synonyms    Click to Show/Hide the Synonyms of This API
nicardipine; 55985-32-5; Nicardipinum; Nicardipinum [INN-Latin]; Nicardipino [INN-Spanish]; CHEBI:7550; YC-93 (free base); Cardene (TN); NCGC00015747-03; Nicardipino; DSSTox_CID_3363; Nicardipine [INN:BAN]; DSSTox_RID_76992; DSSTox_GSID_23363; Nicardipine (INN); CAS-55985-32-5; EINECS 259-932-3; BRN 0504321; (R,S)-nicardipine; Spectrum_001372; Prestwick0_000383; Prestwick1_000383; Prestwick2_000383; Prestwick3_000383; Spectrum2_001415; Spectrum3_001452; Spectrum4_000422; Spectrum5_001320; CHEMBL1484; CBiol_001802; Lopac0_000809; Oprea1_436998; SCHEMBL34277; BSPBio_000565; BSPBio_001389; BSPBio_002943; KBioGR_000109; KBioGR_000744; KBioSS_000109; KBioSS_001852; BIDD:GT0621; DivK1c_000540; SPBio_001490; SPBio_002486; BPBio1_000623; GTPL2559; CHEMBL3302409; DTXSID6023363; KBio1_000540; KBio2_000109; KBio2_001852; KBio2_002677; KBio2_004420; KBio2_005245; KBio2_006988; KBio3_000217; KBio3_000218; KBio3_002443; NINDS_000540; Bio1_000088; Bio1_000577; Bio1_001066; Bio2_000109; Bio2_000589; HMS1791F11; HMS1989F11; HMS2089C09; HMS3886G17; BCP21397; EX-A4680; Tox21_110211; BDBM50101815; AKOS001637090; Tox21_110211_1; CCG-204893; CS-3685; DB00622; SDCCGSBI-0050786.P004; IDI1_000540; IDI1_033859; NCGC00015747-02; NCGC00015747-04; NCGC00015747-05; NCGC00015747-06; NCGC00015747-07; NCGC00015747-09; NCGC00015747-11; NCGC00015747-18; NCGC00162262-01; NCGC00162262-02; NCGC00162262-03; NCGC00162262-04; AC-19947; AS-56335; HY-12515; SBI-0050786.P003; DB-052833; AB00514658; FT-0630688; C07264; D08270; 45480-EP2269989A1; 45480-EP2270011A1; 45480-EP2272841A1; 45480-EP2275420A1; 45480-EP2280008A2; 45480-EP2295406A1; 45480-EP2298742A1; 45480-EP2298764A1; 45480-EP2298765A1; 45480-EP2298772A1; 45480-EP2298779A1; 45480-EP2301923A1; 45480-EP2301931A1; 45480-EP2301936A1; 45480-EP2305648A1; 45480-EP2308839A1; 45480-EP2311806A2; AB00053604-03; AB00053604_04; AB00053604_05; 985N325; L000715; Q729213; BRD-A26711594-001-02-7; BRD-A26711594-003-05-6; BRD-A26711594-003-06-4; L-GLUTAMICACID,N-(1-DEOXY-D-FRUCTOS-1-YL)-; 106664-28-2
Clinical Status
Approved
Disease Indication Essential hypertension ICD-11: BA00 [1]
PubChem CID
4474
Formula
C26H29N3O6
Canonical SMILES
CC1=C(C(C(=C(N1)C)C(=O)OCCN(C)CC2=CC=CC=C2)C3=CC(=CC=C3)[N+](=O)[O-])C(=O)OC
InChI
1S/C26H29N3O6/c1-17-22(25(30)34-4)24(20-11-8-12-21(15-20)29(32)33)23(18(2)27-17)26(31)35-14-13-28(3)16-19-9-6-5-7-10-19/h5-12,15,24,27H,13-14,16H2,1-4H3
InChIKey
ZBBHBTPTTSWHBA-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=4474"></iframe>
3D MOL 2D MOL
Physicochemical Properties Molecular Weight 479.5 Topological Polar Surface Area 114
XlogP 3.8 Complexity 856
Heavy Atom Count 35 Rotatable Bond Count 10
Hydrogen Bond Donor Count 1 Hydrogen Bond Acceptor Count 8
Full List of Drug Formulations (DFMs) Containing This API
          Nicardipine 30 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
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; Ferric oxide yellow; Ferrosoferric oxide; Propylene glycol; Titanium dioxide; Silicon dioxide; Fd&c green no. 3; Gelatin; Starch, corn
                   Dosage Form Oral Capsule
                   Company Avera McKennan Hospital
                   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]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [5]
Silicon dioxide DIG Info Albendazole monooxygenase (Protein expression downregulation) [5]
             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
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; Ferric oxide yellow; Ferrosoferric oxide; Propylene glycol; Titanium dioxide; Silicon dioxide; Fd&c green no. 3; Gelatin; Shellac; Starch, corn
                   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]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [5]
Silicon dioxide DIG Info Albendazole monooxygenase (Protein expression downregulation) [5]
             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
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; Ferric oxide yellow; Ferrosoferric oxide; Propylene glycol; Titanium dioxide; Silicon dioxide; Fd&c green no. 3; Gelatin, unspecified; Shellac; Starch, corn
                   Dosage Form Oral Capsule
                   Company 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]
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]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [5]
Silicon dioxide DIG Info Albendazole monooxygenase (Protein expression downregulation) [5]
             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
Fd&c red no. 40; Fd&c blue no. 1; Fd&c blue no. 2; Magnesium stearate; Ferrosoferric oxide; Propylene glycol; Titanium dioxide; Gelatin; Starch, corn
                   Dosage Form Oral Capsule
                   Company AvKARE; Avera McKennan Hospital; Epic Pharma; PuraCap Laboratories
                   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]
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) [5]
             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; Magnesium stearate; Cellulose, microcrystalline; Corn; Methacrylic acid - ethyl acrylate copolymer (1:1) type a; Starch, corn
                   Dosage Form 12 HR Extended Release Capsule
                   Company EKR Therapeutics
                   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) [5]
             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
Lactose; Magnesium stearate; Cellulose, microcrystalline; Corn; Methacrylic acid - ethyl acrylate copolymer (1:1) type a; Starch, corn
                   Dosage Form 12 HR Extended Release Oral Capsule
                   Company Carilion Materials Management
                   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) [5]
          Nicardipine 20 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
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; Silicon dioxide; Fd&c green no. 3; Gelatin; Starch, corn
                   Dosage Form Oral Capsule
                   Company 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]
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]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [5]
Silicon dioxide DIG Info Albendazole monooxygenase (Protein expression downregulation) [5]
             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
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; Silicon dioxide; Fd&c green no. 3; Gelatin; Shellac; Starch, corn
                   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]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [5]
Silicon dioxide DIG Info Albendazole monooxygenase (Protein expression downregulation) [5]
             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
D&c yellow no. 10; Fd&c red no. 40; Fd&c blue no. 1; Fd&c blue no. 2; Magnesium stearate; Ferrosoferric oxide; Titanium dioxide; Gelatin; Starch, corn
                   Dosage Form Oral Capsule
                   Company AvKARE; Avera McKennan Hospital; Epic Pharma; PuraCap Laboratories
                   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]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [5]
          Nicardipine 45 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
Lactose; Magnesium stearate; Cellulose, microcrystalline; Corn; Methacrylic acid - ethyl acrylate copolymer (1:1) type a; Starch, corn
                   Dosage Form 12 HR Extended Release Capsule
                   Company EKR Therapeutics
                   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) [5]
          Nicardipine 60 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
Lactose; Magnesium stearate; Cellulose, microcrystalline; Corn; Methacrylic acid - ethyl acrylate copolymer (1:1) type a; Starch, corn
                   Dosage Form 12 HR Extended Release Capsule
                   Company EKR Therapeutics
                   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) [5]
References
1 FDA label for approved nicardipine 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 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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