Details of the Active Pharmaceutical Ingredient (API)

General Information of API (ID: D00336)
Name
Isradipine
Synonyms    Click to Show/Hide the Synonyms of This API
isradipine; 75695-93-1; DynaCirc; Isradipin; Isrodipine; Prescal; Esradin; Dynacirc CR; Clivoten; Dynacrine; Isradipinum [Latin]; PN 200-110; Isradipino [Spanish]; Rebriden; (+-)-Isradipine; DynaCire; PN-200-110; DynaCire CR; (+/-)-Isradipine; Isradipine (Dynacirc); PN 200; C19H21N3O5; MFCD00153820; Isradipinum; Isradipino; DSSTox_CID_3179; DSSTox_RID_76907; DSSTox_GSID_23179; (+)-isradipine; SMR000466320; SMR002529690; DynaCirc (TN); Isradipine (USP/INN); SR-01000597526; Isradipine [USAN:USP:INN:BAN]; NCGC00016931-01; (-)-Isradipine; (plusmn)-isradipine; CAS-75695-93-1; Spectrum_000218; PN-200110; Prestwick0_001021; Prestwick1_001021; Prestwick2_001021; Prestwick3_001021; (.+/-.)-Isradipine; CHEMBL1648; SCHEMBL34555; BSPBio_001201; KBioSS_000698; cc-164; MLS000759425; MLS001424076; MLS002154106; MLS003915633; MLS006010138; SPBio_003062; BPBio1_001323; CHEBI:6073; CHEMBL315436; GTPL4488; CHEMBL3211306; DTXSID4023179; KBio2_000698; KBio2_003266; KBio2_005834; AOB5974; 2,1,3-Benzoxadiazole, 3,5-pyridinedicarboxylic acid deriv.; HMS1571M03; HMS2051J12; HMS2098M03; HMS2235O12; HMS3268D21; HMS3393J12; HMS3413A15; HMS3655C17; HMS3677A15; HMS3715M03; HMS3884E06; Pharmakon1600-02300234; (non-Isotopelabelled)Isradipine-d7; ACT02697; BCP06719; HY-B0233; Benzo[1,2,5]oxadiazol-4-aldehyde; Tox21_110690; BDBM50436176; CI0041; NSC759892; AKOS015895129; Isradipine, >=98% (HPLC), solid; Tox21_110690_1; AC-8539; CCG-101027; CCG-213711; DB00270; HS-0085; NC00277; NSC-759892; VA11116; NCGC00025341-01; NCGC00025341-02; NCGC00025341-03; NCGC00025341-06; 131970-21-3; AK163124; DB-055981; AB00514007; FT-0627542; SW220017-1; D00349; AB00514007_02; AB00514007_03; 695I931; Q414873; J-513454; SR-01000597526-1; SR-01000597526-2; BRD-A90799790-001-03-3; BRD-A90799790-001-10-8; Isradipine, European Pharmacopoeia (EP) Reference Standard; Isradipine, United States Pharmacopeia (USP) Reference Standard; Isopropyl Methyl 4-(2,1,3-Benzoxadiazol-4-yl)-1,4-dihydro-2,6-dimet
Clinical Status
Approved
Disease Indication Essential hypertension ICD-11: BA00 [1]
PubChem CID
3784
Formula
C19H21N3O5
Canonical SMILES
CC1=C(C(C(=C(N1)C)C(=O)OC(C)C)C2=CC=CC3=NON=C32)C(=O)OC
InChI
1S/C19H21N3O5/c1-9(2)26-19(24)15-11(4)20-10(3)14(18(23)25-5)16(15)12-7-6-8-13-17(12)22-27-21-13/h6-9,16,20H,1-5H3
InChIKey
HMJIYCCIJYRONP-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=3784"></iframe>
3D MOL 2D MOL
Physicochemical Properties Molecular Weight 371.4 Topological Polar Surface Area 104
XlogP 4.3 Complexity 685
Heavy Atom Count 27 Rotatable Bond Count 6
Hydrogen Bond Donor Count 1 Hydrogen Bond Acceptor Count 8
Full List of Drug Formulations (DFMs) Containing This API
          Isradipine 5 mg capsule Click to Show/Hide the Full List of Formulation(s):          2 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; Sodium lauryl sulfate; D&c yellow no. 10; Fd&c red no. 40; Butyl alcohol; Fd&c blue no. 1; Fd&c blue no. 2; Ferric oxide red; Ferrosoferric oxide; Propylene glycol; Titanium dioxide; Silicon dioxide; Cellulose, microcrystalline; Gelatin; Polyethylene glycol 8000; Shellac; Starch, corn
                   Dosage Form Oral Capsule
                   Company Epic Pharma; Golden State Medical Supply
                   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]
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
Anhydrous lactose; Sodium lauryl sulfate; Magnesium stearate; Ferric oxide yellow; Ferrosoferric oxide; Potassium hydroxide; Titanium dioxide; Silicon dioxide; Gelatin; Shellac; Starch, corn
                   Dosage Form Oral Capsule
                   Company Actavis Pharma; AvPAK; Carilion Materials Management
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Sodium lauryl sulfate DIG Info Solute carrier SLCO2B1 (Ki = 1.98 uM) [3]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [5]
Silicon dioxide DIG Info Albendazole monooxygenase (Protein expression downregulation) [5]
          Isradipine 2.5 mg capsule Click to Show/Hide the Full List of Formulation(s):          2 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; Sodium lauryl sulfate; D&c yellow no. 10; Fd&c red no. 40; Butyl alcohol; Fd&c blue no. 1; Fd&c blue no. 2; Ferrosoferric oxide; Propylene glycol; Titanium dioxide; Silicon dioxide; Cellulose, microcrystalline; Gelatin; Polyethylene glycol 8000; Shellac; Starch, corn
                   Dosage Form Oral Capsule
                   Company Epic Pharma; Golden State Medical Supply
                   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]
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
Anhydrous lactose; Sodium lauryl sulfate; Magnesium stearate; Ferric oxide red; Ferric oxide yellow; Ferrosoferric oxide; Potassium hydroxide; Titanium dioxide; Silicon dioxide; Gelatin; Shellac; Starch, corn
                   Dosage Form Oral Capsule
                   Company Actavis Pharma; AvPAK
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Sodium lauryl sulfate DIG Info Solute carrier SLCO2B1 (Ki = 1.98 uM) [3]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [5]
Silicon dioxide DIG Info Albendazole monooxygenase (Protein expression downregulation) [5]
References
1 FDA label for approved isradipine 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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