General Information of API (ID: D00079)
Name
Bromocriptine
Synonyms    Click to Show/Hide the Synonyms of This API
bromocriptine; Bromocryptine; 25614-03-3; Bromocriptin; Bromoergocryptine; Bromoergocriptine; Bromergocryptine; 2-Bromo-alpha-ergocryptine; Parlodel; 2-Bromo-alpha-ergokryptine; Bromocriptina; Bromocriptinum; 2-Bromo-alpha-ergokryptin; Bromocriptinum [INN-Latin]; Bromocriptina [INN-Spanish]; Bagren; BROMOCRIPTINE MESYLATE; Bromocriptine methanesulfonate; UNII-3A64E3G5ZO; CB-154; 2-Bromoergocryptine; 3A64E3G5ZO; CHEBI:3181; Ergoset; Bromergon; CB 154; Bromocriptine (mesylate); C32H40BrN5O5; CCRIS 3244; NSC169774; EINECS 247-128-5; Bromocriptine (USAN/INN); SR-01000075356; Bromocriptine [USAN:INN:BAN]; NCGC00024584-03; Bromocriptine+ (GTP-); Prestwick0_000121; Prestwick1_000121; Prestwick2_000121; Carboprost Methylate,(S); DSSTox_CID_2687; Biomol-NT_000005; CHEMBL493; GTPL35; (5'alpha)-2-bromo-12'-hydroxy-5'-isobutyl-2'-isopropyl-3',6',18-trioxoergotaman; DSSTox_RID_76692; DSSTox_GSID_22687; Lopac0_000171; SCHEMBL25297; BIDD:GT0464; SPBio_002101; BPBio1_001131; DTXSID1022687; SANDOZ 15-754; BDBM81993; Ergocryptine, 2-bromo- (8CI); Tox21_110907; PDSP2_001500; ZINC53683151; AKOS015961273; CCG-204266; DB01200; SDCCGSBI-0050159.P003; dioxooctahydro-2H-oxazolo[3,2-a]pyrrolo; NCGC00024584-04; NCGC00024584-05; NCGC00024584-07; NCGC00024584-09; AC-13601; NCI60_001365; 10b-hydroxy-5-isobutyl-2-isopropyl-3,6-; CAS-25614-03-3; C06856; D03165; hexahydroindolo[4,3-fg]quinoline-9-carboxamide; 13177-EP2272832A1; 13177-EP2275420A1; 13177-EP2277876A1; 13177-EP2280008A2; 13177-EP2287165A2; 13177-EP2287166A2; 13177-EP2292614A1; 13177-EP2292620A2; 13177-EP2295412A1; 13177-EP2295413A1; 13177-EP2295439A1; 13177-EP2298731A1; 13177-EP2298738A1; 13177-EP2298779A1; 13177-EP2311808A1; 13177-EP2311818A1; 13177-EP2311829A1; 13177-EP2311837A1; 13177-EP2316470A2; 13177-EP2316834A1; 88085-EP2298415A1; 88085-EP2298742A1; 88085-EP2305648A1; Q413581; J-016067; SR-01000075356-5; (6aR,9R)-5-bromo-N-((2R,5S,10aS,10bS)-; [2,1-c]pyrazin-2-yl)-7-methyl-4,6,6a,7,8,9-; BRD-K14496212-001-01-1; BRD-K14496212-066-04-8
Clinical Status
Approved
Disease Indication Diabetes mellitus ICD-11: 5A10 [1]
PubChem CID
31101
Formula
C32H40BrN5O5
Canonical SMILES
CC(C)C[C@H]1C(=O)N2CCC[C@H]2[C@]3(N1C(=O)[C@](O3)(C(C)C)NC(=O)[C@H]4CN([C@@H]5CC6=C(NC7=CC=CC(=C67)C5=C4)Br)C)O
InChI
1S/C32H40BrN5O5/c1-16(2)12-24-29(40)37-11-7-10-25(37)32(42)38(24)30(41)31(43-32,17(3)4)35-28(39)18-13-20-19-8-6-9-22-26(19)21(27(33)34-22)14-23(20)36(5)15-18/h6,8-9,13,16-18,23-25,34,42H,7,10-12,14-15H2,1-5H3,(H,35,39)/t18-,23-,24+,25+,31-,32+/m1/s1
InChIKey
OZVBMTJYIDMWIL-AYFBDAFISA-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=31101"></iframe>
3D MOL 2D MOL
Physicochemical Properties Molecular Weight 654.6 Topological Polar Surface Area 118
XlogP 3.8 Complexity 1230
Heavy Atom Count 43 Rotatable Bond Count 5
Hydrogen Bond Donor Count 3 Hydrogen Bond Acceptor Count 6
Full List of Drug Formulations (DFMs) Containing This API
          Bromocriptine 5 mg capsule Click to Show/Hide the Full List of Formulation(s):          7 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; Maleic acid; Butyl alcohol; Fd&c blue no. 1; Fd&c blue no. 2; Magnesium stearate; Ferric oxide red; Ferric oxide yellow; Ferrosoferric oxide; Propylene glycol; Titanium dioxide; Gelatin; Shellac; Starch, corn
                   Dosage Form Oral Capsule
                   Company Avera McKennan Hospital; 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]
Maleic acid DIG Info D-amino acid oxidase (IC50 = 357000 nM) [4]
Propylene glycol DIG Info Albendazole monooxygenase (Inhibition ratio < 20 %) [5]
Magnesium stearate 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
D&c red no. 28; Lactose monohydrate; Maleic acid; Fd&c blue no. 1; Fd&c yellow no. 6; Magnesium stearate; Titanium dioxide; Silicon dioxide; Gelatin
                   Dosage Form Oral Capsule
                   Company Cadila Healthcare
                   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]
Sunset yellow FCF DIG Info Solute carrier SLCO2B1 (Ki = 68.4 uM) [3]
D&C red no. 28 DIG Info Organic anion transporter 1 (Ki = 0.064 uM) [2]
Maleic acid DIG Info D-amino acid oxidase (IC50 = 357000 nM) [4]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [6]
Silicon dioxide 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; Maleic acid; Butyl alcohol; Isopropyl alcohol; Magnesium stearate; Ammonia; Ferric oxide red; Ferrosoferric oxide; Potassium hydroxide; Propylene glycol; Titanium dioxide; Water; Silicon dioxide; Alcohol; Carrageenan; Hypromellose 2910 (15 mpa.s); Shellac
                   Dosage Form Oral Capsule
                   Company Zydus Pharmaceuticals
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Maleic acid DIG Info D-amino acid oxidase (IC50 = 357000 nM) [4]
Isopropyl alcohol DIG Info Lymphoma P388/ADR cells (IC50 = 0.22 uM) [7]
Propylene glycol DIG Info Albendazole monooxygenase (Inhibition ratio < 20 %) [5]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [6]
Silicon dioxide 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
Lactose; Sodium lauryl sulfate; Isopropyl alcohol; Magnesium stearate; Ferric oxide red; Ferric oxide yellow; Titanium dioxide; Silicon dioxide; Gelatin; Povidones; Starch, corn
                   Dosage Form Oral Capsule
                   Company Validus Pharmaceuticals
                   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]
Isopropyl alcohol DIG Info Lymphoma P388/ADR cells (IC50 = 0.22 uM) [7]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [6]
Silicon dioxide 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, unspecified form; Sodium lauryl sulfate; Isopropyl alcohol; Magnesium stearate; Ferric oxide red; Ferric oxide yellow; Titanium dioxide; Silicon dioxide; Gelatin; Povidones; Starch, corn
                   Dosage Form Oral Capsule
                   Company Sun Pharmaceutical Industries
                   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]
Isopropyl alcohol DIG Info Lymphoma P388/ADR cells (IC50 = 0.22 uM) [7]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [6]
Silicon dioxide DIG Info Albendazole monooxygenase (Protein expression downregulation) [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
Lactose; Sodium lauryl sulfate; Magnesium stearate; Ferric oxide red; Ferric oxide yellow; Titanium dioxide; Silicon dioxide; Silicon dioxide; Gelatin; Starch, corn
                   Dosage Form Oral Capsule
                   Company Sandoz
                   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) [6]
Silicon dioxide DIG Info Albendazole monooxygenase (Protein expression downregulation) [6]
             Drug Formulation 7 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; Sodium lauryl sulfate; Magnesium stearate; Ferric oxide red; Ferric oxide yellow; Titanium dioxide; Silicon dioxide; Gelatin; Starch, corn
                   Dosage Form Oral Capsule
                   Company Novartis Pharmaceuticals Corporation; Validus Pharmaceuticals
                   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) [6]
Silicon dioxide DIG Info Albendazole monooxygenase (Protein expression downregulation) [6]
          Bromocriptine 2.5 mg tablet Click to Show/Hide the Full List of Formulation(s):          7 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; Maleic acid; Isopropyl alcohol; Magnesium stearate; Silicon dioxide; Povidones; Starch, corn
                   Dosage Form Oral Tablet
                   Company Validus Pharmaceuticals
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Maleic acid DIG Info D-amino acid oxidase (IC50 = 357000 nM) [4]
Isopropyl alcohol DIG Info Lymphoma P388/ADR cells (IC50 = 0.22 uM) [7]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [6]
Silicon dioxide 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
Lactose, unspecified form; Maleic acid; Isopropyl alcohol; Magnesium stearate; Silicon dioxide; Povidones; Starch, corn
                   Dosage Form Oral Tablet
                   Company Sun Pharmaceutical Industries
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Maleic acid DIG Info D-amino acid oxidase (IC50 = 357000 nM) [4]
Isopropyl alcohol DIG Info Lymphoma P388/ADR cells (IC50 = 0.22 uM) [7]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [6]
Silicon dioxide 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; Sodium lauryl sulfate; Maleic acid; Magnesium stearate; Edetate disodium; Starch, corn
                   Dosage Form Oral Tablet
                   Company Kaiser Foundation Hospitals; Mylan Pharamceuticals; Physicians Total Care
                   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]
Maleic acid DIG Info D-amino acid oxidase (IC50 = 357000 nM) [4]
Magnesium stearate 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
Lactose monohydrate; Maleic acid; Magnesium stearate; Edetate disodium; Silicon dioxide; Povidone, unspecified; Starch, corn
                   Dosage Form Oral Tablet
                   Company American Health Packaging
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Maleic acid DIG Info D-amino acid oxidase (IC50 = 357000 nM) [4]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [6]
Silicon dioxide 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; Maleic acid; Magnesium stearate; Edetate disodium; Silicon dioxide; Povidones; Starch, corn
                   Dosage Form Oral Tablet
                   Company Sandoz
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Maleic acid DIG Info D-amino acid oxidase (IC50 = 357000 nM) [4]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [6]
Silicon dioxide DIG Info Albendazole monooxygenase (Protein expression downregulation) [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; Maleic acid; Magnesium stearate; Silicon dioxide; Povidone k25; Starch, corn
                   Dosage Form Oral Tablet
                   Company Carilion Materials Management; Kaiser Foundation Hospitals; Paddock Laboratories,
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Maleic acid DIG Info D-amino acid oxidase (IC50 = 357000 nM) [4]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [6]
Silicon dioxide DIG Info Albendazole monooxygenase (Protein expression downregulation) [6]
             Drug Formulation 7 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; Silicon dioxide; Povidones; Starch, corn
                   Dosage Form Oral Tablet
                   Company Novartis Pharmaceuticals Corporation; Validus Pharmaceuticals
                   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]
Silicon dioxide DIG Info Albendazole monooxygenase (Protein expression downregulation) [6]
          Bromocriptine 0.8 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, unspecified form; Magnesium stearate; Citric acid monohydrate; Silicon dioxide; Starch, corn
                   Dosage Form Oral Tablet
                   Company Santarus
                   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]
Silicon dioxide DIG Info Albendazole monooxygenase (Protein expression downregulation) [6]
References
1 FDA label for approved bromocriptine 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 Identification of novel D-amino acid oxidase inhibitors by in silico screening and their functional characterization in vitro. J Med Chem. 2013 Mar 14; 56(5):1894-907.
5 Pharmaceutical excipients inhibit cytochrome P450 activity in cell free systems and after systemic administration. Eur J Pharm Biopharm. 2008 Sep;70(1):279-88.
6 Effects of commonly used excipients on the expression of CYP3A4 in colon and liver cells. Pharm Res. 2010 Aug;27(8):1703-12.
7 Synthesis and evaluation of dihydropyrroloquinolines that selectively antagonize P-glycoprotein. J Med Chem. 2004 Mar 11; 47(6):1413-22.

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