Details of the Active Pharmaceutical Ingredient (API)

General Information of API (ID: D00082)
Name
Buprenorphine
Synonyms    Click to Show/Hide the Synonyms of This API
buprenorphine; Buprenex; Temgesic; Buprenophine; Buprenorfina; Buprenorphinum; Probuphine; Subutex; Buprenorfina [INN-Spanish]; Buprenorphinum [INN-Latin]; (-)-buprenorphine; 52485-79-7; UNII-40D3SCR4GZ; Butrans; CHEBI:3216; DEA No. 9064; 40D3SCR4GZ; CAM2038; 21-cyclopropyl-7alpha-[(S)-1-hydroxy-1,2,2-trimethylpropyl]-6,14-endo-ethano-6,7,8,14-tetrahydrooripavine; RX 6029M; 17-cyclopropylmethyl-4,5alpha-epoxy-7alpha-((S)-1-hydroxy-1,2,2-trimethylpropyl)-6-methoxy-6,14-endo-ethanomorphinan-3-ol; 2-(N-cyclopropylmethyl-4,5alpha-epoxy-3-hydroxy-6-methoxy-6,14-endo-ethanomorphinan-6alpha-yl)-3,3-dimethyl-2-butanol; Probuphenine; Temgesic (TN); 2-[3-cyclopropylmethyl-11-hydroxy-15-methoxy-(14R)-13-oxa-3-azahexacyclo[13.2.2.12,8.01,6.06,14.07,12]icosa-7,9,11-trien-16-yl]-3,3-dimethyl-2-butanol; 6029-M; Buprenorphine (JAN/INN); CHEMBL560511; buprenorphin; Buvidal; Sublocade; Buprenorphine [INN:BAN:JAN]; EINECS 257-950-6; [5alpha,7alpha(S)]-; SCHEMBL15821; (5alpha,6beta,14beta,18R)-17-(cyclopropylmethyl)-18-[(2S)-2-hydroxy-3,3-dimethylbutan-2-yl]-6-methoxy-18,19-dihydro-4,5-epoxy-6,14-ethenomorphinan-3-ol; 17-Cyclopropylmethyl-4,5alpha-epoxy-7alpha-((S)-1-hydroxy-1,2,2-trimethylpropyl-6-methoxy-6,14-endo-ethanomorphinan-3-ol; 2-(N-Cyclopropylmethyl-4,5alpha-epoxy-3-hydroxy-6-methoxy-6,14-endo-ethanomorphinan-7alpha-yl)-3,3-dimethyl-2-butanol; 21-(Cyclopropyl-7alpha-((S)-1-hydroxy-1,2,2-trimethylpropyl-6,14-endo-ethano-6,7,8,14-tetrahydrooripavine; GTPL1670; DTXSID2022705; Sixmo (buprenorphine hydrochloride); RBP-6000; ZINC1319780; BDBM50026603; DB00921; [5alpha,7alpha(S)]-17-(Cyclopropylmethyl)-alpha-(1,1-dimethylethyl)-4,5-epoxy-18,19-dihydro-3-hydroxy-6-methoxy-alpha-methyl-6,14-ethenomorphinan-7-methanol; 21-cyclopropyl-7alpha-(2-hydroxy-3,3-dimethyl-2-butyl)-6,14-endo-ethano-6,7,8,14-tetrahydrooripavine; C08007; D07132; Q407721; (1S,2R,6S,14R,15R,16R)-3-(cyclopropylmethyl)-16-[(2S)-2-hydroxy-3,3-dimethylbutan-2-yl]-15-methoxy-13-oxa-3-azahexacyclo[13.2.2.1^{2,8}.0^{1,6}.0^{6,14}.0^{7,12}]icosa-7(12),8,10-trien-11-ol; (1S,2R,6S,14R,15R,16R)-3-(cyclopropylmethyl)-16-[(2S)-2-hydroxy-3,3-dimethylbutan-2-yl]-15-methoxy-13-oxa-3-azahexacyclo[13.2.2.1^{2,8}.0^{1,6}.0^{6,14}.0^{7,12}]icosa-7,9,11-trien-11-ol; (2S)-2-[(5R,6R,7R,14S)-9alpha-Cyclopropylmethyl-3-hydroxy-6-methoxy-4,5-epoxy-6,14-ethanomorphinan-7-yl]-3,3-dimethylbutan-2-ol; 6,14-ethenomorphinan-3-ol, 17-(cyclopropylmethyl)-4,5-epoxy-18,19-dihydro-7-[(1S)-1-hydroxy-1,2,2-trimethylpropyl]-6-methoxy-, (5alpha,7alpha)-; 6,14-Ethenomorphinan-7-methanol, 17-(cyclopropylmethyl)-alpha-(1,1-dimethylethyl)-4,5-epoxy-18,19-dihydro-3-hydroxy-6-methoxy-alpha-methyl-,; 6,14-Ethenomorphinan-7-methanol, 17-(cyclopropylmethyl)-alpha-(1,1-dimethylethyl)-4,5-epoxy-18,19-dihydro-3-hydroxy-6-methoxy-alpha-methyl-, (alphaS,5alpha,7alpha)- (9CI)
Clinical Status
Approved
Disease Indication Opiate dependence ICD-11: 6C43 [1]
PubChem CID
644073
Formula
C29H41NO4
Canonical SMILES
C[C@]([C@H]1C[C@@]23CC[C@@]1([C@H]4[C@@]25CCN([C@@H]3CC6=C5C(=C(C=C6)O)O4)CC7CC7)OC)(C(C)(C)C)O
InChI
1S/C29H41NO4/c1-25(2,3)26(4,32)20-15-27-10-11-29(20,33-5)24-28(27)12-13-30(16-17-6-7-17)21(27)14-18-8-9-19(31)23(34-24)22(18)28/h8-9,17,20-21,24,31-32H,6-7,10-16H2,1-5H3/t20-,21-,24-,26+,27-,28+,29-/m1/s1
InChIKey
RMRJXGBAOAMLHD-IHFGGWKQSA-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=644073"></iframe>
3D MOL 2D MOL
Physicochemical Properties Molecular Weight 467.6 Topological Polar Surface Area 62.2
XlogP 5 Complexity 869
Heavy Atom Count 34 Rotatable Bond Count 5
Hydrogen Bond Donor Count 2 Hydrogen Bond Acceptor Count 5
Full List of Drug Formulations (DFMs) Containing This API
          Buprenorphine 2 mg tablet Click to Show/Hide the Full List of Formulation(s):        12 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 citric acid; Lactose monohydrate; Fd&c yellow no. 6; Magnesium stearate; Mannitol; Trisodium citrate dihydrate; Crospovidone; Povidone; Aluminum oxide; Starch, corn
                   Dosage Form Sublingual Tablet
                   Company Contract Pharmacal; RemedyRepack
                   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]
Kyselina citronova DIG Info Perilipin-1 (IC50 = 3708 nM) [3]
Mannitol DIG Info Glycine receptor alpha-1 (EC50 = 12589.25 nM) [4]
Povidone DIG Info Cholesterol 25-hydroxylase (IC50 = 78.3 uM) [5]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [6]
Crospovidone 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
Anhydrous citric acid; Lactose monohydrate; Sodium citrate; Magnesium stearate; Mannitol; Crospovidone; Povidone; Starch, corn
                   Dosage Form Sublingual Tablet
                   Company Cardinal Health; RemedyRepack
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Sodium citrate anhydrous DIG Info Carbonic anhydrase IV (Ki = 99 nM) [7]
Kyselina citronova DIG Info Perilipin-1 (IC50 = 3708 nM) [3]
Mannitol DIG Info Glycine receptor alpha-1 (EC50 = 12589.25 nM) [4]
Povidone DIG Info Cholesterol 25-hydroxylase (IC50 = 78.3 uM) [5]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [6]
Crospovidone 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 citric acid; Anhydrous lactose; Lactose monohydrate; Sodium citrate, unspecified form; Magnesium stearate; Mannitol; Silicon dioxide; Crospovidone, unspecified; Microcrystalline cellulose; Starch, corn
                   Dosage Form Sublingual Tablet
                   Company Contract Pharmacal; Mylan Pharamceuticals; RemedyRepack
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Sodium citrate anhydrous DIG Info Carbonic anhydrase IV (Ki = 99 nM) [7]
Kyselina citronova DIG Info Perilipin-1 (IC50 = 3708 nM) [3]
Mannitol DIG Info Glycine receptor alpha-1 (EC50 = 12589.25 nM) [4]
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
Anhydrous citric acid; Anhydrous lactose; Lactose monohydrate; Sodium citrate, unspecified form; Magnesium stearate; Mannitol; Silicon dioxide; Cellulose, microcrystalline; Crospovidone (15 mpa.s at 5%); Starch, corn
                   Dosage Form Sublingual Tablet
                   Company RemedyRepack
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Sodium citrate anhydrous DIG Info Carbonic anhydrase IV (Ki = 99 nM) [7]
Kyselina citronova DIG Info Perilipin-1 (IC50 = 3708 nM) [3]
Mannitol DIG Info Glycine receptor alpha-1 (EC50 = 12589.25 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
Anhydrous citric acid; Lactose monohydrate; Sodium citrate; Magnesium stearate; Mannitol; Crospovidone; Povidones; Starch, corn
                   Dosage Form Sublingual Tablet
                   Company Lake Eire Medical & Surgical Supply DBA Quality Care Products
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Sodium citrate anhydrous DIG Info Carbonic anhydrase IV (Ki = 99 nM) [7]
Kyselina citronova DIG Info Perilipin-1 (IC50 = 3708 nM) [3]
Mannitol DIG Info Glycine receptor alpha-1 (EC50 = 12589.25 nM) [4]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [6]
Crospovidone 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 citric acid; Lactose monohydrate; Sodium citrate; Magnesium stearate; Mannitol; Povidone; Starch, corn
                   Dosage Form Sublingual Tablet
                   Company RemedyRepack
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Sodium citrate anhydrous DIG Info Carbonic anhydrase IV (Ki = 99 nM) [7]
Kyselina citronova DIG Info Perilipin-1 (IC50 = 3708 nM) [3]
Mannitol DIG Info Glycine receptor alpha-1 (EC50 = 12589.25 nM) [4]
Povidone DIG Info Cholesterol 25-hydroxylase (IC50 = 78.3 uM) [5]
Magnesium stearate 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
Anhydrous citric acid; Lactose monohydrate; Sodium citrate; Magnesium stearate; Mannitol; Butylated hydroxyanisole; Povidones; Starch, corn
                   Dosage Form Sublingual Tablet
                   Company RemedyRepack; Sun Pharmaceutical Industries
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Sodium citrate anhydrous DIG Info Carbonic anhydrase IV (Ki = 99 nM) [7]
Kyselina citronova DIG Info Perilipin-1 (IC50 = 3708 nM) [3]
Mannitol DIG Info Glycine receptor alpha-1 (EC50 = 12589.25 nM) [4]
Butylhydroxyanisole DIG Info Prostaglandin G/H synthase 2 (IC50 = 2.6 uM) [8]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [6]
             Drug Formulation 8 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 citric acid; Lactose monohydrate; Fd&c yellow no. 6; Magnesium stearate; Mannitol; Trisodium citrate dihydrate; Povidone k30; Crospovidone (15 mpa.s at 5%); Starch, corn
                   Dosage Form Sublingual Tablet
                   Company Actavis Pharma
                   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]
Kyselina citronova DIG Info Perilipin-1 (IC50 = 3708 nM) [3]
Mannitol DIG Info Glycine receptor alpha-1 (EC50 = 12589.25 nM) [4]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [6]
             Drug Formulation 9 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 citric acid; Lactose monohydrate; Sodium citrate, unspecified form; Magnesium stearate; Mannitol; Povidone k30; Starch, corn
                   Dosage Form Sublingual Tablet
                   Company Contract Pharmacal; Teva Pharmaceuticals
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Sodium citrate anhydrous DIG Info Carbonic anhydrase IV (Ki = 99 nM) [7]
Kyselina citronova DIG Info Perilipin-1 (IC50 = 3708 nM) [3]
Mannitol DIG Info Glycine receptor alpha-1 (EC50 = 12589.25 nM) [4]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [6]
             Drug Formulation 10 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 citric acid; Lactose monohydrate; Sodium citrate, unspecified form; Magnesium stearate; Mannitol; Crospovidone (15 mpa.s at 5%); Povidones; Starch, corn
                   Dosage Form Sublingual Tablet
                   Company Contract Pharmacal; West-Ward Pharmaceticals
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Sodium citrate anhydrous DIG Info Carbonic anhydrase IV (Ki = 99 nM) [7]
Kyselina citronova DIG Info Perilipin-1 (IC50 = 3708 nM) [3]
Mannitol DIG Info Glycine receptor alpha-1 (EC50 = 12589.25 nM) [4]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [6]
             Drug Formulation 11 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 citric acid; Lactose monohydrate; Magnesium stearate; Mannitol; Trisodium citrate dihydrate; Povidone k30; Crospovidone, unspecified; Starch, corn
                   Dosage Form Sublingual Tablet
                   Company Rhodes Pharmaceuticals
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Kyselina citronova DIG Info Perilipin-1 (IC50 = 3708 nM) [3]
Mannitol DIG Info Glycine receptor alpha-1 (EC50 = 12589.25 nM) [4]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [6]
             Drug Formulation 12 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 citric acid; Lactose monohydrate; Sodium stearyl fumarate; Mannitol; Trisodium citrate dihydrate; Povidone k30
                   Dosage Form Sublingual Tablet
                   Company Bryant Ranch Prepack; Contract Pharmacal; Hi-Tech Pharmacal; RemedyRepack; TYA Pharmaceuticals
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Kyselina citronova DIG Info Perilipin-1 (IC50 = 3708 nM) [3]
Mannitol DIG Info Glycine receptor alpha-1 (EC50 = 12589.25 nM) [4]
Sodium stearyl fumarate DIG Info Leukemia K562 cells (IC50 = 20.2 ug.mL-1) [9]
          Buprenorphine 8 mg tablet Click to Show/Hide the Full List of Formulation(s):        10 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 citric acid; Lactose monohydrate; Fd&c yellow no. 6; Magnesium stearate; Mannitol; Trisodium citrate dihydrate; Crospovidone; Povidone; Aluminum oxide; Starch, corn
                   Dosage Form Sublingual Tablet
                   Company Contract Pharmacal; RemedyRepack
                   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]
Kyselina citronova DIG Info Perilipin-1 (IC50 = 3708 nM) [3]
Mannitol DIG Info Glycine receptor alpha-1 (EC50 = 12589.25 nM) [4]
Povidone DIG Info Cholesterol 25-hydroxylase (IC50 = 78.3 uM) [5]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [6]
Crospovidone 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
Anhydrous citric acid; Anhydrous lactose; Lactose monohydrate; Sodium citrate, unspecified form; Magnesium stearate; Mannitol; Silicon dioxide; Crospovidone, unspecified; Microcrystalline cellulose; Starch, corn
                   Dosage Form Sublingual Tablet
                   Company Contract Pharmacal; Mylan Pharamceuticals
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Sodium citrate anhydrous DIG Info Carbonic anhydrase IV (Ki = 99 nM) [7]
Kyselina citronova DIG Info Perilipin-1 (IC50 = 3708 nM) [3]
Mannitol DIG Info Glycine receptor alpha-1 (EC50 = 12589.25 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
Anhydrous citric acid; Lactose monohydrate; Sodium citrate; Magnesium stearate; Mannitol; Crospovidone; Povidones; Starch, corn
                   Dosage Form Sublingual Tablet
                   Company Lake Eire Medical & Surgical Supply DBA Quality Care Products
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Sodium citrate anhydrous DIG Info Carbonic anhydrase IV (Ki = 99 nM) [7]
Kyselina citronova DIG Info Perilipin-1 (IC50 = 3708 nM) [3]
Mannitol DIG Info Glycine receptor alpha-1 (EC50 = 12589.25 nM) [4]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [6]
Crospovidone 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
Anhydrous citric acid; Lactose monohydrate; Sodium citrate; Magnesium stearate; Mannitol; Butylated hydroxyanisole; Povidones; Starch, corn
                   Dosage Form Sublingual Tablet
                   Company Sun Pharmaceutical Industries
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Sodium citrate anhydrous DIG Info Carbonic anhydrase IV (Ki = 99 nM) [7]
Kyselina citronova DIG Info Perilipin-1 (IC50 = 3708 nM) [3]
Mannitol DIG Info Glycine receptor alpha-1 (EC50 = 12589.25 nM) [4]
Butylhydroxyanisole DIG Info Prostaglandin G/H synthase 2 (IC50 = 2.6 uM) [8]
Magnesium stearate 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
Anhydrous citric acid; Lactose monohydrate; Fd&c yellow no. 6; Magnesium stearate; Mannitol; Trisodium citrate dihydrate; Povidone k30; Crospovidone (15 mpa.s at 5%); Starch, corn
                   Dosage Form Sublingual Tablet
                   Company Actavis Pharma
                   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]
Kyselina citronova DIG Info Perilipin-1 (IC50 = 3708 nM) [3]
Mannitol DIG Info Glycine receptor alpha-1 (EC50 = 12589.25 nM) [4]
Magnesium stearate 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 citric acid; Lactose monohydrate; Sodium citrate, unspecified form; Magnesium stearate; Mannitol; Povidone k30; Starch, corn
                   Dosage Form Sublingual Tablet
                   Company Contract Pharmacal; Teva Pharmaceuticals
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Sodium citrate anhydrous DIG Info Carbonic anhydrase IV (Ki = 99 nM) [7]
Kyselina citronova DIG Info Perilipin-1 (IC50 = 3708 nM) [3]
Mannitol DIG Info Glycine receptor alpha-1 (EC50 = 12589.25 nM) [4]
Magnesium stearate 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
Anhydrous citric acid; Lactose monohydrate; Anhydrous trisodium citrate; Sodium stearyl fumarate; Mannitol; Povidone k30; Starch, corn
                   Dosage Form Sublingual Tablet
                   Company RemedyRepack
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Sodium citrate anhydrous DIG Info Carbonic anhydrase IV (Ki = 99 nM) [7]
Kyselina citronova DIG Info Perilipin-1 (IC50 = 3708 nM) [3]
Mannitol DIG Info Glycine receptor alpha-1 (EC50 = 12589.25 nM) [4]
Sodium stearyl fumarate DIG Info Leukemia K562 cells (IC50 = 20.2 ug.mL-1) [9]
             Drug Formulation 8 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 citric acid; Lactose monohydrate; Sodium citrate, unspecified form; Magnesium stearate; Mannitol; Crospovidone (15 mpa.s at 5%); Povidones; Starch, corn
                   Dosage Form Sublingual Tablet
                   Company Contract Pharmacal; PD-Rx Pharmaceuticals; West-Ward Pharmaceticals
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Sodium citrate anhydrous DIG Info Carbonic anhydrase IV (Ki = 99 nM) [7]
Kyselina citronova DIG Info Perilipin-1 (IC50 = 3708 nM) [3]
Mannitol DIG Info Glycine receptor alpha-1 (EC50 = 12589.25 nM) [4]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [6]
             Drug Formulation 9 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 citric acid; Lactose monohydrate; Magnesium stearate; Mannitol; Trisodium citrate dihydrate; Povidone k30; Crospovidone, unspecified; Starch, corn
                   Dosage Form Sublingual Tablet
                   Company Rhodes Pharmaceuticals
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Kyselina citronova DIG Info Perilipin-1 (IC50 = 3708 nM) [3]
Mannitol DIG Info Glycine receptor alpha-1 (EC50 = 12589.25 nM) [4]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [6]
             Drug Formulation 10 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 citric acid; Lactose monohydrate; Sodium stearyl fumarate; Mannitol; Trisodium citrate dihydrate; Povidone k30
                   Dosage Form Sublingual Tablet
                   Company A-S Medication Solutions; Aidarex Pharmaceuticals; Bryant Ranch Prepack; Contract Pharmacal; Hi-Tech Pharmacal; Lake Eire Medical & Surgical Supply DBA Quality Care Products; PD-Rx Pharmaceuticals; RemedyRepack; TYA Pharmaceuticals
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Kyselina citronova DIG Info Perilipin-1 (IC50 = 3708 nM) [3]
Mannitol DIG Info Glycine receptor alpha-1 (EC50 = 12589.25 nM) [4]
Sodium stearyl fumarate DIG Info Leukemia K562 cells (IC50 = 20.2 ug.mL-1) [9]
          Buprenorphine Hydrochloride eq 0.5mg base film 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
Polyethylene Oxide; Hydroxypropyl Methylcellulose; Maltitol; AcesulfamePotassium; LimeFlavor; CitricAcid; SodiumCitrate; Fd&CYellow 6; WhiteInk
                   Dosage Form Film
                   Company Indivior
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Sodium citrate anhydrous DIG Info Carbonic anhydrase IV (Ki = 99 nM) [7]
Acesulfame DIG Info Carbonic anhydrase IX (Ki = 2400 nM) [10]
Sunset yellow FCF DIG Info Solute carrier SLCO2B1 (Ki = 68.4 uM) [2]
Kyselina citronova DIG Info Perilipin-1 (IC50 = 3708 nM) [3]
Maltitol DIG Info Carcinoma MDA-MB-231 cells (EC50 = 92350 nM) [11]
Hypromellose DIG Info Cytochrome P450 3A5 (IC50 = 19.4 uM) [5]
Polyethylene glycol 4000 DIG Info Albendazole monooxygenase (Inhibition ratio < 40 %) [12]
          Buprenorphine Hydrochloride eq 2mg base film 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
Polyethylene Oxide; Hydroxypropyl Methylcellulose; Maltitol; AcesulfamePotassium; LimeFlavor; CitricAcid; SodiumCitrate; Fd&CYellow 6; WhiteInk
                   Dosage Form Film
                   Company Indivior
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Sodium citrate anhydrous DIG Info Carbonic anhydrase IV (Ki = 99 nM) [7]
Acesulfame DIG Info Carbonic anhydrase IX (Ki = 2400 nM) [10]
Sunset yellow FCF DIG Info Solute carrier SLCO2B1 (Ki = 68.4 uM) [2]
Kyselina citronova DIG Info Perilipin-1 (IC50 = 3708 nM) [3]
Maltitol DIG Info Carcinoma MDA-MB-231 cells (EC50 = 92350 nM) [11]
Hypromellose DIG Info Cytochrome P450 3A5 (IC50 = 19.4 uM) [5]
Polyethylene glycol 4000 DIG Info Albendazole monooxygenase (Inhibition ratio < 40 %) [12]
          Buprenorphine Hydrochloride eq 2mg base 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; Mannitol; Cornstarch; PovidoneK30; CitricAcid; SodiumCitrateAndMagnesiumStearate
                   Dosage Form Tablet
                   Company Indivior
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Sodium citrate anhydrous DIG Info Carbonic anhydrase IV (Ki = 99 nM) [7]
Kyselina citronova DIG Info Perilipin-1 (IC50 = 3708 nM) [3]
Mannitol DIG Info Glycine receptor alpha-1 (EC50 = 12589.25 nM) [4]
Povidone DIG Info Cholesterol 25-hydroxylase (IC50 = 78.3 uM) [5]
Pregelatinized starch DIG Info Multidrug resistance protein 1 (Protein expression downregulation) [6]
          Buprenorphine Hydrochloride eq 0.3mg base/ml injectable 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
Dextrose; Water; Hci
                   Dosage Form Injectable
                   Company Indivior
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Hydrochloric acid DIG Info Carbonic anhydrase V (Ki = 156 nM) [13]
References
1 FDA label for approved buprenorphine 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 PubChem BioAssay data set.
4 Pharmacological property optimization for allosteric ligands: A medicinal chemistry perspective. Bioorg Med Chem Lett. 2017 Jun 1; 27(11):2239-2258.
5 Mediation of in vitro cytochrome p450 activity by common pharmaceutical excipients. Mol Pharm. 2013 Jul 1;10(7):2739-48.
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 Carbonic anhydrase inhibitors. Interaction of isozymes I, II, IV, V, and IX with carboxylates. Bioorg Med Chem Lett. 2005 Feb 1; 15(3):573-8.
8 The activities of drug inactive ingredients on biological targets. Science. 2020 Jul 24;369(6502):403-413.
9 Synthesis and evaluation of (-)-Massoialactone and analogues as potential anticancer and anti-inflammatory agents. Eur J Med Chem. 2014 Apr 9; 76:291-300.
10 Sweet Binders: Carbonic Anhydrase IX in Complex with Sucralose. ACS Med Chem Lett. 2018 May 10; 9(7):657-661.
11 Novel natural compounds from endophytic fungi with anticancer activity. Eur J Med Chem. 2018 Aug 5; 156:316-343.
12 Pharmaceutical excipients inhibit cytochrome P450 activity in cell free systems and after systemic administration. Eur J Pharm Biopharm. 2008 Sep;70(1):279-88.
13 Carbonic anhydrase inhibitors. Inhibition of the newly isolated murine isozyme XIII with anions. Bioorg Med Chem Lett. 2004 Nov 1; 14(21):5435-9.

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