Details of the Active Pharmaceutical Ingredient (API)

General Information of API (ID: D00585)
Name
Rasagiline
Synonyms    Click to Show/Hide the Synonyms of This API
rasagiline; 136236-51-6; (R)-N-(2-Propynyl)-2,3-dihydroinden-1-amine; Azilect; (R)-N-2-Propynyl-1-indanamine; (R)-2,3-dihydro-N-2-propynyl-1H-inden-1-amine; 1-Indanamine, N-2-propynyl-, (R)-; (1R)-N-(prop-2-yn-1-yl)-2,3-dihydro-1H-inden-1-amine; UNII-003N66TS6T; TV-1030; Azilect (TN); CHEMBL887; (1R)-N-propargylindan-1-amine; CHEBI:63620; 003N66TS6T; (R)-Indan-1-yl-prop-2-ynyl-amine; 1H-Inden-1-amine, 2,3-dihydro-N-2-propynyl-, (1R)-; (R)-N-(prop-2-ynyl)-2,3-dihydro-1H-inden-1-amine; (1R)-N-prop-2-ynyl-2,3-dihydro-1H-inden-1-amine; Rasagiline [USAN:INN]; MFCD00866571; HSDB 7699; (1R)-N-prop-2-ynylindan-1-amine; 1H-Inden-1-amine, 2,3-dihydro-N-2-propynyl-, (1R); TV 1030; PubChem23269; Rasagiline (USAN/INN); SCHEMBL74699; cc-221; MLS006012042; N-propargyl-1-(R)aminoindan; GTPL6641; IND057; SCHEMBL2029054; DTXSID3041112; BDBM10989; HMS3264K12; HMS3715L12; HMS3886N03; Pharmakon1600-01502333; AC-723; ANW-49399; HY-14605A; NSC759639; NSC789038; ZINC19875504; AKOS006271452; AKOS015837675; AM84542; CCG-213034; DB01367; FS-3130; MCULE-4385913742; NSC-759639; NSC-789038; BR-39976; SMR002533187; (1R)-N-(prop-2-yn-1-yl)indan-1-amine; AB0035569; DB-001111; D08469; S-3541; AB01562963_01; AB01562963_02; Q420685; SR-00000006359; SR-00000006359-3; 1204184-69-9
Clinical Status
Approved
Disease Indication Parkinsonism ICD-11: 8A00 [1]
PubChem CID
3052776
Formula
C12H13N
Canonical SMILES
C#CCN[C@@H]1CCC2=CC=CC=C12
InChI
1S/C12H13N/c1-2-9-13-12-8-7-10-5-3-4-6-11(10)12/h1,3-6,12-13H,7-9H2/t12-/m1/s1
InChIKey
RUOKEQAAGRXIBM-GFCCVEGCSA-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=3052776"></iframe>
3D MOL 2D MOL
Physicochemical Properties Molecular Weight 171.24 Topological Polar Surface Area 12
XlogP 1.8 Complexity 212
Heavy Atom Count 13 Rotatable Bond Count 2
Hydrogen Bond Donor Count 1 Hydrogen Bond Acceptor Count 1
Full List of Drug Formulations (DFMs) Containing This API
          Rasagiline 0.5 mg tablet Click to Show/Hide the Full List of Formulation(s):          4 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
Stearic acid; Citric acid monohydrate; Croscarmellose sodium; Silicon dioxide; Microcrystalline cellulose; Starch, corn
                   Dosage Form Oral Tablet
                   Company Mylan Pharamceuticals
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Stearic acid DIG Info Phosphodiesterase 3A (IC50 = 3.1 uM) [2]
Carmellose sodium DIG Info Albendazole monooxygenase (Protein expression upregulation) [3]
Silicon dioxide DIG Info Albendazole monooxygenase (Protein expression downregulation) [3]
             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
Stearic acid; Mannitol; Talc; Silicon dioxide; Starch, corn
                   Dosage Form Oral Tablet
                   Company Teva Neuroscience; Teva Pharmaceuticals
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Stearic acid DIG Info Phosphodiesterase 3A (IC50 = 3.1 uM) [2]
Mannitol DIG Info Glycine receptor alpha-1 (EC50 = 12589.25 nM) [4]
Silicon dioxide DIG Info Albendazole monooxygenase (Protein expression downregulation) [3]
             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
Stearic acid; Citric acid monohydrate; Talc; Silicon dioxide; Cellulose, microcrystalline; Starch, corn
                   Dosage Form Oral Tablet
                   Company Ascend Laboratories
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Stearic acid DIG Info Phosphodiesterase 3A (IC50 = 3.1 uM) [2]
Silicon dioxide DIG Info Albendazole monooxygenase (Protein expression downregulation) [3]
             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
Stearic acid; Lactose monohydrate; Citric acid monohydrate; Talc; Starch, corn
                   Dosage Form Oral Tablet
                   Company Alvogen
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Stearic acid DIG Info Phosphodiesterase 3A (IC50 = 3.1 uM) [2]
          Rasagiline 1 mg tablet Click to Show/Hide the Full List of Formulation(s):          5 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
Stearic acid; Citric acid monohydrate; Croscarmellose sodium; Silicon dioxide; Microcrystalline cellulose; Starch, corn
                   Dosage Form Oral Tablet
                   Company Mylan Pharamceuticals
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Stearic acid DIG Info Phosphodiesterase 3A (IC50 = 3.1 uM) [2]
Carmellose sodium DIG Info Albendazole monooxygenase (Protein expression upregulation) [3]
Silicon dioxide DIG Info Albendazole monooxygenase (Protein expression downregulation) [3]
             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
Stearic acid; Mannitol; Talc; Silicon dioxide; Starch, corn
                   Dosage Form Oral Tablet
                   Company Aphena Pharma Solutions-Tennessee; Teva Neuroscience; Teva Pharmaceuticals
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Stearic acid DIG Info Phosphodiesterase 3A (IC50 = 3.1 uM) [2]
Mannitol DIG Info Glycine receptor alpha-1 (EC50 = 12589.25 nM) [4]
Silicon dioxide DIG Info Albendazole monooxygenase (Protein expression downregulation) [3]
             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
Stearic acid; Mannitol; Talc; Silicon dioxide
                   Dosage Form Oral Tablet
                   Company Physicians Total Care
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Stearic acid DIG Info Phosphodiesterase 3A (IC50 = 3.1 uM) [2]
Mannitol DIG Info Glycine receptor alpha-1 (EC50 = 12589.25 nM) [4]
Silicon dioxide DIG Info Albendazole monooxygenase (Protein expression downregulation) [3]
             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
Stearic acid; Citric acid monohydrate; Talc; Silicon dioxide; Cellulose, microcrystalline; Starch, corn
                   Dosage Form Oral Tablet
                   Company Ascend Laboratories
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Stearic acid DIG Info Phosphodiesterase 3A (IC50 = 3.1 uM) [2]
Silicon dioxide DIG Info Albendazole monooxygenase (Protein expression downregulation) [3]
             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
Stearic acid; Lactose monohydrate; Citric acid monohydrate; Talc; Starch, corn
                   Dosage Form Oral Tablet
                   Company Alvogen
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Stearic acid DIG Info Phosphodiesterase 3A (IC50 = 3.1 uM) [2]
References
1 FDA label for approved rasagiline 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 Effects of commonly used excipients on the expression of CYP3A4 in colon and liver cells. Pharm Res. 2010 Aug;27(8):1703-12.
4 Pharmacological property optimization for allosteric ligands: A medicinal chemistry perspective. Bioorg Med Chem Lett. 2017 Jun 1; 27(11):2239-2258.

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