Details of the Active Pharmaceutical Ingredient (API)

General Information of API (ID: D01304)
Name
Osilodrostat
Synonyms    Click to Show/Hide the Synonyms of This API
osilodrostat; LCI699; 928134-65-0; LCI-699; Isturisa; Osilodrostat free base; UNII-5YL4IQ1078; CHEMBL3099695; 5YL4IQ1078; (R)-4-(6,7-Dihydro-5H-pyrrolo[1,2-c]imidazol-5-yl)-3-fluorobenzonitrile; 928134-65-0 (free base); 1304733-26-3; Osilodrostat [USAN:INN]; LCI 699; (+)-Osilodrostat; Osilodrostat (USAN/INN); LCI699-NX; GTPL8310; LCI-699-NX; SCHEMBL12460772; DTXSID40156570; EX-A1397; BDBM50444549; s7456; ZINC72318114; CCG-266774; CS-6896; DB11837; AC-32907; BS-17881; HY-16276; D11061; Z-3271; Q27088216; 4-((5R)-6,7-Dihydro-5H-pyrrolo(1,2-c)imidazol-5-yl)-3-fluoro-benzonitrile; 4-[(5R)-6,7-Dihydro-5H-pyrrolo[1,2-c]imidazol-5-yl]-3-fluorobenzo nitrile; 4-[(5R)-6,7-dihydro-5H-pyrrolo[1,2-c]imidazol-5-yl]-3-fluorobenzonitrile; Benzonitrile, 4-((5R)-6,7-dihydro-5H-pyrrolo(1,2-c)imidazol-5-yl)-3-fluoro-
Clinical Status
Approved
PubChem CID
44139752
Formula
C13H10FN3
Canonical SMILES
C1CC2=CN=CN2[C@H]1C3=C(C=C(C=C3)C#N)F
InChI
1S/C13H10FN3/c14-12-5-9(6-15)1-3-11(12)13-4-2-10-7-16-8-17(10)13/h1,3,5,7-8,13H,2,4H2/t13-/m1/s1
InChIKey
USUZGMWDZDXMDG-CYBMUJFWSA-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=44139752"></iframe>
3D MOL is unavailable 2D MOL
Physicochemical Properties Molecular Weight 227.24 Topological Polar Surface Area 41.6
XlogP 1.9 Complexity 337
Heavy Atom Count 17 Rotatable Bond Count 1
Hydrogen Bond Donor Count 0 Hydrogen Bond Acceptor Count 3
Full List of Drug Formulations (DFMs) Containing This API
          Osilodrostat eq 10mg 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
Colloidal Silicon Dioxide; Croscarmellose Sodium; Mannitol; Microcrystalline Cellulose; Magnesium Stearate; Hypromellose; Titanium Dioxide; Ferric Oxide (Yellow); Ferric Oxide (Red); Ferrosoferric Oxide; Polyethylene Glycol 4000; Talc
                   Dosage Form Tablet
                   Company Recordati Rare Disease
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Mannitol DIG Info Glycine receptor alpha-1 (EC50 = 12589.25 nM) [1]
Hypromellose DIG Info Cytochrome P450 3A5 (IC50 = 19.4 uM) [2]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [3]
Carmellose sodium DIG Info Albendazole monooxygenase (Protein expression upregulation) [3]
Polyethylene glycol 4000 DIG Info Albendazole monooxygenase (Inhibition ratio < 40 %) [4]
          Osilodrostat eq 1mg 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
Colloidal Silicon Dioxide; Croscarmellose Sodium; Mannitol; Microcrystalline Cellulose; Magnesium Stearate; Hypromellose; Titanium Dioxide; Ferric Oxide (Yellow); Ferric Oxide (Red); Polyethylene Glycol 4000; Talc.
                   Dosage Form Tablet
                   Company Recordati Rare Disease
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Mannitol DIG Info Glycine receptor alpha-1 (EC50 = 12589.25 nM) [1]
Hypromellose DIG Info Cytochrome P450 3A5 (IC50 = 19.4 uM) [2]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [3]
Carmellose sodium DIG Info Albendazole monooxygenase (Protein expression upregulation) [3]
Polyethylene glycol 4000 DIG Info Albendazole monooxygenase (Inhibition ratio < 40 %) [4]
          Osilodrostat eq 5mg 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
Colloidal Silicon Dioxide; Croscarmellose Sodium; Mannitol; Microcrystalline Cellulose; Magnesium Stearate; Hypromellose; Titanium Dioxide; Ferric Oxide (Yellow); Polyethylene Glycol 4000; Talc.
                   Dosage Form Tablet
                   Company Recordati Rare Disease
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Mannitol DIG Info Glycine receptor alpha-1 (EC50 = 12589.25 nM) [1]
Hypromellose DIG Info Cytochrome P450 3A5 (IC50 = 19.4 uM) [2]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [3]
Carmellose sodium DIG Info Albendazole monooxygenase (Protein expression upregulation) [3]
Polyethylene glycol 4000 DIG Info Albendazole monooxygenase (Inhibition ratio < 40 %) [4]
References
1 Pharmacological property optimization for allosteric ligands: A medicinal chemistry perspective. Bioorg Med Chem Lett. 2017 Jun 1; 27(11):2239-2258.
2 Mediation of in vitro cytochrome p450 activity by common pharmaceutical excipients. Mol Pharm. 2013 Jul 1;10(7):2739-48.
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 Pharmaceutical excipients inhibit cytochrome P450 activity in cell free systems and after systemic administration. Eur J Pharm Biopharm. 2008 Sep;70(1):279-88.

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