Details of the Active Pharmaceutical Ingredient (API)

General Information of API (ID: D01386)
Name
Ribociclib succinate
Synonyms    Click to Show/Hide the Synonyms of This API
Ribociclib succinate; LEE011 succinate; 1374639-75-4; 7-Cyclopentyl-N,N-dimethyl-2-((5-(piperazin-1-yl)pyridin-2-yl)amino)-7H-pyrrolo[2,3-d]pyrimidine-6-carboxamide succinate; UNII-BG7HLX2919; 1374639-75-4 (succinate); LEE011-BBA; Ribociclib succinate [USAN]; BG7HLX2919; Ribociclib succinate (USAN); Butanedioic acid, compd. with 7-cyclopentyl-N,N-dimethyl-2-[[5-(1-piperazinyl)-2-pyridinyl]amino]-7H-pyrrolo[2,3-d]pyrimidine-6-carboxamide (1:1); Butanedioic acid, compd. with 7-cyclopentyl-N,N-dimethyl-2-((5-(1-piperazinyl)-2-pyridinyl)amino)-7H-pyrrolo(2,3-d)pyrimidine-6-carboxamide (1:1); LEE-011 succinate; Kisqali (TN); LEE011 (succinate); SCHEMBL2684999; CHEMBL3707266; AMY25508; BCP12715; EX-A1586; HY-15777B; ACN-040739; SB18482; AC-30654; AK547289; AS-75241; butanedioic acid;7-cyclopentyl-N,N-dimethyl-2-[(5-piperazin-1-ylpyridin-2-yl)amino]pyrrolo[2,3-d]pyrimidine-6-carboxamide; D10979; LEE-011 succinate salt, Ribociclib succinate salt; J-007026; Q27274660; 7-cyclopentyl-N,N-dimethyl-2-{[5-(piperazin-1-yl)pyridin-2-yl]amino}-7H-pyrrolo[2,3-d]pyrimidine-6-carboxamide; butanedioic acid
Clinical Status
Approved
PubChem CID
57334219
Formula
C27H36N8O5
Canonical SMILES
CN(C)C(=O)C1=CC2=CN=C(N=C2N1C3CCCC3)NC4=NC=C(C=C4)N5CCNCC5.C(CC(=O)O)C(=O)O
InChI
1S/C23H30N8O.C4H6O4/c1-29(2)22(32)19-13-16-14-26-23(28-21(16)31(19)17-5-3-4-6-17)27-20-8-7-18(15-25-20)30-11-9-24-10-12-30;5-3(6)1-2-4(7)8/h7-8,13-15,17,24H,3-6,9-12H2,1-2H3,(H,25,26,27,28);1-2H2,(H,5,6)(H,7,8)
InChIKey
NHANOMFABJQAAH-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=57334219"></iframe>
3D MOL is unavailable 2D MOL
Physicochemical Properties Molecular Weight 552.6 Topological Polar Surface Area 166
XlogP N.A. Complexity 728
Heavy Atom Count 40 Rotatable Bond Count 8
Hydrogen Bond Donor Count 4 Hydrogen Bond Acceptor Count 11
Full List of Drug Formulations (DFMs) Containing This API
          Ribociclib Succinate 200mg 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; Crospovidone; Hydroxypropylcellulose; Magnesium Stearate; Microcrystalline Cellulose; Iron Oxide Black; Iron Oxide Red; Lecithin (Soya); Polyvinyl Alcohol (Partially Hydrolysed); Talc; Titanium Dioxide; Xanthan Gum
                   Dosage Form Tablet
                   Company Novartis
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Hydroxypropyl cellulose DIG Info Mephenytoin 4-hydroxylase (EC50 = 89.5 uM) [1]
Polyvinyl alcohol DIG Info Debrisoquine 4-hydroxylase (EC50 = 354.8 uM) [1]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [2]
Crospovidone DIG Info Albendazole monooxygenase (Protein expression downregulation) [2]
Soybean lecithin DIG Info Albendazole monooxygenase (IC50 = 6.61 mg.mL-1) [3]
References
1 Mediation of in vitro cytochrome p450 activity by common pharmaceutical excipients. Mol Pharm. 2013 Jul 1;10(7):2739-48.
2 Effects of commonly used excipients on the expression of CYP3A4 in colon and liver cells. Pharm Res. 2010 Aug;27(8):1703-12.
3 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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