Details of the Active Pharmaceutical Ingredient (API)

General Information of API (ID: D00910)
Name
Capmatinib
Synonyms    Click to Show/Hide the Synonyms of This API
capmatinib; 1029712-80-8; INCB28060; INC-280; INC280; 2-fluoro-N-methyl-4-(7-(quinolin-6-ylmethyl)imidazo[1,2-b][1,2,4]triazin-2-yl)benzamide; UNII-TY34L4F9OZ; INCB-28060; Capmatinib (INCB28060); INC28060; NVP-INC280-NX; NVP-INC280; TY34L4F9OZ; 2-fluoro-N-methyl-4-[7-(quinolin-6-ylmethyl)imidazo[1,2-b][1,2,4]triazin-2-yl]benzamide; INCB 28060; BenzaMide, 2-fluoro-N-Methyl-4-[7-(6-quinolinylMethyl)iMidazo[1,2-b][1,2,4]triazin-2-yl]-; 1029712-80-8 (free base); 2-Fluoro-N-methyl-4-[7-[(quinolin-6-yl)methyl]imidazo[1,2-b]-[1,2,4]triazin-2-yl]benzamide; C23H17FN6O; 2-Fluoro-N-methyl-4-[7-(6-quinolinylmethyl)imidazo[1,2-b][1,2,4]triazin-2-yl]benzamide; Benzamide, 2-fluoro-N-methyl-4-[7-(6-quinolinylmethyl)imidazo[1,2-b][1,2,4]triazin-2-yl]-;Benzamide, 2-fluoro-N-methyl-4-[7-(6-quinolinylmethyl)imidazo[1,2-b][1,2,4]triazin-2-yl]-; Tabrecta; benzamide hcl; Capmatinib [USAN]; Capmatinib (USAN/INN); Capmatinib [USAN:INN]; Capmatinib(INCB28060); INCB28060(Capmatinib); NYP-INC280-NX; cc-219; MLS006010965; GTPL7904; SCHEMBL1426819; CHEMBL3188267; DTXSID90145595; EX-A446; INCB-28060 FREE BASE; AMY18553; AOB87335; BCP23444; ABP000812; BDBM50146167; MFCD18633285; NSC777878; NSC800067; s2788; ZINC43195321; AKOS025396439; BCP9000785; CCG-268791; CS-1541; DB11791; NSC-777878; NSC-800067; QC-7530; SB16608; NCGC00346702-01; NCGC00346702-02; NCGC00346702-05; AC-25890; AK174338; AS-74142; DA-33530; HY-13404; SMR004702769; AB0035895; FT-0746310; Y0337; D10696; W-5775; J-509516; Q27075685; 2-fluoro-n-methyl-4-[7-(quinolin-6-ylmethyl)imidazolo[1,2-b][1,2,4]triazin-2-yl]benzamide; 2-fluoro-N-methyl-4-{7-[(quinolin-6-yl)methyl]imidazo[1,2-b][1,2,4]triazin-2-yl}benzamide
Clinical Status
Approved
PubChem CID
25145656
Formula
C23H17FN6O
Canonical SMILES
CNC(=O)C1=C(C=C(C=C1)C2=NN3C(=CN=C3N=C2)CC4=CC5=C(C=C4)N=CC=C5)F
InChI
1S/C23H17FN6O/c1-25-22(31)18-6-5-16(11-19(18)24)21-13-28-23-27-12-17(30(23)29-21)10-14-4-7-20-15(9-14)3-2-8-26-20/h2-9,11-13H,10H2,1H3,(H,25,31)
InChIKey
LIOLIMKSCNQPLV-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=25145656"></iframe>
3D MOL 2D MOL
Physicochemical Properties Molecular Weight 412.4 Topological Polar Surface Area 85.1
XlogP 2.9 Complexity 637
Heavy Atom Count 31 Rotatable Bond Count 4
Hydrogen Bond Donor Count 1 Hydrogen Bond Acceptor Count 6
Full List of Drug Formulations (DFMs) Containing This API
          Capmatinib eq 150mg 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; Crospovidone; Magnesium Stearate; Mannitol; Microcrystalline Cellulose; Povidone; Sodium Lauryl Sulfate; Ferric Oxide; Red Ferric Oxide; Yellow Ferrosoferric Oxide; Hypromellose; Polyethylene Glycol (Peg) 4000; Talc; Titanium Dioxide
                   Dosage Form Tablet
                   Company Novartis Pharm
                   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) [1]
Mannitol DIG Info Glycine receptor alpha-1 (EC50 = 12589.25 nM) [2]
Hypromellose DIG Info Cytochrome P450 3A5 (IC50 = 19.4 uM) [3]
Povidone DIG Info Cholesterol 25-hydroxylase (IC50 = 78.3 uM) [3]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [4]
Crospovidone DIG Info Albendazole monooxygenase (Protein expression downregulation) [4]
Polyethylene glycol 4000 DIG Info Albendazole monooxygenase (Inhibition ratio < 40 %) [5]
References
1 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.
2 Pharmacological property optimization for allosteric ligands: A medicinal chemistry perspective. Bioorg Med Chem Lett. 2017 Jun 1; 27(11):2239-2258.
3 Mediation of in vitro cytochrome p450 activity by common pharmaceutical excipients. Mol Pharm. 2013 Jul 1;10(7):2739-48.
4 Effects of commonly used excipients on the expression of CYP3A4 in colon and liver cells. Pharm Res. 2010 Aug;27(8):1703-12.
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.

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