Details of the Active Pharmaceutical Ingredient (API)

General Information of API (ID: D00512)
Name
Pazopanib
Synonyms    Click to Show/Hide the Synonyms of This API
Pazopanib; 444731-52-6; GW786034; UNII-7RN5DR86CK; Pazopanib (GW-786034); 790713-33-6; 7RN5DR86CK; GW 78603; CHEBI:71219; MFCD11616589; GW 786034; NCGC00188865-01; DSSTox_CID_28659; DSSTox_RID_82929; DSSTox_GSID_48733; GW-786034; C21H23N7O2S; CAS-444731-52-6; Pazopanib [INN:BAN]; pazopanibum; HSDB 8210; indazolylpyrimidine 13; Pazopanib (free base); Kinome_3790; PubChem22448; Pazopanib/GW-786034; SCHEMBL588608; CHEMBL477772; GTPL5698; JMC514632 Compound 13; DTXSID8048733; BDBM26474; QCR-110; SYN1058; cid_10113978; BCPP000129; HMS3244C21; HMS3244C22; HMS3244D21; HMS3656L14; HMS3745G05; AOB87179; BCP01839; EX-A1241; Tox21_113174; ABP000868; ABP000882; NSC752782; NSC800839; ZINC11617039; AKOS005145819; Tox21_113174_1; AC-8522; BCP9001053; CCG-265010; CS-0269; DB06589; MCULE-2193898201; NSC-752782; NSC-800839; SB17290; NCGC00188865-02; NCGC00188865-03; NCGC00188865-10; AS-11066; HY-10208; AB0008634; AM20090659; FT-0659928; FT-0684794; SW218082-3; Pazopanib Hydrochloride /GW786034,VOTRIENT; A11518; A19406; P-6706; Q-1426; S-7750; AB01273967-01; AB01273967-02; AB01273967_05; AB01273967_06; A839572; AR-270/43507999; Q-101400; Q7157043; BRD-K74514084-003-02-7; Z1541638525
Clinical Status
Approved
Disease Indication Renal cell carcinoma ICD-11: 2C90 [1]
PubChem CID
10113978
Formula
C21H23N7O2S
Canonical SMILES
CC1=C(C=C(C=C1)NC2=NC=CC(=N2)N(C)C3=CC4=NN(C(=C4C=C3)C)C)S(=O)(=O)N
InChI
1S/C21H23N7O2S/c1-13-5-6-15(11-19(13)31(22,29)30)24-21-23-10-9-20(25-21)27(3)16-7-8-17-14(2)28(4)26-18(17)12-16/h5-12H,1-4H3,(H2,22,29,30)(H,23,24,25)
InChIKey
CUIHSIWYWATEQL-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=10113978"></iframe>
3D MOL 2D MOL
Physicochemical Properties Molecular Weight 437.5 Topological Polar Surface Area 127
XlogP 3.1 Complexity 717
Heavy Atom Count 31 Rotatable Bond Count 5
Hydrogen Bond Donor Count 2 Hydrogen Bond Acceptor Count 8
Full List of Drug Formulations (DFMs) Containing This API
          Pazopanib Hydrochloride eq 200mg 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
Magnesium Stearate; Microcrystalline Cellulose; Povidone; Sodium Starch Glycolate; Hypromellose; Iron Oxide Black; Macrogol/Polyethylene Glycol 400 (Peg 400); Polysorbate 80; Titanium Dioxide
                   Dosage Form Tablet
                   Company Novartis
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Hypromellose DIG Info Cytochrome P450 3A5 (IC50 = 19.4 uM) [2]
Polysorbate 80 DIG Info Prostaglandin G/H synthase 1 (IC50 = 1 uM) [3]
Povidone DIG Info Cholesterol 25-hydroxylase (IC50 = 78.3 uM) [2]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [4]
Polyethylene glycol 400 DIG Info Albendazole monooxygenase (IC50 = 10.77 mg.mL-1) [5]
          Pazopanib Hydrochloride eq 400mg 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
Magnesium Stearate; Microcrystalline Cellulose; Povidone; Sodium Starch Glycolate; Hypromellose; Iron Oxide Black; Macrogol/Polyethylene Glycol 400 (Peg 400); Polysorbate 80; Titanium Dioxide
                   Dosage Form Tablet
                   Company Novartis
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Hypromellose DIG Info Cytochrome P450 3A5 (IC50 = 19.4 uM) [2]
Polysorbate 80 DIG Info Prostaglandin G/H synthase 1 (IC50 = 1 uM) [3]
Povidone DIG Info Cholesterol 25-hydroxylase (IC50 = 78.3 uM) [2]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [4]
Polyethylene glycol 400 DIG Info Albendazole monooxygenase (IC50 = 10.77 mg.mL-1) [5]
          Pazopanib 200 mg tablet Click to Show/Hide the Full List of Formulation(s):          2 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
Magnesium stearate; Ferrosoferric oxide; Titanium dioxide; Polyethylene glycol 400; Polysorbate 80; Povidone; Cellulose, microcrystalline; Hypromelloses; Sodium starch glycolate type a potato
                   Dosage Form Oral Tablet
                   Company Novartis Pharmaceuticals Corporation
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Polysorbate 80 DIG Info Prostaglandin G/H synthase 1 (IC50 = 1 uM) [3]
Povidone DIG Info Cholesterol 25-hydroxylase (IC50 = 78.3 uM) [2]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [4]
Polyethylene glycol 400 DIG Info Albendazole monooxygenase (IC50 = 10.77 mg.mL-1) [5]
             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
Magnesium stearate; Ferrosoferric oxide; Titanium dioxide; Polyethylene glycol 400; Polysorbate 80; Cellulose, microcrystalline; Hypromelloses; Povidones; Sodium starch glycolate type a potato
                   Dosage Form Oral Tablet
                   Company GlaxoSmithKline
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Polysorbate 80 DIG Info Prostaglandin G/H synthase 1 (IC50 = 1 uM) [3]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [4]
Polyethylene glycol 400 DIG Info Albendazole monooxygenase (IC50 = 10.77 mg.mL-1) [5]
References
1 FDA label for approved pazopanib from the official website of the U.S. Food and Drug Administration.
2 Mediation of in vitro cytochrome p450 activity by common pharmaceutical excipients. Mol Pharm. 2013 Jul 1;10(7):2739-48.
3 The activities of drug inactive ingredients on biological targets. Science. 2020 Jul 24;369(6502):403-413.
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.

If you find any error in data or bug in web service, please kindly report it to Dr. Zhang and Dr. Mou.