Details of the Active Pharmaceutical Ingredient (API)

General Information of API (ID: D00611)
Name
Ruxolitinib
Synonyms    Click to Show/Hide the Synonyms of This API
Ruxolitinib; 941678-49-5; INCB018424; Ruxolitinib (INCB018424); (R)-3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-3-cyclopentylpropanenitrile; INCB-018424; INCB 018424; UNII-82S8X8XX8H; Ruxolitinib free base; (3R)-3-cyclopentyl-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]propanenitrile; 82S8X8XX8H; INC424; INCB018424 (Ruxolitinib); CHEBI:66919; (R)-ruxolitinib; C17H18N6; 941678-49-5 (free base); R-Ruxolitinib; (betaR)-beta-Cyclopentyl-4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazole-1-propanenitrile; INC-424; INCB-18424; INCB18424; Ruxolitinib [USAN:INN]; INCB 18424; (3R)-3-cyclopentyl-3-(4-{7H-pyrrolo[2,3-d]pyrimidin-4-yl}-1H-pyrazol-1-yl)propanenitrile; INC 424; Ruxolitinib (USAN/INN); INCB18424,Ruxolitinib; cc-189; SCHEMBL171319; GTPL5688; INCB018424 - Ruxolitinib; CHEMBL1789941; SCHEMBL16546708; HSDB 8259; DTXSID10240930; SYN1120; ACT06813; AOB87783; EX-A1670; ABP000827; ABP000833; BDBM50355501; MFCD12031592; NSC763371; NSC800874; ZINC43207851; AKOS016842401; ACN-031567; BCP9000784; CCG-264889; CS-0864; DB08877; INCB018424(Ruxolitinib)/Ruxolitinib; NSC-763371; NSC-800874; PB28380; NCGC00244253-01; NCGC00244253-02; NCGC00244253-11; NCGC00244253-12; AC-24280; AK-48608; AS-18619; BR-48608; HY-50856; QC-11806; 1092939-15-5; INCB018424 /INCB-018424; A14955; D09959; Q-4578; AB01565782_02; Q7383611; BRD-K53972329-001-02-1; BRD-K53972329-001-03-9; (3R)-3-cyclopentyl-3-[4-(1H-pyrrolo[2,3-d]pyrimidin-4-yl)pyrazol-1-yl]propanenitrile; (3R)-3-cyclopentyl-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)pyrazol-1-yl]propanenitrile; (R)-3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H -pyrazol-1-yl)-3-cyclopentylpropanenitrile; 3-Cyclopentyl-4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-(beta-R)-1H-pyrazole-1-propanenitrile; A-Cyclopentyl-4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-(AR)-1H-pyrazole-1-propanenitrile; 1H-Pyrazole-1-propanenitrile, beta-cyclopentyl-4-(7H-pyrrolo(2,3-d)pyrimidin-4-yl)-,(betaR)-
Clinical Status
Approved
Disease Indication Thrombocytosis ICD-11: 3B63 [1]
PubChem CID
25126798
Formula
C17H18N6
Canonical SMILES
C1CCC(C1)[C@@H](CC#N)N2C=C(C=N2)C3=C4C=CNC4=NC=N3
InChI
1S/C17H18N6/c18-7-5-15(12-3-1-2-4-12)23-10-13(9-22-23)16-14-6-8-19-17(14)21-11-20-16/h6,8-12,15H,1-5H2,(H,19,20,21)/t15-/m1/s1
InChIKey
HFNKQEVNSGCOJV-OAHLLOKOSA-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=25126798"></iframe>
3D MOL 2D MOL
Physicochemical Properties Molecular Weight 306.4 Topological Polar Surface Area 83.2
XlogP 2.1 Complexity 453
Heavy Atom Count 23 Rotatable Bond Count 4
Hydrogen Bond Donor Count 1 Hydrogen Bond Acceptor Count 4
Full List of Drug Formulations (DFMs) Containing This API
          Ruxolitinib Phosphate 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
Microcrystalline Cellulose; Lactose Monohydrate; Magnesium Stearate; Colloidal Silicon Dioxide; Sodium Starch Glycolate; Povidone; Hydroxypropyl Cellulose
                   Dosage Form Tablet
                   Company yte Corp
                   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) [2]
Povidone DIG Info Cholesterol 25-hydroxylase (IC50 = 78.3 uM) [2]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [3]
          Ruxolitinib Phosphate 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
Microcrystalline Cellulose; Lactose Monohydrate; Magnesium Stearate; Colloidal Silicon Dioxide; Sodium Starch Glycolate; Povidone; Hydroxypropyl Cellulose
                   Dosage Form Tablet
                   Company yte Corp
                   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) [2]
Povidone DIG Info Cholesterol 25-hydroxylase (IC50 = 78.3 uM) [2]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [3]
          Ruxolitinib Phosphate eq 15mg 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
Microcrystalline Cellulose; Lactose Monohydrate; Magnesium Stearate; Colloidal Silicon Dioxide; Sodium Starch Glycolate; Povidone; Hydroxypropyl Cellulose
                   Dosage Form Tablet
                   Company yte Corp
                   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) [2]
Povidone DIG Info Cholesterol 25-hydroxylase (IC50 = 78.3 uM) [2]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [3]
          Ruxolitinib Phosphate eq 20mg 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
Microcrystalline Cellulose; Lactose Monohydrate; Magnesium Stearate; Colloidal Silicon Dioxide; Sodium Starch Glycolate; Povidone; Hydroxypropyl Cellulose
                   Dosage Form Tablet
                   Company yte Corp
                   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) [2]
Povidone DIG Info Cholesterol 25-hydroxylase (IC50 = 78.3 uM) [2]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [3]
          Ruxolitinib Phosphate eq 25mg 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
Microcrystalline Cellulose; Lactose Monohydrate; Magnesium Stearate; Colloidal Silicon Dioxide; Sodium Starch Glycolate; Povidone; Hydroxypropyl Cellulose
                   Dosage Form Tablet
                   Company yte Corp
                   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) [2]
Povidone DIG Info Cholesterol 25-hydroxylase (IC50 = 78.3 uM) [2]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [3]
          Ruxolitinib 10 mg 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
Lactose monohydrate; Magnesium stearate; Povidone; Silicon dioxide; Cellulose, microcrystalline; Hydroxypropyl cellulose (type e); Sodium starch glycolate type a potato
                   Dosage Form Oral Tablet
                   Company Incyte Corporation
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Povidone DIG Info Cholesterol 25-hydroxylase (IC50 = 78.3 uM) [2]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [3]
Silicon dioxide DIG Info Albendazole monooxygenase (Protein expression downregulation) [3]
          Ruxolitinib 15 mg 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
Lactose monohydrate; Magnesium stearate; Povidone; Silicon dioxide; Cellulose, microcrystalline; Hydroxypropyl cellulose (type e); Sodium starch glycolate type a potato
                   Dosage Form Oral Tablet
                   Company Incyte Corporation
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Povidone DIG Info Cholesterol 25-hydroxylase (IC50 = 78.3 uM) [2]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [3]
Silicon dioxide DIG Info Albendazole monooxygenase (Protein expression downregulation) [3]
          Ruxolitinib 20 mg 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
Lactose monohydrate; Magnesium stearate; Povidone; Silicon dioxide; Cellulose, microcrystalline; Hydroxypropyl cellulose (type e); Sodium starch glycolate type a potato
                   Dosage Form Oral Tablet
                   Company Incyte Corporation
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Povidone DIG Info Cholesterol 25-hydroxylase (IC50 = 78.3 uM) [2]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [3]
Silicon dioxide DIG Info Albendazole monooxygenase (Protein expression downregulation) [3]
          Ruxolitinib 25 mg 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
Lactose monohydrate; Magnesium stearate; Povidone; Silicon dioxide; Cellulose, microcrystalline; Hydroxypropyl cellulose (type e); Sodium starch glycolate type a potato
                   Dosage Form Oral Tablet
                   Company Incyte Corporation
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Povidone DIG Info Cholesterol 25-hydroxylase (IC50 = 78.3 uM) [2]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [3]
Silicon dioxide DIG Info Albendazole monooxygenase (Protein expression downregulation) [3]
          Ruxolitinib 5 mg 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
Lactose monohydrate; Magnesium stearate; Povidone; Silicon dioxide; Cellulose, microcrystalline; Hydroxypropyl cellulose (type e); Sodium starch glycolate type a potato
                   Dosage Form Oral Tablet
                   Company Incyte Corporation
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Povidone DIG Info Cholesterol 25-hydroxylase (IC50 = 78.3 uM) [2]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [3]
Silicon dioxide DIG Info Albendazole monooxygenase (Protein expression downregulation) [3]
References
1 FDA label for approved ruxolitinib 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 Effects of commonly used excipients on the expression of CYP3A4 in colon and liver cells. Pharm Res. 2010 Aug;27(8):1703-12.

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