Details of the Drug

General Information of Drug (ID: DM958QB)

Drug Name
Ripretinib
Synonyms
1442472-39-0; Ripretinib [USAN]; UNII-9XW757O13D; GTPL9175; SCHEMBL14999718; 9XW757O13D; HY-112306; CS-0044835; N-(4-bromo-5-(1-ethyl-7-(methylamino)-2-oxo-1,2-dihydro-1,6-naphthyridin-3-yl)-2-fluorophenyl)-N'-phenylurea; 1-[4-bromo-5-[1-ethyl-7-(methylamino)-2-oxo-1,6-naphthyridin-3-yl]-2-fluorophenyl]-3-phenylurea; Urea, N-(4-bromo-5-(1-ethyl-1,2-dihydro-7-(methylamino)-2-oxo-1,6-naphthyridin-3-yl)-2-fluorophenyl)-N'-phenyl-
Indication
Disease Entry ICD 11 Status REF
Gastrointestinal stromal tumour 2B5B Approved [1]
Glioma 2A00.0 Phase 1 [2]
Solid tumour/cancer 2A00-2F9Z Phase 1 [2]
Systemic mastocytosis 2A21.0 Phase 1 [2]
Structure
3D MOL 2D MOL
#Ro5 Violations (Lipinski): 1 Molecular Weight (mw) 510.4
Logarithm of the Partition Coefficient (xlogp) 4.1
Rotatable Bond Count (rotbonds) 5
Hydrogen Bond Donor Count (hbonddonor) 3
Hydrogen Bond Acceptor Count (hbondacc) 5
ADMET Property
Absorption Tmax
The time to maximum plasma concentration (Tmax) is 4 h [3]
Clearance
The clearance of drug is 15.3 L/h [3]
Elimination
34% of drug is excreted in the feces and 0.2% of drug is excreted in the urine [3]
Half-life
The concentration or amount of drug in body reduced by one-half in 14.8 hours [3]
Metabolism
The drug is metabolized via the CYP3A subfamily of enzyme [3]
Vd
The volume of distribution (Vd) of drug is 307 L [3]
Chemical Identifiers
Formula
C24H21BrFN5O2
IUPAC Name
1-[4-bromo-5-[1-ethyl-7-(methylamino)-2-oxo-1,6-naphthyridin-3-yl]-2-fluorophenyl]-3-phenylurea
Canonical SMILES
CCN1C2=CC(=NC=C2C=C(C1=O)C3=CC(=C(C=C3Br)F)NC(=O)NC4=CC=CC=C4)NC
InChI
InChI=1S/C24H21BrFN5O2/c1-3-31-21-12-22(27-2)28-13-14(21)9-17(23(31)32)16-10-20(19(26)11-18(16)25)30-24(33)29-15-7-5-4-6-8-15/h4-13H,3H2,1-2H3,(H,27,28)(H2,29,30,33)
InChIKey
CEFJVGZHQAGLHS-UHFFFAOYSA-N
Cross-matching ID
PubChem CID
71584930
CAS Number
1442472-39-0
DrugBank ID
DB14840
TTD ID
D09AAK
ACDINA ID
D01395
Repurposed Drugs (RPD) Click to Jump to the Detailed RPD Information of This Drug

Molecular Interaction Atlas of This Drug


Drug Therapeutic Target (DTT)
DTT Name DTT ID UniProt ID MOA REF
Platelet-derived growth factor receptor alpha (PDGFRA) TT8FYO9 PGFRA_HUMAN Inhibitor [1]
Tyrosine-protein kinase Kit (KIT) TTX41N9 KIT_HUMAN Inhibitor [1]
Molecular Interaction Atlas (MIA) Jump to Detail Molecular Interaction Atlas of This Drug

Molecular Expression Atlas of This Drug

The Studied Disease Gastrointestinal stromal tumour
ICD Disease Classification 2B5B
Molecule Name Molecule Type Gene Name p-value Fold-Change Z-score
Tyrosine-protein kinase Kit (KIT) DTT KIT 5.94E-06 -1.17 -2.77
Platelet-derived growth factor receptor alpha (PDGFRA) DTT PDGFRA 1.48E-03 -0.38 -1.26
Molecular Expression Atlas (MEA) Jump to Detail Molecular Expression Atlas of This Drug

Drug-Drug Interaction (DDI) Information of This Drug

Coadministration of a Drug Treating the Disease Different from Ripretinib (Comorbidity)
DDI Drug Name DDI Drug ID Severity Mechanism Comorbidity REF
Selpercatinib DMZR15V Moderate Decreased metabolism of Ripretinib caused by Selpercatinib mediated inhibition of CYP450 enzyme. Lung cancer [2C25] [4]
Voxelotor DMCS6M5 Moderate Decreased metabolism of Ripretinib caused by Voxelotor mediated inhibition of CYP450 enzyme. Sickle-cell disorder [3A51] [4]

Drug Inactive Ingredient(s) (DIG) and Formulation(s) of This Drug

DIG
DIG Name DIG ID PubChem CID Functional Classification
Crospovidone E00626 Not Available Disintegrant
Lactose monohydrate E00393 104938 Binding agent; Diluent; Dry powder inhaler carrier; Lyophilization aid
Magnesium stearate E00208 11177 lubricant
Silicon dioxide E00670 Not Available Anticaking agent; Opacifying agent; Viscosity-controlling agent
Cellulose microcrystalline E00698 Not Available Adsorbent; Suspending agent; Diluent
Hypromellose acetate succinate E00696 Not Available Coating agent; Solubilizing agent; Modified-release agent;Film/membrane-forming agent
⏷ Show the Full List of 6 Pharmaceutical Excipients of This Drug
Pharmaceutical Formulation
Formulation Name Drug Dosage Dosage Form Route
Ripretinib 50 mg tablet 50 mg Tablet Oral
Jump to Detail Pharmaceutical Formulation Page of This Drug

References

1 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services. 2020
2 Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
3 FDA Approved Drug Products: QINLOCK (ripretinib) tablets, for oral use
4 Cerner Multum, Inc. "Australian Product Information.".