Details of the Drug

General Information of Drug (ID: DM819JF)

Drug Name
Pemigatinib
Synonyms
Unii-Y6BX7BL23K; UNII-Y6BX7BL23K; Y6BX7BL23K; GTPL9767; SCHEMBL15556271; HCDMJFOHIXMBOV-UHFFFAOYSA-N; example 126 [WO2014007951]; 3-(2,6-difluoro-3,5-dimethoxyphenyl)-1-ethyl-8-(morpholin-4-ylmethyl)-4,7-dihydropyrrolo[4,5]pyrido[1,2-d]pyrimidin-2-one; 3-(2,6-difluoro-3,5-dimethoxyphenyl)-1-ethyl-8-(morpholin-4-ylmethyl)-1,3,4,7-tetrahydro-2H-pyrrolo[3',2':5,6]pyrido[4,3-d]pyrimidin-2-one; INCB54828
Indication
Disease Entry ICD 11 Status REF
Cholangiocarcinoma 2C12.10 Approved [1]
Bladder cancer 2C94 Phase 2 [2]
Myeloproliferative syndrome 2A22 Phase 2 [2]
Affected Organisms
Humans and other mammals
ATC Code
L01EN02: Pemigatinib
L01EN: Fibroblast growth factor receptor (FGFR) tyrosine kinase inhibitors
L01E: PROTEIN KINASE INHIBITORS
L01: ANTINEOPLASTIC AGENTS
L: ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS
Structure
3D MOL 2D MOL
#Ro5 Violations (Lipinski): 0 Molecular Weight (mw) 487.5
Logarithm of the Partition Coefficient (xlogp) 1.8
Rotatable Bond Count (rotbonds) 6
Hydrogen Bond Donor Count (hbonddonor) 1
Hydrogen Bond Acceptor Count (hbondacc) 8
ADMET Property
Absorption Tmax
The time to maximum plasma concentration (Tmax) is 1.13 h [3]
Clearance
The clearance of drug is 10.6 L/h [3]
Elimination
Following oral administration of a single radiolabeled dose of 11 mg pemigatinib, about 82.4% of the dose was recovered in feces [3]
Half-life
The concentration or amount of drug in body reduced by one-half in 15.4 hours (a single oral dose of 13.5 mg pemigatinib) [3]
Metabolism
The drug is metabolized via the CYP3A4 enzyme [3]
Vd
The volume of distribution (Vd) of drug is 235 L [3]
Chemical Identifiers
Formula
C24H27F2N5O4
IUPAC Name
11-(2,6-difluoro-3,5-dimethoxyphenyl)-13-ethyl-4-(morpholin-4-ylmethyl)-5,7,11,13-tetrazatricyclo[7.4.0.02,6]trideca-1,3,6,8-tetraen-12-one
Canonical SMILES
CCN1C2=C3C=C(NC3=NC=C2CN(C1=O)C4=C(C(=CC(=C4F)OC)OC)F)CN5CCOCC5
InChI
InChI=1S/C24H27F2N5O4/c1-4-30-21-14(11-27-23-16(21)9-15(28-23)13-29-5-7-35-8-6-29)12-31(24(30)32)22-19(25)17(33-2)10-18(34-3)20(22)26/h9-11H,4-8,12-13H2,1-3H3,(H,27,28)
InChIKey
HCDMJFOHIXMBOV-UHFFFAOYSA-N
Cross-matching ID
PubChem CID
86705695
ChEBI ID
CHEMBL4297522
CAS Number
1513857-77-6
UNII
Y6BX7BL23K
DrugBank ID
DB15102
TTD ID
D0O6UY
ACDINA ID
D01328
Drug-Molecule Activity Atlas (DMA)NEW Click to Jump to the Detailed DMA Information of This Drug
Drug ADMET Endpoint Profile (DAE)NEW Click to Jump to the Detailed DAE Information of This Drug
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
Fibroblast growth factor receptor 1 (FGFR1) TTRLW2X FGFR1_HUMAN Inhibitor [1]
Fibroblast growth factor receptor 2 (FGFR2) TTGJVQM FGFR2_HUMAN Inhibitor [1]
Fibroblast growth factor receptor 3 (FGFR3) TTST7KB FGFR3_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 Cholangiocarcinoma
ICD Disease Classification 2C12.10
Molecule Name Molecule Type Gene Name p-value Fold-Change Z-score
Fibroblast growth factor receptor 3 (FGFR3) DTT FGFR3 5.83E-03 0.08 0.1
Fibroblast growth factor receptor 1 (FGFR1) DTT FGFR1 4.79E-02 -0.03 -0.15
Fibroblast growth factor receptor 2 (FGFR2) DTT FGFR2 4.82E-01 -0.03 -0.2
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 Pemigatinib (Comorbidity)
DDI Drug Name DDI Drug ID Severity Mechanism Comorbidity REF
Berotralstat DMWA2DZ Major Decreased metabolism of Pemigatinib caused by Berotralstat mediated inhibition of CYP450 enzyme. Innate/adaptive immunodeficiency [4A00] [4]
Selpercatinib DMZR15V Moderate Decreased metabolism of Pemigatinib caused by Selpercatinib mediated inhibition of CYP450 enzyme. Lung cancer [2C25] [5]

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

DIG
DIG Name DIG ID PubChem CID Functional Classification
Magnesium stearate E00208 11177 lubricant
Cellulose microcrystalline E00698 Not Available Adsorbent; Suspending agent; Diluent
Pharmaceutical Formulation
Formulation Name Drug Dosage Dosage Form Route
Pemigatinib 4.5 mg tablet 4.5 mg Tablet Oral
Pemigatinib 9 mg tablet 9 mg Tablet Oral
Pemigatinib 13.5 mg tablet 13.5 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: PEMAZYRE (pemigatinib) tablets, for oral use
4 Product Information. Pemazyre (pemigatinib). Incyte Corporation, Wilmington, DE.
5 Product Information. Accolate (zafirlukast). Zeneca Pharmaceuticals, Wilmington, DE.