pemigatinib 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definitionDrug idCAS RN
tyrosine kinase inhibitors 5390 1513857-77-6

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • pemigatinib
  • pemazyre
  • INCB054828
Pemigatinib inhibited FGFR1-3 phosphorylation and signaling and decreased cell viability in cancer cell lines with activating FGFR amplifications and fusions that resulted in constitutive activation of FGFR signaling.
  • Molecular weight: 487.51
  • Formula: C24H27F2N5O4
  • CLOGP: 2.93
  • LIPINSKI: 0
  • HAC: 9
  • HDO: 1
  • TPSA: 83.16
  • ALOGS: -3.53
  • ROTB: 6
  • Status: ONP
    • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

DoseUnitRoute
9 mg O

ADMET properties:

PropertyValueReference
S (Water solubility) 0.00 mg/mL Bocci G, Oprea TI, Benet LZ
BDDCS (Biopharmaceutical Drug Disposition Classification System) 2 Bocci G, Oprea TI, Benet LZ

Approvals:

DateAgencyCompanyOrphan
March 26, 2021 EMA Incyte Biosciences Distribution B.V.
April 17, 2020 FDA INCYTE CORP
March 23, 2021 PMDA Incyte Biosciences Japan GK

FDA Adverse Event Reporting System (Female)

None

FDA Adverse Event Reporting System (Male)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Hospice care 36.44 31.66 5 4 6935 34949987

FDA Adverse Event Reporting System (Geriatric)

None

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC L01EN02 ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS
ANTINEOPLASTIC AGENTS
PROTEIN KINASE INHIBITORS
Fibroblast growth factor receptor (FGFR) tyrosine kinase inhibitors
FDA MoA N0000175082 Kinase Inhibitors
FDA EPC N0000175605 Kinase Inhibitor
FDA MoA N0000185503 P-Glycoprotein Inhibitors
FDA MoA N0000187061 Organic Cation Transporter 2 Inhibitors
FDA MoA N0000191423 Multidrug and Toxin Extrusion Transporter 1 Inhibitors

Drug Use | Suggest Off label Use Form| |View source of the data|

DiseaseRelationSNOMED_IDDOID
Malignant neoplasm of common bile duct (& [carcinoma]) indication 187785004
Biliary tract cancer indication 363415003 DOID:4607
FGFR1 fusion genepositive myeloid/lymphoid neoplasm indication 721301004




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 4.44 Basic

Orange Book patent data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRoutePatent numberPatent expiration datePatent use
13.5MG PEMAZYRE INCYTE CORP N213736 April 17, 2020 RX TABLET ORAL 10131667 June 12, 2033 FOR THE TREATMENT OF PREVIOUSLY TREATED, UNRESECTABLE LOCALLY ADVANCED OR METASTATIC CHOLANGIOCARCINOMA WITH A FIBROBLAST GROWTH FACTOR RECEPTOR 2 (FGFR2) FUSION OR OTHER REARRANGEMENT
4.5MG PEMAZYRE INCYTE CORP N213736 April 17, 2020 RX TABLET ORAL 10131667 June 12, 2033 FOR THE TREATMENT OF PREVIOUSLY TREATED, UNRESECTABLE LOCALLY ADVANCED OR METASTATIC CHOLANGIOCARCINOMA WITH A FIBROBLAST GROWTH FACTOR RECEPTOR 2 (FGFR2) FUSION OR OTHER REARRANGEMENT
9MG PEMAZYRE INCYTE CORP N213736 April 17, 2020 RX TABLET ORAL 10131667 June 12, 2033 FOR THE TREATMENT OF PREVIOUSLY TREATED, UNRESECTABLE LOCALLY ADVANCED OR METASTATIC CHOLANGIOCARCINOMA WITH A FIBROBLAST GROWTH FACTOR RECEPTOR 2 (FGFR2) FUSION OR OTHER REARRANGEMENT
13.5MG PEMAZYRE INCYTE CORP N213736 April 17, 2020 RX TABLET ORAL 11466004 May 3, 2039 TREATMENT OF PREVIOUSLY TREATED, UNRESECTABLE LOCALLY ADVANCED OR METASTATIC CHOLANGIOCARCINOMA WITH A FGFR2 FUSION OR OTHER REARRANGEMENT BY ADMINISTERING ONCE DAILY A TABLET CONTAINING ABOUT 0.5 MG TO ABOUT 10 MG OF PEMIGATINIB
13.5MG PEMAZYRE INCYTE CORP N213736 April 17, 2020 RX TABLET ORAL 11466004 May 3, 2039 TREATMENT OF PREVIOUSLY TREATED, UNRESECTABLE LOCALLY ADVANCED OR METASTATIC CHOLANGIOCARCINOMA WITH A FGFR2 FUSION OR OTHER REARRANGEMENT BY ADMINISTERING PEMIGATINIB IN A DAILY DOSE OF ABOUT 5 MG TO ABOUT 20 MG
13.5MG PEMAZYRE INCYTE CORP N213736 April 17, 2020 RX TABLET ORAL 11466004 May 3, 2039 TREATMENT OF PREVIOUSLY TREATED, UNRESECTABLE LOCALLY ADVANCED OR METASTATIC CHOLANGIOCARCINOMA WITH A FGFR2 FUSION OR OTHER REARRANGEMENT BY ADMINISTERING PEMIGATINIB QD FOR 14 DAYS THEN NOT ADMINISTERING PEMIGATINIB FOR 7 DAYS IN A 21-DAY CYCLE
4.5MG PEMAZYRE INCYTE CORP N213736 April 17, 2020 RX TABLET ORAL 11466004 May 3, 2039 TREATMENT OF PREVIOUSLY TREATED, UNRESECTABLE LOCALLY ADVANCED OR METASTATIC CHOLANGIOCARCINOMA WITH A FGFR2 FUSION OR OTHER REARRANGEMENT BY ADMINISTERING ONCE DAILY A TABLET CONTAINING ABOUT 0.5 MG TO ABOUT 10 MG OF PEMIGATINIB
4.5MG PEMAZYRE INCYTE CORP N213736 April 17, 2020 RX TABLET ORAL 11466004 May 3, 2039 TREATMENT OF PREVIOUSLY TREATED, UNRESECTABLE LOCALLY ADVANCED OR METASTATIC CHOLANGIOCARCINOMA WITH A FGFR2 FUSION OR OTHER REARRANGEMENT BY ADMINISTERING PEMIGATINIB IN A DAILY DOSE OF ABOUT 5 MG TO ABOUT 20 MG
4.5MG PEMAZYRE INCYTE CORP N213736 April 17, 2020 RX TABLET ORAL 11466004 May 3, 2039 TREATMENT OF PREVIOUSLY TREATED, UNRESECTABLE LOCALLY ADVANCED OR METASTATIC CHOLANGIOCARCINOMA WITH A FGFR2 FUSION OR OTHER REARRANGEMENT BY ADMINISTERING PEMIGATINIB QD FOR 14 DAYS THEN NOT ADMINISTERING PEMIGATINIB FOR 7 DAYS IN A 21-DAY CYCLE
9MG PEMAZYRE INCYTE CORP N213736 April 17, 2020 RX TABLET ORAL 11466004 May 3, 2039 TREATMENT OF PREVIOUSLY TREATED, UNRESECTABLE LOCALLY ADVANCED OR METASTATIC CHOLANGIOCARCINOMA WITH A FGFR2 FUSION OR OTHER REARRANGEMENT BY ADMINISTERING ONCE DAILY A TABLET CONTAINING ABOUT 0.5 MG TO ABOUT 10 MG OF PEMIGATINIB
9MG PEMAZYRE INCYTE CORP N213736 April 17, 2020 RX TABLET ORAL 11466004 May 3, 2039 TREATMENT OF PREVIOUSLY TREATED, UNRESECTABLE LOCALLY ADVANCED OR METASTATIC CHOLANGIOCARCINOMA WITH A FGFR2 FUSION OR OTHER REARRANGEMENT BY ADMINISTERING PEMIGATINIB IN A DAILY DOSE OF ABOUT 5 MG TO ABOUT 20 MG
9MG PEMAZYRE INCYTE CORP N213736 April 17, 2020 RX TABLET ORAL 11466004 May 3, 2039 TREATMENT OF PREVIOUSLY TREATED, UNRESECTABLE LOCALLY ADVANCED OR METASTATIC CHOLANGIOCARCINOMA WITH A FGFR2 FUSION OR OTHER REARRANGEMENT BY ADMINISTERING PEMIGATINIB QD FOR 14 DAYS THEN NOT ADMINISTERING PEMIGATINIB FOR 7 DAYS IN A 21-DAY CYCLE
13.5MG PEMAZYRE INCYTE CORP N213736 April 17, 2020 RX TABLET ORAL 11628162 Aug. 30, 2040 TREATMENT OF PREVIOUSLY TREATED, UNRESECTABLE LOCALLY ADVANCED OR METASTATIC CHOLANGIOCARCINOMA WITH A FGFR2 FUSION OR OTHER REARRANGEMENT BY ADMINISTERING PEMIGATINIB WHILE AVOIDING THE CONCOMITANT USE OF STRONG AND MODERATE CYP3A INDUCERS
13.5MG PEMAZYRE INCYTE CORP N213736 April 17, 2020 RX TABLET ORAL 11628162 Aug. 30, 2040 TREATMENT OF PREVIOUSLY TREATED, UNRESECTABLE LOCALLY ADVANCED OR METASTATIC CHOLANGIOCARCINOMA WITH A FGFR2 FUSION OR OTHER REARRANGEMENT BY ADMINISTERING PEMIGATINIB WHILE AVOIDING THE CONCOMITANT USE OF STRONG AND MODERATE CYP3A INHIBITORS
13.5MG PEMAZYRE INCYTE CORP N213736 April 17, 2020 RX TABLET ORAL 11628162 Aug. 30, 2040 TREATMENT OF RELAPSED OR REFRACTORY MYELOID/LYMPHOID NEOPLASMS WITH FGFR1 REARRANGEMENT BY ADMINISTERING PEMIGATINIB WHILE AVOIDING THE CONCOMITANT USE OF STRONG AND MODERATE CYP3A INDUCERS
13.5MG PEMAZYRE INCYTE CORP N213736 April 17, 2020 RX TABLET ORAL 11628162 Aug. 30, 2040 TREATMENT OF RELAPSED OR REFRACTORY MYELOID/LYMPHOID NEOPLASMS WITH FGFR1 REARRANGEMENT BY ADMINISTERING PEMIGATINIB WHILE AVOIDING THE CONCOMITANT USE OF STRONG AND MODERATE CYP3A INHIBITORS
4.5MG PEMAZYRE INCYTE CORP N213736 April 17, 2020 RX TABLET ORAL 11628162 Aug. 30, 2040 TREATMENT OF PREVIOUSLY TREATED, UNRESECTABLE LOCALLY ADVANCED OR METASTATIC CHOLANGIOCARCINOMA WITH A FGFR2 FUSION OR OTHER REARRANGEMENT BY ADMINISTERING PEMIGATINIB WHILE AVOIDING THE CONCOMITANT USE OF STRONG AND MODERATE CYP3A INDUCERS
4.5MG PEMAZYRE INCYTE CORP N213736 April 17, 2020 RX TABLET ORAL 11628162 Aug. 30, 2040 TREATMENT OF PREVIOUSLY TREATED, UNRESECTABLE LOCALLY ADVANCED OR METASTATIC CHOLANGIOCARCINOMA WITH A FGFR2 FUSION OR OTHER REARRANGEMENT BY ADMINISTERING PEMIGATINIB WHILE AVOIDING THE CONCOMITANT USE OF STRONG AND MODERATE CYP3A INHIBITORS
4.5MG PEMAZYRE INCYTE CORP N213736 April 17, 2020 RX TABLET ORAL 11628162 Aug. 30, 2040 TREATMENT OF RELAPSED OR REFRACTORY MYELOID/LYMPHOID NEOPLASMS WITH FGFR1 REARRANGEMENT BY ADMINISTERING PEMIGATINIB WHILE AVOIDING THE CONCOMITANT USE OF STRONG AND MODERATE CYP3A INDUCERS
4.5MG PEMAZYRE INCYTE CORP N213736 April 17, 2020 RX TABLET ORAL 11628162 Aug. 30, 2040 TREATMENT OF RELAPSED OR REFRACTORY MYELOID/LYMPHOID NEOPLASMS WITH FGFR1 REARRANGEMENT BY ADMINISTERING PEMIGATINIB WHILE AVOIDING THE CONCOMITANT USE OF STRONG AND MODERATE CYP3A INHIBITORS
9MG PEMAZYRE INCYTE CORP N213736 April 17, 2020 RX TABLET ORAL 11628162 Aug. 30, 2040 TREATMENT OF PREVIOUSLY TREATED, UNRESECTABLE LOCALLY ADVANCED OR METASTATIC CHOLANGIOCARCINOMA WITH A FGFR2 FUSION OR OTHER REARRANGEMENT BY ADMINISTERING PEMIGATINIB WHILE AVOIDING THE CONCOMITANT USE OF STRONG AND MODERATE CYP3A INDUCERS
9MG PEMAZYRE INCYTE CORP N213736 April 17, 2020 RX TABLET ORAL 11628162 Aug. 30, 2040 TREATMENT OF PREVIOUSLY TREATED, UNRESECTABLE LOCALLY ADVANCED OR METASTATIC CHOLANGIOCARCINOMA WITH A FGFR2 FUSION OR OTHER REARRANGEMENT BY ADMINISTERING PEMIGATINIB WHILE AVOIDING THE CONCOMITANT USE OF STRONG AND MODERATE CYP3A INHIBITORS
9MG PEMAZYRE INCYTE CORP N213736 April 17, 2020 RX TABLET ORAL 11628162 Aug. 30, 2040 TREATMENT OF RELAPSED OR REFRACTORY MYELOID/LYMPHOID NEOPLASMS WITH FGFR1 REARRANGEMENT BY ADMINISTERING PEMIGATINIB WHILE AVOIDING THE CONCOMITANT USE OF STRONG AND MODERATE CYP3A INDUCERS
9MG PEMAZYRE INCYTE CORP N213736 April 17, 2020 RX TABLET ORAL 11628162 Aug. 30, 2040 TREATMENT OF RELAPSED OR REFRACTORY MYELOID/LYMPHOID NEOPLASMS WITH FGFR1 REARRANGEMENT BY ADMINISTERING PEMIGATINIB WHILE AVOIDING THE CONCOMITANT USE OF STRONG AND MODERATE CYP3A INHIBITORS

Orange Book exclusivity data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRouteExclusivity dateDescription
13.5MG PEMAZYRE INCYTE CORP N213736 April 17, 2020 RX TABLET ORAL April 17, 2025 NEW CHEMICAL ENTITY
4.5MG PEMAZYRE INCYTE CORP N213736 April 17, 2020 RX TABLET ORAL April 17, 2025 NEW CHEMICAL ENTITY
9MG PEMAZYRE INCYTE CORP N213736 April 17, 2020 RX TABLET ORAL April 17, 2025 NEW CHEMICAL ENTITY
13.5MG PEMAZYRE INCYTE CORP N213736 April 17, 2020 RX TABLET ORAL Aug. 26, 2025 TREATMENT OF ADULTS WITH RELAPSED OR REFRACTORY MYELOID/LYMPHOID NEOPLASMS (MLNS) WITH FIBROBLAST GROWTH FACTOR RECEPTOR 1 (FGFR1) REARRANGEMENT
4.5MG PEMAZYRE INCYTE CORP N213736 April 17, 2020 RX TABLET ORAL Aug. 26, 2025 TREATMENT OF ADULTS WITH RELAPSED OR REFRACTORY MYELOID/LYMPHOID NEOPLASMS (MLNS) WITH FIBROBLAST GROWTH FACTOR RECEPTOR 1 (FGFR1) REARRANGEMENT
9MG PEMAZYRE INCYTE CORP N213736 April 17, 2020 RX TABLET ORAL Aug. 26, 2025 TREATMENT OF ADULTS WITH RELAPSED OR REFRACTORY MYELOID/LYMPHOID NEOPLASMS (MLNS) WITH FIBROBLAST GROWTH FACTOR RECEPTOR 1 (FGFR1) REARRANGEMENT
13.5MG PEMAZYRE INCYTE CORP N213736 April 17, 2020 RX TABLET ORAL April 17, 2027 INDICATED FOR THE TREATMENT OF ADULTS WITH PREVIOUSLY TREATED, UNRESECTABLE LOCALLY ADVANCED OR METASTATIC CHOLANGIOCARCINOMA WITH A FIBROBLAST GROWTH FACTOR RECEPTOR 2 (FGFR2) FUSION OR OTHER REARRANGEMENT AS DETECTED BY AN FDA-APPROVED TEST
4.5MG PEMAZYRE INCYTE CORP N213736 April 17, 2020 RX TABLET ORAL April 17, 2027 INDICATED FOR THE TREATMENT OF ADULTS WITH PREVIOUSLY TREATED, UNRESECTABLE LOCALLY ADVANCED OR METASTATIC CHOLANGIOCARCINOMA WITH A FIBROBLAST GROWTH FACTOR RECEPTOR 2 (FGFR2) FUSION OR OTHER REARRANGEMENT AS DETECTED BY AN FDA-APPROVED TEST
9MG PEMAZYRE INCYTE CORP N213736 April 17, 2020 RX TABLET ORAL April 17, 2027 INDICATED FOR THE TREATMENT OF ADULTS WITH PREVIOUSLY TREATED, UNRESECTABLE LOCALLY ADVANCED OR METASTATIC CHOLANGIOCARCINOMA WITH A FIBROBLAST GROWTH FACTOR RECEPTOR 2 (FGFR2) FUSION OR OTHER REARRANGEMENT AS DETECTED BY AN FDA-APPROVED TEST
13.5MG PEMAZYRE INCYTE CORP N213736 April 17, 2020 RX TABLET ORAL Aug. 26, 2029 TREATMENT OF ADULTS WITH RELAPSED OR REFRACTORY MYELOID/LYMPHOID NEOPLASMS (MLNS) WITH FIBROBLAST GROWTH FACTOR RECEPTOR 1 (FGFR1) REARRANGEMENT
4.5MG PEMAZYRE INCYTE CORP N213736 April 17, 2020 RX TABLET ORAL Aug. 26, 2029 TREATMENT OF ADULTS WITH RELAPSED OR REFRACTORY MYELOID/LYMPHOID NEOPLASMS (MLNS) WITH FIBROBLAST GROWTH FACTOR RECEPTOR 1 (FGFR1) REARRANGEMENT
9MG PEMAZYRE INCYTE CORP N213736 April 17, 2020 RX TABLET ORAL Aug. 26, 2029 TREATMENT OF ADULTS WITH RELAPSED OR REFRACTORY MYELOID/LYMPHOID NEOPLASMS (MLNS) WITH FIBROBLAST GROWTH FACTOR RECEPTOR 1 (FGFR1) REARRANGEMENT

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])		Mechanism
action		Bioact sourceMoA source
Fibroblast growth factor receptor 3 Kinase INHIBITOR IC50 9 SCIENTIFIC LITERATURE DRUG LABEL
Fibroblast growth factor receptor 1 Kinase INHIBITOR IC50 9.40 SCIENTIFIC LITERATURE DRUG LABEL
Fibroblast growth factor receptor 2 Kinase INHIBITOR IC50 9.30 SCIENTIFIC LITERATURE DRUG LABEL
Fibroblast growth factor receptor 4 Kinase INHIBITOR IC50 7.52 SCIENTIFIC LITERATURE

External reference:

IDSource
Y6BX7BL23K UNII
C4724807 UMLSCUI
8ZF PDB_CHEM_ID
CHEMBL4297522 ChEMBL_ID
86705695 PUBCHEM_CID
DB15102 DRUGBANK_ID
10712 INN_ID
D11417 KEGG_DRUG
9767 IUPHAR_LIGAND_ID
018334 NDDF
871699001 SNOMEDCT_US
871709004 SNOMEDCT_US
4039347 VANDF
2359268 RXNORM
333127 MMSL
38333 MMSL
d09543 MMSL
C000705477 MESH_SUPPLEMENTAL_RECORD_UI

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
PEMAZYRE HUMAN PRESCRIPTION DRUG LABEL 1 50881-026 TABLET 4.50 mg ORAL NDA 29 sections
PEMAZYRE HUMAN PRESCRIPTION DRUG LABEL 1 50881-026 TABLET 4.50 mg ORAL NDA 29 sections
PEMAZYRE HUMAN PRESCRIPTION DRUG LABEL 1 50881-026 TABLET 4.50 mg ORAL NDA 29 sections
PEMAZYRE HUMAN PRESCRIPTION DRUG LABEL 1 50881-027 TABLET 9 mg ORAL NDA 29 sections
PEMAZYRE HUMAN PRESCRIPTION DRUG LABEL 1 50881-027 TABLET 9 mg ORAL NDA 29 sections
PEMAZYRE HUMAN PRESCRIPTION DRUG LABEL 1 50881-027 TABLET 9 mg ORAL NDA 29 sections
PEMAZYRE HUMAN PRESCRIPTION DRUG LABEL 1 50881-028 TABLET 13.50 mg ORAL NDA 29 sections
PEMAZYRE HUMAN PRESCRIPTION DRUG LABEL 1 50881-028 TABLET 13.50 mg ORAL NDA 29 sections
PEMAZYRE HUMAN PRESCRIPTION DRUG LABEL 1 50881-028 TABLET 13.50 mg ORAL NDA 29 sections