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

Stem definitionDrug idCAS RN
tyrosine kinase inhibitors 5394 1442472-39-0

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • ripretinib
  • qinlock
  • DCC-2618
Ripretinib is a tyrosine kinase inhibitor that inhibits KIT proto-oncogene receptor tyrosine kinase (KIT) and platelet derived growth factor receptor A (PDGFRA) kinase, including wild type, primary, and secondary mutations. Ripretinib also inhibits other kinases in vitro, such as PDGFRB, TIE2, VEGFR2, and BRAF
  • Molecular weight: 510.37
  • Formula: C24H21BrFN5O2
  • CLOGP: 5.06
  • LIPINSKI: 1
  • HAC: 7
  • HDO: 3
  • TPSA: 86.36
  • ALOGS: -4.94
  • ROTB: 5
  • Status: ONP
    • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

DoseUnitRoute
0.15 g O

ADMET properties:

PropertyValueReference
BDDCS (Biopharmaceutical Drug Disposition Classification System) 2 Bocci G, Oprea TI, Benet LZ

Approvals:

DateAgencyCompanyOrphan
Nov. 18, 2021 EMA DECIPHERA PHARMACEUTICALS (NETHERLANDS) B.V.
May 15, 2020 FDA DECIPHERA PHARMS

FDA Adverse Event Reporting System (Female)

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
Extra dose administered 133.90 37.04 30 1262 6320 63481410
Disease progression 131.31 37.04 59 1233 122699 63365031
Underdose 119.22 37.04 37 1255 27419 63460311
Palmar-plantar erythrodysaesthesia syndrome 75.14 37.04 25 1267 22990 63464740
Neoplasm progression 71.08 37.04 27 1265 36401 63451329
Alopecia 69.33 37.04 56 1236 337480 63150250
Hospitalisation 60.50 37.04 31 1261 85050 63402680
Death 46.75 37.04 47 1245 374334 63113396
Hyperkeratosis 43.20 37.04 12 1280 6006 63481724

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
Extra dose administered 305.87 41.90 63 1547 3946 34951375
Disease progression 154.60 41.90 82 1528 107995 34847326
Alopecia 149.43 41.90 52 1558 24303 34931018
Fatigue 94.23 41.90 99 1511 370554 34584767
Underdose 86.58 41.90 30 1580 13750 34941571
Neoplasm progression 58.14 41.90 26 1584 23274 34932047
Hospitalisation 56.07 41.90 34 1576 56868 34898453
Hair texture abnormal 55.50 41.90 10 1600 302 34955019
Death 54.41 41.90 78 1532 397971 34557350
Adverse event 50.09 41.90 22 1588 18855 34936466

FDA Adverse Event Reporting System (Geriatric)

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
Extra dose administered 176.65 43.44 37 1074 8378 79734899
Alopecia 77.65 43.44 45 1066 231310 79511967
Fatigue 73.27 43.44 76 1035 929651 78813626
Underdose 71.53 43.44 24 1087 33127 79710150
Palmar-plantar erythrodysaesthesia syndrome 63.68 43.44 22 1089 33112 79710165
Death 62.69 43.44 56 1055 566458 79176819
Disease progression 56.84 43.44 34 1077 184328 79558949
Tumour excision 54.40 43.44 9 1102 557 79742720

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC L01EX19 ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS
ANTINEOPLASTIC AGENTS
PROTEIN KINASE INHIBITORS
Other protein kinase inhibitors
FDA MoA N0000020028 Platelet-derived Growth Factor alpha Receptor Inhibitors
FDA MoA N0000020034 Stem Cell Factor (KIT) Receptor Inhibitors
FDA EPC N0000175605 Kinase Inhibitor
FDA MoA N0000185503 P-Glycoprotein Inhibitors
FDA MoA N0000187062 Cytochrome P450 2C8 Inhibitors
FDA MoA N0000190113 Breast Cancer Resistance Protein Inhibitors

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

DiseaseRelationSNOMED_IDDOID
Gastrointestinal stromal tumor indication 420120006 DOID:9253




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

None

Orange Book patent data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRoutePatent numberPatent expiration datePatent use
50MG QINLOCK DECIPHERA PHARMS N213973 May 15, 2020 RX TABLET ORAL RE48731 June 7, 2032 TREATMENT OF GASTROINTESTINAL STROMAL TUMOR
50MG QINLOCK DECIPHERA PHARMS N213973 May 15, 2020 RX TABLET ORAL 10966966 Aug. 12, 2040 TREATMENT OF ADVANCED GASTROINTESTINAL STROMAL TUMOR IN PATIENTS HAVING PROGRESSED FROM A FIRST LINE ADMINISTRATION OF IMATINIB, A SECOND LINE ADMINISTRATION OF SUNITINIB, AND A THIRD LINE ADMINISTRATION OF REGORAFENIB
50MG QINLOCK DECIPHERA PHARMS N213973 May 15, 2020 RX TABLET ORAL 11266635 Aug. 12, 2040 TREATMENT OF GASTROINTESTINAL STROMAL TUMORS IN PATIENTS SUFFERING FROM PALMER-PLANTER ERYTHRODYSESTHESIA SYNDROME
50MG QINLOCK DECIPHERA PHARMS N213973 May 15, 2020 RX TABLET ORAL 11344536 Aug. 12, 2040 TREATMENT OF GASTROINTESTINAL STROMAL TUMORS IN PATIENTS SUFFERING FROM HYPERTENSION
50MG QINLOCK DECIPHERA PHARMS N213973 May 15, 2020 RX TABLET ORAL 11426390 Aug. 12, 2040 TREATMENT OF GASTROINTESTINAL STROMAL TUMORS IN PATIENTS BEING TREATED CONCURRENTLY WITH A CYP3A4 INHIBITOR
50MG QINLOCK DECIPHERA PHARMS N213973 May 15, 2020 RX TABLET ORAL 11433056 Aug. 12, 2040 METHOD OF TREATING GASTROINTESTINAL STROMAL TUMORS IN PATIENTS SUFFERING FROM GRADE 2 OR GRADE 3 MYALGIA WHILE BEING ADMINISTERED RIPRETINIB DAILY
50MG QINLOCK DECIPHERA PHARMS N213973 May 15, 2020 RX TABLET ORAL 11529336 Aug. 12, 2040 TREATMENT OF GASTROINTESTINAL STROMAL TUMORS IN PATIENTS SUFFERING FROM A GRADE 3 ADVERSE REACTION WHILE BEING ADMINISTERED RIPRETINIB DAILY
50MG QINLOCK DECIPHERA PHARMS N213973 May 15, 2020 RX TABLET ORAL 11534432 Aug. 12, 2040 TREATMENT OF ADVANCED GASTROINTESTINAL STROMAL TUMOR IN PATIENTS PREVIOUSLY ADMINISTERED AT LEAST THREE TYROSINE KINASE INHIBITORS, WHERE ONE OF THE KINASE INHIBITORS IS IMATINIB
50MG QINLOCK DECIPHERA PHARMS N213973 May 15, 2020 RX TABLET ORAL 11576904 Aug. 12, 2040 TREATMENT OF GASTROINTESTINAL STROMAL TUMORS IN PATIENTS SUFFERING FROM GRADE 2 OR GRADE 3 ARTHRALGIA WHILE BEING ADMINISTERED RIPRETINIB DAILY

Orange Book exclusivity data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRouteExclusivity dateDescription
50MG QINLOCK DECIPHERA PHARMS N213973 May 15, 2020 RX TABLET ORAL May 15, 2025 NEW CHEMICAL ENTITY
50MG QINLOCK DECIPHERA PHARMS N213973 May 15, 2020 RX TABLET ORAL May 15, 2027 INDICATED FOR THE TREATMENT OF ADULT PATIENTS WITH ADVANCED GASTROINTESTINAL STROMAL TUMOR (GIST) WHO HAVE RECEIVED PRIOR TREATMENT WITH 3 OR MORE KINASE INHIBITORS, INCLUDING IMATINIB

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])		Mechanism
action		Bioact sourceMoA source
Mast/stem cell growth factor receptor Kit Kinase INHIBITOR IC50 8.52 SCIENTIFIC LITERATURE DRUG LABEL
Platelet-derived growth factor receptor alpha Kinase INHIBITOR IC50 8.44 SCIENTIFIC LITERATURE DRUG LABEL
Platelet-derived growth factor receptor beta Kinase INHIBITOR IC50 8.05 DRUG LABEL
Vascular endothelial growth factor receptor 2 Kinase INHIBITOR IC50 8.47 DRUG LABEL
Macrophage colony-stimulating factor 1 receptor Kinase INHIBITOR IC50 6.91 DRUG LABEL
Angiopoietin-1 receptor Kinase INHIBITOR IC50 8.27 DRUG LABEL

External reference:

IDSource
D11353 KEGG_DRUG
9XW757O13D UNII
C5139749 UMLSCUI
CHEMBL4216467 ChEMBL_ID
71584930 PUBCHEM_CID
DB14840 DRUGBANK_ID
9175 IUPHAR_LIGAND_ID
018369 NDDF
874906002 SNOMEDCT_US
876860008 SNOMEDCT_US
4039405 VANDF
2369389 RXNORM
334366 MMSL
38467 MMSL
d09563 MMSL
C000707850 MESH_SUPPLEMENTAL_RECORD_UI
10808 INN_ID

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
QINLOCK HUMAN PRESCRIPTION DRUG LABEL 1 73207-101 TABLET 50 mg ORAL NDA 28 sections
QINLOCK HUMAN PRESCRIPTION DRUG LABEL 1 73207-101 TABLET 50 mg ORAL NDA 28 sections
QINLOCK HUMAN PRESCRIPTION DRUG LABEL 1 73207-101 TABLET 50 mg ORAL NDA 28 sections