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

Stem definitionDrug idCAS RN
tyrosine kinase inhibitors 5412 2097132-94-8

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • pralsetinib
  • BLU-667
  • BLU123244
  • X581238
  • gavreto
Pralsetinib is a kinase inhibitor of wild-type RET and oncogenic RET fusions (CCDC6-RET) and mutations (RET V804L, RET V804M and RET M918T) with half maximal inhibitory concentrations (IC50s) less than 0.5 nM. In purified enzyme assays, pralsetinib inhibited DDR1, TRKC, FLT3, JAK1-2, TRKA, VEGFR2, PDGFRb, and FGFR1 at higher concentrations that were still clinically achievable at Cmax. In cellular assays, pralsetinib inhibited RET at approximately 14-, 40-, and 12-fold lower concentrations than VEGFR2, FGFR2, and JAK2, respectively.
  • Molecular weight: 533.61
  • Formula: C27H32FN9O2
  • CLOGP: 3.23
  • LIPINSKI: 2
  • HAC: 11
  • HDO: 3
  • TPSA: 135.53
  • ALOGS: -4.72
  • ROTB: 8
  • Status: ONP
    • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

DoseUnitRoute
0.40 g O

ADMET properties:

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

Approvals:

DateAgencyCompanyOrphan
Nov. 18, 2021 EMA ROCHE REGISTRATION GMBH
Sept. 4, 2020 FDA BLUEPRINT MEDICINES

FDA Adverse Event Reporting System (Female)

None

FDA Adverse Event Reporting System (Male)

None

FDA Adverse Event Reporting System (Geriatric)

None

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC L01EX23 ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS
ANTINEOPLASTIC AGENTS
PROTEIN KINASE INHIBITORS
Other protein kinase inhibitors
MeSH PA D000970 Antineoplastic Agents
FDA EPC N0000175605 Kinase Inhibitor
FDA MoA N0000193947 Rearranged during Transfection (RET) Inhibitors

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

DiseaseRelationSNOMED_IDDOID
Non-small cell lung cancer indication 254637007 DOID:3908
Medullary thyroid carcinoma indication 255032005 DOID:3973
Metastatic non-small cell lung cancer indication




🐶 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
100MG GAVRETO GENENTECH INC N213721 Sept. 4, 2020 RX CAPSULE ORAL 10030005 Nov. 1, 2036 TREATMENT OF ADULT AND PEDIATRIC PATIENTS 12 YEARS OF AGE AND OLDER WITH ADVANCED OR METASTATIC RET FUSION-POSITIVE THYROID CANCER WHO REQUIRE SYSTEMIC THERAPY AND WHO ARE RADIOACTIVE IODINE-REFRACTORY (IF RADIOACTIVE IODINE IS APPROPRIATE)
100MG GAVRETO GENENTECH INC N213721 Sept. 4, 2020 RX CAPSULE ORAL 10030005 Nov. 1, 2036 TREATMENT OF ADULT AND PEDIATRIC PATIENTS 12 YEARS OF AGE AND OLDER WITH ADVANCED OR METASTATIC RET-MUTANT MEDULLARY THYROID CANCER (MTC) WHO REQUIRE SYSTEMIC THERAPY
100MG GAVRETO GENENTECH INC N213721 Sept. 4, 2020 RX CAPSULE ORAL 10030005 Nov. 1, 2036 TREATMENT OF ADULT PATIENTS WITH METASTATIC REARRANGED DURING TRANSFECTION (RET) FUSION-POSITIVE NON-SMALL CELL LUNG CANCER (NSCLC) AS DETECTED BY AN FDA APPROVED TEST
100MG GAVRETO GENENTECH INC N213721 Sept. 4, 2020 RX CAPSULE ORAL 11273160 April 3, 2039 TREATMENT OF ADULT PATIENTS WITH METASTATIC REARRANGED DURING TRANSFECTION (RET) FUSION-POSITIVE NON-SMALL CELL LUNG CANCER (NSCLC) AS DETECTED BY AN FDA APPROVED TEST

Orange Book exclusivity data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRouteExclusivity dateDescription
100MG GAVRETO GENENTECH INC N213721 Sept. 4, 2020 RX CAPSULE ORAL Sept. 4, 2025 NEW CHEMICAL ENTITY
100MG GAVRETO GENENTECH INC N213721 Sept. 4, 2020 RX CAPSULE ORAL Sept. 4, 2027 TREATMENT OF ADULT PATIENTS WITH METASTATIC RET FUSION-POSITIVE NON-SMALL CELL LUNG CANCER (NSCLC) AS DETECTED BY AN FDA APPROVED TEST
100MG GAVRETO GENENTECH INC N213721 Sept. 4, 2020 RX CAPSULE ORAL Dec. 1, 2027 TREATMENT OF ADULT AND PEDIATRIC PATIENTS 12 YEARS OF AGE AND OLDER WITH ADVANCED OR METASTATIC RET FUSION-POSITIVE THYROID CANCER WHO REQUIRE SYSTEMIC THERAPY AND WHO ARE RADIOACTIVE IODINE-REFRACTORY (IF RADIOACTIVE IODINE IS APPROPRIATE)
100MG GAVRETO GENENTECH INC N213721 Sept. 4, 2020 RX CAPSULE ORAL Dec. 1, 2027 TREATMENT OF ADULT AND PEDIATRIC PATIENTS 12 YEARS OF AGE AND OLDER WITH ADVANCED OR METASTATIC RET-MUTANT MEDULLARY THYROID CANCER (MTC) WHO REQUIRE SYSTEMIC THERAPY

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])		Mechanism
action		Bioact sourceMoA source
Proto-oncogene tyrosine-protein kinase receptor Ret Kinase INHIBITOR IC50 9.39 SCIENTIFIC LITERATURE DRUG LABEL
Vascular endothelial growth factor receptor 2 Kinase INHIBITOR IC50 7.46 SCIENTIFIC LITERATURE
Platelet-derived growth factor receptor beta Kinase INHIBITOR IC50 7 DRUG LABEL
Receptor-type tyrosine-protein kinase FLT3 Kinase INHIBITOR IC50 7.80 DRUG LABEL
Tyrosine-protein kinase JAK1 Kinase INHIBITOR IC50 8.66 DRUG LABEL
Tyrosine-protein kinase JAK2 Kinase INHIBITOR IC50 7.72 DRUG LABEL
Fibroblast growth factor receptor 1 Kinase INHIBITOR IC50 7.96 DRUG LABEL
Epithelial discoidin domain-containing receptor 1 Kinase INHIBITOR IC50 8.70 DRUG LABEL
NT-3 growth factor receptor Kinase INHIBITOR IC50 8.05 DRUG LABEL
High affinity nerve growth factor receptor Kinase INHIBITOR IC50 7.24 DRUG LABEL

External reference:

IDSource
D11712 KEGG_DRUG
1WPE73O1WV UNII
C5226874 UMLSCUI
Q4J PDB_CHEM_ID
CHEMBL4582651 ChEMBL_ID
129073603 PUBCHEM_CID
DB15822 DRUGBANK_ID
10033 IUPHAR_LIGAND_ID
018493 NDDF
926312002 SNOMEDCT_US
926317008 SNOMEDCT_US
4039706 VANDF
2394936 RXNORM
338525 MMSL
38786 MMSL
d09624 MMSL
C000655704 MESH_SUPPLEMENTAL_RECORD_UI
11004 INN_ID

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Gavreto HUMAN PRESCRIPTION DRUG LABEL 1 50242-210 CAPSULE 100 mg ORAL NDA 31 sections
Gavreto HUMAN PRESCRIPTION DRUG LABEL 1 50242-210 CAPSULE 100 mg ORAL NDA 31 sections
GAVRETO HUMAN PRESCRIPTION DRUG LABEL 1 72064-210 CAPSULE 100 mg ORAL NDA 31 sections