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

Stem definitionDrug idCAS RN
SMO receptor antagonists 5304 1095173-27-5

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • glasdegib
  • daurismo
  • PF-04449913
Glasdegib is an inhibitor of the Hedgehog pathway. Glasdegib binds to and inhibits Smoothened, a transmembrane protein involved in hedgehog signal transduction.
  • Molecular weight: 374.45
  • Formula: C21H22N6O
  • CLOGP: 2.27
  • LIPINSKI: 0
  • HAC: 7
  • HDO: 3
  • TPSA: 96.84
  • ALOGS: -3.90
  • ROTB: 3
  • Status: ONP
    • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

None

ADMET properties:

None

Approvals:

DateAgencyCompanyOrphan
Nov. 21, 2018 FDA PFIZER INC

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
Febrile neutropenia 104.44 45.20 30 163 97637 50507294
Death 46.68 45.20 23 170 325356 50279575

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
Febrile neutropenia 90.14 46.93 36 276 112204 29462011
Pneumonia 47.06 46.93 33 279 320139 29254076

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
Febrile neutropenia 183.30 46.13 66 498 187591 64310577
Death 74.67 46.13 48 516 482657 64015511
Pneumonia 47.91 46.13 39 525 559537 63938631

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC L01XJ03 ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS
ANTINEOPLASTIC AGENTS
OTHER ANTINEOPLASTIC AGENTS
Hedgehog pathway inhibitors
FDA MoA N0000184148 Smoothened Receptor Antagonists
FDA EPC N0000184149 Hedgehog Pathway Inhibitor
CHEBI has role CHEBI:35610 antineoplastic agents
CHEBI has role CHEBI:66908 SMO receptor antagonists
CHEBI has role CHEBI:140921 Hedgehog pathway inhibitors

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

DiseaseRelationSNOMED_IDDOID
Acute myeloid leukemia, disease indication 91861009




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 12.45 acidic
pKa2 12.88 acidic
pKa3 13.49 acidic
pKa4 7.85 Basic
pKa5 6.86 Basic

Orange Book patent data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRoutePatent numberPatent expiration datePatent use
EQ 25MG BASE DAURISMO PFIZER N210656 Nov. 21, 2018 RX TABLET ORAL 11168066 April 13, 2036 USE, IN COMBINATION WITH LOW-DOSE CYTARABINE, FOR THE TREATMENT OF NEWLY-DIAGNOSED ACUTE MYELOID LEUKEMIA (AML) IN ADULT PATIENTS WHO ARE >= 75 YEARS OLD OR WHO HAVE COMORBIDITIES THAT PRECLUDE USE OF INTENSIVE INDUCTION CHEMOTHERAPY

Orange Book exclusivity data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRouteExclusivity dateDescription
EQ 25MG BASE DAURISMO PFIZER N210656 Nov. 21, 2018 RX TABLET ORAL Nov. 21, 2023 NEW CHEMICAL ENTITY
EQ 25MG BASE DAURISMO PFIZER N210656 Nov. 21, 2018 RX TABLET ORAL Nov. 21, 2025 INDICATED, IN COMBINATION WITH LOW-DOSE CYTARABINE, FOR THE TREATMENT OF NEWLY-DIAGNOSED ACUTE MYELOID LEUKEMIA (AML) IN ADULT PATIENTS WHO ARE >=75 YEARS OLD OR WHO HAVE COMORBIDITIES THAT PRECLUDE USE OF INTENSIVE INDUCTION CHEMOTHERAPY

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])		Mechanism
action		Bioact sourceMoA source
Smoothened homolog GPCR ANTAGONIST IC50 8.30 SCIENTIFIC LITERATURE DRUG LABEL
Smoothened homolog GPCR IC50 8.30 CHEMBL

External reference:

IDSource
K673DMO5H9 UNII
C4519273 UMLSCUI
CHEBI:145428 CHEBI
CHEMBL2043437 ChEMBL_ID
25166913 PUBCHEM_CID
DB11978 DRUGBANK_ID
CHEMBL4297534 ChEMBL_ID
D10636 KEGG_DRUG
8201 IUPHAR_LIGAND_ID
2105845 RXNORM
299196 MMSL
d09075 MMSL
782978008 SNOMEDCT_US
783019002 SNOMEDCT_US
4038031 VANDF
017851 NDDF
C000592580 MESH_SUPPLEMENTAL_RECORD_UI
9930 INN_ID

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Daurismo HUMAN PRESCRIPTION DRUG LABEL 1 0069-0298 TABLET, FILM COATED 25 mg ORAL NDA 31 sections
Daurismo HUMAN PRESCRIPTION DRUG LABEL 1 0069-1531 TABLET, FILM COATED 100 mg ORAL NDA 31 sections