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

Stem definition	Drug id	CAS RN
SMO receptor antagonists	5304	1095173-27-5

Description:

Molecule	Description
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

Molecule

Description

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:

Date	Agency	Company	Orphan
Nov. 21, 2018	FDA	PFIZER INC

FDA Adverse Event Reporting System (Female)

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MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Febrile neutropenia	108.54	51.72	32	199	118417	63370374
Death	59.62	51.72	28	203	374353	63114438

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FDA Adverse Event Reporting System (Male)

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MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Febrile neutropenia	93.57	48.75	38	295	136811	34819787
Pneumonia	53.50	48.75	36	297	362591	34594007

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FDA Adverse Event Reporting System (Geriatric)

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MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Febrile neutropenia	193.17	47.27	70	541	230929	79512848
Death	88.56	47.27	54	557	566460	79177317
Pneumonia	53.10	47.27	42	569	660204	79083573
Neoplasm progression	47.54	47.27	17	594	51665	79692112

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FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

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

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

Disease	Relation	SNOMED_ID	DOID
Acute myeloid leukemia, disease	indication	91861009

🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

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Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	12.45	acidic
pKa2	12.88	acidic
pKa3	13.49	acidic
pKa4	7.85	Basic
pKa5	6.86	Basic

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Orange Book patent data (new drug applications)

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Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Patent number	Patent expiration date	Patent 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

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Orange Book exclusivity data (new drug applications)

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Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Exclusivity date	Description
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

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Bioactivity Summary:

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Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Mechanism action	Bioact source	MoA source
Smoothened homolog	GPCR	Q99835	SMO_HUMAN	ANTAGONIST	IC50	8.30		SCIENTIFIC LITERATURE	DRUG LABEL
Smoothened homolog	GPCR		SMO_MOUSE		IC50	8.30		CHEMBL

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External reference:

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ID	Source
017851	NDDF
2105845	RXNORM
25166913	PUBCHEM_CID
299196	MMSL
4038031	VANDF
782978008	SNOMEDCT_US
783019002	SNOMEDCT_US
8201	IUPHAR_LIGAND_ID
9930	INN_ID
C000592580	MESH_SUPPLEMENTAL_RECORD_UI

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Pharmaceutical products:

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Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
Daurismo	HUMAN PRESCRIPTION DRUG LABEL	1	0069-0298	TABLET, FILM COATED	25 mg	ORAL	NDA	31 sections
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
Daurismo	HUMAN PRESCRIPTION DRUG LABEL	1	0069-1531	TABLET, FILM COATED	100 mg	ORAL	NDA	31 sections

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