All FDA-approved EMA-approved PMDA-approved
Target Card Uniprot Example: P23975

glasdegib 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | 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

Drug dosage:

None

ADMET properties:

Property	Value	Reference
BA (Bioavailability)	77.12 %

Predicted pharmacokinetic/toxicological properties (PK-AZ):

Property	Description	Value	Unit	Confidence	Similarity
kinase-safety-class	ACVR2B,AXL,BRAF,CAMK2D,EGFR,EIF2AK3,ERBB2,GRK2,ITK,MET,PDK1,PDK2,PDK4,PRKDC	14
kinase-selectivity-class	DYRK1B,MAP3K21	2
pfas-class	PFAS structural alert (1 = True, 0 = False)	0

Approvals:

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

FDA Adverse Event Reporting System (Female)

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	128.35	55.82	37	227	158312	90469871
Death	69.69	55.82	31	233	456520	90171663

FDA Adverse Event Reporting System (Male)

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	95.08	47.48	42	362	185661	42435270
Death	56.09	47.48	41	363	471144	42149787
Pneumonia	53.02	47.48	38	366	422111	42198820

FDA Adverse Event Reporting System (Geriatric)

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	215.68	44.86	79	638	316688	110271894
Death	107.12	44.86	62	655	698807	109889775
Pneumonia	52.78	44.86	44	673	876670	109711912
Neoplasm progression	46.57	44.86	17	700	64578	110524004

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

Source	Code	Description
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 agent
CHEBI has role	CHEBI:66908	SMO receptor antagonist
CHEBI has role	CHEBI:140921	Hedgehog signaling pathway inhibitor

Related Drugs by ATC class:

L01XJ Hedgehog pathway inhibitors 2 drugs

sonidegibvismodegib

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

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

Orange Book patent data (new drug applications)

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
EQ 25MG BASE	DAURISMO	PFIZER	N210656	Nov. 21, 2018	RX	TABLET	ORAL	11891372	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)

None

Bioactivity Summary:

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

External reference:

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

Pharmaceutical products:

Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
Daurismo	HUMAN PRESCRIPTION DRUG LABEL	1	0069-0298	TABLET, FILM COATED	25 mg	ORAL	NDA	30 sections
Daurismo	HUMAN PRESCRIPTION DRUG LABEL	1	0069-0298	TABLET, FILM COATED	25 mg	ORAL	NDA	30 sections
Daurismo	HUMAN PRESCRIPTION DRUG LABEL	1	0069-1531	TABLET, FILM COATED	100 mg	ORAL	NDA	30 sections
Daurismo	HUMAN PRESCRIPTION DRUG LABEL	1	0069-1531	TABLET, FILM COATED	100 mg	ORAL	NDA	30 sections