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

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

Stem definition	Drug id	CAS RN
tyrosine kinase inhibitors	5306	1254053-43-4

Description:

Molecule

Description

Molfile Inchi Smiles Synonyms: gilteritinib fumarate gilteritinib xospata ASP2215

Gilteritinib is a small molecule that inhibits multiple receptor tyrosine kinases, including FMS-like tyrosine kinase 3 (FLT3). Gilteritinib demonstrated the ability to inhibit FLT3 receptor signaling and proliferation in cells exogenously expressing FLT3 including FLT3-ITD, tyrosine kinase domain mutations (TKD) FLT3-D835Y and FLT3-ITD-D835Y, and it induced apoptosis in leukemic cells expressing FLT3-ITD. Molecular weight: 552.72 Formula: C29H44N8O3 CLOGP: 2.48 LIPINSKI: 2 HAC: 11 HDO: 3 TPSA: 121.11 ALOGS: -4.39 ROTB: 9 Status: ONP Legend: OFP - off patent OFM - off market ONP - on patent

Drug dosage:

Dose	Unit	Route
0.12	g	O

ADMET properties:

Property	Value	Reference
S (Water solubility)	0.09 mg/mL	Bocci G, Oprea TI, Benet LZ
BDDCS (Biopharmaceutical Drug Disposition Classification System)	2	Bocci G, Oprea TI, Benet LZ

Approvals:

Date	Agency	Company	Orphan
Oct. 24, 2019	EMA	ASTELLAS PHARMA EUROPE BV
Nov. 28, 2018	FDA	ASTELLAS
Sept. 21, 2018	PMDA	Astellas Pharma 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	327.85	45.21	139	2615	118310	63367958
Myelosuppression	193.87	45.21	62	2692	23641	63462627
Hepatic function abnormal	155.65	45.21	59	2695	37083	63449185
Platelet count decreased	130.77	45.21	74	2680	116048	63370220
Acute myeloid leukaemia recurrent	127.90	45.21	26	2728	1597	63484671
Cytopenia	122.76	45.21	37	2717	11564	63474704
Acute myeloid leukaemia	120.42	45.21	40	2714	17107	63469161
Differentiation syndrome	113.01	45.21	22	2732	1081	63485187
Neutrophil count decreased	103.72	45.21	50	2704	56356	63429912
Blast cell count increased	91.55	45.21	16	2738	430	63485838
Acute febrile neutrophilic dermatosis	91.27	45.21	22	2732	2952	63483316
Electrocardiogram QT prolonged	78.00	45.21	42	2712	59488	63426780
Left atrial hypertrophy	74.38	45.21	10	2744	40	63486228
Pneumonia adenoviral	71.16	45.21	11	2743	134	63486134
Septic shock	63.01	45.21	38	2716	66591	63419677
Adenoviral hepatitis	59.98	45.21	11	2743	390	63485878
Electrocardiogram PR shortened	57.06	45.21	10	2744	273	63485995
Graft versus host disease	56.45	45.21	18	2736	6745	63479523
Bacteraemia	53.09	45.21	22	2732	17326	63468942
Pancytopenia	50.07	45.21	38	2716	96895	63389373
Liver disorder	46.60	45.21	29	2725	53658	63432610

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
Myelosuppression	255.67	38.41	81	2298	19184	34935368
Febrile neutropenia	203.89	38.41	122	2257	136727	34817825
Acute myeloid leukaemia	194.28	38.41	65	2314	18205	34936347
Hepatic function abnormal	129.13	38.41	62	2317	44301	34910251
Platelet count decreased	119.00	38.41	83	2296	119634	34834918
Differentiation syndrome	86.58	38.41	20	2359	1418	34953134
Cytopenia	73.86	38.41	29	2350	12694	34941858
Pneumonia	60.18	38.41	96	2283	362531	34592021
Neutrophil count decreased	47.19	38.41	34	2345	51070	34903482
Product use issue	47.15	38.41	37	2342	63179	34891373
Graft versus host disease	44.00	38.41	19	2360	10550	34944002
Blast cell count increased	39.24	38.41	10	2369	1068	34953484
Pyrexia	39.23	38.41	76	2303	332937	34621615

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	490.16	38.93	257	5000	230742	79508389
Myelosuppression	480.19	38.93	155	5102	40141	79698990
Acute myeloid leukaemia	288.46	38.93	99	5158	30786	79708345
Hepatic function abnormal	284.89	38.93	124	5133	72983	79666148
Platelet count decreased	253.53	38.93	158	5099	194506	79544625
Cytopenia	196.68	38.93	67	5190	20316	79718815
Acute myeloid leukaemia recurrent	173.16	38.93	41	5216	3342	79735789
Neutrophil count decreased	149.70	38.93	87	5170	93872	79645259
Differentiation syndrome	147.15	38.93	34	5223	2490	79736641
Blast cell count increased	126.29	38.93	27	5230	1383	79737748
Graft versus host disease	105.38	38.93	39	5218	14987	79724144
Pneumonia	102.56	38.93	167	5090	660079	79079052
Electrocardiogram QT prolonged	99.02	38.93	66	5191	90320	79648811
Acute febrile neutrophilic dermatosis	94.53	38.93	26	5231	3846	79735285
Liver disorder	84.44	38.93	55	5202	72362	79666769
Blood lactate dehydrogenase increased	75.09	38.93	41	5216	39129	79700002
Pyrexia	73.61	38.93	147	5110	678562	79060569
Left atrial hypertrophy	68.37	38.93	10	5247	50	79739081
Pneumonia fungal	60.32	38.93	24	5233	11186	79727945
Bacteraemia	59.17	38.93	33	5224	32791	79706340
Sepsis	58.53	38.93	80	5177	269348	79469783
Thrombocytopenia	56.47	38.93	78	5179	265181	79473950
Anaemia	54.95	38.93	102	5155	444913	79294218
Bronchopulmonary aspergillosis	53.12	38.93	27	5230	22267	79716864
Pneumonia adenoviral	52.70	38.93	11	5246	501	79738630
Electrocardiogram PR shortened	51.80	38.93	10	5247	305	79738826
Product use issue	51.23	38.93	66	5191	209756	79529375
Adenoviral hepatitis	46.20	38.93	11	5246	916	79738215
Infection	45.41	38.93	67	5190	241645	79497486
WT1 gene mutation	43.14	38.93	5	5252	0	79739131
Blood creatine phosphokinase increased	42.37	38.93	35	5222	66055	79673076
Septic shock	42.15	38.93	46	5211	122755	79616376
Pancytopenia	41.79	38.93	53	5204	165692	79573439
Bone marrow failure	41.24	38.93	31	5226	51076	79688055
White blood cell count decreased	39.46	38.93	55	5202	188233	79550898
Neutropenia	39.31	38.93	69	5188	287641	79451490

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

Source	Code	Description
ATC	L01EX13	ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS ANTINEOPLASTIC AGENTS PROTEIN KINASE INHIBITORS Other protein kinase inhibitors
CHEBI has role	CHEBI:35610	antineoplastic agents
CHEBI has role	CHEBI:62434	ALK inhibitor
CHEBI has role	CHEBI:68495	Type I cell-death inducers

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	11.78	acidic
pKa2	8.76	Basic
pKa3	5.0	Basic
pKa4	4.38	Basic
pKa5	3.81	Basic
pKa6	0.35	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 40MG BASE	XOSPATA	ASTELLAS	N211349	Nov. 28, 2018	RX	TABLET	ORAL	9487491	July 28, 2030	TREATMENT OF ACUTE MYELOID LEUKEMIA (AML)

Orange Book exclusivity data (new drug applications)

Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Exclusivity date	Description
EQ 40MG BASE	XOSPATA	ASTELLAS	N211349	Nov. 28, 2018	RX	TABLET	ORAL	Nov. 28, 2023	NEW CHEMICAL ENTITY
EQ 40MG BASE	XOSPATA	ASTELLAS	N211349	Nov. 28, 2018	RX	TABLET	ORAL	Nov. 28, 2025	INDICATED FOR THE TREATMENT OF ADULT PATIENTS WHO HAVE RELAPSED OR REFRACTORY ACUTE MYELOID LEUKEMIA (AML) WITH A FMS-LIKE TYROSINE KINASE 3 (FLT3) MUTATION AS DETECTED BY AN FDA-APPROVED TEST

Bioactivity Summary:

Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Mechanism action	Bioact source	MoA source
Receptor-type tyrosine-protein kinase FLT3	Kinase	P36888	FLT3_HUMAN	INHIBITOR	IC50	8.30		SCIENTIFIC LITERATURE	DRUG LABEL
Ribosyldihydronicotinamide dehydrogenase [quinone]	Enzyme	P16083	NQO2_HUMAN		Kd	5.77		CHEMBL
Platelet-derived growth factor receptor beta	Kinase	P09619	PGFRB_HUMAN		Kd	6.29		CHEMBL
Epidermal growth factor receptor	Kinase	P00533	EGFR_HUMAN		Kd	5.46		CHEMBL
ADP/ATP translocase 2	Enzyme	P05141	ADT2_HUMAN		Kd	6.35		CHEMBL
ADP/ATP translocase 3	Enzyme	P12236	ADT3_HUMAN		Kd	6.30		CHEMBL
Tyrosine-protein kinase Yes	Kinase	P07947	YES_HUMAN		Kd	6.35		CHEMBL
Proto-oncogene tyrosine-protein kinase receptor Ret	Kinase	P07949	RET_HUMAN		IC50	8.47		CHEMBL
Ribosomal protein S6 kinase alpha-3	Kinase	P51812	KS6A3_HUMAN		Kd	5.58		CHEMBL
Phosphorylase b kinase gamma catalytic chain, liver/testis isoform	Kinase	P15735	PHKG2_HUMAN		Kd	7.32		CHEMBL
Myosin light chain kinase, smooth muscle	Kinase	Q15746	MYLK_HUMAN		Kd	6.73		CHEMBL
Mitogen-activated protein kinase 8	Kinase	P45983	MK08_HUMAN		Kd	6.13		CHEMBL
Tyrosine-protein kinase HCK	Kinase	P08631	HCK_HUMAN		Kd	5.80		CHEMBL
Mitogen-activated protein kinase 10	Kinase	P53779	MK10_HUMAN		Kd	6.29		CHEMBL
High affinity nerve growth factor receptor	Kinase	P04629	NTRK1_HUMAN	INHIBITOR	IC50	8.96		IUPHAR
Protein kinase C alpha type	Kinase	P17252	KPCA_HUMAN		Kd	6.23		CHEMBL
Tyrosine-protein kinase SYK	Kinase	P43405	KSYK_HUMAN		Kd	5.39		CHEMBL
Calcium/calmodulin-dependent protein kinase type II subunit delta	Kinase	Q13557	KCC2D_HUMAN		Kd	6.68		CHEMBL
Calcium/calmodulin-dependent protein kinase type II subunit gamma	Kinase	Q13555	KCC2G_HUMAN		Kd	6.77		CHEMBL
AP2-associated protein kinase 1	Kinase	Q2M2I8	AAK1_HUMAN		Kd	7.60		CHEMBL
Serine/threonine-protein kinase Nek2	Kinase	P51955	NEK2_HUMAN		Kd	6.61		CHEMBL
Serine/threonine-protein kinase 10	Kinase	O94804	STK10_HUMAN		Kd	6.83		CHEMBL
Tyrosine-protein kinase Fer	Kinase	P16591	FER_HUMAN		Kd	6.73		CHEMBL
Serine/threonine-protein kinase PLK4	Kinase	O00444	PLK4_HUMAN		Kd	7.75		CHEMBL
Serine/threonine-protein kinase 16	Kinase	O75716	STK16_HUMAN		Kd	6.53		CHEMBL
Aurora kinase A	Kinase	O14965	AURKA_HUMAN		Kd	6.74		CHEMBL
Serine/threonine-protein kinase 26	Kinase	Q9P289	STK26_HUMAN		Kd	5.94		CHEMBL
ALK tyrosine kinase receptor	Kinase	Q9UM73	ALK_HUMAN		IC50	8.82		CHEMBL
BMP-2-inducible protein kinase	Kinase	Q9NSY1	BMP2K_HUMAN		Kd	7.34		CHEMBL
Mitogen-activated protein kinase kinase kinase kinase 5	Kinase	Q9Y4K4	M4K5_HUMAN		Kd	5.51		CHEMBL
Cyclin-G-associated kinase	Kinase	O14976	GAK_HUMAN		Kd	8.05		CHEMBL
Receptor-interacting serine/threonine-protein kinase 2	Kinase	O43353	RIPK2_HUMAN		Kd	6.32		CHEMBL
Activated CDC42 kinase 1	Kinase	Q07912	ACK1_HUMAN		Kd	5.50		CHEMBL
Ephrin type-A receptor 7	Kinase	Q15375	EPHA7_HUMAN		Kd	5.53		CHEMBL
STE20-like serine/threonine-protein kinase	Kinase	Q9H2G2	SLK_HUMAN		Kd	7.17		CHEMBL
Mitogen-activated protein kinase 9	Kinase	P45984	MK09_HUMAN		Kd	6.37		CHEMBL
Calcium/calmodulin-dependent protein kinase kinase 2	Kinase	Q96RR4	KKCC2_HUMAN		Kd	5.58		CHEMBL
Activin receptor type-1	Kinase	Q04771	ACVR1_HUMAN		Kd	7.41		CHEMBL
Dual specificity mitogen-activated protein kinase kinase 1	Kinase	Q02750	MP2K1_HUMAN		Kd	5.56		CHEMBL
Dual specificity mitogen-activated protein kinase kinase 2	Kinase	P36507	MP2K2_HUMAN		Kd	6.30		CHEMBL
Tyrosine-protein kinase receptor UFO	Kinase	P30530	UFO_HUMAN	INHIBITOR	IC50	9.10		IUPHAR
Non-receptor tyrosine-protein kinase TNK1	Kinase	Q13470	TNK1_HUMAN		Kd	7.41		CHEMBL
Protein-tyrosine kinase 2-beta	Kinase	Q14289	FAK2_HUMAN		Kd	6.29		CHEMBL
Casein kinase II subunit alpha'	Kinase	P19784	CSK22_HUMAN		Kd	6.02		CHEMBL
Inhibitor of nuclear factor kappa-B kinase subunit epsilon	Kinase	Q14164	IKKE_HUMAN		Kd	5.83		CHEMBL
Interleukin-1 receptor-associated kinase 3	Kinase	Q9Y616	IRAK3_HUMAN		Kd	8.15		CHEMBL
Serine/threonine-protein kinase LATS1	Kinase	O95835	LATS1_HUMAN		Kd	6.66		CHEMBL
Leukocyte tyrosine kinase receptor	Kinase	P29376	LTK_HUMAN	INHIBITOR	IC50	9.70		IUPHAR
Mitogen-activated protein kinase kinase kinase kinase 1	Kinase	Q92918	M4K1_HUMAN		Kd	6.97		CHEMBL
Mitogen-activated protein kinase kinase kinase kinase 3	Kinase	Q8IVH8	M4K3_HUMAN		Kd	6.22		CHEMBL
Bone morphogenetic protein receptor type-1A	Kinase	P36894	BMR1A_HUMAN		Kd	6.92		CHEMBL
Mitogen-activated protein kinase kinase kinase kinase 4	Kinase	O95819	M4K4_HUMAN		Kd	6.70		CHEMBL
Dual specificity mitogen-activated protein kinase kinase 6	Kinase	P52564	MP2K6_HUMAN		Kd	5.72		CHEMBL
Tyrosine-protein kinase Mer	Kinase	Q12866	MERTK_HUMAN	INHIBITOR	IC50	8.52		IUPHAR
Calcium/calmodulin-dependent protein kinase type IV	Kinase	Q16566	KCC4_HUMAN		Kd	6.38		CHEMBL
Mitogen-activated protein kinase kinase kinase 11	Kinase	Q16584	M3K11_HUMAN		Kd	6.22		CHEMBL
Serine/threonine-protein kinase 24	Kinase	Q9Y6E0	STK24_HUMAN		Kd	6.64		CHEMBL
Citron Rho-interacting kinase	Kinase	O14578	CTRO_HUMAN		Kd	5.63		CHEMBL
Mitogen-activated protein kinase 15	Kinase	Q8TD08	MK15_HUMAN		Kd	6.58		CHEMBL
Proto-oncogene tyrosine-protein kinase ROS	Kinase	P08922	ROS1_HUMAN		IC50	8.72		CHEMBL
Ribosomal protein S6 kinase alpha-1	Kinase	Q15418	KS6A1_HUMAN		Kd	5.46		CHEMBL
Mitogen-activated protein kinase kinase kinase kinase 2	Kinase	Q12851	M4K2_HUMAN		Kd	6.61		CHEMBL
Interleukin-1 receptor-associated kinase 4	Kinase	Q9NWZ3	IRAK4_HUMAN		Kd	5.75		CHEMBL
Cyclin-dependent kinase 4	Kinase	P11802	CDK4_HUMAN		Kd	5.71		CHEMBL
Ephrin type-B receptor 6	Kinase	O15197	EPHB6_HUMAN		Kd	6.62		CHEMBL
Mitogen-activated protein kinase kinase kinase 2	Kinase	Q9Y2U5	M3K2_HUMAN		Kd	6.27		CHEMBL
Serine/threonine-protein kinase ULK3	Kinase	Q6PHR2	ULK3_HUMAN		Kd	8.22		CHEMBL
Bone morphogenetic protein receptor type-1B	Kinase	O00238	BMR1B_HUMAN		Kd	6.24		CHEMBL
Serine/threonine-protein kinase Nek3	Kinase	P51956	NEK3_HUMAN		Kd	5.55		CHEMBL
Serine/threonine-protein kinase TAO2	Kinase	Q9UL54	TAOK2_HUMAN		Kd	5.68		CHEMBL
Dual specificity mitogen-activated protein kinase kinase 5	Kinase	Q13163	MP2K5_HUMAN		Kd	5.69		CHEMBL
Receptor-interacting serine/threonine-protein kinase 3	Kinase	Q9Y572	RIPK3_HUMAN		Kd	5.88		CHEMBL
Mitotic checkpoint serine/threonine-protein kinase BUB1	Kinase	O43683	BUB1_HUMAN		Kd	6.72		CHEMBL
U5 small nuclear ribonucleoprotein 200 kDa helicase	Enzyme	O75643	U520_HUMAN		Kd	5.86		CHEMBL
Cytochrome c1, heme protein, mitochondrial	Enzyme	P08574	CY1_HUMAN		Kd	6.70		CHEMBL
Macrophage-stimulating protein receptor	Kinase	Q04912	RON_HUMAN		Kd	6.09		CHEMBL
Elongation factor Tu, mitochondrial	Enzyme	P49411	EFTU_HUMAN		Kd	6.33		CHEMBL
Actin-related protein 3	Unclassified	P61158	ARP3_HUMAN		Kd	5.26		CHEMBL
GTP-binding nuclear protein Ran	Enzyme	P62826	RAN_HUMAN		Kd	6.12		CHEMBL
Delta(24)-sterol reductase	Enzyme	Q15392	DHC24_HUMAN		Kd	6.37		CHEMBL
Rab-like protein 3	Enzyme	Q5HYI8	RABL3_HUMAN		Kd	5.32		CHEMBL
Uncharacterized protein FLJ45252	Unclassified	Q6ZSR9	YJ005_HUMAN		Kd	7.96		CHEMBL
Uncharacterized aarF domain-containing protein kinase 1	Kinase	Q86TW2	ADCK1_HUMAN		Kd	6.82		CHEMBL
TP53-regulating kinase	Kinase	Q96S44	PRPK_HUMAN		Kd	5.57		CHEMBL
Long-chain-fatty-acid--CoA ligase 5	Enzyme	Q9ULC5	ACSL5_HUMAN		Kd	6.68		CHEMBL
Multifunctional protein ADE2	Enzyme	P22234	PUR6_HUMAN		Kd	5.26		CHEMBL

External reference:

ID	Source
66D92MGC8M	UNII
1254053-84-3	SECONDARY_CAS_RN
C3896940	UMLSCUI
CHEBI:145372	CHEBI
C6F	PDB_CHEM_ID
CHEMBL3301622	ChEMBL_ID
49803313	PUBCHEM_CID
DB12141	DRUGBANK_ID
CHEMBL3301603	ChEMBL_ID
D10709	KEGG_DRUG
10048	INN_ID
8708	IUPHAR_LIGAND_ID
017854	NDDF
017855	NDDF
1217167001	SNOMEDCT_US
782974005	SNOMEDCT_US
782987004	SNOMEDCT_US
4038030	VANDF
2105806	RXNORM
299484	MMSL
35657	MMSL
35755	MMSL
d09076	MMSL
C000609080	MESH_SUPPLEMENTAL_RECORD_UI

Pharmaceutical products:

Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
Xospata	HUMAN PRESCRIPTION DRUG LABEL	1	0469-1425	TABLET	40 mg	ORAL	NDA	28 sections
Xospata	HUMAN PRESCRIPTION DRUG LABEL	1	0469-1425	TABLET	40 mg	ORAL	NDA	28 sections
Xospata	HUMAN PRESCRIPTION DRUG LABEL	1	0469-1425	TABLET	40 mg	ORAL	NDA	28 sections
Xospata	HUMAN PRESCRIPTION DRUG LABEL	1	0469-1425	TABLET	40 mg	ORAL	NDA	28 sections