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

Stem definition	Drug id	CAS RN
tyrosine kinase inhibitors	5280	901119-35-5

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: tavlesse fostamatinib fostamatinib disodium tavalisse R935788 R788	Fostamatinib is a tyrosine kinase inhibitor with demonstrated activity against spleen tyrosine kinase (SYK). The major metabolite of fostamatinib, R406, inhibits signal transduction of Fc-activating receptors and B-cell receptor. The fostamatinib metabolite R406 reduces antibody-mediated destruction of platelets. Molecular weight: 580.47 Formula: C23H26FN6O9P CLOGP: 1.56 LIPINSKI: 2 HAC: 15 HDO: 4 TPSA: 186.72 ALOGS: -4.05 ROTB: 10 Status: ONP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

tavlesse
fostamatinib
fostamatinib disodium
tavalisse
R935788
R788

Fostamatinib is a tyrosine kinase inhibitor with demonstrated activity against spleen tyrosine kinase (SYK). The major metabolite of fostamatinib, R406, inhibits signal transduction of Fc-activating receptors and B-cell receptor. The fostamatinib metabolite R406 reduces antibody-mediated destruction of platelets.

Molecular weight: 580.47
Formula: C23H26FN6O9P
CLOGP: 1.56
LIPINSKI: 2
HAC: 15
HDO: 4
TPSA: 186.72
ALOGS: -4.05
ROTB: 10

Status: ONP

Legend:
OFP - off patent
OFM - off market
ONP - on patent

Drug dosage:

Dose	Unit	Route
0.20	g	O

ADMET properties:

None

Approvals:

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Date	Agency	Company
April 17, 2018	FDA	RIGEL PHARMS INC
Dec. 23, 2022	PMDA	Kissei Pharmaceutical Co., Ltd.
Jan. 9, 2020	EMA	Instituto Grifols S.A.

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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
Platelet count decreased	88.42	44.43	31	352	116091	63372548
Platelet count	78.80	44.43	8	375	18	63488621

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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
Platelet count decreased	67.50	51.57	26	201	119691	34837013

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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
Platelet count	65.38	40.13	7	283	56	79744042
Platelet count decreased	62.24	40.13	24	266	194640	79549458

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FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

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Source	Code	Description
ATC	B02BX09	BLOOD AND BLOOD FORMING ORGANS ANTIHEMORRHAGICS VITAMIN K AND OTHER HEMOSTATICS Other systemic hemostatics

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

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Disease	Relation	SNOMED_ID	DOID
Immune thrombocytopenia	indication	2897005	DOID:1587
Chronic idiopathic thrombocytopenic purpura	indication	13172003

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🐶 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	1.54	acidic
pKa2	6.59	acidic
pKa3	5.0	Basic
pKa4	4.34	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 100MG BASE	TAVALISSE	RIGEL PHARMS INC	N209299	April 17, 2018	RX	TABLET	ORAL	9266912	Jan. 19, 2026	TREATMENT OF THROMBOCYTOPENIA IN ADULT PATIENTS WITH CHRONIC IMMUNE THROMBOCYTOPENIA (ITP) WHO HAVE HAD AN INSUFFICIENT RESPONSE TO A PREVIOUS TREATMENT
EQ 100MG BASE	TAVALISSE	RIGEL PHARMS INC	N209299	April 17, 2018	RX	TABLET	ORAL	7538108	March 28, 2026	TREATMENT OF THROMBOCYTOPENIA IN ADULT PATIENTS WITH CHRONIC IMMUNE THROMBOCYTOPENIA (ITP) WHO HAVE HAD AN INSUFFICIENT RESPONSE TO A PREVIOUS TREATMENT
EQ 100MG BASE	TAVALISSE	RIGEL PHARMS INC	N209299	April 17, 2018	RX	TABLET	ORAL	7989448	June 12, 2026	TREATMENT OF THROMBOCYTOPENIA IN ADULT PATIENTS WITH CHRONIC IMMUNE THROMBOCYTOPENIA (ITP) WHO HAVE HAD AN INSUFFICIENT RESPONSE TO A PREVIOUS TREATMENT
EQ 100MG BASE	TAVALISSE	RIGEL PHARMS INC	N209299	April 17, 2018	RX	TABLET	ORAL	8163902	June 17, 2026	TREATMENT OF THROMBOCYTOPENIA IN ADULT PATIENTS WITH CHRONIC IMMUNE THROMBOCYTOPENIA (ITP) WHO HAVE HAD AN INSUFFICIENT RESPONSE TO A PREVIOUS TREATMENT
EQ 100MG BASE	TAVALISSE	RIGEL PHARMS INC	N209299	April 17, 2018	RX	TABLET	ORAL	8912170	June 17, 2026	TREATMENT OF THROMBOCYTOPENIA IN ADULT PATIENTS WITH CHRONIC IMMUNE THROMBOCYTOPENIA (ITP) WHO HAVE HAD AN INSUFFICIENT RESPONSE TO A PREVIOUS TREATMENT
EQ 100MG BASE	TAVALISSE	RIGEL PHARMS INC	N209299	April 17, 2018	RX	TABLET	ORAL	9283238	June 17, 2026	TREATMENT OF THROMBOCYTOPENIA IN ADULT PATIENTS WITH CHRONIC IMMUNE THROMBOCYTOPENIA (ITP) WHO HAVE HAD AN INSUFFICIENT RESPONSE TO A PREVIOUS TREATMENT
EQ 100MG BASE	TAVALISSE	RIGEL PHARMS INC	N209299	April 17, 2018	RX	TABLET	ORAL	8951504	July 27, 2032	TREATMENT OF THROMBOCYTOPENIA IN ADULT PATIENTS WITH CHRONIC IMMUNE THROMBOCYTOPENIA (ITP) WHO HAVE HAD AN INSUFFICIENT RESPONSE TO A PREVIOUS TREATMENT
EQ 150MG BASE	TAVALISSE	RIGEL PHARMS INC	N209299	April 17, 2018	RX	TABLET	ORAL	9266912	Jan. 19, 2026	TREATMENT OF THROMBOCYTOPENIA IN ADULT PATIENTS WITH CHRONIC IMMUNE THROMBOCYTOPENIA (ITP) WHO HAVE HAD AN INSUFFICIENT RESPONSE TO A PREVIOUS TREATMENT
EQ 150MG BASE	TAVALISSE	RIGEL PHARMS INC	N209299	April 17, 2018	RX	TABLET	ORAL	7538108	March 28, 2026	TREATMENT OF THROMBOCYTOPENIA IN ADULT PATIENTS WITH CHRONIC IMMUNE THROMBOCYTOPENIA (ITP) WHO HAVE HAD AN INSUFFICIENT RESPONSE TO A PREVIOUS TREATMENT
EQ 150MG BASE	TAVALISSE	RIGEL PHARMS INC	N209299	April 17, 2018	RX	TABLET	ORAL	7989448	June 12, 2026	TREATMENT OF THROMBOCYTOPENIA IN ADULT PATIENTS WITH CHRONIC IMMUNE THROMBOCYTOPENIA (ITP) WHO HAVE HAD AN INSUFFICIENT RESPONSE TO A PREVIOUS TREATMENT

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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 100MG BASE	TAVALISSE	RIGEL PHARMS INC	N209299	April 17, 2018	RX	TABLET	ORAL	April 17, 2023	NEW CHEMICAL ENTITY
EQ 100MG BASE	TAVALISSE	RIGEL PHARMS INC	N209299	April 17, 2018	RX	TABLET	ORAL	April 17, 2025	FOR THE TREATMENT OF THROMBOCYTOPENIA IN ADULT PATIENTS WITH CHRONIC IMMUNE THROMBOCYTOPENIA (ITP) WHO HAVE HAD AN INSUFFICIENT RESPONSE TO A PREVIOUS TREATMENT
EQ 150MG BASE	TAVALISSE	RIGEL PHARMS INC	N209299	April 17, 2018	RX	TABLET	ORAL	April 17, 2023	NEW CHEMICAL ENTITY
EQ 150MG BASE	TAVALISSE	RIGEL PHARMS INC	N209299	April 17, 2018	RX	TABLET	ORAL	April 17, 2025	FOR THE TREATMENT OF THROMBOCYTOPENIA IN ADULT PATIENTS WITH CHRONIC IMMUNE THROMBOCYTOPENIA (ITP) WHO HAVE HAD AN INSUFFICIENT RESPONSE TO A PREVIOUS TREATMENT

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Bioactivity Summary:

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Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Bioact source	MoA source
Tyrosine-protein kinase SYK	Kinase	P43405	KSYK_HUMAN	INHIBITOR	IC50	7.39	SCIENTIFIC LITERATURE	DRUG LABEL
Tyrosine-protein kinase JAK3	Kinase	P52333	JAK3_HUMAN		Kd	7.44	CHEMBL
Macrophage-stimulating protein receptor	Kinase	Q04912	RON_HUMAN		Kd	6.33	CHEMBL
ATP-binding cassette sub-family G member 2	Transporter	Q9UNQ0	ABCG2_HUMAN		IC50	7.30	CHEMBL
Platelet-derived growth factor receptor beta	Kinase	P09619	PGFRB_HUMAN		Kd	8.48	CHEMBL
Tyrosine-protein kinase ABL1	Kinase	P00519	ABL1_HUMAN		Kd	6.77	CHEMBL
Mast/stem cell growth factor receptor Kit	Kinase	P10721	KIT_HUMAN		Kd	8.60	CHEMBL
Epidermal growth factor receptor	Kinase	P00533	EGFR_HUMAN		Kd	7.21	CHEMBL
Proto-oncogene tyrosine-protein kinase Src	Kinase	P12931	SRC_HUMAN		Kd	8.08	CHEMBL
Tyrosine-protein kinase Lck	Kinase	P06239	LCK_HUMAN		Kd	7.52	CHEMBL

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External reference:

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ID	Source
2RC	PDB_CHEM_ID
017516	NDDF
017517	NDDF
11213558	PUBCHEM_CID
11671467	PUBCHEM_CID
2044896	RXNORM
276522	MMSL
4037543	VANDF
5706	IUPHAR_LIGAND_ID
772033003	SNOMEDCT_US

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Pharmaceutical products:

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Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
TAVALISSE	HUMAN PRESCRIPTION DRUG LABEL	1	71332-001	TABLET	100 mg	ORAL	NDA	28 sections
TAVALISSE	HUMAN PRESCRIPTION DRUG LABEL	1	71332-001	TABLET	100 mg	ORAL	NDA	28 sections
TAVALISSE	HUMAN PRESCRIPTION DRUG LABEL	1	71332-002	TABLET	150 mg	ORAL	NDA	28 sections
TAVALISSE	HUMAN PRESCRIPTION DRUG LABEL	1	71332-002	TABLET	150 mg	ORAL	NDA	28 sections

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