FOSTAMATINIB DISODIUM

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Trade Names:	TAVALISSE
Synonyms:	Fostamatinib disodium Fostamatinib disodium salt hexahydrate R-788 SODIUM R788 SODIUM R-788 SODIUM HYDRATE R788 SODIUM HYDRATE R-935788 SODIUM R935788 SODIUM R-935788 SODIUM HYDRATE R935788 SODIUM HYDRATE Tavalisse
Status:	Approved (2018)
Entry Type:	Small molecule
Molecule Category:	Salt Prodrug
UNII:	86EEZ49YVB
Parent Compound:	FOSTAMATINIB

Structure


InChI Key	ZQGJCHHKJNSPMS-UHFFFAOYSA-L
Smile	COc1cc(Nc2ncc(F)c(Nc3ccc4c(n3)N(COP(=O)([O-])[O-])C(=O)C(C)(C)O4)n2)cc(OC)c1OC.O.O.O.O.O.O.[Na+].[Na+]
InChI	InChI=1S/C23H26FN6O9P.2Na.6H2O/c1-23(2)21(31)30(11-38-40(32,33)34)20-14(39-23)6-7-17(28-20)27-19-13(24)10-25-22(29-19)26-12-8-15(35-3)18(37-5)16(9-12)36-4;;;;;;;;/h6-10H,11H2,1-5H3,(H2,32,33,34)(H2,25,26,27,28,29);;;61H2/q;2+1;;;;;;/p-2

Physicochemical Descriptors

Property Name	Value
Molecular Formula	C23H36FN6Na2O15P
Molecular Weight	732.52
AlogP	3.09
Hydrogen Bond Acceptor	12.0
Hydrogen Bond Donor	4.0
Number of Rotational Bond	10.0
Polar Surface Area	186.72
Molecular species	ACID
Aromatic Rings	3.0
Heavy Atoms	40.0

Pharmacology

Action	Mechanism of Action	Reference
INHIBITOR	Tyrosine-protein kinase SYK inhibitor	FDA PubMed

Targets	EC50(nM)	IC50(nM)	Kd(nM)	Ki(nM)	Inhibition(%)
Enzyme Kinase Protein Kinase TK protein kinase group Tyrosine protein kinase Syk family	-	17	-	-	-
Enzyme Kinase Protein Kinase TK protein kinase group Tyrosine protein kinase VEGFR family	-	-	70	-	-

Indications

Mesh Heading	Maximum Phase	Mesh ID	Reference
Purpura, Thrombocytopenic, Idiopathic	4	D016553	FDA
Anemia, Hemolytic, Autoimmune	3	D000744	ClinicalTrials
Lymphoma	2	D008223	ClinicalTrials
Glomerulonephritis, IGA	2	D005922	ClinicalTrials
Arthritis, Rheumatoid	2	D001172	ClinicalTrials
Lupus Erythematosus, Systemic	2	D008180	ClinicalTrials

Related Entries

Scaffolds

Target Level :

Level 3

Level 4

Level 5

Level 6

Extend network:

Indication

Mechanism of Action

Primary Target

Target Level

Parent

Adverse Reactions

SOC By Demographic Distribution

System Organ Classification (SOC)

	Relative Frequency (%)
General disorders and administration site conditions	15.21
Gastrointestinal disorders	15.12
Injury, poisoning and procedural complications	13.41
Investigations	12.48
Nervous system disorders	8.25
Vascular disorders	7.5
Psychiatric disorders	3.85
Skin and subcutaneous tissue disorders	3.6
Cardiac disorders	3.27
Musculoskeletal and connective tissue disorders	3.23
Respiratory, thoracic and mediastinal disorders	3.02
Infections and infestations	2.89

Cross References

Resources	Reference
ChEMBL	CHEMBL3989516
FDA SRS	86EEZ49YVB
PubChem	24828759
SureChEMBL	SCHEMBL15110498

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