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

Stem definition	Drug id	CAS RN
tyrosine kinase inhibitors	5343	1029044-16-3

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: pexidartinib pexidartinib hydrochloride PLX3397 CML-261 turalio	Pexidartinib is a small molecule tyrosine kinase inhibitor that targets colony stimulating factor 1 receptor (CSF1R), KIT proto-oncogene receptor tyrosine kinase (KIT), and FMS-like tyrosine kinase 3 (FLT3) harboring an internal tandem duplication (ITD) mutation. Overexpression of the CSF1R ligand promotes cell proliferation and accumulation in the synovium. In vitro, pexidartinib inhibited proliferation of cell lines dependent on CSF1R and ligand-induced autophosphorylation of CSF1R. Pexidartinib also inhibited the proliferation of a CSF1R dependent cell line in vivo. Molecular weight: 417.82 Formula: C20H15ClF3N5 CLOGP: 4.39 LIPINSKI: 0 HAC: 5 HDO: 2 TPSA: 66.49 ALOGS: -5.12 ROTB: 6 Status: ONP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

pexidartinib
pexidartinib hydrochloride
PLX3397
CML-261
turalio

Pexidartinib is a small molecule tyrosine kinase inhibitor that targets colony stimulating factor 1 receptor (CSF1R), KIT proto-oncogene receptor tyrosine kinase (KIT), and FMS-like tyrosine kinase 3 (FLT3) harboring an internal tandem duplication (ITD) mutation. Overexpression of the CSF1R ligand promotes cell proliferation and accumulation in the synovium. In vitro, pexidartinib inhibited proliferation of cell lines dependent on CSF1R and ligand-induced autophosphorylation of CSF1R. Pexidartinib also inhibited the proliferation of a CSF1R dependent cell line in vivo.

Molecular weight: 417.82
Formula: C20H15ClF3N5
CLOGP: 4.39
LIPINSKI: 0
HAC: 5
HDO: 2
TPSA: 66.49
ALOGS: -5.12
ROTB: 6

Status: ONP

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

Drug dosage:

Dose	Unit	Route
0.80	g	O

ADMET properties:

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Property	Value	Reference
BDDCS (Biopharmaceutical Drug Disposition Classification System)	2	Bocci G, Oprea TI, Benet LZ
S (Water solubility)	0.00 mg/mL	Bocci G, Oprea TI, Benet LZ

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Approvals:

Date	Agency	Company	Orphan
Aug. 2, 2019	FDA	DAIICHI SANKYO 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
Hair colour changes	310.98	42.51	53	1095	3074	63484800
Product dose omission issue	78.58	42.51	50	1098	234263	63253611
Periorbital swelling	64.27	42.51	14	1134	2904	63484970
Aspartate aminotransferase increased	53.52	42.51	28	1120	90249	63397625
Gamma-glutamyltransferase increased	50.41	42.51	20	1128	34011	63453863
Alanine aminotransferase increased	49.86	42.51	28	1120	103742	63384132
Blood alkaline phosphatase increased	42.66	42.51	19	1129	42948	63444926

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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
Hair colour changes	273.43	46.08	43	489	1834	34954565
Product dose omission issue	80.52	46.08	38	494	119673	34836726
No adverse event	65.80	46.08	21	511	22906	34933493

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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
Hair colour changes	218.19	41.91	37	687	4195	79739469
Product dose omission issue	64.10	41.91	35	689	247502	79496162
Aspartate aminotransferase increased	48.37	41.91	24	700	138617	79605047

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FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

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Source	Code	Description
ATC	L01EX15	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
FDA EPC	N0000175605	Kinase Inhibitor
FDA MoA	N0000020001	Tyrosine Kinase Inhibitors
FDA MoA	N0000020036	Colony Stimulating Factor Receptor Type 1 (CSF-1R) Inhibitors
FDA MoA	N0000175082	Kinase Inhibitors
FDA MoA	N0000182139	Cytochrome P450 2B6 Inhibitors
FDA MoA	N0000190118	Cytochrome P450 3A Inducers
FDA MoA	N0000191272	UGT1A1 Inhibitors

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

Disease	Relation	SNOMED_ID	DOID
Tenosynovial giant cell tumor	indication	128777004

🐶 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	11.65	acidic
pKa2	6.1	Basic
pKa3	2.77	Basic
pKa4	0.39	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 125MG BASE	TURALIO	DAIICHI SANKYO INC	N211810	Oct. 14, 2022	RX	CAPSULE	ORAL	8461169	April 19, 2028	TREATMENT OF ADULT PATIENTS WITH SYMPTOMATIC TENOSYNOVIAL GIANT CELL TUMOR (TGCT) ASSOCIATED WITH SEVERE MORBIDITY OR FUNCTIONAL LIMITATIONS AND NOT AMENABLE TO IMPROVEMENT WITH SURGERY
EQ 125MG BASE	TURALIO	DAIICHI SANKYO INC	N211810	Oct. 14, 2022	RX	CAPSULE	ORAL	9358235	June 8, 2033	TREATMENT OF ADULT PATIENTS WITH SYMPTOMATIC TENOSYNOVIAL GIANT CELL TUMOR (TGCT) ASSOCIATED WITH SEVERE MORBIDITY OR FUNCTIONAL LIMITATIONS AND NOT AMENABLE TO IMPROVEMENT WITH SURGERY
EQ 125MG BASE	TURALIO	DAIICHI SANKYO INC	N211810	Oct. 14, 2022	RX	CAPSULE	ORAL	10189833	May 5, 2036	TREATMENT OF ADULT PATIENTS WITH SYMPTOMATIC TENOSYNOVIAL GIANT CELL TUMOR (TGCT) ASSOCIATED WITH SEVERE MORBIDITY OR FUNCTIONAL LIMITATIONS AND NOT AMENABLE TO IMPROVEMENT WITH SURGERY
EQ 125MG BASE	TURALIO	DAIICHI SANKYO INC	N211810	Oct. 14, 2022	RX	CAPSULE	ORAL	10961240	July 24, 2038	TREATMENT OF ADULT PATIENTS WITH SYMPTOMATIC TENOSYNOVIAL GIANT CELL TUMOR (TGCT) ASSOCIATED WITH SEVERE MORBIDITY OR FUNCTIONAL LIMITATIONS AND NOT AMENABLE TO IMPROVEMENT WITH SURGERY
EQ 200MG BASE	TURALIO	DAIICHI SANKYO INC	N211810	Aug. 2, 2019	DISCN	CAPSULE	ORAL	8461169	April 19, 2028	TREATMENT OF ADULT PATIENTS WITH SYMPTOMATIC TENOSYNOVIAL GIANT CELL TUMOR (TGCT) ASSOCIATED WITH SEVERE MORBIDITY OR FUNCTIONAL LIMITATIONS AND NOT AMENABLE TO IMPROVEMENT WITH SURGERY
EQ 200MG BASE	TURALIO	DAIICHI SANKYO INC	N211810	Aug. 2, 2019	DISCN	CAPSULE	ORAL	9358235	June 8, 2033	TREATMENT OF ADULT PATIENTS WITH SYMPTOMATIC TENOSYNOVIAL GIANT CELL TUMOR (TGCT) ASSOCIATED WITH SEVERE MORBIDITY OR FUNCTIONAL LIMITATIONS AND NOT AMENABLE TO IMPROVEMENT WITH SURGERY
EQ 200MG BASE	TURALIO	DAIICHI SANKYO INC	N211810	Aug. 2, 2019	DISCN	CAPSULE	ORAL	10189833	May 5, 2036	TREATMENT OF ADULT PATIENTS WITH SYMPTOMATIC TENOSYNOVIAL GIANT CELL TUMOR (TGCT) ASSOCIATED WITH SEVERE MORBIDITY OR FUNCTIONAL LIMITATIONS AND NOT AMENABLE TO IMPROVEMENT WITH SURGERY
EQ 200MG BASE	TURALIO	DAIICHI SANKYO INC	N211810	Aug. 2, 2019	DISCN	CAPSULE	ORAL	10961240	July 24, 2038	TREATMENT OF ADULT PATIENTS WITH SYMPTOMATIC TENOSYNOVIAL GIANT CELL TUMOR (TGCT) ASSOCIATED WITH SEVERE MORBIDITY OR FUNCTIONAL LIMITATIONS AND NOT AMENABLE TO IMPROVEMENT WITH SURGERY

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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 125MG BASE	TURALIO	DAIICHI SANKYO INC	N211810	Oct. 14, 2022	RX	CAPSULE	ORAL	Aug. 2, 2024	NEW CHEMICAL ENTITY
EQ 125MG BASE	TURALIO	DAIICHI SANKYO INC	N211810	Oct. 14, 2022	RX	CAPSULE	ORAL	Aug. 2, 2026	FDA HAS NOT RECOGNIZED ORPHAN-DRUG EXCLUSIVITY (ODE) FOR THIS DRUG, BUT IT CONTAINS THE SAME ACTIVE MOIETY OR MOIETIES AS ANOTHER DRUG(S) THAT WAS ELIGIBLE FOR ODE, AND ALSO SHARES ODE-PROTECTED USE(S) OR INDICATION(S) WITH THAT DRUG(S). AN APPLICATION SEEKING APPROVAL FOR THE SAME ACTIVE MOIETY OR MOIETIES, INCLUDING AN ANDA THAT CITES THIS NDA AS ITS BASIS OF SUBMISSION, MAY NOT BE APPROVED FOR SUCH ODE-PROTECTED USE(S) AND INDICATION(S)
EQ 200MG BASE	TURALIO	DAIICHI SANKYO INC	N211810	Aug. 2, 2019	DISCN	CAPSULE	ORAL	Aug. 2, 2024	NEW CHEMICAL ENTITY
EQ 200MG BASE	TURALIO	DAIICHI SANKYO INC	N211810	Aug. 2, 2019	DISCN	CAPSULE	ORAL	Aug. 2, 2026	INDICATED FOR THE TREATMENT OF ADULT PATIENTS WITH SYMPTOMATIC TENOSYNOVIAL GIANT CELL TUMOR (TGCT) ASSOCIATED WITH SEVERE MORBIDITY OR FUNCTIONAL LIMITATIONS AND NOT AMENABLE TO IMPROVEMENT WITH SURGERY

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Bioactivity Summary:

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Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Bioact source	MoA source
Mast/stem cell growth factor receptor Kit	Kinase	P10721	KIT_HUMAN	INHIBITOR	IC50	7.56	SCIENTIFIC LITERATURE	SCIENTIFIC LITERATURE
Receptor-type tyrosine-protein kinase FLT3	Kinase	P36888	FLT3_HUMAN	INHIBITOR	IC50	6.79	SCIENTIFIC LITERATURE	SCIENTIFIC LITERATURE
Macrophage colony-stimulating factor 1 receptor	Kinase	P07333	CSF1R_HUMAN	INHIBITOR	IC50	7.88	SCIENTIFIC LITERATURE	SCIENTIFIC LITERATURE
Vascular endothelial growth factor receptor 2	Kinase	P35968	VGFR2_HUMAN	INHIBITOR	IC50	6.36	IUPHAR
Platelet-derived growth factor receptor alpha	Kinase	P16234	PGFRA_HUMAN		IC50	8.02	CHEMBL
AP2-associated protein kinase 1	Kinase	Q2M2I8	AAK1_HUMAN		Kd	4.86	CHEMBL
Protein kinase C theta type	Kinase	Q04759	KPCT_HUMAN		Kd	8.22	CHEMBL
Platelet-derived growth factor receptor beta	Kinase	P09619	PGFRB_HUMAN		IC50	7.44	CHEMBL
Aurora kinase B	Kinase	Q96GD4	AURKB_HUMAN		IC50	6.19	CHEMBL
Cyclin-dependent kinase 19	Kinase	Q9BWU1	CDK19_HUMAN	INHIBITOR	IC50	6.85	IUPHAR

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External reference:

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ID	Source
P30	PDB_CHEM_ID
018075	NDDF
018076	NDDF
10056	INN_ID
2040295-03-0	SECONDARY_CAS_RN
2183102	RXNORM
25151352	PUBCHEM_CID
321181	MMSL
37252	MMSL
4038623	VANDF

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Pharmaceutical products:

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Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
Turalio	HUMAN PRESCRIPTION DRUG LABEL	1	65597-402	CAPSULE	200 mg	ORAL	NDA	34 sections
Turalio	HUMAN PRESCRIPTION DRUG LABEL	1	65597-402	CAPSULE	200 mg	ORAL	NDA	34 sections
Turalio	HUMAN PRESCRIPTION DRUG LABEL	1	65597-407	CAPSULE	125 mg	ORAL	NDA	35 sections

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