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

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

Stem definition	Drug id	CAS RN
tyrosine kinase inhibitors	5507	937272-79-2

Description:

Molecule

Description

Molfile Inchi Smiles Synonyms: pacritinib pacritinib citrate vonjo SB1518 SB-1518

Pacritinib is a kinase inhibitor with activity against Janus-associated kinase 2 (JAK2) and Fms-like receptor tyrosine kinase 3 (FLT3). Pacritinib inhibits both wild-type JAK2 and the JAK2V617F mutant form that is common in patients with myeloproliferative neoplasms. Pacritinib also exhibits inhibitory activity against additional cellular kinases (such as colony-stimulating factor 1 and interleukin 1 receptor-associated kinase 1), the clinical relevance of which is unknown. Molecular weight: 472.59 Formula: C28H32N4O3 CLOGP: 2.84 LIPINSKI: 0 HAC: 7 HDO: 1 TPSA: 67.68 ALOGS: -5.31 ROTB: 4 Status: ONP Legend: OFP - off patent OFM - off market ONP - on patent

Drug dosage:

None

ADMET properties:

None

Predicted pharmacokinetic/toxicological properties (PK-AZ):

Property	Description	Value	Unit	Confidence	Similarity
kinase-safety-class	ACVR2B,ACVRL1,AKT2,AKT3,ALK,AURKA,AXL,BRAF,BTK,CAMK2B,CAMK2D,CDK5,CDK9,DDR1,DYRK1B,EGFR,EIF2AK3,EPHB4,ERBB2,FLT3,GAK,GRK2,GSK3B,INSR,ITK,JAK2,JAK3,KDR,KIT,MAP3K1,MAP3K21,MAP3K7,MAP4K1,MAP4K3,MAPK10,MAPK7,MAPKAPK2,MARK4,MELK,MET,NTRK2,PDK1,PDK2,PDK4,PDPK1,PIK3CA,PIK3CB,PIK3CD,PIK3CG,PIM2,PRKCD,PRKDC,SIK2,SIK3,STK33,SYK,TEK,TGFBR1,TTK	59
kinase-selectivity-class	AXL,CDK4,SIK2	3
pfas-class	PFAS structural alert (1 = True, 0 = False)	0

Approvals:

Date	Agency	Company	Orphan
March 18, 2022	FDA	MARINUS PHARMA INC

FDA Adverse Event Reporting System (Female)

None

FDA Adverse Event Reporting System (Male)

None

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
Off label use	98.94	56.12	61	321	1500124	109088793
Platelet count abnormal	90.01	56.12	16	366	6266	110582651
Haemoglobin abnormal	71.77	56.12	14	368	9024	110579893
Death	56.98	56.12	33	349	698836	109890081

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

Source	Code	Description
ATC	L01EJ03	ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS ANTINEOPLASTIC AGENTS PROTEIN KINASE INHIBITORS Janus-associated kinase (JAK) inhibitors
FDA MoA	N0000020001	Tyrosine Kinase Inhibitors
MeSH PA	D000075242	Janus Kinase Inhibitors
MeSH PA	D000092004	Tyrosine Kinase Inhibitors
MeSH PA	D000970	Antineoplastic Agents
MeSH PA	D004791	Enzyme Inhibitors
MeSH PA	D047428	Protein Kinase Inhibitors
FDA EPC	N0000175605	Kinase Inhibitor
FDA MoA	N0000182138	Cytochrome P450 1A2 Inhibitors
FDA MoA	N0000182141	Cytochrome P450 3A4 Inhibitors
FDA MoA	N0000185503	P-Glycoprotein Inhibitors
FDA MoA	N0000190113	Breast Cancer Resistance Protein Inhibitors
FDA MoA	N0000190857	Janus Kinase Inhibitors
FDA MoA	N0000191265	Organic Cation Transporter 1 Inhibitors
CHEBI has role	CHEBI:35610	antineoplastic agent
CHEBI has role	CHEBI:67079	anti-inflammatory agent
CHEBI has role	CHEBI:68495	apoptosis inducer
CHEBI has role	CHEBI:76617	EC 2.7.10.2 (non-specific protein-tyrosine kinase) inhibitor
CHEBI has role	CHEBI:233423	antifibrotic agent

Related Drugs by ATC class:

L01EJ Janus-associated kinase (JAK) inhibitors 3 drugs

fedratinibmomelotinibruxolitinib

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

Disease	Relation	SNOMED_ID	DOID
Myelofibrosis	indication	52967002	DOID:4971
Drug inhibition of cytochrome p450 CYP3A enzyme	contraindication	423819001

🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

None

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 100MG BASE	VONJO	SOBI	N208712	Feb. 28, 2022	RX	CAPSULE	ORAL	9573964	May 5, 2028	TREATMENT OF MYELOFIBROSIS WITH PACRITINIB
EQ 100MG BASE	VONJO	SOBI	N208712	Feb. 28, 2022	RX	CAPSULE	ORAL	9573964	May 5, 2028	USE OF PACRITINIB FOR INHIBITING JANUS ASSOCIATED KINASE 2(JAK2)
EQ 100MG BASE	VONJO	SOBI	N208712	Feb. 28, 2022	RX	CAPSULE	ORAL	8153632	Jan. 17, 2029	TREATMENT OF MYELOFIBROSIS WITH PACRITINIB
EQ 100MG BASE	VONJO	SOBI	N208712	Feb. 28, 2022	RX	CAPSULE	ORAL	8153632	Jan. 17, 2029	USE OF PACRITINIB FOR INHIBITING JANUS ASSOCIATED KINASE 2(JAK2)
EQ 100MG BASE	VONJO	SOBI	N208712	Feb. 28, 2022	RX	CAPSULE	ORAL	8980873	March 25, 2030	TREATMENT OF MYELOFIBROSIS WITH PACRITINIB
EQ 100MG BASE	VONJO	SOBI	N208712	Feb. 28, 2022	RX	CAPSULE	ORAL	8980873	March 25, 2030	USE OF PACRITINIB FOR INHIBITING JANUS ASSOCIATED KINASE 2(JAK2)

Orange Book exclusivity data (new drug applications)

Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Exclusivity date	Description
EQ 100MG BASE	VONJO	SOBI	N208712	Feb. 28, 2022	RX	CAPSULE	ORAL	Feb. 28, 2027	NEW CHEMICAL ENTITY
EQ 100MG BASE	VONJO	SOBI	N208712	Feb. 28, 2022	RX	CAPSULE	ORAL	Feb. 28, 2029	TREATMENT OF ADULTS WITH INTERMEDIATE OR HIGH-RISK PRIMARY OR SECONDARY (POST-POLYCYTHEMIA VERA OR POST-ESSENTIAL THROMBOCYTHEMIA) MYELOFIBROSIS (MF) WITH A PLATELET COUNT BELOW 50 X 10^9/L

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	8.52		DRUG LABEL	DRUG LABEL
Tyrosine-protein kinase JAK2	Kinase	O60674	JAK2_HUMAN	INHIBITOR	IC50	9		DRUG LABEL	DRUG LABEL
Ribosyldihydronicotinamide dehydrogenase [quinone]	Enzyme	P16083	NQO2_HUMAN		Kd	8.40		CHEMBL
Platelet-derived growth factor receptor beta	Kinase	P09619	PGFRB_HUMAN		Kd	5.57		CHEMBL
Tyrosine-protein kinase Lck	Kinase	P06239	LCK_HUMAN		Kd	5.18		CHEMBL
Mitogen-activated protein kinase 8	Kinase	P45983	MK08_HUMAN		Kd	5.71		CHEMBL
Tyrosine-protein kinase JAK1	Kinase	P23458	JAK1_HUMAN	INHIBITOR	IC50	5.89		IUPHAR
Protein kinase C beta type	Kinase	P05771	KPCB_HUMAN		Kd	5.14		CHEMBL
Protein kinase C alpha type	Kinase	P17252	KPCA_HUMAN		Kd	6.03		CHEMBL
AP2-associated protein kinase 1	Kinase	Q2M2I8	AAK1_HUMAN		Kd	7.38		CHEMBL
Serine/threonine-protein kinase 10	Kinase	O94804	STK10_HUMAN		Kd	5.54		CHEMBL
Tyrosine-protein kinase Fer	Kinase	P16591	FER_HUMAN		Kd	5.44		CHEMBL
Serine/threonine-protein kinase 16	Kinase	O75716	STK16_HUMAN		Kd	5.73		CHEMBL
TRAF2 and NCK-interacting protein kinase	Kinase	Q9UKE5	TNIK_HUMAN		Kd	7.05		CHEMBL
BMP-2-inducible protein kinase	Kinase	Q9NSY1	BMP2K_HUMAN		Kd	7.41		CHEMBL
Dual specificity protein kinase CLK1	Kinase	P49759	CLK1_HUMAN		Kd	6.86		CHEMBL
Cyclin-G-associated kinase	Kinase	O14976	GAK_HUMAN		Kd	6.17		CHEMBL
Cyclin-dependent kinase 16	Kinase	Q00536	CDK16_HUMAN		Kd	5.51		CHEMBL
Activated CDC42 kinase 1	Kinase	Q07912	ACK1_HUMAN		Kd	5.03		CHEMBL
Calcium/calmodulin-dependent protein kinase kinase 2	Kinase	Q96RR4	KKCC2_HUMAN		Kd	5.11		CHEMBL
Epithelial discoidin domain-containing receptor 1	Kinase	Q08345	DDR1_HUMAN		Kd	4.15		CHEMBL
Activin receptor type-1	Kinase	Q04771	ACVR1_HUMAN		Kd	7.66		CHEMBL
Cyclin-dependent kinase 9	Kinase	P50750	CDK9_HUMAN		Kd	6		CHEMBL
Glycogen synthase kinase-3 alpha	Kinase	P49840	GSK3A_HUMAN		Kd	5.29		CHEMBL
Non-receptor tyrosine-protein kinase TNK1	Kinase	Q13470	TNK1_HUMAN		Kd	6.05		CHEMBL
Non-receptor tyrosine-protein kinase TYK2	Kinase	P29597	TYK2_HUMAN		Kd	7.42		CHEMBL
Mitogen-activated protein kinase kinase kinase MLT	Kinase	Q9NYL2	MLTK_HUMAN		Kd	5.53		CHEMBL
Casein kinase II subunit alpha'	Kinase	P19784	CSK22_HUMAN		Kd	6.41		CHEMBL
Inhibitor of nuclear factor kappa-B kinase subunit epsilon	Kinase	Q14164	IKKE_HUMAN		Kd	6.15		CHEMBL
LIM domain kinase 2	Kinase	P53671	LIMK2_HUMAN		Kd	4.28		CHEMBL
Serine/threonine-protein kinase STK11	Kinase	Q15831	STK11_HUMAN		Kd	8.52		CHEMBL
Interleukin-1 receptor-associated kinase 3	Kinase	Q9Y616	IRAK3_HUMAN		Kd	7.46		CHEMBL
Mitogen-activated protein kinase kinase kinase kinase 1	Kinase	Q92918	M4K1_HUMAN		Kd	6.80		CHEMBL
Aurora kinase B	Kinase	Q96GD4	AURKB_HUMAN		Kd	6.19		CHEMBL
Mitogen-activated protein kinase kinase kinase kinase 4	Kinase	O95819	M4K4_HUMAN		Kd	6.53		CHEMBL
Serine/threonine-protein kinase Nek9	Kinase	Q8TD19	NEK9_HUMAN		Kd	5.75		CHEMBL
Mitogen-activated protein kinase kinase kinase kinase 2	Kinase	Q12851	M4K2_HUMAN		Kd	5.43		CHEMBL
Serine/threonine-protein kinase TBK1	Kinase	Q9UHD2	TBK1_HUMAN		Kd	4.30		CHEMBL
Serine/threonine-protein kinase ICK	Kinase	Q9UPZ9	ICK_HUMAN		Kd	6.57		CHEMBL
Interleukin-1 receptor-associated kinase 1	Kinase	P51617	IRAK1_HUMAN		Kd	6.59		CHEMBL
Serine/threonine-protein kinase TAO1	Kinase	Q7L7X3	TAOK1_HUMAN		Kd	5.66		CHEMBL
Serine/threonine-protein kinase TAO2	Kinase	Q9UL54	TAOK2_HUMAN		Kd	5.47		CHEMBL
Macrophage colony-stimulating factor 1 receptor	Kinase	P07333	CSF1R_HUMAN		IC50	7.40		CHEMBL
cGMP-dependent protein kinase 1	Kinase	Q13976	KGP1_HUMAN		Kd	5.82		CHEMBL
Ferrochelatase, mitochondrial	Enzyme	P22830	HEMH_HUMAN		Kd	4.17		CHEMBL
Uncharacterized protein FLJ45252	Unclassified	Q6ZSR9	YJ005_HUMAN		Kd	7.28		CHEMBL
Uncharacterized aarF domain-containing protein kinase 1	Kinase	Q86TW2	ADCK1_HUMAN		Kd	7.48		CHEMBL
Tyrosine-protein kinase JAK3	Kinase	P52333	JAK3_HUMAN	INHIBITOR	IC50	6.28		IUPHAR
Tyrosine-protein kinase JAK2	Kinase		JAK2_MOUSE		IC50	5.97		CHEMBL

External reference:

ID	Source
CHEBI:231350	CHEBI
6T3	PDB_CHEM_ID
CHEMBL2035187	ChEMBL_ID
C561234	MESH_SUPPLEMENTAL_RECORD_UI
7793	IUPHAR_LIGAND_ID
DB11697	DRUGBANK_ID
4041252	VANDF
C3467842	UMLSCUI
CHEMBL5095049	ChEMBL_ID
D04300	KEGG_DRUG
9385	INN_ID
1228923-42-9	SECONDARY_CAS_RN
46216796	PUBCHEM_CID
357763	MMSL
40530	MMSL
40560	MMSL
d09865	MMSL
018971	NDDF
018972	NDDF
G22N65IL3O	UNII
2595242	RXNORM
G22N65IL3O	INXIGHT DRUGS

Pharmaceutical products:

Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
Vonjo	HUMAN PRESCRIPTION DRUG LABEL	1	72482-100	CAPSULE	100 mg	ORAL	NDA	32 sections
Vonjo	HUMAN PRESCRIPTION DRUG LABEL	1	72482-100	CAPSULE	100 mg	ORAL	NDA	32 sections