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

Stem definitionDrug idCAS RN
tyrosine kinase inhibitors 5507 937272-79-2

Description:

MoleculeDescription

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

Approvals:

DateAgencyCompanyOrphan
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)

None

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC L01EJ03 ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS
ANTINEOPLASTIC AGENTS
PROTEIN KINASE INHIBITORS
Janus-associated kinase (JAK) inhibitors
FDA MoA N0000020001 Tyrosine 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

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

DiseaseRelationSNOMED_IDDOID
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 strengthTrade nameApplicantApplication numberApproval dateTypeDose formRoutePatent numberPatent expiration datePatent use
EQ 100MG BASE VONJO CTI BIOPHARMA CORP N208712 Feb. 28, 2022 RX CAPSULE ORAL 9573964 May 5, 2028 TREATMENT OF MYELOFIBROSIS WITH PACRITINIB
EQ 100MG BASE VONJO CTI BIOPHARMA CORP 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 CTI BIOPHARMA CORP N208712 Feb. 28, 2022 RX CAPSULE ORAL 8153632 Jan. 17, 2029 TREATMENT OF MYELOFIBROSIS WITH PACRITINIB
EQ 100MG BASE VONJO CTI BIOPHARMA CORP 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 CTI BIOPHARMA CORP N208712 Feb. 28, 2022 RX CAPSULE ORAL 8980873 March 25, 2030 TREATMENT OF MYELOFIBROSIS WITH PACRITINIB
EQ 100MG BASE VONJO CTI BIOPHARMA CORP 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 strengthTrade nameApplicantApplication numberApproval dateTypeDose formRouteExclusivity dateDescription
EQ 100MG BASE VONJO CTI BIOPHARMA CORP N208712 Feb. 28, 2022 RX CAPSULE ORAL Feb. 28, 2027 NEW CHEMICAL ENTITY
EQ 100MG BASE VONJO CTI BIOPHARMA CORP 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:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])		Mechanism
action		Bioact sourceMoA source
Receptor-type tyrosine-protein kinase FLT3 Kinase INHIBITOR IC50 8.52 DRUG LABEL DRUG LABEL
Tyrosine-protein kinase JAK2 Kinase INHIBITOR IC50 9 DRUG LABEL DRUG LABEL
Platelet-derived growth factor receptor beta Kinase Kd 5.57 CHEMBL
Tyrosine-protein kinase Lck Kinase Kd 5.18 CHEMBL
Mitogen-activated protein kinase 8 Kinase Kd 5.71 CHEMBL
Tyrosine-protein kinase JAK1 Kinase INHIBITOR IC50 5.89 IUPHAR
Protein kinase C beta type Kinase Kd 5.14 CHEMBL
Protein kinase C alpha type Kinase Kd 6.03 CHEMBL
AP2-associated protein kinase 1 Kinase Kd 7.38 CHEMBL
Serine/threonine-protein kinase 10 Kinase Kd 5.54 CHEMBL
Tyrosine-protein kinase Fer Kinase Kd 5.44 CHEMBL
Serine/threonine-protein kinase 16 Kinase Kd 5.73 CHEMBL
TRAF2 and NCK-interacting protein kinase Kinase Kd 7.05 CHEMBL
BMP-2-inducible protein kinase Kinase Kd 7.41 CHEMBL
Dual specificity protein kinase CLK1 Kinase Kd 6.86 CHEMBL
Cyclin-G-associated kinase Kinase Kd 6.17 CHEMBL
Cyclin-dependent kinase 16 Kinase Kd 5.51 CHEMBL
Activated CDC42 kinase 1 Kinase Kd 5.03 CHEMBL
Calcium/calmodulin-dependent protein kinase kinase 2 Kinase Kd 5.11 CHEMBL
Epithelial discoidin domain-containing receptor 1 Kinase Kd 4.15 CHEMBL
Activin receptor type-1 Kinase Kd 7.66 CHEMBL
Cyclin-dependent kinase 9 Kinase Kd 6 CHEMBL
Glycogen synthase kinase-3 alpha Kinase Kd 5.29 CHEMBL
Non-receptor tyrosine-protein kinase TNK1 Kinase Kd 6.05 CHEMBL
Non-receptor tyrosine-protein kinase TYK2 Kinase Kd 7.42 CHEMBL
Mitogen-activated protein kinase kinase kinase MLT Kinase Kd 5.53 CHEMBL
Casein kinase II subunit alpha' Kinase Kd 6.41 CHEMBL
Inhibitor of nuclear factor kappa-B kinase subunit epsilon Kinase Kd 6.15 CHEMBL
LIM domain kinase 2 Kinase Kd 4.28 CHEMBL
Serine/threonine-protein kinase STK11 Kinase Kd 8.52 CHEMBL
Interleukin-1 receptor-associated kinase 3 Kinase Kd 7.46 CHEMBL
Mitogen-activated protein kinase kinase kinase kinase 1 Kinase Kd 6.80 CHEMBL
Aurora kinase B Kinase Kd 6.19 CHEMBL
Mitogen-activated protein kinase kinase kinase kinase 4 Kinase Kd 6.53 CHEMBL
Serine/threonine-protein kinase Nek9 Kinase Kd 5.75 CHEMBL
Mitogen-activated protein kinase kinase kinase kinase 2 Kinase Kd 5.43 CHEMBL
Serine/threonine-protein kinase TBK1 Kinase Kd 4.30 CHEMBL
Serine/threonine-protein kinase ICK Kinase Kd 6.57 CHEMBL
Interleukin-1 receptor-associated kinase 1 Kinase Kd 6.59 CHEMBL
Serine/threonine-protein kinase TAO1 Kinase Kd 5.66 CHEMBL
Serine/threonine-protein kinase TAO2 Kinase Kd 5.47 CHEMBL
Tyrosine-protein kinase JAK3 Kinase INHIBITOR IC50 6.28 IUPHAR
cGMP-dependent protein kinase 1 Kinase Kd 5.82 CHEMBL
Ferrochelatase, mitochondrial Enzyme Kd 4.17 CHEMBL
Uncharacterized protein FLJ45252 Unclassified Kd 7.28 CHEMBL
Uncharacterized aarF domain-containing protein kinase 1 Kinase Kd 7.48 CHEMBL
Ribosyldihydronicotinamide dehydrogenase [quinone] Enzyme Kd 8.40 CHEMBL
Tyrosine-protein kinase JAK2 Kinase IC50 5.97 CHEMBL

External reference:

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

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Vonjo HUMAN PRESCRIPTION DRUG LABEL 1 72482-100 CAPSULE 100 mg ORAL NDA 30 sections