Pacritinib

Kinase Inhibitor — ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS

Key facts

Pacritinib is an onp drug in the Kinase Inhibitor class catalogued in DrugCentral. It was first approved by the FDA in 2022. Its mechanism of action is classified as Breast Cancer Resistance Protein Inhibitors, Cytochrome P450 1A2 Inhibitors and Cytochrome P450 3A4 Inhibitors. DrugCentral lists 49 molecular targets, including JAK2, STK11 and FLT3. Recorded indications include Myelofibrosis.

• Approval status: onp (first approved 2022 by the FDA).
• Drug class: Kinase Inhibitor.
• Mechanism of action: Breast Cancer Resistance Protein Inhibitors; Cytochrome P450 1A2 Inhibitors; Cytochrome P450 3A4 Inhibitors.
• Molecular targets: JAK2, STK11, FLT3 and NQO2 (49 listed in DrugCentral).
• Indications: Myelofibrosis.
• ATC code: L01EJ03 (Janus-associated kinase (JAK) inhibitors).
• Molecular formula: C28H32N4O3; molecular weight 472.59 g/mol.

Indications & contraindications

Drug–disease relationships curated by DrugCentral (OMOP / SNOMED concepts).

Indications (1)

• Myelofibrosis

Contraindications (1)

• Drug inhibition of cytochrome p450 CYP3A enzyme

Mechanism & targets

• Mechanism of action (MoA): Breast Cancer Resistance Protein Inhibitors; Cytochrome P450 1A2 Inhibitors; Cytochrome P450 3A4 Inhibitors; Janus Kinase Inhibitors; Organic Cation Transporter 1 Inhibitors; P-Glycoprotein Inhibitors; Tyrosine Kinase Inhibitors
• Established pharmacologic class: Kinase Inhibitor

Molecular targets (49)

Target	Gene	Action	Activity
Tyrosine-protein kinase JAK2	JAK2	inhibitor	IC50 9.00
Serine/threonine-protein kinase STK11	STK11	unknown	Kd 8.52
Receptor-type tyrosine-protein kinase FLT3	FLT3	inhibitor	IC50 8.52
Ribosyldihydronicotinamide dehydrogenase [quinone]	NQO2	unknown	Kd 8.40
Activin receptor type-1	ACVR1	unknown	Kd 7.66
Uncharacterized aarF domain-containing protein kinase 1	ADCK1	unknown	Kd 7.48
Interleukin-1 receptor-associated kinase 3	IRAK3	unknown	Kd 7.46
Non-receptor tyrosine-protein kinase TYK2	TYK2	unknown	Kd 7.42
BMP-2-inducible protein kinase	BMP2K	unknown	Kd 7.41
Macrophage colony-stimulating factor 1 receptor	CSF1R	unknown	IC50 7.40
AP2-associated protein kinase 1	AAK1	unknown	Kd 7.38
Uncharacterized protein FLJ45252	—	unknown	Kd 7.28
TRAF2 and NCK-interacting protein kinase	TNIK	unknown	Kd 7.05
Dual specificity protein kinase CLK1	CLK1	unknown	Kd 6.86
Mitogen-activated protein kinase kinase kinase kinase 1	MAP4K1	unknown	Kd 6.80
Interleukin-1 receptor-associated kinase 1	IRAK1	unknown	Kd 6.59
Serine/threonine-protein kinase ICK	ICK	unknown	Kd 6.57
Mitogen-activated protein kinase kinase kinase kinase 4	MAP4K4	unknown	Kd 6.53
Casein kinase II subunit alpha'	CSNK2A2	unknown	Kd 6.41
Tyrosine-protein kinase JAK3	JAK3	inhibitor	IC50 6.28

Regulatory approvals (1)

Date	Agency	Marketed as	Applicant	Orphan
2022-03-18	FDA	—	MARINUS PHARMA INC	Yes

ATC classification

ATC code	Therapeutic hierarchy
L01EJ03	ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS › ANTINEOPLASTIC AGENTS › PROTEIN KINASE INHIBITORS › Janus-associated kinase (JAK) inhibitors

Reported adverse-event signals

Strongest FDA FAERS disproportionality signals (log-likelihood ratio). A signal is a statistical association in spontaneous reports, not proof that the drug causes the event.

MedDRA term	LLR
Death	149.6
Platelet count decreased	121.9
Platelet count abnormal	92.0
Off label use	69.6
Haemoglobin decreased	68.2
Haemoglobin abnormal	63.9
Diarrhoea	51.8
Splenomegaly	50.1

Chemical structure

• Molecular formula: C₂₈H₃₂N₄O₃
• Molecular weight: 472.59 g/mol
• CAS number: 937272-79-2
• InChIKey: HWXVIOGONBBTBY-ONEGZZNKSA-N
• PubChem CID: 46216796

C(CN1CCCC1)OC1=CC=C2C=C1COC\C=C\COCC1=CC=CC(=C1)C1=CC=N\C(N1)=N\2

Frequently asked questions

Answers are generated from the structured data on this page, not written by hand.

What is Pacritinib used for?

DrugCentral lists the following indications for Pacritinib: Myelofibrosis.

How does Pacritinib work?

Pacritinib is classified as Breast Cancer Resistance Protein Inhibitors, Cytochrome P450 1A2 Inhibitors and Cytochrome P450 3A4 Inhibitors; its molecular targets in DrugCentral include JAK2 (inhibitor), STK11, FLT3 (inhibitor) and NQO2.

When was Pacritinib first approved?

Pacritinib was first approved by the FDA in 2022.

What drug class does Pacritinib belong to?

Pacritinib is in the Kinase Inhibitor class.

What is the chemical formula of Pacritinib?

Pacritinib has the molecular formula C28H32N4O3 and a molecular weight of 472.59 g/mol.

Sources

• DrugCentral drug card 5507 — structure, indications, targets, approvals, pharmacologic classes (CC BY-SA 4.0)
• ChEMBL CHEMBL2035187 — compound record and bioactivity
• PubChem CID 46216796 — chemical identifiers
• DrugBank DB11697 — drug record
• FDA UNII G22N65IL3O — substance identity
• DailyMed: FDA labels for Pacritinib — current prescribing information (label search)
• UniProt O60674 (JAK2) — target protein
• UniProt Q15831 (STK11) — target protein
• UniProt P36888 (FLT3) — target protein
• UniProt P16083 (NQO2) — target protein
• UniProt Q04771 (ACVR1) — target protein
• UniProt Q86TW2 (ADCK1) — target protein
• FDA Adverse Event Reporting System (openFDA FAERS) — adverse-event signals, as aggregated by DrugCentral

How this page is built: methodology · editorial policy & corrections.