Ponatinib

Kinase Inhibitor — ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS

Key facts

Ponatinib is an onp drug in the Kinase Inhibitor class catalogued in DrugCentral. It was first approved by the FDA in 2012. Its mechanism of action is classified as Protein Kinase Inhibitors. DrugCentral lists 74 molecular targets, including LYN, FLT3 and ABL1. Recorded indications include Chronic myeloid leukemia and Philadelphia chromosome-positive acute lymphoblastic leukemia.

• Approval status: onp (first approved 2012 by the FDA).
• Drug class: Kinase Inhibitor.
• Mechanism of action: Protein Kinase Inhibitors.
• Molecular targets: LYN, FLT3, ABL1 and ABL1|BCR (74 listed in DrugCentral).
• Indications: Chronic myeloid leukemia and Philadelphia chromosome-positive acute lymphoblastic leukemia.
• ATC code: L01EA05 (BCR-ABL tyrosine kinase inhibitors).
• Molecular formula: C29H27F3N6O; molecular weight 532.57 g/mol.

Indications & contraindications

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

Indications (2)

• Chronic myeloid leukemia
• Philadelphia chromosome-positive acute lymphoblastic leukemia

Mechanism & targets

• Mechanism of action (MoA): Protein Kinase Inhibitors
• Established pharmacologic class: Kinase Inhibitor

Molecular targets (74)

Target	Gene	Action	Activity
Tyrosine-protein kinase Lyn	LYN	inhibitor	IC50 9.62
Receptor-type tyrosine-protein kinase FLT3	FLT3	unknown	IC50 9.52
Tyrosine-protein kinase ABL1	ABL1	inhibitor	IC50 9.43
Bcr/Abl fusion protein	ABL1|BCR	unknown	IC50 9.30
Proto-oncogene tyrosine-protein kinase Src	SRC	unknown	IC50 9.05
Platelet-derived growth factor receptor alpha	PDGFRA	inhibitor	IC50 8.96
Platelet-derived growth factor receptor beta	PDGFRB	unknown	IC50 8.92
Fibroblast growth factor receptor 2	FGFR2	unknown	IC50 8.89
Vascular endothelial growth factor receptor 2	KDR	inhibitor	IC50 8.82
Receptor-interacting serine/threonine-protein kinase 3	RIPK3	inhibitor	Ki 8.80
Fibroblast growth factor receptor 1	FGFR1	inhibitor	IC50 8.66
Proto-oncogene tyrosine-protein kinase Src	SRC	unknown	IC50 8.52
Vascular endothelial growth factor receptor 1	FLT1	unknown	IC50 8.43
Tyrosine-protein kinase CSK	CSK	inhibitor	IC50 8.27
Receptor-interacting serine/threonine-protein kinase 2	RIPK2	unknown	IC50 8.17
Cyclin-dependent kinase 8	CDK8	inhibitor	Kd 8.17
Fibroblast growth factor receptor 4	FGFR4	unknown	IC50 8.15
Ephrin type-A receptor 5	EPHA5	unknown	Kd 8.10
Macrophage colony-stimulating factor 1 receptor	CSF1R	unknown	IC50 8.07
Fibroblast growth factor receptor 3	FGFR3	unknown	IC50 8.03

Regulatory approvals (1)

Date	Agency	Marketed as	Applicant	Orphan
2012-12-14	FDA	—	ARIAD	Yes

ATC classification

ATC code	Therapeutic hierarchy
L01EA05	ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS › ANTINEOPLASTIC AGENTS › PROTEIN KINASE INHIBITORS › BCR-ABL tyrosine kinase inhibitors

Pharmacogenomics

Drug-label and guideline annotations from PharmGKB and CPIC.

• EMA label: ABL1, BCR · Testing Required
• FDA label: ABL1, BCR · Testing Required
• HCSC label: ABL1, BCR · Testing Required

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
Acute lymphocytic leukaemia recurrent	869.2
Drug resistance	462.6
Cytogenetic analysis abnormal	445.5
Death	440.1
Philadelphia chromosome positive	436.5
Blast crisis in myelogenous leukaemia	411.3
Chronic myeloid leukaemia recurrent	391.6
Neoplasm progression	344.9
Cytopenia	204.0
Blast cell crisis	198.3
Thrombocytopenia	181.8
Lipase increased	177.9

Chemical structure

Full physicochemical, ADMET and 3D-structure analysis of Ponatinib is on its molecule page.

• Molecular formula: C₂₉H₂₇F₃N₆O
• Molecular weight: 532.57 g/mol
• CAS number: 943319-70-8
• InChIKey: PHXJVRSECIGDHY-UHFFFAOYSA-N
• PubChem CID: 24826799

CN1CCN(CC2=CC=C(NC(=O)C3=CC=C(C)C(=C3)C#CC3=CN=C4C=CC=NN34)C=C2C(F)(F)F)CC1

Frequently asked questions

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

What is Ponatinib used for?

DrugCentral lists the following indications for Ponatinib: Chronic myeloid leukemia and Philadelphia chromosome-positive acute lymphoblastic leukemia.

How does Ponatinib work?

Ponatinib is classified as Protein Kinase Inhibitors; its molecular targets in DrugCentral include LYN (inhibitor), FLT3, ABL1 (inhibitor) and ABL1|BCR.

When was Ponatinib first approved?

Ponatinib was first approved by the FDA in 2012.

What drug class does Ponatinib belong to?

Ponatinib is in the Kinase Inhibitor class.

What is the chemical formula of Ponatinib?

Ponatinib has the molecular formula C29H27F3N6O and a molecular weight of 532.57 g/mol.

Sources

• DrugCentral drug card 4716 — structure, indications, targets, approvals, pharmacologic classes (CC BY-SA 4.0)
• ChEMBL CHEMBL1171837 — compound record and bioactivity
• PubChem CID 24826799 — chemical identifiers
• DrugBank DB08901 — drug record
• FDA UNII 4340891KFS — substance identity
• DailyMed: FDA labels for Ponatinib — current prescribing information (label search)
• UniProt P07948 (LYN) — target protein
• UniProt P36888 (FLT3) — target protein
• UniProt P00519 (ABL1) — target protein
• UniProt P16234 (PDGFRA) — target protein
• UniProt P09619 (PDGFRB) — target protein
• UniProt P21802 (FGFR2) — target protein
• FDA Adverse Event Reporting System (openFDA FAERS) — adverse-event signals, as aggregated by DrugCentral
• PharmGKB / CPIC — pharmacogenomic label annotations

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