Defactinib

Kinase Inhibitor

Key facts

Defactinib is a drug in the Kinase Inhibitor class catalogued in DrugCentral. It was first approved by the FDA in 2025. Its mechanism of action is classified as Focal Adhesion Kinase Inhibitors, Proline-rich Tyrosine Kinase 2 Inhibitors and UGT1A1 Inhibitors. DrugCentral lists 49 molecular targets, including PTK2, PTK2B and CDKL5. Recorded indications include Ovarian cancer.

• Drug class: Kinase Inhibitor.
• Mechanism of action: Focal Adhesion Kinase Inhibitors; Proline-rich Tyrosine Kinase 2 Inhibitors; UGT1A1 Inhibitors.
• Molecular targets: PTK2, PTK2B, CDKL5 and NTRK1 (49 listed in DrugCentral).
• Indications: Ovarian cancer.

Indications & contraindications

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

Indications (1)

• Ovarian cancer

Mechanism & targets

• Mechanism of action (MoA): Focal Adhesion Kinase Inhibitors; Proline-rich Tyrosine Kinase 2 Inhibitors; UGT1A1 Inhibitors
• Established pharmacologic class: Kinase Inhibitor

Molecular targets (49)

Target	Gene	Action	Activity
Focal adhesion kinase 1	PTK2	inhibitor	IC50 9.22
Protein-tyrosine kinase 2-beta	PTK2B	inhibitor	IC50 9.22
Cyclin-dependent kinase-like 5	CDKL5	unknown	Kd 7.80
High affinity nerve growth factor receptor	NTRK1	unknown	IC50 7.58
Adenosine receptor A3	ADORA3	unknown	Ki 7.57
Tyrosine-protein kinase JAK2	JAK2	unknown	IC50 7.55
BDNF/NT-3 growth factors receptor	NTRK2	unknown	IC50 7.26
NT-3 growth factor receptor	NTRK3	unknown	IC50 7.24
Mitogen-activated protein kinase kinase kinase 9	MAP3K9	unknown	IC50 7.12
Tyrosine-protein kinase JAK3	JAK3	unknown	IC50 6.94
Non-receptor tyrosine-protein kinase TYK2	TYK2	unknown	IC50 6.89
Vascular endothelial growth factor receptor 2	KDR	unknown	IC50 6.56
Receptor-type tyrosine-protein kinase FLT3	FLT3	unknown	Kd 6.47
Adenosine receptor A2a	ADORA2A	unknown	Ki 6.43
NUAK family SNF1-like kinase 2	NUAK2	unknown	Kd 6.34
Aurora kinase A	AURKA	unknown	Kd 6.21
Cyclin-dependent kinase 12	CDK12	unknown	Kd 6.14
Maternal embryonic leucine zipper kinase	MELK	unknown	Kd 6.05
Serine/threonine-protein kinase 16	STK16	unknown	Kd 6.05
Mitogen-activated protein kinase kinase kinase 11	MAP3K11	unknown	Kd 6.04

Regulatory approvals (1)

Date	Agency	Marketed as	Applicant	Orphan
2025-05-08	FDA	—	Verastem Oncology

Chemical structure

• Molecular formula: —
• Molecular weight: —
• CAS number: —
• InChIKey: —
• PubChem CID: 25117126

Frequently asked questions

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

What is Defactinib used for?

DrugCentral lists the following indications for Defactinib: Ovarian cancer.

How does Defactinib work?

Defactinib is classified as Focal Adhesion Kinase Inhibitors, Proline-rich Tyrosine Kinase 2 Inhibitors and UGT1A1 Inhibitors; its molecular targets in DrugCentral include PTK2 (inhibitor), PTK2B (inhibitor), CDKL5 and NTRK1.

When was Defactinib first approved?

Defactinib was first approved by the FDA in 2025.

What drug class does Defactinib belong to?

Defactinib is in the Kinase Inhibitor class.

Sources

• DrugCentral drug card 5771 — structure, indications, targets, approvals, pharmacologic classes (CC BY-SA 4.0)
• ChEMBL CHEMBL3137305 — compound record and bioactivity
• PubChem CID 25117126 — chemical identifiers
• DrugBank DB12282 — drug record
• FDA UNII 53O87HA2QU — substance identity
• DailyMed: FDA labels for Defactinib — current prescribing information (label search)
• UniProt Q05397 (PTK2) — target protein
• UniProt Q14289 (PTK2B) — target protein
• UniProt O76039 (CDKL5) — target protein
• UniProt P04629 (NTRK1) — target protein
• UniProt P0DMS8 (ADORA3) — target protein
• UniProt O60674 (JAK2) — target protein

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