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

Stem definitionDrug idCAS RN
tyrosine kinase inhibitors 5771 1073154-85-4

Description:

MoleculeDescription

Molfile

Synonyms:

  • defactinib
  • defactinib hydrochloride
  • VS-6063
  • PF-04554878
  • fakzynja
Defactinib is an inhibitor of focal adhesion kinase (FAK) and proline-rich tyrosine kinase 2 (PYK2). FAK and PYK2 are non-receptor tyrosine kinases that regulate cellular signaling pathways involved in cell proliferation, survival, migration, and invasion. Defactinib inhibited FAK autophosphorylation in cancer cells in vitro and in mouse xenograft models. Avutometinib in combination with defactinib enhanced inhibition of cell proliferation in vitro and antitumor activity in mouse tumor models including LGSOC.
  • Molecular weight: 510.50
  • Formula: C20H21F3N8O3S
  • CLOGP: 2.40
  • LIPINSKI: None
  • HAC: None
  • HDO: None
  • TPSA: 142.10
  • ALOGS:
  • ROTB: None

Drug dosage:

None

ADMET properties:

None

Predicted pharmacokinetic/toxicological properties (PK-AZ):

None

Approvals:

DateAgencyCompanyOrphan
May 8, 2025 FDA Verastem Oncology

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
FDA EPC N0000175605 Kinase Inhibitor
FDA MoA N0000191272 UGT1A1 Inhibitors
FDA MoA N0000194167 Focal Adhesion Kinase Inhibitors
FDA MoA N0000194169 Proline-rich Tyrosine Kinase 2 Inhibitors
CHEBI has role CHEBI:35610 antineoplastic agent

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

DiseaseRelationSNOMED_IDDOID
Ovarian cancer indication 363443007 DOID:2394




🐶 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 0.8MG BASE;EQ 200MG BASE AVMAPKI FAKZYNJA CO-PACK (COPACKAGED) VERASTEM INC N219616 May 8, 2025 RX CAPSULE, TABLET ORAL 11400090 Oct. 29, 2038 TREATMENT OF ADULT PATIENTS WITH KRAS-MUTATED RECURRENT LOW-GRADE SEROUS OVARIAN CANCER (LGSOC) WHO HAVE RECEIVED PRIOR SYSTEMIC THERAPY, IN COMBINATION WITH DEFACTINIB
EQ 0.8MG BASE;EQ 200MG BASE AVMAPKI FAKZYNJA CO-PACK (COPACKAGED) VERASTEM INC N219616 May 8, 2025 RX CAPSULE, TABLET ORAL 11517573 Sept. 11, 2040 TREATMENT OF ADULT PATIENTS WITH KRAS-MUTATED RECURRENT LOW-GRADE SEROUS OVARIAN CANCER (LGSOC) WHO HAVE RECEIVED PRIOR SYSTEMIC THERAPY, IN COMBINATION WITH AVUTOMETINIB
EQ 0.8MG BASE;EQ 200MG BASE AVMAPKI FAKZYNJA CO-PACK (COPACKAGED) VERASTEM INC N219616 May 8, 2025 RX CAPSULE, TABLET ORAL 11517573 Sept. 11, 2040 TREATMENT OF ADULT PATIENTS WITH KRAS-MUTATED RECURRENT LOW-GRADE SEROUS OVARIAN CANCER (LGSOC) WHO HAVE RECEIVED PRIOR SYSTEMIC THERAPY, IN COMBINATION WITH DEFACTINIB
EQ 0.8MG BASE;EQ 200MG BASE AVMAPKI FAKZYNJA CO-PACK (COPACKAGED) VERASTEM INC N219616 May 8, 2025 RX CAPSULE, TABLET ORAL 11873296 Dec. 29, 2042 TREATMENT OF ADULT PATIENTS WITH KRAS-MUTATED RECURRENT LOW-GRADE SEROUS OVARIAN CANCER (LGSOC) WHO HAVE RECEIVED PRIOR SYSTEMIC THERAPY, IN COMBINATION WITH DEFACTINIB

Orange Book exclusivity data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRouteExclusivity dateDescription
EQ 0.8MG BASE;EQ 200MG BASE AVMAPKI FAKZYNJA CO-PACK (COPACKAGED) VERASTEM INC N219616 May 8, 2025 RX CAPSULE, TABLET ORAL May 8, 2030 NEW CHEMICAL ENTITY
EQ 0.8MG BASE;EQ 200MG BASE AVMAPKI FAKZYNJA CO-PACK (COPACKAGED) VERASTEM INC N219616 May 8, 2025 RX CAPSULE, TABLET ORAL May 8, 2032 TREATMENT OF ADULT PATIENTS WITH KRAS-MUTATED RECURRENT LOW-GRADE SEROUS OVARIAN CANCER (LGSOC) WHO HAVE RECEIVED PRIOR SYSTEMIC THERAPY

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])		Mechanism
action		Bioact sourceMoA source
Focal adhesion kinase 1 Kinase INHIBITOR IC50 9.22 DRUG LABEL DRUG LABEL
Protein-tyrosine kinase 2-beta Kinase INHIBITOR IC50 9.22 DRUG LABEL DRUG LABEL
Tyrosine-protein kinase JAK3 Kinase IC50 6.94 CHEMBL
D(1A) dopamine receptor GPCR Ki 5 CHEMBL
Adenosine receptor A2a GPCR Ki 6.43 CHEMBL
Receptor-type tyrosine-protein kinase FLT3 Kinase Kd 6.47 CHEMBL
Proto-oncogene tyrosine-protein kinase receptor Ret Kinase Kd 4.56 CHEMBL
Vascular endothelial growth factor receptor 1 Kinase IC50 5.60 CHEMBL
Vascular endothelial growth factor receptor 2 Kinase IC50 6.56 CHEMBL
Cyclin-dependent kinase 1 Kinase Kd 5.70 CHEMBL
Cyclin-dependent kinase 2 Kinase Kd 5.78 CHEMBL
Tyrosine-protein kinase JAK2 Kinase IC50 7.55 CHEMBL
Serine/threonine-protein kinase MARK2 Kinase Kd 5.58 CHEMBL
Tyrosine-protein kinase Lyn Kinase IC50 5.96 CHEMBL
Cyclin-dependent-like kinase 5 Kinase Kd 5.85 CHEMBL
Tyrosine-protein kinase Fer Kinase Kd 5.88 CHEMBL
Serine/threonine-protein kinase 16 Kinase Kd 6.05 CHEMBL
Aurora kinase A Kinase Kd 6.21 CHEMBL
Glycogen synthase kinase-3 beta Kinase Kd 5.88 CHEMBL
Serine/threonine-protein kinase 4 Kinase Kd 5.61 CHEMBL
STE20-like serine/threonine-protein kinase Kinase Kd 4.39 CHEMBL
MAP/microtubule affinity-regulating kinase 3 Kinase Kd 5.35 CHEMBL
Cyclin-dependent kinase 9 Kinase Kd 5.75 CHEMBL
Glycogen synthase kinase-3 alpha Kinase Kd 5.83 CHEMBL
BDNF/NT-3 growth factors receptor Kinase IC50 7.26 CHEMBL
Cyclin-dependent kinase 7 Kinase Kd 5.76 CHEMBL
Serine/threonine-protein kinase 3 Kinase Kd 5.30 CHEMBL
NUAK family SNF1-like kinase 2 Kinase Kd 6.34 CHEMBL
Non-receptor tyrosine-protein kinase TNK1 Kinase Kd 4.95 CHEMBL
Non-receptor tyrosine-protein kinase TYK2 Kinase IC50 6.89 CHEMBL
Wee1-like protein kinase Kinase Kd 5.58 CHEMBL
NT-3 growth factor receptor Kinase IC50 7.24 CHEMBL
Casein kinase II subunit alpha' Kinase Kd 5.92 CHEMBL
Maternal embryonic leucine zipper kinase Kinase Kd 6.05 CHEMBL
Serine/threonine-protein kinase LATS1 Kinase INHIBITOR Kd 5.04 IUPHAR
Mitogen-activated protein kinase kinase kinase kinase 1 Kinase Kd 5.50 CHEMBL
Aurora kinase B Kinase Kd 5.83 CHEMBL
Mitogen-activated protein kinase kinase kinase 9 Kinase IC50 7.12 CHEMBL
Mitogen-activated protein kinase kinase kinase 11 Kinase Kd 6.04 CHEMBL
Serine/threonine-protein kinase PAK 4 Kinase Kd 4.66 CHEMBL
Dual specificity tyrosine-phosphorylation-regulated kinase 1A Kinase Kd 5.04 CHEMBL
Serine/threonine-protein kinase TAO1 Kinase Kd 5.49 CHEMBL
Adenosine receptor A3 GPCR Ki 7.57 CHEMBL
Cyclin-dependent kinase-like 5 Kinase Kd 7.80 CHEMBL
TFIIH basal transcription factor complex helicase XPD subunit Enzyme Kd 5.65 CHEMBL
Cyclin-dependent kinase 13 Kinase Kd 5.51 CHEMBL
Cyclin-dependent kinase 12 Kinase Kd 6.14 CHEMBL
Serine/threonine-protein kinase TAO3 Kinase Kd 4.97 CHEMBL
High affinity nerve growth factor receptor Kinase IC50 7.58 CHEMBL

External reference:

IDSource
CHEMBL3137331 ChEMBL_ID
C584510 MESH_SUPPLEMENTAL_RECORD_UI
7910 IUPHAR_LIGAND_ID
DB12282 DRUGBANK_ID
C3899400 UMLSCUI
CHEBI:755159 CHEBI
CHEMBL3137305 ChEMBL_ID
9928 INN_ID
D10618 KEGG_DRUG
1073160-26-5 SECONDARY_CAS_RN
25117126 PUBCHEM_CID
44327 MMSL
d10301 MMSL
020107 NDDF
020109 NDDF
53O87HA2QU UNII
2714501 RXNORM
53O87HA2QU INXIGHT DRUGS

Pharmaceutical products:

None