Defactinib
Highest phase reached
Phase 3
Drug type
Small molecule
- Listing at source
- Listed
- Highest phase reached
- Phase 3
- Drug type
- Small molecule
- Drug name
- Defactinib
- Molecular weight
- 510.5
- Structure (SMILES)
- CNC(=O)c1ccc(Nc2ncc(C(F)(F)F)c(NCc3nccnc3N(C)S(C)(=O)=O)n2)cc1
- defacitinib
- DEFACITINIB
- defactinib
- Defactinib
- DEFACTINIB
- DEFACTINIB (VS-6063)
- defactinib [INN]
- DEFACTINIB [USAN]
- Defactinib [WHO-DD]
- defactinib hydrochloride
- DEFACTINIB HYDROCHLORIDE
- defactinib inn
- defactinib usan
- defactinib vs 6063
- defactinib who dd
- pf 04554878
- PF-04554878
- vs 6063
- Vs-6063
- VS-6063
- CAS registry numbers
- 1073154-85-4
- ChEMBL ID
- CHEMBL3137331
- InChIKey
- FWLMVFUGMHIOAA-UHFFFAOYSA-N
- PubChem compound IDs
- 25117126
- FDA ingredient codes (UNII)
- 53O87HA2QU
- 2714501
- 2714502
- Patents
- 0
- Designations
- 1
- First in class
- No
- Fast track
- No
- Breakthrough designation
- No
- Orphan designation
- No
- Priority review
- No
- Orphan exclusivity
- No
- Accelerated approval
- No
- Pharmacology name
- defactinib
- Type
- Synthetic organic
- Drug name stem
- -tinib
- Approval recorded by Guide to Pharmacology
- Yes
- Action
- Inhibition
- Action type
- Inhibitor
- Target
- large tumor suppressor kinase 1
- Gene symbol
- LATS1
- Protein identifier
- O95835
- Median affinity
- 5.04
- Affinity units
- pKd
- Mechanism
- Focal adhesion kinase 1 inhibitor
- Action type
- Inhibitor
- Target
- Focal adhesion kinase 1
- Protein identifier
- Q05397
- Mechanism
- Protein tyrosine kinase 2 beta inhibitor
- Action type
- Inhibitor
- Target
- Protein-tyrosine kinase 2-beta
- Protein identifier
- Q14289
- Mechanism
- Focal adhesion kinase 1 inhibitor
- Action type
- Inhibitor
- Target
- Focal adhesion kinase 1
- Mechanism
- Protein tyrosine kinase 2 beta inhibitor
- Action type
- Inhibitor
- Target
- Protein-tyrosine kinase 2-beta
- Condition
- Carcinoma, Endometrioid
- Highest recorded phase
- 1
- Condition identifier
- EFO:0000466
- Subject identifier
- D018269
- Condition
- Glioblastoma
- Highest recorded phase
- 0.5
- Condition identifier
- EFO:0000519
- Subject identifier
- D005909
- Condition
- Melanoma
- Highest recorded phase
- 1
- Condition identifier
- EFO:0000756
- Subject identifier
- D008545
- Condition
- Mesothelioma
- Highest recorded phase
- 2
- Condition identifier
- EFO:0000770
- Subject identifier
- D008654
- Condition
- Pancreatic Neoplasms
- Highest recorded phase
- 2
- Condition identifier
- EFO:0002618
- Subject identifier
- D010190
- Condition
- Thyroid Neoplasms
- Highest recorded phase
- 2
- Condition identifier
- EFO:0002892
- Subject identifier
- D013964
- Condition
- Carcinoma, Non-Small-Cell Lung
- Highest recorded phase
- 2
- Condition identifier
- EFO:0003060
- Subject identifier
- D002289
- Condition
- Neoplasms
- Highest recorded phase
- 1
- Condition identifier
- MONDO:0004992
- Subject identifier
- D009369
- Condition
- Carcinoma, Pancreatic Ductal
- Highest recorded phase
- 2
- Condition identifier
- MONDO:0005184
- Subject identifier
- D021441
- Condition
- Colorectal Neoplasms
- Highest recorded phase
- 2
- Condition identifier
- MONDO:0005575
- Subject identifier
- D015179
- Condition
- Ovarian Neoplasms
- Highest recorded phase
- 3
- Condition identifier
- MONDO:0008170
- Subject identifier
- D010051
- Condition
- Lung Neoplasms
- Highest recorded phase
- 2
- Condition identifier
- MONDO:0008903
- Subject identifier
- D008175
- Condition
- Genital Neoplasms, Female
- Highest recorded phase
- 2
- Condition identifier
- MONDO:0021148
- Subject identifier
- D005833
- Condition identifier
- EFO_0000519
- Condition identifier
- EFO_0000588
- Highest recorded phase
- 2
- Condition identifier
- EFO_0000770
- Highest recorded phase
- 2
- Condition identifier
- EFO_0003060
- Condition identifier
- EFO_0003860
- Condition identifier
- EFO_1000359
- Highest recorded phase
- 1
- Condition identifier
- MONDO_0001056
- Highest recorded phase
- 2
- Condition identifier
- MONDO_0001657
- Highest recorded phase
- 1
- Condition identifier
- MONDO_0004992
- Highest recorded phase
- 1
- Condition identifier
- MONDO_0005061
- Highest recorded phase
- 2
- Condition identifier
- MONDO_0005062
- Highest recorded phase
- 2
- Condition identifier
- MONDO_0005065
- Highest recorded phase
- 2
- Condition identifier
- MONDO_0005105
- Highest recorded phase
- 1
- Condition identifier
- MONDO_0005112
- Highest recorded phase
- 2
- Condition identifier
- MONDO_0005184
- Highest recorded phase
- 2
- Condition identifier
- MONDO_0005192
- Highest recorded phase
- 1
- Condition identifier
- MONDO_0005211
- Highest recorded phase
- 2
- Condition identifier
- MONDO_0005233
- Highest recorded phase
- 2
- Condition identifier
- MONDO_0005575
- Highest recorded phase
- 2
- Condition identifier
- MONDO_0006047
- Highest recorded phase
- 2
- Condition identifier
- MONDO_0006292
- Highest recorded phase
- 1
- Condition identifier
- MONDO_0006468
- Highest recorded phase
- 2
- Condition identifier
- MONDO_0008170
- Highest recorded phase
- 2
- Condition identifier
- MONDO_0008170
- Highest recorded phase
- 3
- Condition identifier
- MONDO_0009693
- Highest recorded phase
- 2
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- Hydrogen bond acceptors
- 9
- Hydrogen bond donors
- 3
- Polar surface area
- 142.1
- Calculated partition coefficient (ALogP)
- 2.4
- Calculated partition coefficient (XLogP)
- 1.4
- Prodrug
- No
- Chirality
- Achiral
- Inorganic
- No
- Rule-of-five violations
- 1
- Rotatable bonds
- 8
- Heavy atoms
- 35
- Molecular formula
- C20H21F3N8O3S
- Monoisotopic mass
- 510.14094222
- Natural product
- No
- Recorded assays
- 3,238
- Active assays
- 270
- Confirmatory
- Screening
Related records
Trials (39)
- 5G-RUBY: Avutometinib and Defactinib in Malignant Brain Tumours
- A Phase 1/2 Study of VS-7375 in Patients With KRAS G12D-Mutated Solid Tumors
- A Phase 2 Study of Avutometinib (VS-6766) Plus Defactinib
- A Phase I, Open-label Study of Absorption, Metabolism, and Excretion of Defactinib (VS-6063) in Healthy Male Subjects
- A Study of Avutometinib (VS-6766) + Defactinib (VS-6063) in Recurrent Low-Grade Serous Ovarian Cancer
- A Study of Avutometinib (VS-6766) + Defactinib in Recurrent KRAS G12V, Other KRAS and BRAF Non-Small Cell Lung Cancer
- A Study of Avutometinib (VS-6766) and Defactinib in People With Mesonephric Gynecologic Cancer
- A Study of Avutometinib (VS-6766) v. Avutometinib (VS-6766) + Defactinib in Recurrent Low-Grade Serous Ovarian Cancer With and Without a KRAS Mutation
- A Study of Avutometinib + Defactinib in Recurrent Low-Grade Serous Ovarian Cancer in Japanese Patients
- A Study of Avutometinib and Defactinib in People With Thyroid Cancer
- A Study of Avutometinib, Defactinib, and Letrozole in People With Low-Grade Serous Ovarian Cancer
- A Study Of PF-04554878 In Patients With Advanced Non-Hematologic Malignancies
- Avutometinib and Defactinib in Diffuse Gastric Cancer
- Combination of Avutometinib and Defactinib for Treatment of Relapsed, Refractory, Metastatic, or Unresectable Malignant Peripheral Nerve Sheath Tumor
- Combined Evaluation of Epigenetic and Sensitising Therapy in AML and MDS
- Continued Access to Avutometinib in Combination With Defactinib in Patients With Recurrent Low-Grade Serous Ovarian Cancer (LGSOC)
- Defactinib and Avutometinib, With or Without Encorafenib, for the Treatment of Patients With Brain Metastases From Cutaneous Melanoma
- Defactinib Combined With Pembrolizumab and Gemcitabine in Patients With Advanced Cancer
- Defactinib, Avutometinib and Nivolumab for the Treatment of Anti-PD1 Refractory LKB1-Mutant Advanced Non-Small Cell Lung Cancer
- Identification of Treatment Concentrations of Defactinib or VS-6766 for the Treatment of Patients With Glioblastoma
In development for (32)
- Acute myeloid leukemia Phase 1
- Brain cancer Phase 1
- Cancer Phase 1
- Chronic myelomonocytic leukemia Phase 1
- Colorectal cancer Phase 2
- Differentiated thyroid carcinoma Phase 2
- Endometrial cancer Phase 1
- Endometrioid adenocarcinoma Phase 1
- Exocrine pancreatic carcinoma Phase 2
- Female reproductive system neoplasm Phase 2
- Gastric cancer Phase 2
- Gastric neoplasm Phase 2
- Glioblastoma Early phase 1
- Lung adenocarcinoma Phase 2
- Lung cancer Phase 2
- Lymphoma Phase 2
- Malignant mesothelioma Phase 1
- Malignant pancreatic neoplasm Phase 2
- Malignant pleural mesothelioma Phase 2
- Melanoma Phase 1