Drugs / Defactinib
Defactinib
also known as
VS-6063 · PF-04554878 · DEFACITINIB · defactinib (VS-6063) · defactinib hydrochloride · VS-6063 HYDROCHLORIDE
Small molecule targets PTK2, PTK2B via inhibition
Regulatory milestones approvals, filings & regulatory actions · 1 recorded
| Milestone | Jurisdiction | Brand | Indication | Date | Sentence it was read from |
|---|---|---|---|---|---|
| Approved | US (FDA) | AVMAPKI FAKZYNJA CO-PACK (COPACKAGED) | — | 2025-05-08 | fda.gov ↗ |
Trials 36 · a red edge is where a trial was stopped
| Phase | Registry id | Dates | Indication | Sponsor | Status | Outcome |
|---|---|---|---|---|---|---|
| Phase 01 trial | ||||||
| Phase 0 | NCT05798507 | Jul 2023 → Dec 2026 expected | glioblastoma | Emory University | Active not recruiting | No outcome recorded |
| Phase 110 trials | ||||||
| Phase 1 | NCT07318324 | May 2026 → Aug 2028 expected | endometrial cancer | M.D. Anderson Cancer Center | Recruiting | No outcome recorded |
| Phase 1 | NCT05636514 | Dec 2022 → Aug 2026 overdue | acute myeloid leukemia, chronic myelomonocytic leukemia, myelodysplastic syndrome | Clinical Hub for Interventional Research (CHOIR) | Recruiting | No outcome recorded |
| Phase 1 | NCT04201145 | Sep 2020 → Dec 2021 | malignant pleural mesothelioma | Raphael Bueno, MD | Withdrawn | No outcome recorded |
| Phase 1 | NCT03875820 | Dec 2017 → Apr 2023 overdue | endometrioid adenocarcinoma, malignant pancreatic neoplasm, non-small cell lung carcinoma, ovarian serous tumor | Institute of Cancer Research, United Kingdom | Active not recruiting | No outcome recorded |
| Phase 1 | NCT02943317 | Oct 2016 → Aug 2018 | malignant epithelial tumor of ovary | Verastem, Inc. | Terminated | No outcome recorded |
| Phase 1 | NCT02546531 | Feb 2016 → Nov 2017 | malignant pancreatic neoplasm | Washington University School of Medicine | Completed | No outcome recorded |
| Phase 1 | NCT02913716 | Aug → Sep 2015 | — | Verastem, Inc. | Completed | No outcome recorded |
| Phase 1 | NCT01943292 | Sep 2013 → Jun 2014 | — | Verastem, Inc. | Completed | No outcome recorded |
| Phase 1 | NCT01778803 | Feb 2013 → Feb 2015 | ovarian cancer | Verastem, Inc. | Completed | No outcome recorded |
| Phase 1 | NCT00787033 | Dec 2008 → Mar 2011 | cancer | Verastem, Inc. | Completed | No outcome recorded |
| Phase 1/26 trials | ||||||
| Phase 1/2 | NCT06630260 | Nov 2024 → Sep 2029 expected | diffuse glioma, H3 G34 mutant, glioblastoma | Institute of Cancer Research, United Kingdom | Recruiting | No outcome recorded |
| Phase 1/2 | NCT06194929 | Mar 2024 → Jan 2028 expected | cutaneous melanoma, metastatic malignant neoplasm in the brain | University of Utah | Recruiting | No outcome recorded |
| Phase 1/2 | NCT05669482 | Mar 2023 → Aug 2026 overdue | malignant pancreatic neoplasm, metastatic malignant neoplasm | Verastem, Inc. | Active not recruiting | No outcome recorded |
| Phase 1/2 | NCT05074810 | Apr 2022 → Jun 2026 overdue | non-small cell lung carcinoma | Verastem, Inc. | Active not recruiting | No outcome recorded |
| Phase 1/2 | NCT03287271 | Feb 2018 → Apr 2025 overdue | ovarian cancer | Michael McHale | Recruiting | No outcome recorded |
| Phase 1/2 | NCT02758587 | Jul 2017 → May 2019 | mesothelioma, non-small cell lung carcinoma, pancreatic neoplasm | NHS Greater Glasgow and Clyde | Unknown | No outcome recorded |
| Phase 218 trials | ||||||
| Phase 2 | NCT07126158 | Apr 2026 → Apr 2030 expected | pancreatic adenocarcinoma | Washington University School of Medicine | Recruiting | No outcome recorded |
| Phase 2 | NCT06369259 | Feb 2025 → Feb 2029 expected | colorectal cancer | M.D. Anderson Cancer Center | Recruiting | No outcome recorded |
| Phase 2 | NCT06682572 | Oct 2024 → Dec 2025 overdue | ovarian cancer, ovarian serous tumor | Verastem, Inc. | Active not recruiting | No outcome recorded |
| Phase 2 | NCT06487221 | Oct 2024 → Nov 2028 expected | diffuse gastric cancer | Ryan H. Moy, MD, PhD | Recruiting | No outcome recorded |
| Phase 2 | NCT06495125 | Jul 2024 → Mar 2029 expected | lung adenocarcinoma | Emory University | Recruiting | No outcome recorded |
| Phase 2 | NCT06394804 | Apr 2024 → Apr 2027 expected | malignant ovarian serous tumor | Memorial Sloan Kettering Cancer Center | Recruiting | No outcome recorded |
| Phase 2 | NCT06007924 | Aug 2023 → Aug 2027 expected | thyroid cancer | Memorial Sloan Kettering Cancer Center | Recruiting | No outcome recorded |
| Phase 2 | NCT05787561 | Mar 2023 → Mar 2027 expected | mesonephric neoplasm | Memorial Sloan Kettering Cancer Center | Recruiting | No outcome recorded |
| Phase 2 | NCT05512208 | Feb 2023 → Dec 2027 expected | cervical cancer, endometrioid adenocarcinoma, malignant ovarian serous tumor, mucinous ovarian cancer | University of Oklahoma | Recruiting | No outcome recorded |
| Phase 2 | NCT04331041 | Aug 2021 → Feb 2026 overdue | pancreatic adenocarcinoma | Washington University School of Medicine | Active not recruiting | No outcome recorded |
| Phase 2 | NCT04720417 | Jan 2021 → Apr 2024 | uveal melanoma | Thomas Jefferson University | Terminated | No outcome recorded |
| Phase 2 | NCT04620330 | Dec 2020 → Aug 2023 | non-small cell lung carcinoma | Verastem, Inc. | Completed | No outcome recorded |
| Phase 2 | NCT04625270 | Dec 2020 → Nov 2024 overdue | ovarian serous adenocarcinoma | Verastem, Inc. | Active not recruiting | No outcome recorded |
| Phase 2 | NCT03727880 | Jun 2019 → Jan 2025 | pancreatic ductal adenocarcinoma | Lei Zheng | Completed | No outcome recorded |
| Phase 2 | NCT04439331 | Nov 2015 → Nov 2020 overdue | adult lymphoma, plasma cell myeloma, refractory malignant neoplasm | National Cancer Institute (NCI) | Active not recruiting | No outcome recorded |
| Phase 2 | NCT02465060 | Aug 2015 → Dec 2026 expected | breast carcinoma, carcinoma of esophagus, cervical carcinoma, colon carcinoma +17 | National Cancer Institute (NCI) | Active not recruiting | No outcome recorded |
| Phase 2 | NCT02004028 | Dec 2013 → Jun 2019 | malignant pleural mesothelioma | Verastem, Inc. | Terminated | No outcome recorded |
| Phase 2 | NCT01951690 | Sep 2013 → Jun 2016 | non-small cell lung carcinoma | Verastem, Inc. | Completed | No outcome recorded |
| Phase 31 trial | ||||||
| Phase 3 | NCT06072781 | Mar 2024 → Oct 2028 expected | ovarian serous tumor | Verastem, Inc. | Recruiting | No outcome recorded |
Also used as a comparator or background therapy in 2 trials
| Phase | Registry id | Dates | Indication | Sponsor | Status | Outcome |
|---|---|---|---|---|---|---|
| Phase 11 trial | ||||||
| Phase 1 | NCT02372227 Background | Jan → Oct 2015 | malignant mesothelioma | Verastem, Inc. | Terminated | No outcome recorded |
| Phase 21 trial | ||||||
| Phase 2 | NCT01870609 Comparator | Sep 2013 → Jan 2016 | malignant pleural mesothelioma | Verastem, Inc. | Terminated | No outcome recorded |
Evidence & citations 12 cited values
Every value below carries the sentence it was read from. 41 sources stand behind the page.
| Field | Value | Cited text |
|---|---|---|
| Known as | defactinib | “VS-6063 (also known as defactinib or PF-04554878) is a second-generation inhibitor of focal adhesion kinase (FAK) and proline-rich tyrosine kinase-2 (Pyk2).” PMID 26334219 ↗ Sep 201533 |
| Known as | DEFACITINIB | ChEMBL registry synonym — accepted as the source's own label CHEMBL3137331 ↗ |
| Known as | defactinib (VS-6063) | “defactinib (VS-6063)” NCT06072781 ↗ |
| Known as | defactinib hydrochloride | “Patients receive defactinib hydrochloride (defactinib) orally (PO) 400 mg twice daily (BID) on days 1-28.” NCT04439331 ↗ |
| Known as | PF-04554878 | “PURPOSE: VS-6063 (also known as defactinib or PF-04554878) is a second-generation inhibitor of focal adhesion kinase and proline-rich tyrosine kinase-2.” PMID 27025608 ↗ Mar 2016 |
| Known as | VS-6063 | “This study is a Phase 2, randomized, double-blind, placebo-controlled, multicenter study of defactinib (VS-6063) in subjects with malignant pleural mesothelioma (MPM)” NCT01870609 ↗8“VS-6063 (also known as defactinib or PF-04554878) is a second-generation inhibitor of focal adhesion kinase (FAK) and proline-rich tyrosine kinase-2 (Pyk2).” PMID 26334219 ↗ Sep 2015 “PURPOSE: VS-6063 (also known as defactinib or PF-04554878) is a second-generation inhibitor of focal adhesion kinase and proline-rich tyrosine kinase-2.” PMID 27025608 ↗ Mar 2016 “Avutometinib (VS-6766) + Defactinib (VS-6063)” NCT06682572 ↗ “VS-6063” NCT03875820 ↗ |
| Known as | VS-6063 HYDROCHLORIDE | ChEMBL registry synonym — accepted as the source's own label CHEMBL3137331 ↗ |
| Action | Inhibit | “Protein tyrosine kinase 2 beta inhibitor” CHEMBL3137331 ↗2“a focal adhesion kinase inhibitor” NCT01943292 ↗ “Focal adhesion kinase 1 inhibitor” CHEMBL3137331 ↗ |
| Modality | Small molecule | — CHEMBL3137331 ↗ |
| Route | Oral | “Oral defactinib (VS-6063) administered twice daily” NCT01778803 ↗ |
| Target | PTK2 | “Focal adhesion kinase 1 inhibitor” CHEMBL3137331 ↗ |
| Target | PTK2B | “Protein tyrosine kinase 2 beta inhibitor” CHEMBL3137331 ↗ |