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 · 2 recorded
| Milestone | Jurisdiction | Brand | Indication | Date | Sentence it was read from |
|---|---|---|---|---|---|
| Approved | US (FDA) | AVMAPKI FAKZYNJA CO-PACK (COPACKAGED) | — | 2025-05-08 | fda.gov ↗ |
| Filed | US (FDA) | — | KRAS-mutant low-grade serous ovarian cancer | 2024-10-31 | “Verastem completed its rolling New Drug Application (NDA) submission to the to the U.S. Food and Drug Administration (FDA), for the investigational combination of avutometinib...” verastem.com ↗ “Initiated rolling NDA submission for avutometinib and defactinib combination in recurrent low-grade serous ovarian cancer in Q2 2024” verastem.com ↗ “Verastem has initiated a rolling NDA submission for avutometinib and defactinib combination in adults with recurrent LGSOC” verastem.com ↗ |
Trials 37
| 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 · 1 met primary | ||||||
| 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| Phase 1 | NCT04201145 | Sep 2020 → Dec 2021 | malignant pleural mesothelioma | Raphael Bueno, MD | Withdrawn | No outcome recorded Stop: Business |
| 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 | Met primary |
| 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 1/27 trials | ||||||
| Phase 1/2 | NCT07824960 | Oct 2026 → Apr 2029 expected | pancreatic ductal adenocarcinoma | University of Virginia | Not yet recruiting | No outcome recorded |
| 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 · 1 met primary | ||||||
| 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 | Active not 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 Stop: Enrollment |
| 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 | Met primary |
| 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 2027 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 |
| Comparator or background therapy2 trials | ||||||
| Phase 1 | NCT02372227 Background | Jan → Oct 2015 | malignant mesothelioma | Verastem, Inc. | Terminated | No outcome recorded |
| Phase 2 | NCT01870609 Comparator | Sep 2013 → Jan 2016 | malignant pleural mesothelioma | Verastem, Inc. | Terminated | No outcome recorded |
News releases announcing trial results or a regulatory action · 48
| Date | Issuer | Release |
|---|---|---|
| 2026-10-02 | Verastem, Inc. | Results Verastem Oncology Announces New RAMP 201 Molecular Profiling and External Control Arm Analyses Describing Outcomes for Avutometinib Plus Defactinib in Recurrent Low-Grade Serous Ovarian Cancer to be Presented at IGCS 2026 verastem.com ↗
RAMP 201 molecular profiling showed clinically meaningful activity in KRAS wild-type recurrent LGSOC, including ORRs of 22% in patients with NRAS- or BRAF-mutated tumors and 18% in patients with KRAS/NRAS/BRAF triple wild-type tumors |
| 2026-09-28 | Verastem, Inc. | Results Verastem Oncology Announces Publication in Gynecologic Oncology of Two-Year Median Follow-Up Data from RAMP 201 Study of AVMAPKI® FAKZYNJA® CO-PACK (avutometinib capsules; defactinib tablets) in Recurrent Low-Grade Serous Ovarian Cancer verastem.com ↗
Across patients with KRAS wild-type and KRAS-mutated recurrent LGSOC, the combination had a median duration of response of 31.1 months, median progression free survival of 12.9 months, and a safety profile consistent with the primary analysis |
| 2026-06-17 | Verastem, Inc. | Results Verastem Oncology Announces Positive Updated Results from RAMP 205 Evaluating Avutometinib Plus Defactinib in Combination with Standard-of-Care Chemotherapy in First-Line Metastatic Pancreatic Cancer verastem.com ↗
The updated data from the RAMP 205 trial provide important clinical insights into the potential impact of combined RAF/MEK and FAK inhibition as a therapeutic option for pancreatic cancer. |
| 2026-04-10 | Verastem, Inc. | Results Verastem Oncology Announces Two-Year Median Follow-Up Data on AVMAPKI® FAKZYNJA® Combination Therapy (avutometinib capsules; defactinib tablets) in Recurrent Low-Grade Serous Ovarian Cancer at the SGO 2026 Annual Meeting on Women’s Cancers verastem.com ↗
Patients in the Phase 2 RAMP 201 clinical trial demonstrated sustained clinical benefits across multiple efficacy measures highlighting durability of response with a median follow-up of two years |
| 2025-12-29 | Verastem, Inc. | Results Verastem Oncology Provides Update on RAMP 203 Phase 1/2 Clinical Trial for Advanced KRAS G12C Mutant Non-Small Cell Lung Cancer verastem.com ↗
While avutometinib plus defactinib combined well with a G12C inhibitor to drive early and sustained anti-tumor responses, next generation G12C inhibitors are establishing a new benchmark with higher response rates. |
| 2025-07-11 | Verastem, Inc. | Results Verastem Oncology Announces Publication of the Primary Results from the Phase 2 RAMP 201 Trial of Avutometinib in Combination with Defactinib in Patients with Recurrent Low-Grade Serous Ovarian Cancer in the Journal of Clinical Oncology verastem.com ↗
The data reported in the publication showed that avutometinib plus defactinib demonstrated a confirmed overall response rate (ORR) of 31% in all patients with recurrent low-grade serous ovarian cancer (LGSOC). |
| 2025-06-30 | Verastem, Inc. | Results Verastem Oncology Announces Nature Medicine Publication of the Results from the First-in-Human Phase 1 FRAME Study of Avutometinib in Combination with Defactinib in Solid Tumors, including Low-Grade Serous Ovarian Cancer verastem.com ↗
FRAME study demonstrated a 42.3% ORR and 20.1 months median PFS for all patients with low-grade serous ovarian cancer (LGSOC), regardless of KRAS mutation; for patients with KRAS-mutated LGSOC, ORR and mPFS were 58.3% and 30.8 months, respectively |
| 2025-05-22 | Verastem, Inc. | Results Verastem Oncology Announces Positive Updated Results from RAMP 205 Evaluating Avutometinib Plus Defactinib in Combination with Standard-of-Care Chemotherapy in Frontline Metastatic Pancreatic Ductal Adenocarcinoma verastem.com ↗
today announced positive updated safety and efficacy results from the RAMP 205 Phase 1/2 trial evaluating avutometinib plus defactinib in combination with gemcitabine and Nab-paclitaxel in the front-line for patients with metastatic pancreatic ductal adenocarcinoma (PDAC). |
| 2025-05-08 | Verastem, Inc. | Regulatory FDA Approves the AVMAPKI™ FAKZYNJA™ Combination Therapy as the First-Ever Treatment for Adult Patients with KRAS-mutated Recurrent Low-Grade Serous Ovarian Cancer verastem.com ↗
AVMAPKI FAKZYNJA CO-PACK is the first and only FDA-approved medicine for this disease. |
| 2025-03-25 | Verastem, Inc. | Results Verastem Oncology Announces Multiple Presentations Focused on RAS/MAPK Pathway Inhibition at AACR Annual Meeting 2025 verastem.com ↗
In a patient-derived LGSOC xenograft model, an FAK inhibitor addition to avutometinib augmented tumor regression with stronger inhibition of MAPK, PI3K and YAP/TEAD signaling than either agent alone |
| 2024-12-30 | Verastem, Inc. | Regulatory Verastem Oncology Announces FDA Acceptance and Priority Review of New Drug Application for Avutometinib in Combination with Defactinib for the Treatment of Recurrent KRAS Mutant Low-Grade Serous Ovarian Cancer verastem.com ↗ |
| 2024-12-18 | Verastem, Inc. | Results Verastem Oncology Provides a Clinical Update for RAMP 203 Trial in Advanced KRAS G12C Mutant Non-Small Cell Lung Cancer verastem.com ↗
No dose-limiting toxicities (DLTs) have been observed in the triplet combination. |
| 2024-10-31 | Verastem, Inc. | Regulatory Verastem Oncology Completes Rolling NDA Submission to the FDA for Avutometinib Plus Defactinib as a Treatment for Recurrent KRAS Mutant Low-Grade Serous Ovarian Cancer verastem.com ↗
Verastem submitted the NDA under the FDA’s Accelerated Approval pathway and requested a Priority Review based on the combination’s potential to address significant unmet medical need among patients with recurrent LGSOC. |
| 2024-10-17 | Verastem, Inc. | Results Verastem Oncology Presents Positive Updated RAMP 201 Data for Avutometinib and Defactinib Combination in Recurrent Low-Grade Serous Ovarian Cancer at the International Gynecologic Cancer Society (IGCS) 2024 Annual Meeting verastem.com ↗
Verastem Oncology (Nasdaq: VSTM), a biopharmaceutical company committed to advancing new medicines for patients with cancer, today announced updated data from the Phase 2 RAMP 201 (ENGOTov60/GOG3052) clinical trial evaluating the combination of avutometinib, an oral RAF/MEK clamp, and defactinib, an oral, selective FAK inhibitor, in patients with recurrent low-grade serous ovarian cancer (LGSOC). |
| 2024-07-29 | Verastem, Inc. | Regulatory Verastem Oncology Receives FDA Orphan Drug Designation for Avutometinib and Defactinib for the Treatment of Pancreatic Cancer verastem.com ↗
today announced that the U.S. Food and Drug Administration (FDA) has granted Orphan Drug Designation (ODD) to avutometinib, a RAF/MEK clamp, in combination with defactinib, a selective FAK inhibitor, for the treatment of pancreatic cancer. |
| 2024-05-24 | Verastem, Inc. | Regulatory Verastem Oncology Announces the Initiation of a Rolling Submission of NDA to FDA Seeking Accelerated Approval of Avutometinib and Defactinib Combination for the Treatment of Adult Patients with Recurrent KRAS Mutant Low-Grade Serous Ovarian Cancer verastem.com ↗
today announced that it has initiated the rolling submission of a New Drug Application (NDA) to the U.S. Food and Drug Administration (FDA) |
| 2024-05-23 | Verastem, Inc. | Results Verastem Oncology Announces Positive Initial Interim Safety and Efficacy Results from RAMP 205 Trial Evaluating Avutometinib Plus Defactinib in Combination with Gemcitabine and Nab-paclitaxel in First-Line Metastatic Pancreatic Cancer verastem.com ↗
83% (5/6) of patients achieved a confirmed partial response in cohort 1, the most mature dose level; one dose-limiting toxicity was observed, however, the dose level was subsequently cleared after additional patients were enrolled |
| 2024-03-05 | Verastem, Inc. | Regulatory Verastem Oncology Receives Orphan Drug Designation from FDA for Avutometinib Alone or in Combination With Defactinib in Recurrent Low-Grade Serous Ovarian Cancer verastem.com ↗ |
| 2024-03-05 | Verastem, Inc. | Results Verastem Oncology Announces Preclinical Presentations for New Oral G12D Inhibitor and for Avutometinib and Defactinib Combination as a Backbone of Therapy for RAS/MAPK Driven Cancers at AACR Annual Meeting 2024 verastem.com ↗
Additionally, preclinical data will be presented demonstrating that the combination of avutometinib and a FAK inhibitor with standard-of-care chemotherapy can induce tumor regressions in pancreatic cancer models |
| 2023-11-06 | Verastem, Inc. | Results Verastem Oncology Announces Efficacy and Safety Data of Avutometinib and Defactinib in Recurrent Low-Grade Serous Ovarian Cancer (LGSOC) in Heavily Pretreated Patient Population verastem.com ↗
Verastem Oncology (Nasdaq: VSTM) (the “Company”), a biopharmaceutical company committed to advancing new medicines for patients with cancer, announced today results of the efficacy and safety of avutometinib and defactinib in recurrent low-grade serous ovarian cancer (LGSOC) following prior systemic therapy. |
| 2023-09-28 | Verastem, Inc. | Results Verastem Presents Avutometinib and Defactinib Combination Program Updates at the 5th Annual RAS-Targeted Drug Development Summit verastem.com ↗
The clinical presentation includes updated FRAME study efficacy data showing an overall response rate (ORR) of 42% (11 of 26) in evaluable patients with low grade serous ovarian cancer (LGSOC) (n=26). |
| 2023-05-25 | Verastem, Inc. | Results Updated Data from Part A of Verastem Oncology's RAMP 201 Trial Show an Objective Response Rate of 45% in Patients with Recurrent Low-Grade Serous Ovarian Cancer Treated with Avutometinib and Defactinib verastem.com ↗
In the RAMP 201 study, treatment with the combination of avutometinib and defactinib resulted in an objective response rate (ORR) of 45% (13/29) and tumor shrinkage in 86% (25/29) of evaluable patients. |
| 2023-01-24 | Verastem, Inc. | Results Verastem Oncology Announces Positive Data and Regulatory Update from Planned Interim Analysis of Registration-Directed Phase 2 RAMP-201 Trial of Avutometinib and Defactinib in Recurrent Low-Grade Serous Ovarian Cancer verastem.com ↗ |
| 2022-10-04 | Verastem, Inc. | Results Verastem Oncology Announces RAMP VS-6766 Clinical Trials and Corporate Updates verastem.com ↗
Results of Part A of RAMP 202 Trial in KRAS G12V-Mutant NSCLC Show VS-6766 ± Defactinib Did Not Meet Criteria to Continue to Expansion Phase |
| 2022-06-06 | Verastem, Inc. | Results Verastem Oncology Provides Update on RAMP 201 Study Evaluating VS-6766 ± Defactinib in Low-Grade Serous Ovarian Cancer verastem.com ↗
The analysis indicated encouraging efficacy results with confirmed responses by independent review in patients treated with VS-6766 monotherapy and patients treated with VS-6766 in combination with defactinib. |
| 2021-09-19 | Verastem, Inc. | Results Verastem Oncology Announces Updated Investigator-Sponsored Phase 1/2 FRAME Study Data of VS-6766 with Defactinib in Low-Grade Serous Ovarian Cancer Showing Encouraging Response Rates and Progression-Free Survival Presented at ESMO 2021 verastem.com ↗
Median progression-free survival (mPFS) across all patients treated with VS-6766 in combination with defactinib in the study is 23.0 months. |
| 2021-05-24 | Verastem, Inc. | Regulatory Verastem Oncology Receives Breakthrough Therapy Designation for VS-6766 with Defactinib in Recurrent Low-Grade Serous Ovarian Cancer verastem.com ↗ |
| 2021-05-11 | Verastem, Inc. | Results Verastem Oncology Reports First Quarter 2021 Financial Results and Highlights Recent Company Progress verastem.com ↗
Updated Phase 1/2 Data in Recurrent Low-Grade Serous Ovarian Cancer (LGSOC) Continues to Demonstrate Activity, Durability and a Favorable Tolerability Profile for VS-6766 + Defactinib Combination |
| 2021-03-18 | Verastem, Inc. | Results Verastem Oncology Reports Fourth Quarter and Full Year 2020 Financial Results, Clinical Updates and Guidance for Key Milestones in 2021 and 1H 2022 verastem.com ↗
In the FRAME study, additional patients with recurrent LGSOC have now responded to treatment with clinically meaningful results for patients with KRAS wild-type tumors, which represents approximately 70% of all LGSOC patients. |
| 2020-09-16 | Verastem, Inc. | Results Verastem Oncology Announces Presentation of Updated Phase 1/2 FRAME Study Data at the 2nd Annual RAS-Targeted Drug Development Summit verastem.com ↗
Preliminary Data on VS-6766 and Defactinib Combination Continues to Show Encouraging Response Rates, Durability and a Favorable Safety Profile in KRAS Mutant Low-Grade Serous Ovarian Cancer in Investigator-Initiated Trial |
| 2020-06-22 | Verastem, Inc. | Results Verastem Oncology Announces Presentation of Preclinical Data Supporting the Combination of VS-6766 and Defactinib in Metastatic Uveal Melanoma verastem.com ↗
Data Presented at the American Association for Cancer Research 2020 Virtual Annual Meeting II Show Synergism between FAK and RAF/MEK Inhibition Supporting Clinical Evaluation of Defactinib with VS-6766 in Metastatic Uveal Melanoma |
| 2020-04-27 | Verastem, Inc. | Results Verastem Oncology Announces Preliminary Data from Investigator-initiated Study Highlighting Clinical Activity of RAF/MEK and FAK Combination in KRAS Mutant Tumors Presented at the American Association for Cancer Research 2020 Virtual Annual Meeting I verastem.com ↗
Verastem, Inc. (Nasdaq:VSTM) (also known as Verastem Oncology), a biopharmaceutical company committed to developing and commercializing new medicines for patients battling cancer, today announced results from the ongoing investigator-initiated Phase 1 clinical study investigating VS-6766, its RAF/MEK inhibitor, in combination with defactinib, its FAK inhibitor, in patients with KRAS mutant advanced solid tumors. |
| 2018-06-04 | Verastem, Inc. | Results Verastem Oncology Presents Data on Two Lead Drug Candidates at ASCO 2018 Annual Meeting verastem.com ↗
Phase I results show defactinib in combination with pembrolizumab and gemcitabine is well tolerated and shows early signs of clinical activity in pancreatic cancer including confirmed partial response and long-term stable disease |
| 2018-05-16 | Verastem, Inc. | Results Verastem Oncology to Present Data on Two Lead Drug Candidates at ASCO 2018 Annual Meeting verastem.com ↗
Promising initial clinical activity of defactinib, an oral FAK inhibitor, in combination with pembrolizumab and gemcitabine in patients with pancreatic cancer whose disease progressed on one or more prior lines of chemotherapy |
| 2017-04-02 | Verastem, Inc. | Results Data on Verastem’s Focal Adhesion Kinase Inhibitor Defactinib Presented at the 2017 American Association for Cancer Research Annual Meeting verastem.com ↗
Our initial biomarker data, indicating an increase in activated proliferating cytotoxic T cells together with a reduction in tumor-associated macrophages (TAMs) appear promising. |
| 2016-05-03 | Verastem, Inc. | Results Verastem Announces the Presentation of Clinical Data at iMig 2016 verastem.com ↗
Data analysis from Cohort 1 and Cohort 2 (n=20) showed that VS-6063 was generally well tolerated with no apparent negative impact on surgical outcome. |
| 2016-03-16 | Verastem, Inc. | Results Verastem to Present Data Supporting FAK/PYK2 Inhibition at the 2016 American Academy of Cancer Research Annual Meeting verastem.com ↗
Key immune-related observations include VS-6063 and VS-4718 dose-dependently stimulating proliferation of CD8+ cytotoxic T cells. |
| 2015-09-28 | Verastem, Inc. | Results Verastem Stops Enrollment Due to Futility in the COMMAND Study of VS-6063 for the Treatment of Malignant Pleural Mesothelioma verastem.com ↗
The results of the analysis demonstrated that VS-6063 had a generally well tolerated safety profile but that there was not a sufficient level of efficacy to warrant continuation of the study. |
| 2015-09-10 | Verastem, Inc. | Results Verastem Presents Clinical and Preclinical Data at the 16th World Conference on Lung Cancer verastem.com ↗
Four oral presentations included results from a Phase 2 clinical trial of VS-6063 (defactinib) in advanced refractory KRAS-Mutated Non-Small Cell Lung Cancer (NSCLC) and presentations on preclinical studies of VS-6063 and VS-5584 in Small-Cell Lung Cancer (SCLC) and Mesothelioma. |
| 2015-08-26 | Verastem, Inc. | Results Verastem Issues Statement Regarding WCLC Presentations verastem.com ↗
Verastem believes the study has met its goals, with encouraging outcomes that the Company plans to explore in future studies. |
| 2015-04-22 | Verastem, Inc. | Results Verastem Presents Encouraging Scientific Data on the Preferential Targeting of Cancer Stem Cells at the 2015 American Association of Cancer Research Annual Meeting verastem.com ↗
The data presented provide continued evidence that VS-6063, VS-4718 and VS-5584 effectively target cancer stem cells, reduce tumor initiating capability and prolong the anti-tumor response to standard of care chemotherapy in preclinical models of multiple tumor types. |
| 2014-12-08 | Verastem, Inc. | Results Verastem Presents Data at the 2014 American Society of Hematology Annual Meeting verastem.com ↗
BCR-ABL1+ Ikaros-mutant B-ALLs exhibit stroma-mediated resistance to ABL1 TKIs, while the FAK inhibitors VS-4718 and VS-6063 were effective in blocking stromal adhesion and inducing apoptosis in both mouse and human Ikaros-mutant B-ALL samples. |
| 2014-11-21 | Verastem, Inc. | Results Verastem Presents Data at the 2014 EORTC-NCI-AACR Symposium on Molecular Targets and Cancer Therapeutics verastem.com ↗
Results were presented from a first-in- Asia , Phase 1 trial evaluating the safety and pharmacokinetics of single agent VS-6063 (defactinib) in Japanese patients with advanced solid tumors, including one patient with mesothelioma. |
| 2014-10-24 | Verastem, Inc. | Results Verastem Presents New Data on Mesothelioma Programs at the 12th International Mesothelioma Interest Group Meeting verastem.com ↗
Results from a Window of Opportunity study in surgically-eligible patients demonstrate a reduction in pFAK, cancer stem cell markers and tumor size following 12 days of treatment with VS-6063 |
| 2014-07-10 | Verastem, Inc. | Results Verastem Presents Results and Updated Development Plans at Annual Research and Development Day verastem.com ↗
An additional partial response has been reported since our interim report at ASCO on the combination of VS-6063 and weekly paclitaxel in twenty-two patients with ovarian cancer. |
| 2014-06-02 | Verastem, Inc. | Results Verastem Presents Updated Clinical Data from VS-6063 and Paclitaxel Combination Phase 1/1b Study in Patients with Ovarian Cancer at the 2014 ASCO Annual Meeting verastem.com ↗
The study, which has completed enrollment, is evaluating 22 patients at three sites in the US. |
| 2014-04-09 | Verastem, Inc. | Results Verastem Presents Data on Cancer Stem Cell-Targeting Agents at the 2014 AACR Annual Meeting verastem.com ↗
Here we report that VS-6063 targets cancer stem cells directly and through an immunomodulatory effect by reducing tumor-associated macrophages. |
| 2014-03-05 | Verastem, Inc. | Results Verastem Reports Data from Phase 1 Study of VS-6063 (defactinib) in Japanese Patients verastem.com ↗
The study results demonstrated that VS-6063 was well tolerated at all dose levels. |
All press releases naming this drug 64 releases
Evidence & citations 12 cited values
Every value below carries the sentence it was read from. 42 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 2015 |
| 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 ↗9“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 ↗ “Avutometinib (VS-6766) + Defactinib (VS-6063)” NCT07824960 ↗ “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“Focal adhesion kinase 1 inhibitor” CHEMBL3137331 ↗ “a focal adhesion kinase inhibitor” NCT01943292 ↗ |
| 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 ↗ |