Defactinib

Phase 3Small molecule

Defactinib is being investigated as a cancer treatment that works by blocking a protein called FAK, which helps cancer cells survive and spread. It's being tested in clinical trials for various solid tumors.[1] Defactinib is currently being investigated across 21 indications[3], with its most advanced program in Phase 3.[1]

Defactinib is one of 499 small molecule programs targeting Pancreatic Neoplasm. It is currently in Phase 3.

Indications

Total Trials

Active Trials

498

Competitors

Pipeline

Status by Indication[3][1]

Indication

Pancreatic NeoplasmActive, not recruiting

Malignant Pleural MesotheliomaActive, not recruiting

Pleural MesotheliomaActive, not recruiting

Cutaneous MelanomaActive, not recruiting

AdenocarcinomaActive, not recruiting

MesotheliomaActive, not recruiting

Malignant Pancreatic NeoplasmActive, not recruiting

Pancreatic Ductal AdenocarcinomaActive, not recruiting

Pancreatic AdenocarcinomaActive, not recruiting

Non-Small Cell Lung CancerActive, not recruiting

Pancreatic NeoplasmPhase 1

Active, not recruiting

Malignant Pleural MesotheliomaPhase 2

Active, not recruiting

Pleural MesotheliomaPhase 1

Active, not recruiting

Cutaneous MelanomaPhase 1/Phase 2

Active, not recruiting

AdenocarcinomaPhase 2

Active, not recruiting

MesotheliomaPhase 2

Active, not recruiting

Malignant Pancreatic NeoplasmPhase 1

Active, not recruiting

Pancreatic Ductal AdenocarcinomaPhase 2

Active, not recruiting

Pancreatic AdenocarcinomaPhase 2

Active, not recruiting

Non-Small Cell Lung CancerPhase 1

Active, not recruiting

Showing 10 of 21 indications

Competition

Competitive Landscape

1639 competitors in Non-Small Cell Lung Cancer

#DrugCompanyPhaseTrials

Defactinib

VVerastem, Inc.

Phase 3

2 2

Gemzar

GGynecologic Oncology Group

Preclinical

72 3

PORTRAZZA

Eli Lilly

Preclinical

8 4

Vizimpro

Pfizer

Preclinical

4 5

Ofev

Boehringer Ingelheim

Preclinical

7 6

PD-1 Inhibitor

Johnson & Johnson

Preclinical

2 7

Tyrosine Kinase Inhibitor

Pfizer

Preclinical

2 8

Vibramycin

PPfizer's Upjohn has merged with Mylan to form Viatris Inc.

Treatment

1 10

Vidaza

Bristol-Myers Squibb

Preclinical

Ranked by pipeline maturity and clinical activity. Current drug highlighted in teal.

Timeline

Expected Milestones

Q4 2026

Phase 1Active, not recruiting

Trial

NCT03875820

Phase 2Active, not recruiting

Advanced Lymphoma

NCT02465060

Q1 2027

Phase 2Recruiting

Gynecologic Cancer

NCT05787561

Q2 2027

Phase 2Recruiting

Ovarian Cancer

NCT06394804

Phase 2Active, not recruiting

Adenocarcinoma

NCT04331041

Q3 2027

Phase 2Recruiting

Thyroid Cancer

NCT06007924

Clinical

Trials by Indication[1]

Ovarian Cancer3 trials

A Study of Avutometinib, Defactinib, and Letrozole in People With Low-Grade Serous Ovarian Cancer

Recruiting·MMemorial Sloan Kettering Cancer Center·Phase 2·NCT06394804·20 enrolled

A Study of Avutometinib (VS-6766) + Defactinib (VS-6063) in Recurrent Low-Grade Serous Ovarian Cancer

Recruiting·VVerastem, Inc.·Phase 3·NCT06072781·270 enrolled

Phase I/Ib Study of Paclitaxel in Combination With VS-6063 in Patients With Advanced Ovarian Cancer

Completed·VVerastem, Inc.·Phase 1·NCT01778803·22 enrolled

Avutometinib2 trials

5G-RUBY: Avutometinib and Defactinib in Malignant Brain Tumours

Recruiting·IInstitute of Cancer Research, United Kingdom·Phase 1/2·NCT06630260·182 enrolled

Phase Ib Study of Avutometinib, Defactinib, and Everolimus in RAS Pathway Mutant Endometrial Cancer

Recruiting·MM.D. Anderson Cancer Center·Phase 1·NCT07318324·31 enrolled

Non-Small Cell Lung Cancer2 trials

Defactinib, Avutometinib and Nivolumab for the Treatment of Anti-PD1 Refractory LKB1-Mutant Advanced Non-Small Cell Lung Cancer

Recruiting·EEmory University·Phase 2·NCT06495125·50 enrolled

Phase II Study of VS-6063 in Patients With KRAS Mutant Non-Small Cell Lung Cancer

Completed·VVerastem, Inc.·Phase 2·NCT01951690·55 enrolled

Pancreatic Ductal Adenocarcinoma1 trial

Study of Pembrolizumab With or Without Defactinib Following Chemotherapy as a Neoadjuvant and Adjuvant Treatment for Resectable Pancreatic Ductal Adenocarcinoma

Completed·LLei Zheng·Phase 2·NCT03727880·28 enrolled

Colorectal Cancer1 trial

Open-label Phase 2 Study of Avutometinib (RAF/MEK Clamp) in Combination With Defactinib (FAK Inhibitor) and Cetuximab in Patients With Unresectable, Anti-EGFR-Refractory Advanced Colorectal Cancer

Recruiting·MM.D. Anderson Cancer Center·Phase 2·NCT06369259·33 enrolled

16 more indications

Glioblastoma1 trial

Identification of Treatment Concentrations of Defactinib or VS-6766 for the Treatment of Patients With Glioblastoma

Active, not recruiting·EEmory University·Phase 1·NCT05798507·14 enrolled

Advanced Cancer1 trial

Defactinib Combined With Pembrolizumab and Gemcitabine in Patients With Advanced Cancer

Completed·WWashington University School of Medicine·Phase 1·NCT02546531·43 enrolled

Advanced Solid Malignancies1 trial

Study of FAK (Defactinib) and PD-1 (Pembrolizumab) Inhibition in Advanced Solid Malignancies (FAK-PD1)

Unknown status·NNHS Greater Glasgow and Clyde·Phase 1/2·NCT02758587·59 enrolled

Pleural Mesothelioma1 trial

Pembrolizumab + Defactinib In Pleural Mesothelioma

Withdrawn·—·Phase 1·NCT04201145

Absorption1 trial

A Phase I, Open-label Study of Absorption, Metabolism, and Excretion of Defactinib (VS-6063) in Healthy Male Subjects

Completed·VVerastem, Inc.·Phase 1·NCT02913716·5 enrolled

Pancreatic Adenocarcinoma1 trial

Stereotactic Body Radiotherapy Plus FAK and RAF/MEK Inhibition in Advanced Pancreatic Adenocarcinoma

Not yet recruiting·WWashington University School of Medicine·Phase 2·NCT07126158·36 enrolled

Gynecologic Cancer1 trial

A Study of Avutometinib (VS-6766) and Defactinib in People With Mesonephric Gynecologic Cancer

Recruiting·MMemorial Sloan Kettering Cancer Center·Phase 2·NCT05787561·40 enrolled

Adenocarcinoma1 trial

Stereotactic Body Radiotherapy and Focal Adhesion Kinase Inhibitor in Advanced Pancreas Adenocarcinoma

Active, not recruiting·WWashington University School of Medicine·Phase 2·NCT04331041·42 enrolled

Gastric Cancer1 trial

Avutometinib and Defactinib in Diffuse Gastric Cancer

Recruiting·—·Phase 2·NCT06487221·27 enrolled

MDS1 trial

Combined Evaluation of Epigenetic and Sensitising Therapy in AML and MDS

Recruiting·CClinical Hub for Interventional Research (CHOIR)·Phase 1·NCT05636514·12 enrolled

Hematologic Malignancies1 trial

Phase I Dose Escalation Study of VS-6063 in Japanese Subjects With Non-Hematologic Malignancies

Completed·VVerastem, Inc.·Phase 1·NCT01943292·9 enrolled

Cutaneous Melanoma1 trial

Defactinib and Avutometinib, With or Without Encorafenib, for the Treatment of Patients With Brain Metastases From Cutaneous Melanoma

Recruiting·UUniversity of Utah·Phase 1/2·NCT06194929·33 enrolled

Trial1 trial

Phase I Trial of Defactinib and VS-6766.

Active, not recruiting·IInstitute of Cancer Research, United Kingdom·Phase 1·NCT03875820·87 enrolled

Malignant Pleural Mesothelioma1 trial

Placebo Controlled Study of VS-6063 in Subjects With Malignant Pleural Mesothelioma

Terminated·VVerastem, Inc.·Phase 2·NCT01870609·344 enrolled

Advanced Lymphoma1 trial

Molecular Analysis for Therapy Choice (MATCH)

Active, not recruiting·NNational Cancer Institute (NCI)·Phase 2·NCT02465060·6,452 enrolled

Thyroid Cancer1 trial

Phase II of Avutometinib (VS-6766) and Defactinib In RAF Dimer-Driven RAI-Refractory Differentiated and Anaplastic Thyroid Cancer Patients

Recruiting·MMemorial Sloan Kettering Cancer Center·Phase 2·NCT06007924·30 enrolled

Sources

References

[1]
ClinicalTrials.gov — 25 trial records for Defactinib. U.S. National Library of Medicine, National Institutes of Health.
[2]
ChEMBL — Defactinib compound record. European Bioinformatics Institute (EMBL-EBI).
[3]
Open Targets Platform — Drug–disease associations for Defactinib. EMBL-EBI & Wellcome Sanger Institute.
[4]
SEC EDGAR — Verastem, Inc. company filings. U.S. Securities and Exchange Commission.

Details

Drug Info

Quick Facts

Mechanism of Action: Focal Adhesion Kinase 1 Inhibitor; Protein Tyrosine Kinase 2 Beta Inhibitor[2]
Modality: Small molecule[2]
Highest Phase: Phase 3[1]
Company: VVerastem, Inc.

Defactinib

Status by Indication[3][1]

Competitive Landscape

Expected Milestones

Q4 2026

Q1 2027

Q2 2027

Q3 2027

Trials by Indication[1]

Ovarian Cancer3 trials

Avutometinib2 trials

Non-Small Cell Lung Cancer2 trials

Pancreatic Ductal Adenocarcinoma1 trial

Colorectal Cancer1 trial

Glioblastoma1 trial

Advanced Cancer1 trial

Advanced Solid Malignancies1 trial

Pleural Mesothelioma1 trial

Absorption1 trial

Pancreatic Adenocarcinoma1 trial

Gynecologic Cancer1 trial

Adenocarcinoma1 trial

Gastric Cancer1 trial

MDS1 trial

Hematologic Malignancies1 trial

Cutaneous Melanoma1 trial

Trial1 trial

Malignant Pleural Mesothelioma1 trial

Advanced Lymphoma1 trial

Thyroid Cancer1 trial

References

Drug Info

Quick Facts

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