Synonyms: PND-1186 | PND1186
Compound class:
Synthetic organic
Comment: VS-4718 is an investigational, potent, reversible and orally active inhibitor of focal adhesion kinase (FAK; PTK2) [3]. FAK inhibitors are being investigated for their anti-cancer effects due to the association of increased FAK expression with tumor progression, and the links between integrins and FAK in the adhesion pathways [1].
Ligand Activity Visualisation ChartsThese are box plot that provide a unique visualisation, summarising all the activity data for a ligand taken from ChEMBL and GtoPdb across multiple targets and species. Click on a plot to see the median, interquartile range, low and high data points. A value of zero indicates that no data are available. A separate chart is created for each target, and where possible the algorithm tries to merge ChEMBL and GtoPdb targets by matching them on name and UniProt accession, for each available species. However, please note that inconsistency in naming of targets may lead to data for the same target being reported across multiple charts. ✖ |
|
No information available. |
Summary of Clinical Use |
VS-4718 is being evaluated in Phase 1 clinical trials in patients with leukemias (NCT02215629) and with metastatic non-hematologic malignancies (NCT01849744). |
Mechanism Of Action and Pharmacodynamic Effects |
FAK inhibition disrupts the integrin signaling axis which controls anchorage-independent growth of ovarian cancer cells and induces cell-cycle arrest followed by cell death [2]. This effect is observed in other cancer cell types [3]. |
Clinical Trials | |||||
Clinical Trial ID | Title | Type | Source | Comment | References |
NCT01849744 | Phase I Dose Escalation Study of VS-4718 in Subjects With Metastatic Non-Hematologic Malignancies | Phase 1 Interventional | Verastem, Inc. | ||
NCT02215629 | Dose Escalation Study in Acute Myeloid or B-Cell Acute Lymphoblastic Leukemia | Phase 1 Interventional | Verastem, Inc. |