Table 1.
Summary of FAK inhibitors in clinical trials.
| Drug (Code Name), Trade Name |
Target (IC50) | Clinical Trial Studies (a, b) | No. of Clinical Trials (a) |
Phase (a) |
|---|---|---|---|---|
| GSK2256098 (GTPL7939) |
FAK (0.4 nM) | adenocarcinoma, adult healthy subject, intracranial and recurrent meningioma mesothelioma, pancreatic cancer, pulmonary arterial hypertension, solid cancer | 6; 4 completed, 2 active |
Phase I: 4 Phase II: 2 |
| VS-4718 (PND-1186) |
FAK (1.5 nM) | relapsed or refractory AML, relapsed or refractory B-Cell ALL, metastatic cancer, non-hematologic cancers, pancreatic cancer | 3; 2 terminated, 1 withdrawn |
Phase I: 3 |
| Defactinib (PF04554878, VS-6063) |
FAK (0.6 nM) Pyk2 (0.6 nM) |
advanced solid cancer, lung cancer, relapsed malignant and pleural mesothelioma, non-hematologic cancers, NSCLC, ovarian cancer, pancreatic cancer, PDAC | 21; 4 terminated, 6 completed 10 active 1 withdrawn |
Phase I: 9 Phase I/II: 2 Phase II: 10 |
| VS-6062 (PF00562271) |
FAK (1.5 nM) Pyk2 (14 nM) |
head and neck cancer, pancreatic cancer, prostatic cancer | 1; 1 completed | Phase I: 1 |
| CEP-37440 | FAK (2.3 nM) ALK (120 nM) |
advanced or metastatic solid tumors | 1; 1 completed | Phase I: 1 |
| BI-853520 (IN10018) |
FAK | colorectal cancer, metastatic melanoma, metastatic non hematologic malignancies, soft tissue sarcoma, stomach cancer | 3; 2 completed, 1 active |
Phase I: 3 |
(a) From www.clinicaltrials.gov (accessed 18 October 2021); (b) AML—acute myeloid leukemia; ALL—acute lymphocytic leukemia; NSCLC—non-small-cell lung carcinoma; PDAC—pancreatic ductal adenocarcinoma.