From: Colony-stimulating factor 1 receptor (CSF1R) inhibitors in cancer therapy
Class | Target | Compound | Clinical Phase | Sponsor | Indication | ClinicalTrials.gov identifier | Status/Results | Reference |
---|---|---|---|---|---|---|---|---|
Small molecules | CSF1R (and cKIT, Flt3) | Pexidartinib (PLX3397, PLX108-01) | 2 | The Christie NHS Foundation Trust | KIT-mutated advanced acral and mucosal melanoma | NCT02071940 | Ongoing | - |
1/2 | Plexxikon | Unresectable or metastatic KIT-mutated melanoma | NCT02975700 | Ongoing | - | |||
2 | Plexxikon | Advanced castration-resistant prostate cancer with bone metastasis and high circulating tumor cell counts | NCT01499043 | Not yet reported | - | |||
2 | Plexxikon | Recurrent GBM | NCT01349036 | ORR: 0% CBR: 7/38 (18%) | ||||
1/2 | NCI | Refractory leukemias and refractory solid tumors, including neurofibromatosis type 1-associated plexiform neurofibromas | NCT02390752 | Ongoing | - | |||
2 | Plexxikon | Relapsed or refractory cHL | NCT01217229 | ORR: 1/20 (5%) | [15] | |||
1/2 | Plexxikon | Relapsed or refractory FLT3-ITD-positive acute myeloid leukemia | NCT01349049 | Ongoing | - | |||
1 | Plexxikon | Advanced, incurable, solid tumors in which the target kinases are linked to disease pathophysiology | NCT01004861 | Ongoing | - | |||
CSF1R (and Trk) | PLX7486 | 1 | Plexxikon | Solid tumors | NCT01804530 | Ongoing | - | |
CSF1R | ARRY-382 | 1 | Array BioPharma | Solid tumors | NCT01316822 | ORR: 0% CBR: 4/26 (15%) | [17] | |
CSF1R | JNJ-40346527 | 1/2 | Johnson& Johnson | cHL | NCT01572519 | ORR: 1/21 (5%) CBR: 11/21 (52%) | [16] | |
CSF1R | BLZ945 | 1/2 | Novartis | Solid tumors | NCT02829723 | Ongoing | - | |
Monoclonal antibodies | CSF1R | Emactuzumab (RG7155) | 1 | Roche | Solid tumors | NCT01494688 | PMR: 5/44 (11%) ORR: 0% CBR: 6/40 (24%) | [18] |
CSF1R | AMG820 | 1 | Amgen | Solid tumors | NCT01444404 | ORR: 1/25 (4%) CBR: 6/25 (24%) | [19] | |
CSF1R | IMC-CS4 (LY3022855) | 1 | Eli Lilly | Solid tumors | NCT01346358 | Ongoing | - | |
1 | Eli Lilly | Breast and prostate cancer | NCT02265536 | Ongoing | - | |||
CSF1 | MCS110 | 1/2 | Novartis | Prostate cancer | NCT00757757 | Terminated | - |