Table 4 FDA-approved drugs targeting macrophage in cancers
Drug | Sponsor/company | Mechanism of action/administration | Type of cancer | FDA approval | Ref. |
|---|---|---|---|---|---|
Plexxikon, (Pexidartinib (PLX-3397) | Daiichi Sankyo | Orally administered Pexidartinib is a small-molecule TKI with robust and specific action against the CSF1 receptor. CSF1, is overexpressed in many solid tumors, promotes the survival of TAMs and the development of monocytes into TAMs; capsules | Tenosynovial giant cell tumor | 2019 | |
Trabectedin (Yondelis) | Janssen | Induces apoptosis through the tumor necrosis factor receptor superfamily member 10 (TNFRSF10, also known as TRAIL) in monocytes and TAMs, reducing their numbers in human patients and mice; intravenous infusion. | Soft tissue sarcomas, ovarian cancer | 2015 | |
Sipuleucel-T (Provenge) | Dendreon | It is a fusion protein consisting of GM-CSF and prostatic acid phosphatase, which is utilized to stimulate antigen-specific T lymphocytes against the tumor. | Prostate cancer | 2010 | |
Carboplatin | Bristol-Myers Squibb | Treatment with platinum-based neoadjuvant chemotherapy has been shown to decrease markers associated with alternative macrophage activation. Macrophage depletion by CSF1R inhibitors (CSF1Ri) in the mouse models provides further evidence of a switch in TAM functions; intravenous infusion | High-grade ovarian cancer | 2003 | |
Paclitaxel (Taxol) | Mylan Pharmaceuticals | 2002 | |||
5-fluorouracil (Eloxatin) | Sanofi | The synergistic impact between 5-fluorouracil and macrophages leads to enhanced CRC cell death; intravenous infusion | Colorectal cancer | Initial approval in 1962, 2002 for CRC | |
Gemcitabine | Eli Lilly | Changes in innate immune cells, including increased infiltration of protumoral M2 TAMs and metabolic reprogramming, are an outcome of gemcitabine treatment; intravenous infusion | Pancreatic ductal adenocarcinoma (PDAC) | 1996 |
