FDA-approved medications for colon and rectal cancer consisting of both generic and brand names
FDA-approved individual drugs (CRC) | Mechanism of action |
---|---|
Ipilimumab | Prevent inhibition of T-cell mediated immune responses to tumors by binding CTLA-4 |
Bevacizumab (Mvasi) | Mvasi, a mAb, inactivates serum VEGF treating metastatic CRC |
Pembrolizumab | Binds to PD-1 inhibiting its interaction with PD-L1 and PD-L2. Enhances anti-tumor immune response and tumor immune monitoring |
Tucatinib | Inhibits HER-2 suppressing tumors by affecting cell proliferation and AKT and MAPK signaling |
Ziv-aflibercept (Zaltrap) | Inhibits VEGF-A and PIGF to reduce vascular permeability and inhibit neovascularization. Delay vision loss and advancement of metastatic CRC |
Irinotecan hydrochloride | Restricts DNA strands from elegating by attaching to the topoisomerase I-DNA complex and inhibiting its action, which causes fatal double-stranded splits in the DNA. Causes apoptosis as DNA damage is ineffectively repaired |
Nivolumab | Restores tumor-specific T-cell response in patients. Binds to PD-1, avert PD-L1 and PD-L2 from blocking the action of T-cells |
Ramucirumab | By binding to VEGFR2, it halts the ligands (VEGF-A, VEGF-C, and VEGF-D) from binding to it, blocking VEGF-stimulated receptor phosphorylation and the proliferation, permeability, and migration of human endothelial cells that are later caused by ligands |
Cetuximab | Blocks the binding of EGF, which in turn prevents EGFR activation. It also binds selectively to the EGFR and phosphorylates and activates receptor-associated kinases (MAPK, PI3K/AKT, and JAK/STAT) |
Regorafenib | At clinically attained concentrations it inhibits the function of VEGFR1, VEGFR2, VEGFR3, RET, PDGFR-alpha, PDGFR-beta, KIT, FGFR1, FGFR2, BRAFV600E, PTK5, TIE2, TrkA, RAF-1, BRAF, DDR2, SAPK2, Eph2A, and Abl |
Panitumumab | Panitumumab binds primarily to EGFR and prevents ligands from binding to EGFR |
Leucovorin calcium | By strengthening the bond between the active metabolite (5-FdUMP) and the enzyme thymidylate synthetase, leucovorin increases the action of fluorouracil |
CTLA-4: cytotoxic T lymphocyte antigen-4; mAb: monoclonal antibody; PD-1: programmed death-1; PD-L1: PD-ligand-1; HER-2: human epidermal growth factor receptor-2; AKT: AKT serine/threonine kinase; MAPK: mitogen-activated protein kinase; VEGF-A: vascular endothelial growth factor-A; PIGF: placental growth factor; I-DNA: I-motif DNA; VEGFR2: VEGF receptor 2 ; EGF: epidermal growth factor; EGFR: EGF receptor; PI3K: phosphatidylinositol-4,5-bisphosphate 3-kinase; JAK: Janus kinase; STAT: signal transducer and activator of transcription; RET: Ret proto-oncogene; PDGFR-alpha: platelet derived growth factor receptor alpha; KIT: KIT proto-oncogene, receptor tyrosine kinase; FGFR1: fibroblast growth factor receptor 1; PTK5: protein tyrosine kinase 5; TIE2: tyrosine kinase with immunoglobulin like and EGF like domains 2; RAF-1: Raf-1 proto-oncogene, serine/threonine kinase; BRAF: B-Raf proto-oncogene, serine/threonine kinase; DDR2: discoidin domain receptor tyrosine kinase 2; SAPK2: sucrose non-fermenting-1-related protein kinase 2; Eph2A: ephrin type-A receptor 2; Abl: a gene; 5-FdUMP: 5-fluorodeoxyuridine monophosphate; BRAFV600E: B-Raf proto-oncogene; TrkA: tropomyosin receptor kinase A