Table 1 List of drugs and their targets used against HCC
From: Resistance a major hindrance to chemotherapy in hepatocellular carcinoma: an insight
S. No. | Name of the drug | Target molecule | Mechanism | Limitation | Year and references |
|---|---|---|---|---|---|
1 | Tamoxifen | Antagonist of estrogen receptor | To inhibit P-glycoprotein-mediated drug resistance | Minimum effect | 2000 [88] |
2 | 5-Fluoracil | Thymidylate synthase | Incorporated its metabolites into RNA and DNA | Requires co-treatment with leucovorin and methotrexate, to increase the anticancer activity of 5-Fu | 2003 [89] |
3 | Thalidomide | VEGF, inhibits TNF-α synthesis, inhibition of Ikβ kinase activity | Anti-angiogenic activity and immune-modulatory | Fatigue, somnolence, constipation | |
4 | Octreotide | Analogue of somatostatin receptors | Anti-tumor effect. | Somatostatin receptor type 2 (SSTR2) was found in some but not all patients with HCC | |
5 | Sorafenib | Raf, VEGFR2, VEGFR3, PDGFRs | Inhibits tumor angiogenesis by blocking the activation of the tyrosine kinase receptors | Hypertension, diarrhea, proteinuria, skin-related toxicities, an increased risk for thromboembolism and bleeding events | |
6 | Sunitinib | PDGFRs, KIT, RET, and FLT3 | Inhibits tumor angiogenesis by blocking the activation of the tyrosine kinase receptors | Modest clinical efficacy | 2009 [94] |
7 | Bevacizumab | VEGF | Blocks VEGF binding to its receptor | Low rate of response, gastrointestinal bleeding, including variceal bleeding | 2009 [95] |
8 | Erlotinib, gefitinib and cetuximab | EGFR | Tyrosine kinase inhibitor, acts on the epidermal growth factor receptor (EGFR) | Minimum effect | 2009 [96] |
9 | Doxorubicin | DNA topoisomerase II inhibitors | Induce histone eviction | The use of single agents in therapy is practically non-existent currently because of its erratic and low response | 2013 [97] |
10 | Cisplatin | DNA | Cross link with purine causes DNA damage and ultimately induces apoptosis | Allergic reactions, gastrointestinal disorders, decrease immunity to infections, kidney problems, hemorrhage | 2014 [98] |
11 | Oxaliplatin | DNA | Binds to guanine and cytosine leading to cross-linking of DNA | Increase autophagy level results in a tumor resistance Reduction of DYRK2 promotes cell proliferation, and resistance to Oxaliplatin | 2016 [99] |