Table 1.
Molecule targeted drugs for the treatment of HCC
Drug | Molecular targets | Pharmacology | Treatment | Registrat |
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approved treatment in China | approval date in China | approved treatment globally | global approval date | ||||
Sorafenib | BRAF, c-KIT, FLT-3, VEGFR-2, 3, and PDGFR-p | LMW-TKI | 1st | HCC | Jun 2008 | HCC | Nov 2007 |
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Lenvatinib | VEGFR-1–3, FGFR-1–4, PDGFR-α, RET, and KIT | LMW-TKI | 1st | HCC | Sep 2018 | HCC | Aug 2018 |
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Regorafenib | VEGFR-1–3,TIE-2, FGFR-1–2, KIT, and RAF | LMW-TKI | 2nd | HCC | Dec 2017 | HCC | Apr 2017 |
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Cabozantinib | VEGFR-1–3, C-MET, AXL, KIT, RET, FLT3,and TIE-2 | LMW-TKI | 2nd | − | HCC | Jan 2019 | |
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Ramucirumab | VEGFR-2 | Monoclonal antibody | 2nd | − | HCC | May 2019 | |
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Apatinib | VEGFR-2 | LMW-TKI | 2nd | HCC | Dec 2020 | Orphan Drug Designation (FDA) for adenoid cystic carcinoma | Feb 2021 |
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Donafenib | Raf-1, mVEGFR-2, mVEGFR-3, and B-RAF | LMW-MKI | 1st | IND application for late-stage gastrointestinal tumors | Aug 2020 | − | − |
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Anlotinib | VEGFR, FGFR, PDGFR, and c-kit | LMW-MKI | 2nd 3rd | NSCLC and sarcoma | Jun 2019 | − | − |
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Bevacizumab + atezolizumab | VEGFR-2, VEGF-A, and VEGF | Monoclonal antibody | 1st | HCC | Oct 2020 | HCC | May 2020 |
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PD-L1 | Monoclonal antibody | ||||||
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Pembrolizumab | PD-1 | Monoclonal antibody | 2nd | ESCC | Jun 2020 | HCC | Nov 2018 |
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Camrelizumab | PD-1 | lgG4 antibody | 2nd | HCC | Mar 2020 | − | − |
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Nivolumab | PD-1 | 2nd | NSCLC | Jun 2018 | HCC | Sep 2017 | |
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Sintilimab + IBI305 | PD-1 | lgG4 antibody | 1st | HCC | Jan 2021 | − | − |
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VEGFR-2, VEGF-A, and VEGF (biosimilar of bevacizumab) | Monoclonal antibody | − | − |
BRAF, B-rapidly accelerated fibrosarcoma; LMW, low-molecular-weight; NSCLC, non-small-cell lung carcinoma, IND, investigational new drug; ESCC, esophageal squamous-cell carcinoma.