Common solid tumour-targeted therapies and their toxicities19
| Drug class/target | Drug name | Cancer sites | Common or significant toxicities |
|---|---|---|---|
| ALK | Alectinib, brigatinib, ceritinib, lorlatinib | Non-small cell lung cancer | Diarrhoea |
| BRAF | Dabrafenib, encorafenib, vemurafenib | Melanoma | Electrolyte derangement, QTc prolongation, hepatoxicity, uveitis, iritis and retinal vein occlusion, cutaneous and non-cutaneous squamous cell carcinoma, new primary melanoma |
| Sorafenib (and VEGF) | Renal cell, hepatocellular and thyroid cancers | QTc prolongation, thyroid dysfunction, hypocalcaemia, aneurysm, artery dissection in patients with or without hypertension | |
| CDK4/6 | Abemaciclib, palbociclib, ribociclib | Breast cancer | Interstitial lung disease, hepatotoxicity, myelosuppression |
| EGFR | Afatinib, erlotinib, gefitinib, mobocertinib, osimertinib | Non-small cell lung cancer | Diarrhoea, QTc prolongation |
| Cetuximab, panitumumab | Colorectal and head and neck cancer | Electrolyte derangement, hypersensitivity reactions, interstitial lung disease | |
| FGFR2 | Pemigatinib | Cholangiocarcinoma | Hyperphosphataemia, eye and vision changes |
| HER2 monoclonal antibody | Trastuzumab, pertuzumab | Breast, gastric, oesophageal and lung cancers | Cardiotoxicity |
| HER2 antibody drug conjugate | Trastuzumab emtansine | Breast cancer | Hepatic toxicity, neurotoxicity, hypersensitivity reactions, interstitial lung disease |
| Trastuzumab deruxtecan | Breast cancer | Myelosuppression, cardiotoxicity, pneumonitis | |
| HER2 TKI | Lapatinib, neratinib (also EGFR), tucatinib | Breast cancer | Diarrhoea |
| KRAS (G12C) | Sotorasib | Non-small cell lung cancer | Hepatotoxicity, cough |
| MEK | Binimetinib, cobimetinib, trametinib | Melanoma and non-small cell lung cancer | Gastrointestinal perforation, hypertension |
| MET | Tepotinib | Non-small cell lung cancer | Interstitial lung disease, hepatoxicity |
| mTOR | Everolimus, temsirolimus | Neuroendocrine, renal cell and breast cancers | Suicidal thoughts, hyperglycaemia, nephrotoxicity |
| PARP | Niraparib, olaparib | Ovarian, fallopian and peritoneal cancers | Diarrhoea |
| PI3K | Alpelisib | Breast cancer | Hyperglycaemia |
| RET | Selpercatinib | Non-small cell lung cancer | Hypertension |
| ROS1 | Crizotinib (also ALK) entrectinib | Non-small cell lung cancer | Cardiac failure |
| SMO | Vismodegib | Basal cell carcinoma | Diarrhoea |
| TRK | Entrectinib (also ROS1), larotrectinib | NTRK fusion-positive solid tumours | QT prolongation, hepatoxicity |
| VEGF | Bevacizumab | Colorectal, breast, renal cell, non-small cell lung, ovarian, cervical and hepatocellular cancers | Osteonecrosis of the jaw, aneurysm, and artery dissection in patients with or without hypertension, necrotising fasciitis, congestive heart failure, posterior reversible encephalopathy syndrome |
| Axitinib, cabozantinib, lenvatinib, nintedanib, pazopanib, regorafenib (and others), sorafenib (and BRAF), sunitinib (and others), vandetanib | Renal cell, thyroid (lenvatinib, vandetanib), non-small cell lung (nintedanib), colorectal, GIST and hepatocellular cancers (regorafenib) | Aneurysm and artery dissection in patients with or without hypertension |
GIST = gastrointestinal stromal tumor; TKI = tyrosine kinase inhibitor.