Review Article
Role of ErbB1 in the Underlying Mechanism of Lapatinib-Induced Diarrhoea: A Review
Table 1
Comparison of incidence of diarrhoea in ErbB1 targeted therapies.
| Type of ErbB1 TKI | Receptor binding | Target | Indication | Route of administration | Diarrhoea incidence | References | All grades (%) | Severe grade 3-4 (%) |
| Monoclonal antibodies (mAbs) Cetuximab (Erbitux®/C225) | Irreversible | Extracellular domain III of ErbB1 | HNSCC, metastatic colorectal cancer | Intravenous | 3% | 1.7% | [45] | Panitumumab (Vectibix®) | Irreversible | Extracellular domain III of ErbB1 | Metastatic colorectal cancer, solid tumours | Intravenous | 20% | 1.3% | [46] | Nimotuzumab (h-R3) | Irreversible | Competitive binding to extracellular domain III of ErbB1 (353–358) with ligand | HNSCC, metastatic pancreatic cancer, oesophageal cancer, gastric cancer | Intravenous | 2.73% | 0.91% | [47] | Necitumumab (Portrazza™) | Irreversible | Competitive binding to extracellular domain III of ErbB1 (384–409) with ligand | NSCLC, solid tumours | Intravenous | 7% | 2% | [48] | First generation Erlotinib (Tarceva®) | Reversible | ErbB1 | NSCLC, pancreatic cancer | Oral | 43.4%-69.2% | 1%-17% | [49–51] | Gefitinib (Iressa®) | Reversible | ErbB1 | NSCLC | Oral | 35.7%-56% | 1%-3.8% | [42, 50] | Lapatinib (Tykerb/Tyverb®) | Reversible | ErbB1, ErbB2 | Breast cancer | Oral | 58%-78% | 23.3%-25% | [8, 52] | Second generation Neratinib (Nerlynx®) | Irreversible | ErbB1, ErbB2, ErbB4 | ErbB2-positive breast cancer | Oral | 95% | 39.8% | [53] | Afatinib (Giotrif®) | Irreversible | ErbB1, ErbB2, ErbB3, ErbB4 | NSCLC | Oral | 42%-92.9% | 10%-16% | [50, 54] | Dacomitinib (Vizimpro®) | Irreversible | ErbB1, ErbB2, ErbB4 | NSCLC | Oral | 87% | 8% | [55] | Third generation Osimertinib (Tagrisso®) | Irreversible | T790M ErbB1 mutation | NSCLC | Oral | 47%-58% | 2%-3.3% | [42, 56] | Tucatinib (Tukys®) | Reversible | ErbB2 | ErbB2-positive breast cancer | Oral | 81% | 12.5% | [57] |
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Abbreviation: HNSCC: head and neck squamous cell carcinoma; NSCLC: non-small-cell lung cancer; T790M: Threonine790Methionine mutation.
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