Expansion
Monoclonal antibodies, tyrosine kinase inhibitors and checkpoint inhibitors
Expansion
Naming conventions
- -mab: monoclonal antibody
- -nib: small molecule kinase inhibitor
- -ximab chimeric, -zumab humanised, -umab fully human
Monoclonal antibodies
- Trastuzumab: HER2 in breast and gastric cancer. Causes cardiomyopathy, requiring echocardiographic monitoring, and it is additive with anthracyclines
- Rituximab: CD20 on B cells. Risk of hepatitis B reactivation
- Bevacizumab: VEGF. Hypertension, bleeding, impaired wound healing, perforation
- Cetuximab: EGFR; ineffective if KRAS is mutated
Tyrosine kinase inhibitors
- Imatinib: BCR-ABL in chronic myeloid leukaemia, the landmark example
- Erlotinib, osimertinib: EGFR in lung cancer
- Class effects: rash, diarrhoea, hypertension, QT prolongation
Immune checkpoint inhibitors
- PD-1 (nivolumab, pembrolizumab) and CTLA-4 (ipilimumab)
- Release the brakes on T cells, causing immune-related adverse events in any organ: colitis, hepatitis, pneumonitis, thyroiditis, hypophysitis. Treated with steroids, not by stopping alone
The unifying principle is that toxicity follows the target’s normal function rather than affecting all dividing cells.