Table 2. Examples of covalent inhibitors in clinical trials.
No. | Structure and name | Target (therapeutic) | Warhead | Clinical stage |
1 |
![]() |
BTK inhibitor | α,β-Unsaturated carbonyl | III |
2 |
![]() |
BTK inhibitor | α,β-Unsaturated carbonyl | III |
3 |
![]() |
KRAS inhibitor | α,β-Unsaturated carbonyl | II |
4 |
![]() |
EGFR inhibitor | α,β-Unsaturated carbonyl | II |
5 |
![]() |
JAK3 inhibitor | α,β-Unsaturated carbonyl | II |
6 |
![]() |
BTK inhibitor | α,β-Unsaturated carbonyl | II |
7 |
![]() |
FGFR inhibitor | α,β-Unsaturated carbonyl | II |
8 |
![]() |
BTK inhibitor | α,β-Unsaturated propargylamide | II |
9 |
![]() |
BTK inhibitor | α,β-Unsaturated carbonyl | II |