TABLE 1.
Targeting Bruton's tyrosine kinase through the use of covalent and non‐covalent inhibitors
| Inhibitor | Binding mechanism | Present use | Stage | Reference |
|---|---|---|---|---|
| Ibrutinib |
Covalent Irreversible |
Lymphoproliferative disorders SARS‐CoV‐2 |
FDA Approved Phase III trials |
[100] |
| Acalabrutinib |
Covalent Irreversible |
Lymphoproliferative disorders |
FDA Approved Phase III trials |
[90] |
| Zanubrutinib |
Covalent Irreversible |
Lymphoproliferative disorders |
FDA Approved Phase III trials |
[93] |
| Evobrutinib |
Covalent Irreversible |
MS, SLE | Phase III trials | [63] |
| Fenebrutinib |
Non‐covalent Reversible |
CLL, DLBCL, MS | Phase III trials | [70] |
| Branebrutinib |
Covalent Irreversible |
RA, SLE, Sjögren's syndrome | Phase II trials | [68] |
| Tolebrutinib |
Covalent Irreversible |
MS | Phase III trials | [75] |
| Tirabrutinib |
Covalent Irreversible |
R/R lymphoproliferative disorders | Phase II trials | [94] |
| Remibrutinib |
Covalent Irreversible |
Urticaria | Phase II trials | [98] |
| Pirtobrutinib |
Non‐covalent Reversible |
Lymphoproliferative disorders C481‐mutant CLL |
Phase I trials Phase II trials |
[99] |
Abbreviations: CLL, chronic lymphocytic leukaemia; DLBCL, diffuse large B‐cell lymphoma; MS, multiple sclerosis; R/R, relapsed/refractory; RA, rheumatoid arthritis; SLE, systemic lupus erythematosus.