Pirtobrutinib

Non-covalent (reversible) BTK inhibitor

Response rate
~68% ORR (after covalent BTKi); 56% VGPR with venetoclax combo
Onset
Weeks
Route
Oral 200mg daily
Line
2nd
IgM effect
Reduction

Evidence summary

Non-covalent BTK inhibitor that retains activity after covalent BTK inhibitor resistance or intolerance. Being studied in combination with venetoclax (pirtobrutinib + venetoclax: 100% ORR, 56% VGPR in interim analysis). May overcome acquired BTK C481S resistance mutations.

Molecular targets (1)

MoleculeRoleExpressionEvidence
BTK (Bruton's Tyrosine Kinase)Key signaling kinase downstream of MYD88Constitutively activatedestablished