Table 3.

Clinical trials with non-covalent BTK inhibitors

Non-covalent BTK inhibitor	Phase	Patient population	Strategy	ClinicalTrials.gov ID	Status
Vecabrutinib	I/II dose escalation and expansion trial	CLL/SLL or NHL (including LPL/WM, MCL, MZL, ABC-DLBCL, FL) patients who have failed prior standard of care therapies including a BTK inhibitor where one is approved for the indication	Monotherapy	NCT03037645	Terminated
ARQ 531	I/II dose escalation and expansion trial	Dose escalation cohorts: R/R CLL/SLL, FL, MCL, MZL, and WM patients who have received ≥ 2 prior systemic therapies; expansion cohorts include R/R CLL/SLL after ≥ 2 prior systemic therapies including a covalent BTKi, with or without a C481 mutation	Monotherapy	NCT03162536	Recruiting
Fenebrutinib	Ia dose escalation trial	R/R NHL (including FL, DLBCL, MCL, PLL/WM) or CLL	Monotherapy	NCT01991184	Active, not recruiting
LOXO-305	I/II dose escalation and expansion trial	CLL/SLL or NHL patients who have failed or are intolerant to standard of care	Monotherapy; combination therapy	NCT03740529	Recruiting
LOXO-305	III	MCL patients who have been previously treated with at least one prior line of systemic therapy and were BTK inhibitor naive	Monotherapy (versus investigator choice of BTK Inhibitor)	NCT04662255	Not yet recruiting
LOXO-305	III	CLL/SLL patients who were previously treated with a covalent BTK inhibitor	Monotherapy (versus idelalisib plus rituximab or bendamustine plus rituximab)	NCT04666038	Not yet recruiting

CLL/SLL chronic lymphocytic leukemia/small lymphocytic lymphoma, NHL non-Hodgkin's lymphoma, LPL lymphoplasmacytic lymphoma, WM Waldenstrom's macroglobulinemia, MCL mantle cell lymphoma, MZL marginal zone lymphoma, DLBCL diffuse large B cell lymphoma, ABC-DLBCL the activated B cell subtype of DLBCL, FL follicular lymphoma, BTK Bruton tyrosine kinase, R/R relapsed and/or refractory, PLL prolymphocytic leukemia