Nemtabrutinib is Merck's reversible BTK blocker, active against the C481S escape mutation, being tested against ibrutinib and acalabrutinib in first-line CLL.
BELLWAVE-001 (phase 1/2): ORR 53% (including partial response with lymphocytosis) at the 65 mg dose in relapsed CLL/SLL. Phase 3 BELLWAVE-011 (vs ibrutinib or acalabrutinib, untreated CLL) and BELLWAVE-008 (vs chemoimmunotherapy) are recruiting. Also inhibits other kinases (ERK pathway), which may add activity in Richter transformation.
Reversible ATP-competitive inhibitor of wild-type and C481S BTK, with off-target activity on ERK-pathway kinases. Connects to BTK (Bruton tyrosine kinase).
1.Binds the BTK ATP pocket reversibly, unaffected by C481S
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| Adverse event | Any grade | Grade 3+ |
|---|---|---|
| Dysgeusia | 21% | - |
| Neutropenia | - | 17% |
| Hypertension | 15% | - |
Rates read from the source. Blank cells mean the figure was not sourced, not that it is zero.
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Query for this drug: (TITLE:"Nemtabrutinib" OR ABSTRACT:"Nemtabrutinib" OR TITLE:"MK-1026" OR ABSTRACT:"MK-1026" OR TITLE:"ARQ-531" OR ABSTRACT:"ARQ-531") AND (cancer OR tumor OR tumour OR oncology OR carcinoma OR lymphoma OR leukemia OR leukaemia OR myeloma OR sarcoma OR melanoma OR glioma). Results are unfiltered search hits about Nemtabrutinib, not a curated reading list.
Shares Relapsed or refractory chronic lymphocytic leukaemia, BTK (Bruton tyrosine kinase), Chronic lymphocytic leukaemia, first treatment, Chronic lymphocytic leukaemia.
Shares Relapsed or refractory chronic lymphocytic leukaemia, BTK (Bruton tyrosine kinase), Chronic lymphocytic leukaemia, Small-molecule kinase inhibitors.
Shares BTK (Bruton tyrosine kinase), Chronic lymphocytic leukaemia, first treatment, Chronic lymphocytic leukaemia, Small-molecule kinase inhibitors.
Shares BTK (Bruton tyrosine kinase), Chronic lymphocytic leukaemia, first treatment, Chronic lymphocytic leukaemia, Small-molecule kinase inhibitors.
Shares Relapsed or refractory chronic lymphocytic leukaemia, BTK (Bruton tyrosine kinase), Chronic lymphocytic leukaemia, Small-molecule kinase inhibitors.
Shares Relapsed or refractory chronic lymphocytic leukaemia, Chronic lymphocytic leukaemia, Small-molecule kinase inhibitors.
Shares BTK (Bruton tyrosine kinase), Chronic lymphocytic leukaemia, first treatment, Chronic lymphocytic leukaemia, Small-molecule kinase inhibitors.
Shares Relapsed or refractory chronic lymphocytic leukaemia, Chronic lymphocytic leukaemia, Small-molecule kinase inhibitors.