OnCo
drugsProductPhase 3

Nemtabrutinib

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 as of mid-2026. Also inhibits other kinases (ERK pathway), which may add activity in Richter transformation.

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Nemtabrutinib
PubChem
Mechanism, step by step
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1.Binds the BTK ATP pocket reversibly, unaffected by C481S

Modality
Small-molecule non-covalent BTK inhibitor
Mechanism
Reversible ATP-competitive inhibitor of wild-type and C481S BTK, with off-target activity on ERK-pathway kinases.
Brand / code
MK-1026, ARQ-531
Dosing & schedule
Route
Oral
Schedule
65 mg once daily (RP2D)
Monitoring
Dysgeusia, neutropenia, hypertension, infections

Safety

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Toxicity profile
Adverse eventAny gradeGrade 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.

Trials

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Recruiting now (live from ClinicalTrials.gov)

Recruiting trials near you · live from ClinicalTrials.gov
Nemtabrutinib
intervention: Nemtabrutinib
Open on ClinicalTrials.gov →

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Landmark trials in OnCo

Latest papers

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Literature trend5 papers in the last 12 monthsHow this is computed
Latest papers · live from Europe PMC
Open in Europe PMC

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.

Connected

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