Nemtabrutinib
Highest phase reached
Phase 3
Drug type
Small molecule
- Listing at source
- Listed
- Highest phase reached
- Phase 3
- Drug type
- Small molecule
- Drug name
- Nemtabrutinib
- Molecular weight
- 478.94
- Structure (SMILES)
- O=C(c1ccc(Oc2ccccc2)cc1Cl)c1c[nH]c2ncnc(N[C@@H]3CC[C@@H](CO)OC3)c12
- arq 531
- ARQ-531
- mk 1026
- MK-1026
- nemtabrutinib
- Nemtabrutinib
- nemtabrutinib [INN]
- NEMTABRUTINIB [USAN]
- Nemtabrutinib [WHO-DD]
- nemtabrutinib inn
- nemtabrutinib usan
- nemtabrutinib who dd
- CAS registry numbers
- 2095393-15-8
- ChEMBL ID
- CHEMBL4756476
- InChIKey
- JSFCZQSJQXFJDS-QAPCUYQASA-N
- PubChem compound IDs
- 129045720
- FDA ingredient codes (UNII)
- JTZ51LIXN4
- Patents
- 0
- Designations
- 1
- First in class
- No
- Fast track
- No
- Breakthrough designation
- No
- Orphan designation
- No
- Priority review
- No
- Orphan exclusivity
- No
- Accelerated approval
- No
- Pharmacology name
- nemtabrutinib
- Type
- Synthetic organic
- Drug name stem
- -tinib
- Action
- Inhibition
- Action type
- Inhibitor
- Target
- YES proto-oncogene 1, Src family tyrosine kinase
- Gene symbol
- YES1
- Protein identifier
- P07947
- Median affinity
- 8.38
- Affinity units
- pIC50
- Action
- Inhibition
- Action type
- Inhibitor
- Target
- tec protein tyrosine kinase
- Gene symbol
- TEC
- Protein identifier
- P42680
- Median affinity
- 8.24
- Affinity units
- pIC50
- Action
- Inhibition
- Action type
- Inhibitor
- Target
- BLK proto-oncogene, Src family tyrosine kinase
- Gene symbol
- BLK
- Protein identifier
- P51451
- Median affinity
- 8.01
- Affinity units
- pIC50
- Action
- Inhibition
- Action type
- Inhibitor
- Target
- BMX non-receptor tyrosine kinase
- Gene symbol
- BMX
- Protein identifier
- P51813
- Median affinity
- 8.28
- Affinity units
- pIC50
- Action
- Inhibition
- Action type
- Inhibitor
- Target
- Bruton tyrosine kinase
- Gene symbol
- BTK
- Protein identifier
- Q06187
- Median affinity
- 8.6
- Affinity units
- pIC50
- Condition
- Leukemia, Lymphocytic, Chronic, B-Cell
- Highest recorded phase
- 3
- Condition identifier
- EFO:0000095
- Subject identifier
- D015451
- Condition
- Neoplasms
- Highest recorded phase
- 1
- Condition identifier
- EFO:0000616
- Subject identifier
- D009369
- Condition
- Liver Diseases
- Highest recorded phase
- 1
- Condition identifier
- EFO:0001421
- Subject identifier
- D008107
- Condition
- Hematologic Neoplasms
- Highest recorded phase
- 1
- Condition identifier
- EFO:0001642
- Subject identifier
- D019337
- Condition identifier
- EFO_0000095
- Highest recorded phase
- 3
- Condition identifier
- EFO_0000616
- Highest recorded phase
- 1
- Condition identifier
- EFO_0001421
- Highest recorded phase
- 1
- Condition identifier
- EFO_0001642
- Highest recorded phase
- 1
- Condition identifier
- MONDO_0002083
- Highest recorded phase
- 2
- Condition identifier
- MONDO_0004948
- Highest recorded phase
- 3
- Condition identifier
- MONDO_0005059
- Highest recorded phase
- 3
- Condition identifier
- MONDO_0005070
- Highest recorded phase
- 1
- Condition identifier
- MONDO_0005402
- Highest recorded phase
- 3
- Condition identifier
- MONDO_0017604
- Highest recorded phase
- 2
- Condition identifier
- MONDO_0018876
- Highest recorded phase
- 2
- Condition identifier
- MONDO_0018905
- Highest recorded phase
- 2
- Condition identifier
- MONDO_0018906
- Highest recorded phase
- 2
- Condition identifier
- MONDO_0044881
- Highest recorded phase
- 1
- Condition identifier
- MONDO_0100280
- Highest recorded phase
- 2
Reported adverse events
- Event
- acetabulum fracture
- Reports
- 1
- Reporting signal score
- 9.08235
- NCT05347225
- NCT05624554
- NCT05947851
- NCT06136559
- NCT05673460
- NCT06442436
- Hydrogen bond acceptors
- 7
- Hydrogen bond donors
- 3
- Polar surface area
- 109.36
- Calculated partition coefficient (ALogP)
- 4.59
- Calculated partition coefficient (XLogP)
- 4.3
- Prodrug
- No
- Chirality
- Single enantiomer
- Inorganic
- No
- Rule-of-five violations
- 0
- Rotatable bonds
- 7
- Heavy atoms
- 34
- Molecular formula
- C25H23ClN4O4
- Monoisotopic mass
- 478.1407829
- Natural product
- No
- Recorded assays
- 134
- Active assays
- 85
Active assay types
- Confirmatory
Related records
Trials (24)
- A Clinical Study of Nemtabrutinib in Japanese Participants With Hematological Malignancies (MK-1026-002)
- A Clinical Trial of Nemtabrutinib in Participants With Severe Kidney Disease (MK-1026-027)
- A Study of Nemtabrutinib (MK-1026) in China Participants With Relapsed or Refractory Hematologic Malignancies (MK-1026-005)
- A Study of Nemtabrutinib (MK-1026) in Participants With Relapsed or Refractory Hematologic Malignancies (ARQ 531-101/MK-1026-001)
- A Study of Nemtabrutinib (MK-1026) Versus Comparator (Investigator's Choice of Ibrutinib or Acalabrutinib) in First Line (1L) Chronic Lymphocytic Leukemia (CLL)/ Small Lymphocytic Lymphoma (SLL) (MK-1026-011/BELLWAVE-011)
- A Study of Nemtabrutinib in Participants With Moderate Hepatic Impairment (MK-1026-015)
- A Study of Nemtabrutinib Plus Venetoclax vs Venetoclax + Rituximab (VR) in Second-line (2L) + Relapsed/Refractory (R/R) Chronic Lymphocytic Leukemia/Small Lymphocytic Lymphoma (CLL/SLL) (MK-1026-010/BELLWAVE-010).
- A Study of Nemtabrutinib vs Chemoimmunotherapy for Participants With Previously Untreated Chronic Lymphocytic Leukemia/Small Lymphocytic Lymphoma (CLL/SLL) Without TP53 Aberrations (MK-1026-008, BELLWAVE-008)
- A Study of the Effect of Diltiazem on the Plasma Levels of Nemtabrutinib (MK-1026-022)
- A Study of the Effect of Efavirenz on the Plasma Levels of Nemtabrutinib (MK-1026-014)
- A Study of the Effect of Nemtabrutinib (MK-1026) on the Plasma Levels of Digoxin in Healthy Participants (MK-1026-012)
- A Study of the Effects of Itraconazole on the Plasma Levels of Nemtabrutinib (MK-1026-013)
- A Study of Zilovertamab Vedotin (MK-2140) as Monotherapy and in Combination in Participants With Aggressive and Indolent B-cell Malignancies (MK-2140-006)
- A Study to Compare Forms of Nemtabrutinib (MK-1026) in Healthy Adult Participants (MK-1026-007)
- A Study to Evaluate the Effect of Food on Nemtabrutinib (MK-1026) in Healthy Participants (MK-1026-016)
- A Study to Evaluate the Effect of Food on Nemtabrutinib (MK-1026) in Healthy Participants (MK-1026-017)
- Efficacy and Safety of Nemtabrutinib (MK-1026) in Participants With Hematologic Malignancies (MK-1026-003)
- Nemtabrutinib and Lisocabtagene Maraleucel for the Treatment of Relapsed/Refractory Chronic Lymphocytic Leukemia/Small Lymphocytic Lymphoma
- Nemtabrutinib and Pembrolizumab for the Treatment of Richter Transformation, Diffuse Large B-cell Lymphoma Subtype
- Nemtabrutinib and Venetoclax for the Treatment of Patients With Chronic Lymphocytic Leukemia or Small Lymphocytic Lymphoma
In development for (5)
- B-cell chronic lymphocytic leukemia Phase 3
- Hematopoietic and lymphoid cell neoplasm Phase 1
- Liver disorder Phase 1
- Lymphoid neoplasm Phase 1
- Neoplasm Phase 1