> Trialight public data. Index of pages: https://trialight.com/llms.txt
> Web page: https://trialight.com/data/asset/nemtabrutinib-70bd6eb4-bcf5-4265-a8f7-fbcdab7b9e59
> Record changed: 2026-10-13

# Nemtabrutinib

Highest phase reached

Phase 3

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL4756476)

Drug type

Small molecule

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL4756476)

## Development status

**Listing at source**

Listed

**Highest phase reached**

Phase 3

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL4756476)

## Names and chemistry

**Drug type**

Small molecule

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL4756476)

**Drug name**

Nemtabrutinib

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL4756476)

**Molecular weight**

478.94

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL4756476)

**Structure (SMILES)**

O=C(c1ccc(Oc2ccccc2)cc1Cl)c1c\[nH\]c2ncnc(N\[C@@H\]3CC\[C@@H\](CO)OC3)c12

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL4756476)

### Other names (12)

- arq 531
- ARQ-531
- mk 1026
- MK-1026
- nemtabrutinib
- Nemtabrutinib
- nemtabrutinib \[INN\]
- NEMTABRUTINIB \[USAN\]
- Nemtabrutinib \[WHO-DD\]
- nemtabrutinib inn
- nemtabrutinib usan
- nemtabrutinib who dd

## Identifiers

**CAS registry numbers**

- 2095393-15-8

**ChEMBL ID**

CHEMBL4756476

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL4756476)

**InChIKey**

JSFCZQSJQXFJDS-QAPCUYQASA-N

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL4756476)

**PubChem compound IDs**

- 129045720

**FDA ingredient codes (UNII)**

- JTZ51LIXN4

## Regulatory information

### Other regulatory facts

**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

### Drug classification

**Pharmacology name**

nemtabrutinib

**Type**

Synthetic organic

**Drug name stem**

\-tinib

### Mechanisms of action (5)

- **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

### Investigated indications (4)

- **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

### Open Targets indications (15)

- **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

### Trial references (6)

- NCT05347225  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT05347225)
- NCT05624554  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT05624554)
- NCT05947851  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT05947851)
- NCT06136559  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT06136559)
- NCT05673460  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT05673460)
- NCT06442436  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT06442436)

## Chemical properties

**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

## Evidence counts

**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)](https://trialight.com/data/trial/a-study-of-nemtabrutinib-mk-1026-versus-comparator-066c2f19-c33f-4973-b1bd-115b26cde5a8.md)
- 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](https://trialight.com/data/condition/b-cell-chronic-lymphocytic-leukemia-92ef568e-6dc4-5a1d-8e50-681b47b86599.md) Phase 3
- [Hematopoietic and lymphoid cell neoplasm](https://trialight.com/data/condition/hematopoietic-and-lymphoid-cell-neoplasm-ed3616fa-22fe-5984-94b4-745416e01ef9.md) Phase 1
- [Liver disorder](https://trialight.com/data/condition/liver-disorder-8388d30a-2581-5015-9ddf-adc5f6a331d7.md) Phase 1
- Lymphoid neoplasm Phase 1
- Neoplasm Phase 1

---

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