> Trialight public data. Index of pages: https://trialight.com/llms.txt
> Web page: https://trialight.com/data/asset/zeprumetostat-9e11a650-d32c-494d-b12e-8bcef31c567e
> Record changed: 2026-10-29

# Zeprumetostat

Highest phase reached

Phase 2

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL5939817)

Drug type

Small molecule

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL5939817)

## Development status

**Listing at source**

Listed

**Highest phase reached**

Phase 2

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL5939817)

## Names and chemistry

**Drug type**

Small molecule

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL5939817)

**Drug name**

Zeprumetostat

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL5939817)

**Molecular weight**

548.73

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL5939817)

**Structure (SMILES)**

CCc1c(N(CC)C2CCOCC2)cc2oc(CN3CCCCC3)cc2c1C(=O)NCc1c(C)cc(C)\[nH\]c1=O

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL5939817)

### Other names (18)

- linperlisib and shr2554
- shr 2554
- SHR-2554
- shr2554
- SHR2554
- SHR2554 Tablet
- SHR2554 tablets
- SHR2554 Tablets
- tln 254
- TLN-254
- tln254
- TLN254
- zeprumetostat
- Zeprumetostat
- zeprumetostat \[INN\]
- ZEPRUMETOSTAT \[USAN\]
- zeprumetostat inn
- zeprumetostat usan

## Identifiers

**CAS registry numbers**

- 2098545-98-1

**ChEMBL ID**

CHEMBL5939817

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL5939817)

**InChIKey**

YLZVNQZYAYVUCW-UHFFFAOYSA-N

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL5939817)

**PubChem compound IDs**

- 135332280

**FDA ingredient codes (UNII)**

- XLJ9D8HE8Y

## Regulatory information

### Other regulatory facts

**First in class**

No

**Orphan designation**

No

## Pharmacology

### Drug classification

**Pharmacology name**

zeprumetostat

**Type**

Synthetic organic

**Drug name stem**

\-stat

**Approval recorded by Guide to Pharmacology**

Yes

### Mechanisms of action (4)

- **Action**  
Inhibition

**Action type**  
Inhibitor

**Target**  
enhancer of zeste 2 polycomb repressive complex 2 subunit

**Gene symbol**  
EZH2

**Protein identifier**  
Q15910

**Median affinity**

8.24

**Affinity units**  
pIC50
- **Action**  
Inhibition

**Action type**  
Inhibitor

**Target**  
enhancer of zeste 2 polycomb repressive complex 2 subunit

**Gene symbol**  
EZH2

**Protein identifier**  
Q15910

**Median affinity**

8.4

**Affinity units**  
pIC50
- **Action**  
Inhibition

**Action type**  
Inhibitor

**Target**  
enhancer of zeste 2 polycomb repressive complex 2 subunit

**Gene symbol**  
EZH2

**Protein identifier**  
Q15910

**Median affinity**

9.06

**Affinity units**  
pIC50
- **Action**  
Inhibition

**Action type**  
Inhibitor

**Target**  
enhancer of zeste 1 polycomb repressive complex 2 subunit

**Gene symbol**  
EZH1

**Protein identifier**  
Q92800

**Median affinity**

7.72

**Affinity units**  
pIC50

### Investigated indications

- **Condition**  
Neoplasms

**Highest recorded phase**  
2

**Condition identifier**  
EFO:0000616

**Subject identifier**  
D009369

### Open Targets indications (17)

- **Condition identifier**  
EFO\_0000616
- **Condition identifier**  
MONDO\_0000430

**Highest recorded phase**  
3
- **Condition identifier**  
MONDO\_0001056

**Highest recorded phase**  
2
- **Condition identifier**  
MONDO\_0003219

**Highest recorded phase**  
2
- **Condition identifier**  
MONDO\_0004967

**Highest recorded phase**  
2
- **Condition identifier**  
MONDO\_0005036

**Highest recorded phase**  
2
- **Condition identifier**  
MONDO\_0005070
- **Condition identifier**  
MONDO\_0005233

**Highest recorded phase**  
2
- **Condition identifier**  
MONDO\_0005575

**Highest recorded phase**  
2
- **Condition identifier**  
MONDO\_0007254

**Highest recorded phase**  
2
- **Condition identifier**  
MONDO\_0008315

**Highest recorded phase**  
2
- **Condition identifier**  
MONDO\_0009348

**Highest recorded phase**  
1
- **Condition identifier**  
MONDO\_0015759

**Highest recorded phase**  
1
- **Condition identifier**  
MONDO\_0015760

**Highest recorded phase**  
1
- **Condition identifier**  
MONDO\_0018874

**Highest recorded phase**  
2
- **Condition identifier**  
MONDO\_0018881

**Highest recorded phase**  
2
- **Condition identifier**  
MONDO\_0018906

**Highest recorded phase**  
2

## Chemical properties

**Hydrogen bond acceptors**

6

**Hydrogen bond donors**

2

**Polar surface area**

90.81

**Calculated partition coefficient (ALogP)**

5.22

**Calculated partition coefficient (XLogP)**

4.6

**Prodrug**

No

**Chirality**

Achiral

**Inorganic**

No

**Rule-of-five violations**

2

**Rotatable bonds**

9

**Heavy atoms**

40

**Molecular formula**

C32H44N4O4

**Monoisotopic mass**

548.33625590

**Natural product**

No

## Related records

### Trials (42)

- A Clinical Study on the Efficacy and Safety of Zeprumetostat in Relapsed/Refractory Large Granular Lymphocyte Leukemia
- A Food Effect Study of SHR2554 on Healthy Chinese Male Adult Subjects
- A Itraconazole Effect Study of SHR2554 on Healthy Chinese Adult Subjects
- A Phase 1 Study of SHR2554 in Subjects With Relapsed or Refractory Mature Lymphoid Neoplasms
- A Phase II Study of SHR2554 in Patients With Relapsed or Refractory Follicular Lymphoma
- A Relative Bioavailability Study of Different Processes of SHR2554 Tablets in Healthy Adult Subjects
- A Rifampin Effect Study of SHR2554 on Healthy Chinese Adult Subjects
- A Study of HRS-5041 Tablets Combined With Antitumor Therapy in Subjects With Advanced Prostate Cancer
- A Study of SHR2554 Alone or in Combination With SHR3680 in the Treatment of mCRPC
- A Study of SHR2554 With Chemotherapy in Treatment-naïve Patients With Peripheral T-cell Lymphoma
- A Study of SHR3680, HS-20093 and SHR2554 in Subjects With Prostate Cancer
- A Study of TLN-254 in Participants With Relapsed or Refractory T-cell Lymphoma
- A Study to Evaluate the Mass Balance of \[14C\]SHR2554 in Healthy Adult Volunteers
- A Umbrella Study in R/R PTCL Guided by Molecular Subtypes
- Effect of Fluconazole on Pharmacokinetics of SHR2554 in Healthy Subjects
- Effect of Omeprazole on Pharmacokinetics of SHR2554 in Healthy Subjects
- Exploratory Clinical Study of SHR-0302 and SHR-2554 in Patients With Relapsed/Refractory Peripheral T Cell Lymphoma
- EZH2 Inhibitor Zeprumetostat in Combination Therapy for Patients With Relapsed or Refractory Mature T-cell and NK-cell Lymphomas
- Genotype-guided Targeted Agents Plus EZH2i for Primary Refractory PTCL
- Linperlisib Combined With EZH2 Inhibitor in Relapsed/Refractory Peripheral T-cell Lymphoma (PTCL)

### In development for (1)

- Neoplasm Phase 2

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