> Trialight public data. Index of pages: https://trialight.com/llms.txt
> Web page: https://trialight.com/data/asset/valemetostat-tosylate-8197f007-8874-41e5-b0db-826a10c84937
> Record changed: 2026-11-04

# Valemetostat tosylate

Highest phase reached

Phase 2

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL4594405)

Drug type

Small molecule

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL4594405)

## Development status

**Listing at source**

Listed

**Highest phase reached**

Phase 2

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL4594405)

## Names and chemistry

**Drug type**

Small molecule

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL4594405)

**Drug name**

Valemetostat tosylate

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL4594405)

**Molecular weight**

660.23

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL4594405)

**Structure (SMILES)**

Cc1cc(C)c(CNC(=O)c2cc(Cl)c3c(c2C)O\[C@@\](C)(\[C@H\]2CC\[C@H\](N(C)C)CC2)O3)c(=O)\[nH\]1.Cc1ccc(S(=O)(=O)O)cc1

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL4594405)

### Other names (8)

- valemetostat tosilate
- Valemetostat tosilate
- VALEMETOSTAT TOSILATE \[JAN\]
- Valemetostat tosilate \[WHO-DD\]
- valemetostat tosilate jan
- valemetostat tosilate who dd
- valemetostat tosylate
- Valemetostat tosylate

## Identifiers

**CAS registry numbers**

- 1809336-93-3

**ChEMBL ID**

CHEMBL4594405

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL4594405)

**InChIKey**

JSBKGJUYSLVFPF-WJQUPPJOSA-N

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL4594405)

**FDA ingredient codes (UNII)**

- 6N79I7X5II

## 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

**Drug name stem**

\-stat

### Investigated indications (3)

- **Condition**  
Lymphoma

**Highest recorded phase**  
2

**Condition identifier**  
EFO:0000574

**Subject identifier**  
D008223
- **Condition**  
Neoplasms

**Highest recorded phase**  
1

**Condition identifier**  
EFO:0000616

**Subject identifier**  
D009369
- **Condition**  
Leukemia-Lymphoma, Adult T-Cell

**Highest recorded phase**  
2

**Condition identifier**  
MONDO:0019471

**Subject identifier**  
D015459

### Open Targets indications (17)

- **Condition identifier**  
EFO\_0000574

**Highest recorded phase**  
2
- **Condition identifier**  
MONDO\_0000430

**Highest recorded phase**  
2
- **Condition identifier**  
MONDO\_0004952

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

**Highest recorded phase**  
1
- **Condition identifier**  
MONDO\_0005086

**Highest recorded phase**  
1
- **Condition identifier**  
MONDO\_0005233

**Highest recorded phase**  
1
- **Condition identifier**  
MONDO\_0007256

**Highest recorded phase**  
1
- **Condition identifier**  
MONDO\_0008315

**Highest recorded phase**  
2
- **Condition identifier**  
MONDO\_0008433

**Highest recorded phase**  
1
- **Condition identifier**  
MONDO\_0015667

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

**Highest recorded phase**  
2
- **Condition identifier**  
MONDO\_0018874

**Highest recorded phase**  
1
- **Condition identifier**  
MONDO\_0018876

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

**Highest recorded phase**  
2
- **Condition identifier**  
MONDO\_0019471
- **Condition identifier**  
MONDO\_0019471

**Highest recorded phase**  
4
- **Condition identifier**  
MONDO\_0040679

**Highest recorded phase**  
1

### Trial references (3)

- NCT04102150  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT04102150)
- NCT04842877  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT04842877)
- NCT06244485  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT06244485)

## Chemical properties

**Hydrogen bond acceptors**

5

**Hydrogen bond donors**

2

**Polar surface area**

83.66

**Calculated partition coefficient (ALogP)**

4.49

**Prodrug**

No

**Chirality**

Single enantiomer

**Inorganic**

No

**Rule-of-five violations**

0

**Rotatable bonds**

5

**Heavy atoms**

45

**Molecular formula**

C33H42ClN3O7S

**Natural product**

No

## Related records

### Trials (8)

- [A Study of Valemetostat Tosylate in Combination With DXd ADCs in Subjects With Solid Tumors](https://trialight.com/data/trial/a-study-of-valemetostat-tosylate-in-combination-with-dxd-2ead9607-c47a-4f0a-a8f1-9969f30b5926.md)
- A Study of Valemetostat Tosylate Plus Pembrolizumab Versus Pembrolizumab Alone in First-Line NSCLC Without Actionable Genomic Alterations
- Efficacy and Safety of the Valemetostat in Patients With Selected Solid Tumors.
- Medical Access Program for Valemetostat Tosylate (DS 3201b) For The Treatment of Patients With Relapsed/Refractory (R/R) Peripheral T-cell Lymphoma (PTCL)
- Study of Valemetostat Tosylate as a Single Agent in Patients With Relapse/Refractory B-cell Lymphoma
- Targeted Treatment for Metastatic Prostate Cancer, The PREDICT Trial
- Valemetostat Tosylate (DS-3201b) Phase 2 Study in Relapsed or Refractory Adult T-cell Leukemia/Lymphoma
- Valemetostat Tosylate (DS-3201b), an Enhancer of Zeste Homolog (EZH) 1/2 Dual Inhibitor, for Relapsed/Refractory Peripheral T-Cell Lymphoma (VALENTINE-PTCL01)

### In development for (17)

- [Acute lymphoblastic leukemia](https://trialight.com/data/condition/acute-lymphoblastic-leukemia-a7f89294-3477-5920-8fe1-8aa51fcd1d63.md) Phase 1
- [Acute myeloid leukemia](https://trialight.com/data/condition/acute-myeloid-leukemia-b0971a7a-c18d-544e-bd7f-b1a13b9caa30.md) Phase 1
- Acute myeloid leukemia by FAB classification Phase 1
- Adult T-cell leukemia/lymphoma Phase 2
- [B-cell non-Hodgkin lymphoma](https://trialight.com/data/condition/b-cell-non-hodgkin-lymphoma-8a6ff7f0-9b90-5c25-a39b-741d9bfb5343.md) Phase 2
- [Follicular lymphoma](https://trialight.com/data/condition/follicular-lymphoma-88de1ce9-ab0e-5d65-85c4-45a681fa2931.md) Phase 2
- [Hepatocellular carcinoma](https://trialight.com/data/condition/hepatocellular-carcinoma-fc1014ac-5a3c-551d-98ea-95306009e299.md) Phase 1
- Hodgkins lymphoma Phase 2
- [Lymphoma](https://trialight.com/data/condition/lymphoma-de4db685-7419-5e0e-b958-4591ffd69d43.md) Phase 2
- [Mantle cell lymphoma](https://trialight.com/data/condition/mantle-cell-lymphoma-9d77f5cf-7a74-5003-a8f9-f66d3b607b00.md) Phase 2
- Mature T-cell and NK-cell non-Hodgkin lymphoma Phase 2
- [Neoplasm](https://trialight.com/data/condition/neoplasm-2a973797-359b-5982-907e-98f9b7c1a284.md) Phase 1
- [Non-small cell lung carcinoma](https://trialight.com/data/condition/non-small-cell-lung-carcinoma-a86c1d60-523f-5ea7-a5e1-39ed4a2296f8.md) Phase 1
- [Prostate cancer](https://trialight.com/data/condition/prostate-cancer-3659fc70-617b-5868-a093-ae819ffc6755.md) Phase 2
- [Renal cell carcinoma](https://trialight.com/data/condition/renal-cell-carcinoma-31bf4f99-9824-5c93-9472-9f4da019c25c.md) Phase 1
- [Small cell lung carcinoma](https://trialight.com/data/condition/small-cell-lung-carcinoma-505ad14d-ce79-5398-b171-f724c32e1b4e.md) Phase 1
- [Urothelial carcinoma](https://trialight.com/data/condition/urothelial-carcinoma-b2aa266d-2d5f-5e5d-a0de-62274f2dc094.md) Phase 1

---

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