Zeprumetostat
Highest phase reached
Phase 2
Drug type
Small molecule
- Listing at source
- Listed
- Highest phase reached
- Phase 2
- Drug type
- Small molecule
- Drug name
- Zeprumetostat
- Molecular weight
- 548.73
- Structure (SMILES)
- CCc1c(N(CC)C2CCOCC2)cc2oc(CN3CCCCC3)cc2c1C(=O)NCc1c(C)cc(C)[nH]c1=O
- 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
- CAS registry numbers
- 2098545-98-1
- ChEMBL ID
- CHEMBL5939817
- InChIKey
- YLZVNQZYAYVUCW-UHFFFAOYSA-N
- PubChem compound IDs
- 135332280
- FDA ingredient codes (UNII)
- XLJ9D8HE8Y
- First in class
- No
- Orphan designation
- No
- Pharmacology name
- zeprumetostat
- Type
- Synthetic organic
- Drug name stem
- -stat
- Approval recorded by Guide to Pharmacology
- Yes
- 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
- 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
- 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