From: Clinicopathologic significance of protein lysine methyltransferases in cancer
EZH2 | ||
Compound name | Mechanism of action | Clinical trial information (clinicaltrials.gov) |
Tazemetostat (EPZ-6438, Epizyme) | SAM-competitive | Hematologic malignancies: -Tazemetostat monotherapy: NCT03009344, NCT03456726, NCT02220842 (completed) -Tazemetostat in combination: NCT04224493 (Tazemetostat + Lenalidomide/Rituximab) Hematologic + solid tumors: -Tazemetostat monotherapy: NCT02875548, NCT03010982 (completed), NCT01897571, NCT03213665, NCT03028103, NCT03155620 Solid tumors: -Tazemetostat monotherapy: NCT02601950, NCT02860286 (completed), NCT04241835, NCT02601937 -Tazemetostat in combination: NCT04179864 (Tazemetostat + Abiraterone/Enzalutamide), NCT04204941 (Tazemetostat + Doxorubicin), NCT03854474 (Tazemetostat + Pembrolizumab) |
GSK2816126 (GlaxoSmithKline) | SAM-competitive inhibition (PRC2-specific inhibitor) | 1 terminated trial |
CPI-1205 (Constellation Pharmaceuticals) | SAM-competitive inhibition (PRC2-specific inhibitor) | Hematologic malignancies: -CPI-1205 monotherapy: NCT02395601 (completed) Solid tumors: -CPI-1205 in combination: NCT03480646 (CPI-1205 + Abiraterone/Enzalutamide), NCT03525795 (CPI-1205 + Ipilimumab) |
MAK683 (Novartis) | PRC2 complex disruptor (binds to EED) | Hematologic malignancies: -MAK683 monotherapy: NCT02900651 |
PRC2 Complex | ||
Compound name | Mechanism of action | Clinical trial information (clinicaltrials.gov) |
SAH-EZH2 (Calbiochem) | Disruption of PRC2 subunit interactions | Preclinical use |
A-395 | Disruption of PRC2 subunit interactions | Preclinical use |
EZH1/EZH2 | ||
Compound name | Mechanism of action | Clinical trial information (clinicaltrials.gov) |
Valemetostat (DS-3201b, Daiichi Sankyo) | EZH1/EZH2 inhibitor with equal affinity via SAM-competitive inhibition | Hematologic malignancies: -Valemetostat monotherapy: NCT03110354, NCT04102150, NCT02732275 Solid tumors: -Valemetostat in combination: NCT03879798 (Valemetostat + Irinotecan), NCT04388852 (Valemetostat + Ipilimumab) Hepatic impairment: -Valemetostat monotherapy: NCT04276662 |
899145 | SAM-competitive inhibition | Preclinical use |
DOT1L | ||
Compound name | Mechanism of action | Clinical trial information (clinicaltrials.gov) |
Pinometostat (EPZ-5676, Epizyme) | SAM-competitive inhibition | Hematologic malignancies: -Pinometostat in combination: NCT03701295 (Pinometostat + Azacitidine), NCT03724084 (Pinometostat + Cytarabine/Daunorubicin/Daunorubicin Hydrochloride) |
Menin-MLL | ||
Compound name | Mechanism of action | Clinical trial information (clinicaltrials.gov) |
MI-503 | Disruption of MLL complex subunit interactions | Preclinical use |
EHMT1/EHMT2 | ||
Compound name | Mechanism of action | Clinical trial information (clinicaltrials.gov) |
UNC0642 | Peptide-competitive inhibitor | Preclinical use |
SUV420H1/2 | ||
Compound name | Mechanism of action | Clinical trial information (clinicaltrials.gov) |
A-196 | Peptide-competitive inhibitor | Preclinical use |
SMYD2 | ||
Compound name | Mechanism of action | Clinical trial information (clinicaltrials.gov) |
EPZ033294 | Peptide-competitive inhibitor | Preclinical use |
SMYD3 | ||
Compound name | Mechanism of action | Clinical trial information (clinicaltrials.gov) |
EPZ031686 | Peptide-competitive inhibitor | Preclinical use |
SETD7 | ||
Compound name | Mechanism of action | Clinical trial information (clinicaltrials.gov) |
(R)-PFI-2 | Peptide-competitive inhibitor | Preclinical use |
SETD8 | ||
Compound name | Mechanism of action | Clinical trial information (clinicaltrials.gov) |
UNC0379 | Peptide-competitive inhibitor | Preclinical use |