Table 3.
Clinical trials targeting MYC
| Type | Mechanism | Condition(s) | Compound | Phase | NCT number |
|---|---|---|---|---|---|
| Direct MYC inhibition | siRNA against the MYC | Hepatocellular Carcinoma | DCR-MYC |
Phase 1 Phase 2 |
NCT02314052 |
|
Inhibits MYC/MAX dimerization Inhibition of E-box binding |
Advanced Solid Tumors Non-small-cell lung carcinoma (NSCLC) Triple-negative Breast Cancer |
OMO-103 |
Phase 1 Phase 2 |
NCT04808362 | |
| Inhibits MYC/MAX dimerization | Neoplasms | OMO-1 |
Phase 1 Phase 2 |
NCT03138083 | |
| Downregulation of MYC | Ischemic Stroke | miR-494 | - | NCT03577093 | |
| Interrupts the translation of MYC gene | Neoplasms | AVI-4126 (RESTEN-NG) | Phase 1 | NCT00343148 | |
| Indirect MYC inhibition | Alteration of MYC translation (BET Bromodomain inhibitors) |
Castration-Resistant Prostate Carcinoma Metastatic Prostate Adenocarcinoma Metastatic Prostate Small Cell Carcinoma Stage IV Prostate Cancer AJCC v8 Stage IVA Prostate Cancer AJCC v8 Stage IVB Prostate Cancer AJCC v8 |
ZEN-3694 | Phase 2 | NCT04471974 |
|
Solid Tumor Lymphoma Brain Tumor |
BMS-986158 | Phase 1 | NCT03936465 | ||
| Lymphoma, Non- Hodgkin | CC-95775 (FT-1101) | Phase 1 | NCT04089527 | ||
|
Diffuse Large B-cell Lymphoma (DLBCL) High-Grade B-cell Lymphoma |
RO6870810 | Phase 1 | NCT03255096 | ||
| Neoplasms | GSK525762 | Phase 2 | NCT01943851 | ||
|
Myelofibrosis Primary Myelofibrosis Post-polycythemia Vera Myelofibrosis Post-essential Thrombocythemia Myelofibrosis |
CPI-0610 | Phase 3 | NCT04603495 | ||
|
Metastatic Malignant Solid Neoplasm Recurrent Malignant Solid Neoplasm Recurrent Platinum-Resistant Ovarian Carcinoma Refractory Ovarian Carcinoma |
ZEN-3694 | Phase 1 | NCT04840589 | ||
|
Malignant Solid Tumors Lymphoma Ovarian Cancer Breast Cancer Pancreatic Cancer Prostate Cancer |
AZD5153 | Phase 1 | NCT03205176 | ||
|
Neoplasms NUT Carcinoma |
BI 894999 | Phase 1 | NCT02516553 | ||
|
AML Including AML de Novo and AML Secondary to MDS DLBCL |
Birabresib (MK-8628, OTX015) | Phase 1 | NCT02698189 | ||
| MCL-1 inhibitor | Relapsed or Refractory AML | AZD5991 | Phase 1 Phase 2 | NCT03218683 | |
| AML | S64315 (MIK665) | Phase 1 Phase 2 | NCT04629443 | ||
|
Relapsed or Refractory Multiple Myeloma Relapsed or Refractory AML |
AMG 176 | Phase 1 | NCT02675452 | ||
|
Multiple Myeloma Non-Hodgkins Lymphoma Myelodysplastic Syndrome |
AMG 397 | Phase 1 | NCT03465540 | ||
| Inhibiting BCR-signalling |
Prolymphocytic Leukemia Recurrent Adult Diffuse Large Cell Lymphoma Recurrent Mantle Cell Lymphoma Recurrent Small Lymphocytic Lymphoma Refractory Chronic Lymphocytic Leukemia |
Ibrutinib | Phase 1 | NCT02303392 | |
|
Lymphoma, B-Cell Small Lymphocytic Lymphoma CLL Waldenstrom Macroglobulinemia Mantle Cell Lymphoma Diffuse Large B Cell Lymphoma Richter's Transformation Follicular Lymphoma Marginal Zone Lymphoma |
ARQ 531 |
Phase 1 Phase 2 |
NCT03162536 | ||
|
Epigenetic silencing (HDAC inhibitors) |
Diffuse Large B-cell Lymphoma |
Tucidinostat | Phase 3 | NCT04231448 | |
| Relapsed and refractory lymphoma | Entinostat | Phase 2 | NCT03179930 | ||
| PI3K inhibitor |
B Cells-Tumors B Cell Chronic Lymphocytic Leukemia Follicular Lymphoma Mantle Cell Lymphoma Large B-Cell Diffuse Lymphoma of Bone (Diagnosis) |
Idelalisib | Phase 1 | NCT03151057 | |
| Dual inhibitor of PI3Kδ and CK1ε |
CLL B-cell Non-Hodgkin Lymphoma |
TGR-1202 | Phase 1 | NCT03283137 | |
| Dual inhibitor of PI3Kδ and DNA-PK |
Diffuse Large B Cell Lymphoma Follicular Lymphoma CLL Small Lymphocytic Leukemia B Cell Lymphoma Marginal Zone Lymphoma Waldenstrom Macroglobulinemia Peripheral T Cell Lymphoma |
BR101801 | Phase 1 | NCT04018248 | |
| Dual inhibitor of PI3Kδ and HDACs | Relapsed and/or Refractory DLBCL With MYC Alterations | Fimepinostat (CUDC-907) | Phase 2 | NCT02674750 | |
| Inhibitor of CDK1, CDK2, CDK5 and CDK9 |
Advanced or Metastatic Breast Cancer Triple Negative Breast Cancer |
Dinaciclib | Phase 1 | NCT01676753 | |
| CDK9 inhibitor |
Relapsed Solid Tumors Refractory Solid Tumors Non-Hodgkin Lymphoma |
KB-0742 | Phase 1 | NCT04718675 | |
| Multi kinase inhibitor: inhibits CDKs 1, 2, 7 and 9 together with JAK2 and FLT3 |
AML ALL Blast Crisis MDS Multiple Myeloma |
TG02 | Phase 1 | NCT01204164 | |
| G-quadraplex stabilizer at MYC promoter |
AML High Risk Myelodysplasia |
APTO-253 | Phase 1 | NCT02267863 | |
|
Advanced Solid Tumors Lymphoma |
CX-3543 | Phase 1 | NCT00955786 |