Table 2.
SEs-targeting therapeutic inhibitors in clinical trials.
| Target | Inhibitor | Mechanism | Tumor type | Clinical trial |
|---|---|---|---|---|
| BET proteins | BMS-986158 | Decreasing BRD4 occupation and MED1 binding on SEs by blocking BD1 or BD2 of BRD4 | Advanced Solid Tumors | NCT02419417 (phase I/IIa) |
| Hematologic Malignancies | ||||
| OTX015 (Birabresib) |
AML GMA |
NCT02303782 (phase II) | ||
| NCT02296476 (phase II) | ||||
| GSK525762 | Neoplasms | NCT01943851 (phase II) / [87] | ||
| CPI-0610 |
PNTs MF Neoplasms |
NCT02986919 (phase II) | ||
| NCT04603495(phase III) | ||||
| NCT02158858 (phase II) | ||||
| AZD5153 | Decreasing BRD4 occupation and MED1 binding on SEs by blocking BD1 and BD2 of BRD4 | Malignant Solid Tumors Lymphoma | NCT03205176 (phase I) | |
| CDK7 | CT7001 | Blocking TFIIH function by non-covalent binding to the ATP-binding site of CDK7 | Advanced Solid Malignancies | NCT03363893 (phase I/II)/ [88] |
| SY-5609 | Advanced Solid Tumor, BC, SCLC | NCT04247126 (phase I)/ [88] | ||
| SY-1365 | Blocking TFIIH function by covalent binding to the ATP-binding site of CDK7 | Ovarian cancer, breast cancer, advanced solid tumors | NCT03134638 (Phase I) | |
| LY3405105 | / | advanced or metastatic solid cancers | NCT03770494 (phase Ia/Ib) | |
| CDK9 | Fadraciclib | Blocking P-TEFb function by inhibiting the ATP-binding site of CDK9 |
Solid Tumor, Lymphoma MDS |
NCT04983810 (phase II) |
| NCT03593915 (phase II) | ||||
| Dinaciclib | CLL | NCT01580228 (phase III)/ [89] | ||
| Alvocidib |
MDS, Secondary MDS AML Malignant Solid Tumor |
NCT03593915 (Phase I) | ||
| NCT03441555 (Phase I) | ||||
| NCT03604783 (Phase I) | ||||
| AZD4573 | Advanced hematological cancers and relapsed/refractory hematological cancers | NCT03263637 (Phase I) | ||
|
BAY-1143572 (Atuveciclib) |
Acute leukemias and advanced malignancies | NCT02345382 (Phase I) | ||
| NCT01938638 (Phase I) | ||||
| BAY-1251152 | Advanced hematological cancers and advanced malignancies | NCT02745743 (Phase I) | ||
| NCT02635672 (Phase I) |
Abbreviations: Acute Myeloid Leukemia (AML), Glioblastoma Multiforme (GMA), Peripheral Nerve Tumors (PNTs), Myelofibrosis (MF), Myelodysplastic Syndromes (MDS), Breast Cancer (BC), Small-cell Lung Cancer (SCLC), Chronic Lymphocytic Leukemia (CLL).