Table 5 Small-molecule compounds targeting RCD subroutines in TNBC clinical trials
Name in the literature and chemical structure | Target | Mechanism in RCD | Biological activity | TNBC subtype | Clinical trial identifier | References |
|---|---|---|---|---|---|---|
CUDC-907
| DR5↑ | Induce apoptosis | MDA-MB-231 (IC50 = 0.2 − 0.5 μM) | MSL | NCT02307240 (phase 1) | [377] |
ONC201
| TRAIL/DR5↑ | Induce apoptosis | SUM149PT (GI50 = 2 μM); MDA-MB-468 (GI50 = 2 μM) | BL2, BL1 | NCT03733119 (phase 2), NCT03394027 (phase 2) | [378] |
Etoposide (ET)
| DR5↑ | Induce apoptosis | MDA-MB-231 (IC50 = 30 − 40 μM) | MSL | NCT04452370 (phase 2) | [379] |
ENMD-2076
| p53↑ p73↑ | Induce apoptosis | MDA-MB-468, MDA-MB-231, HCC1187, Hs578T (Average: IC50 = 1.4 μM) | BL1, MSL, IM | NCT01639248 (phase 2) | |
NVP-BEZ235
| mutp53↓ Akt/mTOR↓ | Induce autophagy-dependent cell death | MDA-MB-231 (GI50 = 0.02 − 0.04 μM) MDA-MB-468 (GI50 = 0.01 − 0.02 μM) | MSL, BL1 | NCT01337765 (phase 1) | [382] |
Ganetespib
| HSP90 inhibitor | Active mitotic catastrophe | MDA-MB-231 (IC50 = 20 nM) | MSL | NCT01677455 (phase 2) | [358] |
