Table 1.
Summary of anti-tumor activity of MRK-003 alone or in combination with Paclitaxel in TNBC xenograft models.
| Cell line | NOTCH1 status | MRK-003 (300 mpk) |
Paclitaxel (15 mpk) |
MRK-003 + Paclitaxel |
IHC score |
|---|---|---|---|---|---|
| HCC1599 | Rearranged | 90% (TGI) | 1% (TGI) | 98% (TGI) | +++ |
| MB-157 | Rearranged | 22% (Reg) | 73% (TGI) | 72% (Reg) | ++ |
| HBCx-14 | Rearranged | 19% (TGI) | -19 (TGI) | 67% (TGI) | + |
| HBCx-8 | Rearranged | 46% (TGI) | 22% (TGI) | 75% (TGI) | + |
| HCC1187 | WT** | −34% (TGI) | 48% (TGI) | 76% (TGI) | Neg |
| MDA-MB-231 | WT | 27% (TGI) | 74% (TGI) | 86% (TGI) | Neg |
IHC score, N1-ICD staining intensity; TGI, tumor growth inhibition; Reg, tumor regression;
**
NOTCH2 translocation resulting in loss of GSI cleavage site; mgk, mg per kg.