LY3039478 + LY3023414

LY3039478 + LY3023414 is an investigational oral combination regimen used in early-phase oncology clinical trials for advanced or metastatic solid tumors. **LY3039478 (crenigacestat)** is a potent, selective, oral γ-secretase inhibitor that blocks the cleavage of the transmembrane domain of Notch receptors, thereby inhibiting Notch signaling—a pathway implicated in cancer cell proliferation and survival[2][3][7]. **LY3023414** is an oral, dual inhibitor of *phosphoinositide 3-kinases (PI3K)* and *mechanistic target of rapamycin (mTOR)*, both critical components of the PI3K/AKT/mTOR pathway, frequently dysregulated in various malignancies[7][8]. In the Phase 1b clinical study (NCT02784795), this combination was explored for safety, tolerability, and preliminary efficacy in advanced solid tumors, including breast cancer, colon cancer, soft tissue sarcoma, cholangiocarcinoma, and triple-negative breast cancer, using oral dosing on repeating 28-day cycles[1][4][7].

Other names

crenigacestat + LY3023414