Ly3023414 (Not yet branded)

Other Medications

US Experimental EU Experimental ES Not available Oral 2 Clinical Trials
PI3K alpha PI3K beta PI3K delta PI3K gamma mTOR

Description

LY3023414 is a dual PI3K/mTOR kinase inhibitor that targets multiple components of the PI3K/AKT/mTOR signaling pathway. In colorectal cancer treatment, it is particularly relevant for tumors harboring PIK3CA mutations, which occur in approximately 15-20% of CRC cases. The compound blocks both PI3K isoforms and mTOR kinase activity through a single agent, potentially offering enhanced pathway inhibition compared to selective inhibitors.

Mechanism of Action

LY3023414 functions as an ATP-competitive inhibitor that simultaneously targets class I PI3K isoforms ( , ?, ?, ?) and both mTORC1 and mTORC2 complexes. This dual inhibition disrupts critical cellular processes including protein synthesis, cell survival, proliferation, and metabolism that are often dysregulated in PIK3CA-mutated colorectal cancers.

Molecular Targets

Side Effects

Hyperglycemia Fatigue Nausea Decreased appetite Diarrhea Rash Mucositis Thrombocytopenia

Not all side effects are listed. Side effects vary by individual. Always consult your oncologist.

Clinical Trials

NCT02784795 Phase 1
Archived
A Study of LY3039478 in Participants With Advanced or Metastatic Solid Tumors
United States, Denmark, France, Spain
NCT02124148 Phase 1
Archived
A Study of Prexasertib (LY2606368) With Chemotherapy or Targeted Agents in Participants With Advanced Cancer
United States