Enzastaurin (Not yet branded)

Other Medications

US Experimental Oral 2 Clinical Trials
PKCβ PI3K/AKT pathway

Description

Enzastaurin is a selective protein kinase C beta (PKC ) inhibitor that has been evaluated as a combination therapy for metastatic colorectal cancer. The drug has been tested in maintenance regimens with 5-fluorouracil/leucovorin plus bevacizumab following first-line therapy, as well as in combination with irinotecan plus cetuximab. Enzastaurin belongs to the class of serine/threonine kinase inhibitors and was developed to target specific signaling pathways involved in tumor growth and angiogenesis.

Mechanism of Action

Enzastaurin selectively inhibits protein kinase C beta (PKC ) and phosphatidylinositol 3-kinase (PI3K)/AKT signaling pathways, which are critical for tumor cell proliferation, survival, and angiogenesis. By blocking these pathways, the drug aims to suppress tumor growth and reduce blood vessel formation that feeds the tumor.

Molecular Targets

Side Effects

Fatigue Diarrhea Nausea Decreased appetite Thrombocytopenia Hypertension Peripheral edema Abdominal pain

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

Clinical Trials

NCT00612586 Phase 2
Archived
Study of Enzastaurin With 5-Fluorouracil/Leucovorin (5-FU/LV) Plus Bevacizumab as Maintenance Regimen Following First Line Therapy for Metastatic Colon Cancer
United States, Austria, France, Germany, Italy, Puerto Rico
NCT00437268 Phase 2
Archived
A Study of Irinotecan Plus Cetuximab With or Without Enzastaurin in Participants With Colorectal Cancer
United States