BYL719 (Piqray)

Other Medications · Approved since 2019

US Off-label Oral 2 Clinical Trials
PIK3CA

Description

BYL719 (alpelisib) is a selective PI3K alpha inhibitor that has been evaluated in colorectal cancer treatment combinations. In CRC clinical trials, it is used specifically for BRAF-mutated metastatic colorectal cancer in combination with other targeted agents like cetuximab and LGX818 (encorafenib). The drug has also been tested with capecitabine and radiation therapy for rectal cancer treatment.

Mechanism of Action

BYL719 selectively inhibits the PI3K alpha isoform, which is part of the PI3K/AKT/mTOR signaling pathway that regulates cell growth, proliferation, and survival. By blocking PI3K alpha activity, the drug disrupts downstream AKT signaling, leading to reduced tumor cell proliferation and enhanced apoptosis in cancer cells with PI3K pathway alterations.

Molecular Targets

Side Effects

Hyperglycemia Diarrhea Nausea Decreased appetite Rash Fatigue Weight loss Stomatitis

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

Clinical Trials

NCT02550743 Phase 1
Archived
BrUOG 302:BYL719, Capecitabine and Radiation for Rectal Cancer: A Brown University Oncology Research Group Study
United States
NCT01719380 Phase 2
Archived
Study of LGX818 and Cetuximab or LGX818, BYL719, and Cetuximab in BRAF Mutant Metastatic Colorectal Cancer
United States, Australia, Belgium, Canada, France, Germany, Italy, Japan, Nether