Entrectinib-d8 is a deuterated form of Entrectinib, an orally available inhibitor of TrkA/B/C, ROS1, and ALK receptors. It can cross the blood-brain barrier and demonstrates central nervous system activity. This compound is known to induce apoptosis and cell cycle arrest in cancer cells, showing anti-tumor activity and alleviation of bleomycin-induced pulmonary fibrosis in mice.
- Deuterated compound
- Orally available and blood-brain barrier permeable
- Active in the central nervous system
- Inhibits TrkA/B/C, ROS1, and ALK
- Induces apoptosis and cycle arrest in cancer cells
- Has anti-tumor activity
- Alleviates bleomycin-induced pulmonary fibrosis
- Useful as a tracer for drug development
- May impact pharmacokinetic and metabolic profiles of drugs
- Stable solid form