Alisertib

Aurora kinase A inhibitor

Alisertib
INN
Drug class
Routes of administration
Pregnancy category
Bioavailability
Metabolism
Elimination half-life
Excretion
Legal status
CAS Number	1028486-01-2
PubChem	25141694
DrugBank	DB11745
ChemSpider	25071435
KEGG	D09950

Alisertib is a small molecule inhibitor of aurora kinase A, a protein that plays a critical role in cell division by controlling the mitotic spindle apparatus. It is being investigated for its potential use in the treatment of various types of cancer, including hematologic malignancies and solid tumors.

Mechanism of Action

Alisertib selectively inhibits aurora kinase A, which is essential for the proper alignment and segregation of chromosomes during mitosis. By inhibiting this kinase, alisertib disrupts the normal progression of the cell cycle, leading to apoptosis or programmed cell death in rapidly dividing cancer cells. This makes it a promising candidate for targeting cancers that exhibit high levels of aurora kinase A activity.

Clinical Development

Alisertib has been evaluated in several clinical trials for its efficacy and safety in treating different types of cancer. It has shown potential in treating non-Hodgkin lymphoma, acute myeloid leukemia, and breast cancer, among others. The drug is typically administered orally and has been studied both as a monotherapy and in combination with other anticancer agents.

Side Effects

The most common side effects associated with alisertib include neutropenia, anemia, thrombocytopenia, and gastrointestinal symptoms such as nausea and diarrhea. These side effects are consistent with the drug's mechanism of action, as it targets rapidly dividing cells, including those in the bone marrow and gastrointestinal tract.

Research and Future Directions

Ongoing research is focused on identifying biomarkers that can predict response to alisertib, optimizing dosing regimens, and exploring its use in combination with other targeted therapies. The development of resistance to aurora kinase inhibitors is also an area of active investigation, with efforts aimed at understanding the underlying mechanisms and developing strategies to overcome resistance.

Related Pages

• Aurora kinase A
• Cell cycle
• Cancer treatment
• Clinical trial