Karenitecin is primarily used in the field of oncology as an anticancer agent. It belongs to the class of topoisomerase I inhibitors, which work by interfering with the enzyme topoisomerase I, crucial for DNA replication and repair in cancer cells. This interference leads to DNA damage and ultimately induces apoptosis in malignant cells.

Its application is particularly significant in the treatment of various solid tumors, including ovarian cancer, brain tumors, and melanoma. Karenitecin has shown promise in clinical trials due to its ability to cross the blood-brain barrier, making it a potential therapeutic option for brain cancers and metastases. Additionally, its lipophilic nature enhances its uptake and retention in tumor tissues, improving its efficacy.

Research continues to explore its potential in combination therapies and its effectiveness against other types of cancers, aiming to optimize treatment protocols and outcomes for patients.