Hepsulfam is primarily used in the field of oncology as an alkylating agent, which means it plays a crucial role in cancer treatment. It works by interfering with the DNA of cancer cells, preventing them from dividing and growing. This makes it effective in targeting various types of tumors, particularly in chemotherapy regimens.

In clinical settings, hepsulfam is often administered to patients with certain forms of leukemia and lymphoma. Its ability to cross the blood-brain barrier also makes it useful in treating brain tumors. Additionally, it is sometimes used in conditioning regimens prior to bone marrow or stem cell transplants, where it helps to suppress the immune system and eliminate cancerous cells.

The compound is typically given intravenously under strict medical supervision due to its potent effects and potential side effects, such as bone marrow suppression. Its application is carefully monitored to balance efficacy with patient safety.