Pharmacological mechanism and action characteristics of Thiotepa anti-tumor drug

Thiotepa is a traditional alkylating anti-tumor drug that is widely used in the treatment of a variety of solid tumors and hematological tumors. It especially plays an important role in the pretreatment program for hematopoietic stem cell transplantation. Its pharmacological mechanism mainly inhibits the proliferation and division of tumor cells by interfering with the normal replication process of DNA, thereby achieving anti-cancer effects.

From a mechanism perspective, thiotepa is a triethyleneimine alkylating agent. Its active metabolites can form covalent bonds with guanine and adenine bases in DNA chains, causing DNA cross-linking and breakage, interfering with DNA synthesis and repair. This damage is irreversible and has a strong killing effect on rapidly proliferating tumor cells, so it is especially effective in the S phase and G2 phase of the tumor cell cycle.

Another important feature of thiotepa is its high lipid solubility and its ability to better cross the blood-brain barrier, which makes it advantageous in the treatment of brain tumors and the prevention of recurrence of central nervous system leukemia. It is often used clinically in the pretreatment program before bone marrow transplantation, combined with other chemotherapy drugs or whole-body radiotherapy, to further remove residual tumor cells in the body and create good conditions for transplantation.
Generally speaking, thiotepa has strong efficacy, good penetrating power, and wide adaptability. However, it also has common adverse reactions such as bone marrow suppression and immunosuppression. Therefore, it is necessary to closely monitor blood images, liver and kidney functions, and infection risks when using it. Rational combination of drugs and individualized dose adjustment can help improve efficacy, reduce toxic and side effects, and improve the overall treatment prognosis of patients.
Reference: https://www.drugs.com