Drug intelligence / Profile preview

temozolomide + busulfan + thiotepa

Development stage
Phase 2
Lead developer
Aston University
Modality
Small Molecules
Administration
Oral, Intravenous
01

Overview

This is a combination chemotherapy regimen consisting of three alkylating agents: temozolomide, busulfan, and thiotepa. Each drug acts by damaging DNA in cancer cells, leading to cell death. Temozolomide is an oral alkylating agent that methylates DNA at the O6 and N7 positions of guanine, resulting in apoptosis due to irreparable DNA damage[2][6]. Busulfan is also an alkylating agent used primarily for conditioning prior to hematopoietic stem cell transplantation; it crosslinks DNA strands, inhibiting replication and transcription[7]. Thiotepa is another alkylating agent used for various malignancies and as conditioning before stem cell transplantation; it works by crosslinking DNA strands through its aziridine groups[4][5]. This combination has been investigated as high-dose chemotherapy with autologous stem cell rescue for conditions such as primary central nervous system lymphoma (PCNSL) after failure of first-line treatments[1][3].

Brand names
Temomedac
Other names
TEMOZOLOMIDEBUSULFANTHIOTEPA
02

Targets

DNA

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