Drug intelligence / Profile preview

thiotepa + methotrexate

Development stage
Phase 2
Lead developer
Sumitomo Pharma
Modality
Small Molecules
Administration
Intravenous
01

Overview

A combination chemotherapy regimen consisting of thiotepa and high-dose methotrexate (HD-MTX). Thiotepa inhibits tumor growth by disrupting DNA bonds, while methotrexate is an antimetabolite that inhibits dihydrofolate reductase. This combination is primarily used in the treatment of central nervous system lymphoma (CNSL), including primary CNS lymphoma (PCNSL) and secondary CNS lymphoma. The regimen is often administered with other agents such as rituximab and/or Bruton tyrosine kinase (BTK) inhibitors like orelabrutinib or zanubrutinib to enhance efficacy.

Other names
thiotepamethotrexateMTXN,N',N''-triethylenethiophosphoramidetriethylenethiophosphoramideThio-TEPA
02

Targets

DNADHFR (Dihydrofolate reductase)

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