lomustine
Overview
Lomustine (CCNU; 1-(2-chloroethyl)-3-cyclohexyl-1-nitrosourea) is a lipophilic nitrosourea alkylating agent that readily crosses the blood-brain barrier. It alkylates DNA and carbamoylates proteins, inducing DNA strand breaks. It is the “C” (CCNU) component of the PCV regimen (procarbazine, lomustine/CCNU, vincristine) used in oligodendroglioma and other gliomas.
Evidence in the corpus
- Component of PCV (procarbazine/lomustine/vincristine) induction, which served as the historical comparator arm in a phase II trial (NCT00588523) for newly diagnosed 1p/19q-codeleted anaplastic oligodendroglioma (ODG3) and oligoastrocytoma (n=20 prior PCV cohort). In an exploratory cross-trial comparison using the same myeloablative HDC-ASCT backbone, single-agent temozolomide induction was non-inferior to PCV induction for OS (HR 3.38 favoring TMZ, P=0.005, all patients; HR 5.68, P=0.018, 1p/19q-codeleted) — countering concerns that TMZ is inferior to PCV in this disease. PMID:28472509
Resistance mechanisms
- Not specifically reported in the corpus.
Cancer types (linked)
- ODG3 — lomustine as L (CCNU) in PCV induction comparator arm for 1p/19q-codeleted anaplastic oligodendroglioma HDC-ASCT trial; non-inferior to single-agent TMZ in exploratory cross-trial comparison.
Sources
- PMID:28472509 — Thomas et al. 2017, J Clin Oncol. Phase II NCT00588523; lomustine as C (CCNU) in PCV induction for 1p/19q-codeleted anaplastic oligodendroglioma; TMZ found non-inferior in cross-trial comparison.
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