Drug intelligence / Profile preview

eflornithine + lomustine + procarbazine + vincristine

Development stage
Preclinical
Lead developer
Orbus Therapeutics
Modality
Small Molecules
Administration
Oral, Intravenous
01

Overview

This is a four-drug combination chemotherapy regimen consisting of eflornithine, lomustine, procarbazine, and vincristine. Each component has a distinct mechanism of action targeting rapidly dividing cancer cells. Eflornithine (also known as DFMO) is an irreversible inhibitor of ornithine decarboxylase, interfering with polyamine synthesis and cell proliferation. Lomustine is an alkylating nitrosourea that cross-links DNA and RNA, leading to cytotoxicity in tumor cells. Procarbazine is an alkylating agent that inhibits DNA, RNA, and protein synthesis through methylation after metabolic activation; it also acts as a weak monoamine oxidase inhibitor. Vincristine is a vinca alkaloid that binds tubulin and inhibits microtubule formation during mitosis, arresting cell division at metaphase. This specific four-drug combination does not have a widely recognized brand or code name but represents an investigational or protocol-based regimen for the treatment of certain brain tumors such as glioma or glioblastoma multiforme. The three-drug version (PCV: procarbazine + lomustine + vincristine) is established in clinical use for brain tumors[1][2][3][5][6]. The addition of eflornithine to PCV has been explored in clinical trials aiming to improve outcomes in high-grade gliomas[4].

Other names
PCV-D TobPCV plus DFMOprocarbazine, CCNU, vincristine, and eflornithine
02

Targets

ODC1 (Ornithine decarboxylase)DNAMAOB (Monoamine oxidase B)TUBB (Tubulin (alpha and beta subunits))MAOA (Monoamine oxidase A)

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