Drug intelligence / Profile preview

thalidomide + celecoxib + etoposide + cyclophosphamide

Development stage
Unknown
Lead developer
Grünenthal
Modality
Small Molecules
Administration
Oral
01

Overview

A multi-drug, all-oral, metronomic antiangiogenic and cytotoxic combination used investigationally in neuro-oncology and other relapsed/refractory cancers. It combines the immunomodulatory and antiangiogenic agent thalidomide, the COX-2 inhibitor celecoxib (antiangiogenic and anti-inflammatory), and the cytotoxic chemotherapies etoposide (topoisomerase II inhibitor) and cyclophosphamide (alkylating agent). Regimens typically use continuous daily thalidomide and celecoxib with alternating 21-day cycles of low-dose oral etoposide and cyclophosphamide; schedules may vary by protocol. This combination has been studied as an antiangiogenic/metronomic backbone in recurrent malignant glioma and pediatric brain tumors, sometimes without or with additional agents in broader protocols. Mechanistically, it targets tumor vasculature and proliferating tumor cells through COX-2/VEGF pathway modulation and DNA damage/topoisomerase II inhibition.

Other names
thalidomide celecoxib etoposide cyclophosphamidethalidomide plus celecoxib plus etoposide plus cyclophosphamide
02

Targets

CRBN (Cereblon)PTGS2 (Prostaglandin-Endoperoxide Synthase 2)DNATOP2A (DNA topoisomerase II)

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