Drug intelligence / Profile preview

6-thioguanine + capecitabine + celecoxib + lomustine + temozolomide

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

Overview

This is a five-drug combination therapy consisting of 6-thioguanine (a purine analog antimetabolite), capecitabine (a fluoropyrimidine carbamate prodrug), celecoxib (a COX-2 inhibitor), lomustine (an alkylating nitrosourea agent), and temozolomide (an alkylating agent). The combination appears to be investigated for potential use in brain tumors, particularly glioblastoma. Lomustine and temozolomide are both alkylating agents with established efficacy in brain tumors, with temozolomide being standard of care for glioblastoma. The addition of lomustine to temozolomide has shown potential survival benefits in patients with methylated MGMT promoter glioblastoma in some studies.

Other names
6-TG + Capecitabine + Celecoxib + TMZ/CCNU6-Thioguanine, Capecitabine, Celecoxib and Temozolomide or CCNU6-thioguanine-M.D. Anderson Cancer Center-anaplastic glioma-glioblastoma multiforme
02

Targets

IMPDH (Inosine-5'-monophosphate dehydrogenase 1)TS (Thymidylate synthase)PTGS2 (Prostaglandin-Endoperoxide Synthase 2)USP2 (Ubiquitin-specific peptidase 2)DNAPGHS-1 (Prostaglandin G/H Synthase 1)

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