Drug intelligence / Profile preview

NCX 4040

Development stage
Discontinued
Lead developer
NicOx Research Institute
Modality
Small Molecules
Administration
Oral (preclinical Studies, Intended Route), Not Approved For Clinical Use
01

Overview

NCX 4040 is a **nitric oxide (NO)-donating aspirin derivative** developed primarily as an **anti-inflammatory and antitumor agent**. Its mechanism of action involves donating nitric oxide, which leads to inhibition of cyclooxygenases (COX-1 and COX-2), and blocks inflammatory mediator production, such as IL-1β, PGE2, IL-10, and TNF-α in human monocytes. NCX 4040 decreases COX-2 expression and disrupts proteasome-mediated degradation of IκB-α, thus affecting NF-κB signaling[1][3][4]. In cancer models, NCX 4040 exhibits **antiproliferative effects** and has been reported to sensitize drug-resistant tumor cells (including colon and ovarian cancer cells) to cisplatin and reverse resistance to anticancer drugs by inhibiting the ATPase functions of ABC transporters (such as ABCB1/P-gp and ABCG2/BCRP), interfering with drug efflux mechanisms[5]. Originally developed by NicOx, NCX 4040 reached preclinical and early research phases for indications such as **colorectal cancer**, but its highest R&D status is now **discontinued**[2][4]. No known approved indications.

Brand names
NCX 4040NCX4040NCX-4040
Other names
NCX 4040NCX4040NCX-4040NO-donating aspirinnitric oxide-releasing aspirin
02

Targets

ABCG2 (Breast cancer resistance protein)PTGS2 (Prostaglandin-Endoperoxide Synthase 2)ABCB1 (P-glycoprotein)PGHS-1 (Prostaglandin G/H Synthase 1)

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