Drug intelligence / Profile preview

fluorocoxib d

Development stage
Preclinical
Modality
Light/Condition-Responsive Prodrugs → Prodrugs/Conditional Activator Small Molecules → Small Molecules
Administration
Intravenous
01

Overview

**Fluorocoxib D** is a water-soluble, hydrophilic small molecule optical imaging agent designed to target and detect **cyclooxygenase-2 (COX-2)**-expressing cancer cells. It consists of a COX-2-inhibiting scaffold conjugated to a rhodamine dye, providing fluorescence for tumor visualization. The compound is not designed for therapeutic purposes, but rather for image-guided biopsy and surgical margin assessment, especially in cancers that show COX-2 overexpression. Fluorocoxib D inhibits COX-2 with an IC50 of 0.23 μM (COX-2) and is less potent against COX-1 (IC50 4 μM). Administration in dogs demonstrated no significant toxicity or clinically relevant adverse events. Uptake in tumors can be blocked by pretreatment with celecoxib, confirming specificity for COX-2. The agent was synthesized from indomethacin and rhodamine derivatives to improve water solubility and imaging properties[1][4].

Other names
N-[(rhodamin-X-yl)but-4-yl]-2-[1-(4-chlorobenzoyl)-5-methoxy-2-methyl-1H-indol-3-yl]acetamide
02

Targets

PTGS2 (Prostaglandin-Endoperoxide Synthase 2)

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