Drug intelligence / Profile preview

EF24

Development stage
Preclinical
Modality
Small Molecules
Administration
Intraperitoneal (preclinical), Oral (preclinical; Has Oral Bioavailability), Not Clinically Approved For Any Route
01

Overview

EF24 is a **synthetic monocarbonyl analog of curcumin**, specifically a small-molecule compound structurally optimized for improved potency and bioavailability relative to curcumin. Designed to overcome the poor bioavailability and modest efficacy of curcumin, EF24 is approximately 10 times more potent in preclinical models. Its primary investigated use is as an **anticancer agent**, where it exhibits broad chemopreventive and chemotherapeutic effects in various cancers, including breast, lung, prostate, colon, and pancreatic cancer. The mechanism of action involves **inhibition of the NF-κB (nuclear factor-kappa B) signaling pathway**, resulting in reduced inflammation, downregulation of anti-apoptotic signals, **induction of apoptosis**, and cell cycle arrest in tumor cells. EF24 also modulates microRNA expression, notably suppressing the oncogenic miR-21, upregulates tumor suppressors like PTEN and PDCD4, and regulates the **Nrf2 (nuclear factor erythroid 2-related factor 2)** antioxidant response, affecting redox balance and oxidative stress. Additional mechanisms include inhibition of drug efflux pumps (such as P-glycoprotein), chemosensitization, disruption of the HIF-1α pathway via VHL protein, indirect effects on microtubule cytoskeleton, and senolytic activity. EF24 has pronounced lipophilicity, improving tissue penetration but presenting solubility and stability challenges for formulation. It is a research tool compound and has not been advanced to clinical drug status or approved for any indication[1][3][5][6][7][4][8][9].

Other names
3,5-bis(2-fluorobenzylidene)-4-piperidone(3E,5E)-3,5-bis[(2-fluorophenyl)methylene]-4-piperidinonecurcumin analog EF24
02

Targets

ABCB1 (P-glycoprotein)NF-κBPARP1 (Poly (adp-ribose) polymerase 1)HIF1A (Hypoxia-inducible factor 1-alpha)miR-21 (MicroRNA-21)

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