first-in-class membrane lipid modulator.
LAU-7b is a proprietary oral drug candidate based on fenretinide, an atypical retinoid with a well-documented safety profile established in more than 3,000 patients. Existing data suggest that low-dose fenretinide has the potential to modulate certain membrane lipids and exerts antiviral, inflammation-controlling, and antifibroticproperties in a variety of in vitro and ex vivo systems, and animal models of acute and chronic inflammation, cystic fibrosis (CF), and non-CF pulmonary fibrosis.
a balancing act.
Lipids are fundamental cell components responsible for cell membrane structure, fluidity, and function. Membrane lipids play multiple biological roles ranging from first-line host defense against pathogens, to inflammation signaling and protein trafficking. Their potential as therapeutic targets remain largely untapped.
Low-dose LAU-7b focuses on certain phospholipids and sphingolipids that play central roles in the activation/resolution of the inflammation process, as well as in the host defense against pathogens.
LAU-7b’s lipid-modulating mechanism follows a multitarget pharmacology involving desaturases (delta-4 and delta-9) and ceramide synthase (CerS5), all of which playing important roles in fatty acid metabolism. LAU-7b activity was also associated with the modulation of cPLA2, ERK 1/2 and NF-κB inflammation signaling pathways.
LAU-7b was shown to increase phospholipids linked to docosahexaenoic acid (DHA) involved in the resolution phase of inflammation, and indirectly having a downregulating effect on the arachidonic acid (AA) pathway responsible for the inflammation activation process. The balancing effect on DHA/AA mimics body’s own inflammation-controlling process (a “pro-resolving” effect).
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