Pioneering Breakthrough Therapies for Lipid-Related Conditions
LipidEra Therapeutics is a biotech company committed to transforming the treatment landscape for hypercholesterolemia and related metabolic disorders. By leveraging cutting-edge science in nuclear receptor modulation, LipidEra is developing innovative therapies that address lipid-related conditions at their root cause
Unmet Needs in Genetic and Severe Hypercholesterolemia
Despite advances in lipid-lowering therapies, patients with genetic and severe hypercholesterolemia—such as those with familial hypercholesterolemia (FH)—remain at high cardiovascular risk. Many fail to reach LDL-C targets even with maximally tolerated statins, ezetimibe, or PCSK9 inhibitors. Treatment gaps are particularly pronounced in homozygous FH, where options are limited and often invasive. There is a critical need for novel therapies that provide broader lipid-lowering effects, address residual risk factors like inflammation and vascular dysfunction, and offer accessible, long-term solutions for this high-risk population.
CAR and PXR are powerful metabolic switches. We're unlocking their full potential
Unlike classical nuclear receptors, CAR (Constitutive Androstane Receptor) and PXR (Pregnane X Receptor) don’t regulate a single pathway—they orchestrate a network. These receptors integrate lipid, bile acid, and xenobiotic metabolism, modulating genes far beyond cholesterol transport. Their pleiotropic activity influences hepatic inflammation, bile acid synthesis, and cholesterol clearance, making them ideal—but underutilized—targets for treating complex metabolic disorders like hypercholesterolemia.
While CAR and PXR have long been recognized as promising metabolic regulators, previous drug development efforts fell short not due to the targets themselves, but because of poorly optimized molecules. At LipidEra, we’ve solved these challenge with MI-883, a novel imidazo-pyridine derivative that unlock the therapeutic potential of CAR/PXR modulation
MI-883 / A unique selective modulator relying on fine-tuned interactions as dual CAR agonist and PXR inverse agonist
Previous CAR and PXR modulators often suffered from weak drug-like properties, poor metabolic stability and oral bioavailability as well as lack of selectivity and specificity leading to toxicity. We’ve designed a next-generation of novel CAR/PXR modulator that exerts a multifaceted mechanism of action on hypercholesterolemia
MI-883 Unleashes Pleiotropic Power in Hypercholesterolemia
Unlike conventional lipid-lowering therapies that target a single metabolic pathway, MI-883 delivers a multifaceted mechanism of action by modulating CAR/PXR- two master regulators of lipid, bile acid, and inflammatory homeostasis. This unique profile allows MI-883 to not only reduce cholesterol levels, but also improve lipoprotein clearance, rebalance hepatic lipid handling and counteract inflammation. With these combined effects, MI-883 offers a differentiated therapeutic opportunity for patients who remain at risk despite statin or PCSK9 inhibitor therapy.
CAR and PXR have broad therapeutic potential across cardio-metabolic, cancer and intestinal diseases
MI-883 is our pioneering program focused on precise modulation of CAR/PXR-two nuclear receptors at the crossroads of liver function, metabolism and detoxification. Our lead indication is Homozygous Familial Hypercholesterolemia (HoFH), a rare and severe orphan disease that enables accelerated development pathways. We plan to expand into Heterozygous Familial Hypercholesterolemia (HeFH) as well as statin-intolerant and statin-resistant populations, addressing multi-billion-dollar global markets.
Engineered for chronic liver and cardio-metabolic conditions, MI-883 sets the stage for a broader pipeline aimed at reshaping how we target metabolic and inflammatory diseases through nuclear receptor biology.
News from LipidEra Therapeutics
New Nature Communications Study Highlights MI-883’s Therapeutic Potential in Hypercholesterolemia
February 6, 2025 – A recent publication in Nature Communications presents compelling preclinical evidence supporting MI-883 as a promising therapeutic agent for hypercholesterolemia. The study, titled “The hypolipidemic
New CAR-Selective Compounds Show Promise for Liver and Metabolic Disorders
February 3, 2023 – Researchers have discovered a new class of compounds that selectively activate the human constitutive androstane receptor (CAR), offering a potential breakthrough
