New Biopharmaceutical Products Pipeline
Innovative, Cholesterol-Lowering Oral Treatment
Our Current Clinical Candidates
A Novel Candidate for Cardiometabolic and Liver Diseases
CVI-LM001 is a novel, first-in-class, safe and oral once daily PCSK9 modulator with distinct mechanisms of action in lowering blood atherogenic LDL-cholesterol and reducing liver fat respectively. Working synergistically with statins, CVI-LM001 has the potential to target patients with hypercholesterolemia and NAFLD/NASH patients with elevated LDL-C. Currently, a 12-week Phase 2 POC trial is initiated in China in patients with hypercholesterolemia.
MOA-1: CVI-LM001 upregulates liver LDLR expression and accelerates blood LDL-cholesterol removal via a unique mechanism of inhibition of PCSK9 transcription and prevention of LDLR mRNA degradation; statin activates LDLR transcription via SREBP2 pathway.
LDLR: LDL receptor, SRE-1: sterol-regulatory element, mRNABP: mRNA binding protein, 3’UTR: 3’untranslated region
MOA-2: CVI-LM001 activates hepatic adenosine monophosphate-activated protein kinase (AMPK), a master regulator of cellular energy, which turns on pathways that reduce the hepatic fat synthesis and boost fatty acids oxidation.
In a hyperlipidemic hamsters model, treatment with CVI-LM001 (40, 80, and 160 mg/kg, QD) for four weeks dose-dependently increased liver LDLR protein levels up to 3.5-fold and decreased circulating PCSK9 levels to 10% of control at the highest dose; this was accompanied by significant reductions in serum LDL-C, total cholesterol (TC), and triglycerides. In a diet-induced NASH hamster model, four weeks treatment with CVI-LM001 substantially reduced hepatic ballooning and improved NASH score.
In a double-blind, randomized phase 1a study conducted in healthy volunteers, compared to baseline, serum PCSK9 levels were significantly reduced after 10 days of oral treatment with CVI-LM001 (300 mg, QD). Moreover, in a proof-of-mechanism phase 1b study conducted in subjects with elevated LDL-C, compared with the placebo cohort, treatment with CVI-LM001 for 28 days significantly reduced serum LDL-C, TC, Apo B, and PCSK9 levels. CVI-LM001 had a favorable safety profile and was well tolerated in Phase 1 studies conducted in healthy volunteers and hyperlipidemic subjects.
A Novel, Oral, Best-In-Class Small Molecule Targeting Obesity, NAFLD/NASH, and Rare Metabolic Diseases
Ask About Our Biopharmaceutical Product Candidates
If you wish to learn more about the research we’re conducting about new lipid-lowering mechanisms or have any questions about the pharmaceutical products we are developing, get in touch with us. Our team is more than happy to address your inquiries. You may contact us via the phone number or email address featured on this website. We hope to hear from you!