FDA has announced the approval of LIB Therapeutics’ Lerochol (lerodalcibep-liga) for subcutaneous (SC) use as an adjunct to diet and exercise in reducing low-density lipoprotein cholesterol (LDL-C) in adults with hypercholesterolemia, including heterozygous familial hypercholesterolemia (HeFH).

Lerochol is a small protein-binding, third-generation PCSK9 inhibitor. The drug was developed as a once-monthly, single small-volume, SC injection with extended room temperature stability up to three months, making Lerochol a more convenient alternative to other PCSK9 inhibitors.1

The anti-PCSK9 binding domain of Lerochol is an 11-kDa polypeptide called adnectin, which was developed for high-affinity subnanomolar binding to human PCSK9 and fused to human serum albumin to improve plasma half-life.

“While PCSK9 inhibitors as a class deliver powerful cholesterol lowering potential, Lerochol was designed to address the barriers that have limited their use, including ease of use features like a single small monthly injection, self-administered at home with extended room-temperature stability for home storage and travel. For patients with cardiovascular disease who require lifelong cholesterol management, Lerochol offers an important addition to our treatment options,” Dean J. Kereiakes, MD, FACC, MSCAI, chairman of The Christ Hospital Heart and Vascular Institute and professor of medicine at the University of Cincinnati, said in a press release.

Although lower LDL-C levels have improved outcomes for patients with cardiovascular disease (CVD), it remains the leading cause of death both globally and in the United States.1

The PCSK9 inhibitors drug class offer the most effective and safe LDL-C lowering possibilities; however, widespread adoption is limited by inconvenience and access barriers, leaving millions of patients with a need for additional treatment options.1

What was FDA’s approval of Lerochol based on?
FDA’s approval of Lerochol was based on data collected from the global Phase III LIBerate Clinical Trial Program, which enrolled a patient population of over 2,900, including patients with CVD, without CVD at very high risk, patients with high risk for CVD, and heterozygous and homozygous familial hypercholesterolemia.1 Lerochol was administered once per month over a 52-week period, with over 2,400 patients continuing in the 72-week open-label extension trial.1

Results show that Lerochol achieved sustained LDL-C reductions of ≥60% in patients with or at very high or high risk of CVD and ≥50% in those with HeFH who have more severe LDL-C elevations.1 In terms of safety, Lerochol was generally well tolerated with no treatment-related serious adverse events reported in the long-term extension studies.

LIB Therapeutics CEO releases statement following FDA’s approval of Lerochol
“We founded LIB Therapeutics with a mission to bring an effective and more patient-friendly treatment option to the millions of patients who still need additional LDL-C reduction in order to achieve the lower targets recommended in recent guidelines. Today’s FDA approval validates that mission and the focus of my medical career,” Evan Stein, MD, PhD, founder, CEO and chief scientific officer of LIB Therapeutics, said in the press release. “Lerochol was designed for patients who need life-long treatment to achieve and maintain the new lower LDL-C goals especially those with cardiovascular disease and the millions with inherited high cholesterol, familial hypercholesterolemia or FH.

“We look forward to bringing Lerochol to patients in the coming months. I wish to thank the more than 2,500 patients throughout the world who participated in our clinical trials and our small team of very dedicated colleagues at LIB who believed in the drug and worked tirelessly for nearly 10 years, including during the Covid-19 pandemic, to achieve this milestone. I would also like to express our thanks to the FDA Division of Diabetes, Lipid Disorders, and Obesity for their thoroughness, guidance and flexibility during the development and review process and during the government shutdown.”

Sources
U.S. Food and Drug Administration Approves LIB Therapeutics’ Lerochol (lerodalcibep-liga) for Adults with Elevated LDL Cholesterol LIB Therapeutics December 15, 2025 https://www.businesswire.com/news/home/20251215907781/en/U.S.-Food-and-Drug-Administration-Approves-LIB-Therapeutics-LEROCHOL-lerodalcibep-liga-for-Adults-with-Elevated-LDL-Cholesterol