FDA approves Lerochol (Lerodalcibep-liga) for adults with elevated low-density lipoprotein cholesterol (LDL)

On December 15, 2025, LIB Therapeutics announced that the U.S. Food and Drug Administration (FDA) approved its new PCSK9 inhibitor Lerochol (Lerodalcibep-liga) injection for the treatment of patients with hypercholesterolemia, especially patients with heterozygous familial hypercholesterolemia (HeFH). Lerochol is designed to lower low-density lipoprotein cholesterol (LDL-C) in adult patients as an adjunct to diet and exercise. It is innovative in that it provides a convenient once-monthly subcutaneous injection and is room-temperature stable for up to three months, providing patients with greater flexibility.

1.Innovative features of Lerochol

Lerochol is a third-generation PCSK9 inhibitor that can effectively reduce LDL-C levels. Its design features give it unique advantages in use and management:

1. Monthly subcutaneous injection: Lerochol adopts a monthly low-dose subcutaneous injection, which is not only convenient for patients, but also reduces patient dependence and avoids the trouble of daily or weekly injections.

2. Room temperature stability: Unlike traditional PCSK9 inhibitors, Lerochol has extended room temperature stability and can be stored at room temperature for up to three months. This feature allows patients to store medications at home and also facilitates traveluse.

3. Lifelong treatment design:Lerochol is designed for patients who require long-term treatment to achieve and maintain low LDL-C goals, especially patients with cardiovascular disease and patients with hereditary high cholesterol (familial hypercholesterolemia, FH).

II.Clinical research and efficacy

Lerochol's approval is based on its global Phase 3 clinical trial, the LIBerate clinical trial program. The study enrolled more than 2,900 patients and included patients with cardiovascular disease (CVD) and high-risk CVD, including those with heterozygous familial hypercholesterolemia (HeFH) and homozygous familial hypercholesterolemia (HoFH). In the trial, Lerochol was injected once monthly for 52 weeks, followed by a 72-week open-label extension trial.

3.Main efficacy results:

1. In trials, Lerochol successfully reduced LDL-C levels. Lerochol demonstrated sustained LDL-C reductions of ≥60% in patients with cardiovascular disease or high-risk cardiovascular disease.

2. In HeFH patients, Lerochol also showed significant efficacy, with the LDL-C reduction rate reaching more than 50%.

3. Throughout the entireLIBerate clinical trial project, Lerochol was well tolerated, and no treatment-related serious adverse events were reported in the long-term extension study.

IV.Safety and Adverse Reactions

AlthoughLerochol is effective, but there are also some adverse reactions. According to clinical trial data, common adverse reactions of Lerochol include:

1) Nasopharyngitis: This reaction was 15% in the Lerochol treatment group, which was higher than 14% in the placebo group.

2) Injection site reactions:The incidence of injection site reactions in the Lerochol treatment group was 12%, which was more common than the 5% in the placebo group.

3) Peripheral edema:The incidence of peripheral edema was 2% in the Lerochol group and <1% in the placebo group.

4) Diarrhea and nausea: In HeFH clinical trials, diarrhea (3%) and nausea (2%) were also common adverse reactions.

5) For patients who discontinued treatment, the most common reason was injection site reaction, but the overall incidence was low.

5.The mechanism of action of Lerochol

Lerochol is a small protein-binding, third-generation PCSK9 inhibitor whose anti-PCSK9 domain is an 11 kDa polypeptide named adnuctin. This domain has been engineered to bind with high affinity to human PCSK9 protein, thereby blocking the interaction between PCSK9 and low-density lipoprotein receptor (LDLR) and promoting the clearance of LDL-C. In order to increase the half-life of the drug, adnuctin is combined with human serum albumin, further enhancing its stability and sustained release in plasma.

6.The market prospects of Lerochol

The approval of Lerochol is an important breakthrough in the treatment of hypercholesterolemia, especially for patients with high-risk cardiovascular disease who require lifelong treatment. Its convenient administration, room temperature stability, and powerful LDL-C lowering effect make it a unique alternative to other PCSK9 inhibitors. As lipid management requirements become increasingly stringent, the launch of Lerochol provides a new option for patients requiring long-term cholesterol management.

Reference materials: UpdatedDecember 15, 2025, https://www.drugs.com/newdrugs/fda-approves-lerochol-lerodalcibep-liga-adults-elevated-ldl-cholesterol-6693.html