Lerodalcibep-Liga
FDA Drug Information • Also known as: Lerochol
- Brand Names
- Lerochol
- Route
- SUBCUTANEOUS
- Dosage Form
- INJECTION, SOLUTION
- Product Type
- HUMAN PRESCRIPTION DRUG
Description
11 DESCRIPTION Lerodalcibep-liga is a recombinant fusion protein therapeutic agent comprised of a proprotein convertase subtilisin/kexin type 9 (PCSK9)-binding domain and human serum albumin (HSA). Lerodalcibep-liga is produced in genetically engineered mammalian (Chinese hamster ovary) cells as a single protein with an approximate molecular weight of 77 kDa. LEROCHOL (lerodalcibep-liga) injection is a clear to slightly opalescent, brownish-yellow to amber, sterile, preservative-free solution for subcutaneous injection. Each single-dose prefilled syringe contains 1.2 mL of lerodalcibep-liga (300 mg), histidine (3.07 mg), L-histidine monohydrochloride (0.88), polysorbate 80 (0.24 mg), sodium chloride (10.52), and Water for Injection. The pH is 6.8.
What Is Lerodalcibep-Liga Used For?
1 INDICATIONS AND USAGE LEROCHOL TM is indicated as an adjunct to diet and exercise to reduce low-density lipoprotein cholesterol (LDL-C) in adults with hypercholesterolemia, including heterozygous familial hypercholesterolemia (HeFH). LEROCHOL is a proprotein convertase subtilisin kexin type 9 (PCSK9) inhibitor indicated as an adjunct to diet and exercise: to reduce low-density lipoprotein cholesterol (LDL-C) in adults with hypercholesterolemia, including heterozygous familial hypercholesterolemia (HeFH). ( 1 )
Dosage and Administration
2 DOSAGE AND ADMINISTRATION The recommended dosage of LEROCHOL is 300 mg administered subcutaneously once monthly. ( 2.1 ) Inject LEROCHOL subcutaneously into the abdomen or thigh. A caregiver or healthcare professional can administer into the upper arm. ( 2.2 ) Refer to the Instructions for Use for administration of prefilled syringe. ( 2.2 ) 2.1 Recommended Dosage The recommended dosage of LEROCHOL is 300 mg once monthly administered subcutaneously. Assess LDL-C when clinically indicated. The LDL-lowering effect of LEROCHOL may be measured as early as 4 weeks after initiation and, provided monthly dosing is continued, anytime thereafter without regard to timing of the dose. 2.2 Recommendations Regarding Missed Dose(s) If a dose is missed by: Less than 7 days, instruct the patient to administer LEROCHOL as soon as possible and resume the patient's original monthly dosage schedule. Seven (7) or more days, instruct the patient to administer LEROCHOL as soon as possible and start a new monthly dosage schedule based on this date. 2.3 Important Administration Instructions Train patients and/or their caregivers on how to prepare and administer LEROCHOL, according to the Instructions for Use, and instruct them to read and follow the Instructions for Use each time they use LEROCHOL. Prior to use, allow LEROCHOL to warm to room temperature up to 25°C (77°F) for at least 30 minutes if LEROCHOL has been refrigerated [see How Supplied/Storage and Handling ( 16 )] . Visually inspect LEROCHOL prior to administration. LEROCHOL is a clear to slightly opalescent, brownish-yellow to amber solution. Do not use if the solution is cloudy or contains particles. Inject LEROCHOL subcutaneously into the abdomen or the upper front thighs. If injected by a healthcare professional or caregiver, the back of the upper arms can also be a site of injection [see Instructions for Use] . Do not inject in an area of the skin that is tender, bruised, red, or indurated. Rotate injection sites for each administration. To administer the full 300 mg dose, push plunger down until the syringe is empty before removing from the injection site.
Side Effects (Adverse Reactions)
6 ADVERSE REACTIONS Common adverse reactions occurring in ≥1% of patients treated with LEROCHOL were injection site reactions, nasopharyngitis, diarrhea, nausea and peripheral edema. ( 6.1 ) To report SUSPECTED ADVERSE REACTIONS, contact LIB Therapeutics, Inc. at 1-877-2-LEROCHOL or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch . 6.1 Clinical Trials Experience Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in practice. Adverse Reactions in Adults with Primary Hypercholesterolemia Adverse Reactions in Two Pooled 52-week Controlled Trials In two pooled 52-week, double-blind, randomized, placebo-controlled trials (Trials 1 and 2), 1,229 patients received 300 mg of LEROCHOL subcutaneously every 4 weeks [see Clinical Studies ( 14 )] . The mean age was 64 years (range 25 to 90 years), 52% were 65 years of age or older, 37% female, 79% White, 18% Black or African American, 4% Asian; 7% identified as Hispanic or Latino ethnicity. At baseline, 9% of patients had a diagnosis of HeFH, 74% had established atherosclerotic cardiovascular disease (ASCVD), and 26% were at increased risk for ASCVD. Adverse reactions reported in at least 2% of LEROCHOL-treated patients and more frequently than in placebo-treated patients are shown in Table 1 . Adverse reactions led to treatment discontinuation in 4% of LEROCHOL-treated patients and placebo-treated patients. The most frequent adverse reaction leading to treatment discontinuation was injection site reactions, with a higher frequency in the LEROCHOL-treated group compared to placebo-treated patients (1% vs. 0%). Table 1: Adverse Reactions Occurring in ≥2% of LEROCHOL-treated Patients with Hypercholesterolemia and > 1% More Frequently than Placebo-treated Patients in Two Pooled 52-Week Trials (Trials 1 and 2) a Grouped terms composed of several similar terms Adverse Reaction a LEROCHOL 300 mg (N=1,229) % Placebo (N=612) % Nasopharyngitis 15 14 Injection site reactions 12 5 Peripheral edema 2 <1 Adverse Reactions in a 24-Week Controlled Trial In a 24-week, double-blind, randomized, placebo-controlled trial (Trial 3), 318 patients with HeFH received 300 mg of LEROCHOL subcutaneously every 4 weeks [see Clinical Studies ( 14 )]. Adverse reactions reported in at least 2% of LEROCHOL-treated patients, and more frequently than in placebo-treated patients are shown in Table 2 . Table 2: Adverse Reactions Occurring in ≥2% LEROCHOL-treated Patients with HeFH and >1% More Frequently than Placebo-treated Patients at 24 Weeks (Trial 3) Adverse Reaction LEROCHOL 300 mg (N=318) % Placebo (N=159) % a Grouped terms composed of several similar terms Injection site reactions a 18 3 Nasopharyngitis a 13 9 Diarrhea 3 1 Nausea 2 0 Peripheral edema a 2 <1
Contraindications
4 CONTRAINDICATIONS None. None. ( 4 )
Pregnancy and Breastfeeding
8.1 Pregnancy Risk Summary Discontinue LEROCHOL when pregnancy is recognized. Alternatively, consider the ongoing therapeutic needs of the individual patient. LEROCHOL increases LDL-C uptake and lowers LDL-C levels in the circulation, thus decreasing cholesterol and possibly other biologically active substances derived from cholesterol; therefore, LEROCHOL may cause fetal harm when administered to pregnant patients based on the mechanism of action [see Clinical Pharmacology ( 12.1 )]. In addition, treatment of hypercholesterolemia is not generally necessary during pregnancy. Atherosclerosis is a chronic process and the discontinuation of lipid-lowering drugs during pregnancy should have little impact on the outcome of long-term therapy of primary hypercholesterolemia for most patients. Available data from clinical trials on LEROCHOL use in pregnant women are insufficient to evaluate for a drug-associated risk of major birth defects, miscarriage or other adverse maternal or fetal outcomes. In animal reproduction studies, there were no adverse developmental effects observed when pregnant monkeys were administered lerodalcibep-liga subcutaneously during organogenesis and through to parturition at doses up to 100 mg/kg/week [up to 119-fold the exposure at the maximum recommended human dose (MRHD) of 300 mg every month]. The background risk of major birth defects and miscarriage for the indicated population is unknown. In the U.S. general population, the estimated background risk of major birth defects and miscarriage in clinically recognized pregnancies is 2% to 4% and 15% to 20%, respectively. Data Animal Data In cynomolgus monkeys, no effects on embryo-fetal or postnatal development (up to 6 months of age) were observed when lerodalcibep-liga was dosed during organogenesis and through parturition at 30 and 100 mg/kg subcutaneously once weekly (exposures up to 119-fold the MRHD by AUC). An assessment of immune function in the infants showed no treatment-related...
How Supplied
16 HOW SUPPLIED/STORAGE AND HANDLING How Supplied LEROCHOL (lerodalcibep-liga) injection 300 mg/1.2 mL (250 mg/mL) is supplied as a single-dose prefilled syringe for subcutaneous injection and is a clear to slightly opalescent, brownish-yellow to amber, sterile, preservative-free solution. LEROCHOL is supplied in cartons containing one single-dose prefilled syringe (NDC 84685-300-01). Storage and Handling Store refrigerated at 2°C to 8°C (36°F to 46°F) in the original carton to protect from light. Do not freeze. Do not shake. If needed, LEROCHOL may be kept at room temperature up to 25°C (77°F) in the original carton and must be used within 3 months of being removed from the refrigerator. If not used within 3 months, discard LEROCHOL. Do not use beyond the expiration date on the container or package.
About This Information
This drug information is sourced from FDA-approved labeling via the openFDA database. It is intended for educational and reference purposes only. This is not medical advice. Always consult your healthcare provider before making decisions about medication. Drug information may be updated by the FDA; check with your pharmacist for the most current information.
What are side effects?
Side effects are unwanted reactions that can occur when taking a medication. They range from mild (headache, nausea) to severe (allergic reactions, organ damage). Not everyone experiences side effects, and severity varies. Report any concerning side effects to your doctor.
What are drug interactions?
Drug interactions occur when a medication is affected by another drug, food, or supplement. Interactions can make medications less effective or cause dangerous side effects. Always tell your doctor about all medications and supplements you take.