Lerochol Drug Information
Generic name: LERODALCIBEP-LIGA
Uses of Lerochol
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).
Dosage & Administration of Lerochol
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.
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 or more days, instruct the patient to administer LEROCHOL as soon as possible and start a new monthly dosage schedule based on this date.
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 . 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 . 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 of Lerochol
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 . 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. 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
Pregnancy Safety for Lerochol
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.
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. 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 adverse effects. Measurable lerodalcibep-liga serum concentrations were observed in the infant monkeys with infant serum concentrations approximately 2 to 7% of maternal serum concentrations on postnatal days 14, 21 and 28, indicating that lerodalcibep-liga has the potential to be transmitted from the mother to the developing fetus.
Pediatric Use of Lerochol
Pediatric Use The safety and effectiveness of LEROCHOL in pediatric patients have not been established. Clinical trials of LEROCHOL in pediatric patients with HeFH have not been conducted. Effectiveness of LEROCHOL was not demonstrated in a 24-week, randomized, open-label, active-controlled trial (NCT04034485) in 19 pediatric patients aged 10 to 17 years with homozygous familial hypercholesterolemia (HoFH).
Clinical Studies of Lerochol
The efficacy of LEROCHOL was evaluated in three randomized, double-blind, placebo-controlled trials that enrolled 2,017 adults with HeFH, clinical ASCVD, or increased risk for ASCVD, who were on a stable low-fat, low-cholesterol diet and maximally tolerated statin therapy and who required additional LDL-C lowering. Primary Hypercholesterolemia Trial 1 (NCT04797247) and Trial 2 (NCT04806893) were both multicenter, double-blind, randomized, placebo-controlled 52-week trials in which 1,844 adults with ASCVD or at increased risk for ASCVD events were randomized 2:1 to receive subcutaneous injections of either LEROCHOL 300 mg (n=1,229) or placebo (n=615) every 4 weeks. Patients were stable on a low-fat, low-cholesterol diet, maximally tolerated dose of statin with or without other oral lipid modifying therapy, and required additional LDL-C reduction.
Baseline Disease and Demographic Characteristics The mean age in Trial 1 at baseline was 64 years (range: 25 to 90 years), 49% were 65 years or older, 30% were female, 80% were White, 17% were Black or African American, and 3% were Asian; 1.1% identified as Hispanic or Latino ethnicity. Thirty four percent (34%) of patients had diabetes at baseline, 86% established ASCVD, and 14% at increased risk for CVD events. The mean baseline LDL-C was 102 mg/dL. At the time of randomization, 87% of patients were receiving statin therapy and of these 53% were receiving high-intensity statin therapy; 18% were receiving ezetimibe either in combination with a statin or alone.
The mean age in Trial 2 at baseline was 65 years (range: 27 to 87 years), 54% were 65 years or older, 45% were female, 78% were White, 18% were Black or African American, and 4% were Asian; 13% identified as Hispanic or Latino ethnicity. Forty-three percent (43%) of patients had diabetes at baseline, 48% established ASCVD, and 52% at increased risk for CVD events. The mean baseline LDL-C was 116 mg/dL. At the time of randomization, 83% of patients were receiving statin therapy and of these, 39% were on high-intensity doses; 17% were receiving ezetimibe either in combination with a statin or alone.
Endpoint Results The primary efficacy outcome measure in Trial 1 was the placebo adjusted intent to treat (ITT) analysis of percent change in LDL-C from baseline to Week 52. The difference between the LEROCHOL and placebo group in mean percentage change in LDL-C from baseline to Week 52 was -55% (95% CI: -59.2%, -50.8%; p < 0.0001). For additional results, see Table 3 and Figure 1. Table 3: Changes in Lipid Parameters in Patients with Hypercholesterolemia and ASCVD or Increased Risk for ASCVD Events on Maximally Tolerated Statin Therapy (Percent Change from Baseline to Week 52 in Trial 1) Abbreviation: ApoB = apolipoprotein B; CI = confidence interval; HDL-C = high-density lipoprotein cholesterol; LDL-C = low-density lipoprotein cholesterol; n = number of patients randomly assigned to each treatment group; LS Mean= least-squares mean a LDL-C, Total Cholesterol, non-HDL-C and ApoB at Week 52 were missing for 7.5% and 10.4% of patients assigned to placebo and LEROCHOL, respectively. Multiple imputation washout model was implemented for imputing missing values at Week 52. b Least-squares mean from an Analysis of Covariance (ANCOVA) model including treatment as a factor and baseline value as a covariate, assuming unequal variances between groups. c p-value <0.001 for superiority, controlled for Type I error rate. d Not controlled for Type I error rate. Treatment Group LDL-C a Total Cholesterol a Non-HDL-C a ApoB a Placebo (n = 308) -0.1 -0.2 -0.7 +1 LEROCHOL 300mg (n = 614) -55 -31 -46 -39 Difference from placebo (LS Mean) (95% CI) -55 b,c (-59, -51) -31 b,d (-33, -28) -45 b,d (-48, -41) -40 b,d (-44, -37) Figure 1: Mean Percent Change from Baseline in LDL-C Over 52 Weeks in Patients with Hypercholesterolemia and ASCVD or Increased Risk for ASCVD Events on Maximally Tolerated Statin Therapy (Trial 1) The primary efficacy outcome measure in Trial 2 was the percent change in LDL-C from baseline compared to placebo to Week 52. The difference between the LEROCHOL and placebo groups by ITT analysis in mean percentage change in LDL-C from baseline to Week 52 was -50% (95% CI: -54.2%, -45.2%; p < 0.0001). For additional results, see Table 4 and Figure 2. Table 4: Changes in Lipid Parameters in Patients with Hypercholesterolemia and ASCVD or Increased Risk for ASCVD Events on Maximally Tolerated Statin Therapy (Percent Change from Baseline to Week 52 in Trial 2) Abbreviation: ApoB = apolipoprotein B; CI = confidence interval; HDL-C = high-density lipoprotein cholesterol; LDL-C = low-density lipoprotein cholesterol; n = number of patients randomly assigned to each treatment group; LS Mean = least-squares mean a LDL-C and non-HDL-C at Week 52 were missing for 10.7% and 11.2% of patients assigned to placebo and LEROCHOL, respectively.
Total Cholesterol and ApoB at Week 52 were missing for 10.4% and 11.2% of patients assigned to placebo and LEROCHOL, respectively. Multiple imputation washout model was implemented for imputing missing values at Week 52. b Least-squares mean from an Analysis of Covariance (ANCOVA) model including treatment and CVD status as factors and baseline value as a covariate, assuming unequal variances between groups. c p-value <0.001 for superiority, controlled for Type I error rate. d Not controlled for Type I error rate. Treatment Group LDL-C a Total Cholesterol a Non-HDL-C a ApoB a Placebo (n = 307) +0.3 +1 +1 +2 LEROCHOL 300mg (n = 615) -49 -28 -41 -36 Difference from placebo (LS Mean) (95% CI) l -50 b,c (-54, -45) -29 b,d (-32, -26) -42 b,d (-46, -38) -38 b,d (-42, -35) Figure 2: Mean Percent Change from Baseline in LDL-C Over 52 Weeks in Patients with Hypercholesterolemia and ASCVD or Increased Risk for ASCVD Events on Maximally Tolerated Statin Therapy (Trial 2) Figure 1 Figure 2 Heterozygous Familial Hypercholesterolemia in Adults Trial 3 (NCT04797104) was a multicenter, double-blind, randomized, placebo-controlled 24-week trial in which 478 patients with HeFH were randomized 2:1 to receive subcutaneous injections of either LEROHOL 300 mg (n = 319) or placebo (n = 159) every 4 weeks.
Patients were stable on diet, maximally tolerated dose of statin, with or without other oral lipid modifying therapy, and required additional LDL-C reduction. Baseline Disease and Demographic Characteristics The mean age at baseline was 53 years (range: 18 to 80 years), 19% were aged 65 years or older, 52% were female, 87% were White, 8% were Black or African American, and 5% were Asian; 1% identified as Hispanic or Latino ethnicity. Forty-five percent of patients had diabetes at baseline.
The mean baseline LDL-C was 150 mg/dL. At the time of randomization, 89% of patients were receiving statin therapy with 67% receiving high-intensity doses, and 49% also on ezetimibe. Endpoint Results The primary efficacy outcome measure in Trial 3 was the percent change in LDL-C from baseline to Week 24. The difference between the LEROCHOL and placebo groups in mean percentage change in LDL-C from baseline to Week 24 was -59% (95% CI: -65.7%, -51.7%; p < 0.0001). For additional results, see Table 5 and Figure 3. Table 5: Changes in Lipid Parameters in Patients with HeFH, on Maximally Tolerated Statin Therapy (Percent Change from Baseline to Week 24 in Trial 3) Abbreviation: ApoB = apolipoprotein B; CI = confidence interval; HDL-C = high-density lipoprotein cholesterol; LDL-C = low-density lipoprotein cholesterol; n = number of patients randomly assigned to each treatment group; LS Mean = least-squares mean a LDL-C, Total Cholesterol and non-HDL-C at Week 24 were missing for 3.1% and 2.8% of patients assigned to placebo and LEROCHOL, respectively. ApoB at Week 24 was missing for 3.1% and 3.1% of patients assigned to placebo and LEROCHOL, respectively.
Multiple imputation washout model was implemented for imputing missing values at Week 24. b Least-squares mean from an Analysis of Covariance (ANCOVA) model including treatment and CVD status as factors and baseline value as a covariate, assuming unequal variances between groups. c p-value <0.001 for superiority, controlled for Type I error rate. d Not controlled for Type I error rate. Treatment Group LDL-C a Total Cholesterol a Non-HDL-C a ApoB a Placebo (n = 159) + 8 +5 +7 +7 LEROCHOL 300mg (n = 319) -51 -32 -44 -37 Difference from placebo (LS Mean) (95% CI) -59 b,c (-66, -52) -37 b,d (-41, -32) -51 b,d (-57, -45) -44 b,d (-49, -39) Figure 3: Mean Percent Change from Baseline in LDL-C Over 24 Weeks in Patients with HeFH on Maximally Tolerated Statin Therapy (Trial 3) Figure
Drug information sourced from the FDA. This content is for informational purposes only and does not constitute medical advice. Consult a healthcare professional before making any medication decisions.
Ready to save on Lerochol?
Compare prescription prices at over 70,000 pharmacies and start saving today—no enrollment required.
Compare Lerochol Prices