Overview
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.
Mechanism of Action
12 CLINICAL PHARMACOLOGY 12.1 Mechanism of Action Lerodalcibep-liga is a recombinant fusion protein that binds PCSK9 with picomolar affinity. PCSK9 binds to low-density lipoprotein receptor (LDLR) on the surface of hepatocytes to promote LDLR degradation within the liver. By inhibiting the binding of PCSK9 to LDLR, lerodalcibep-liga increases the number of LDLRs available to clear LDL-C from the blood, thereby lowering LDL-C levels. [see Clinical Pharmacology ( 12.3 )] . 12.2 Pharmacodynamics After subcutaneous administration of 300 mg lerodalcibep-liga every month, greater than 90% suppression of PCSK9 occurs within 24 hours after dosing and is maintained throughout the dosing interval, returning toward baseline during the last 7 to 10 days of the monthly dosing period. 12.
Indications
- 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 )
Common Doses
- 300 mg
Dosage
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.
Contraindications
- 4 CONTRAINDICATIONS None. None. ( 4 )
Side Effects
- 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...
Interactions
- No major interactions listed on the FDA label. Always consult a healthcare professional.