Skip to main content

KYNAMRO (Mipomersen) Lipid lowering drug in patients with Homozygous Familial Hypercholesterolemia

KYNAMRO (mipomersen sodium) Injection Solution

Mipomersen is an antisense oligonucleotide targeted to human messenger ribonucleic 399 acid (mRNA) for apo B-100, the principal apolipoprotein of LDL and its metabolic 400 precursor, VLDL. Mipomersen is complementary to the coding region of the mRNA for 401 apo B-100, and binds by Watson and Crick base pairing. The hybridization of 402 mipomersen to the cognate mRNA results in RNase H-mediated degradation of the 403 cognate mRNA thus inhibiting translation of the apo B-100 protein.

KYNAMRO (mipomersen sodium) Injection Solution for Subcutaneous Injection

Initial U.S. Approval: 2013

WARNING: RISK OF HEPATOTOXICITY
  • KYNAMRO can cause elevations in transaminases
  • Measure alanine aminotransferase (ALT), aspartate aminotransferase (AST), alkaline phosphatase, and total bilirubin before initiating treatment and then ALT and AST regularly as recommended.
  • During treatment, withhold the dose of KYNAMRO if the ALT or AST is ≥3 times the upper limit of normal (ULN)
  • Discontinue KYNAMRO for clinically significant liver toxicity. KYNAMRO increases hepatic fat (hepatic steatosis) with or without concomitant increases in transaminases. 
  • Hepatic steatosis associated with KYNAMRO may be a risk factor for progressive liver disease, including steatohepatitis and cirrhosis. Because of the risk of hepatotoxicity, KYNAMRO is available only through a restricted program called the KYNAMRO REMS

INDICATIONS AND USAGE
  • KYNAMRO™ is an oligonucleotide inhibitor of apolipoprotein B-100 synthesis indicated as an adjunct to lipid-lowering medications and diet to reduce low density lipoprotein-cholesterol (LDL-C), apolipoprotein B (apo B), total cholesterol (TC), and non-high density lipoprotein-cholesterol (non HDL-C) in patients with homozygous familial hypercholesterolemia (HoFH). 
  • Limitations of Use:
  • The safety and effectiveness of KYNAMRO have not been established in patients with hypercholesterolemia who do not have HoFH. 
  • The effect of KYNAMRO on cardiovascular morbidity and mortality has not been determined. 

DOSAGE AND ADMINISTRATION
  • 200 mg once weekly as a subcutaneous injection.
  • Before treatment, measure ALT, AST, alkaline phosphatase, and total bilirubin.
  • DOSAGE FORMS AND STRENGTHS
  • Single-use vial containing 1 mL of a 200 mg/mL solution. 
  • Single-use pre-filled syringe containing 1 mL of a 200 mg/mL solution

CONTRAINDICATIONS
  • Moderate or severe hepatic impairment, or active liver disease, including unexplained persistent elevations of serum transaminases 
  • Known sensitivity to product components 

WARNINGS AND PRECAUTIONS
  • Injection site reactions occur in 84% of patients and typically consist of one or more of the following: erythema, pain, tenderness, pruritus and local swelling.
  • Flu-like symptoms, which typically occur within 2 days after injection, occur in 30% of patients and include one or more of the following: influenza-like illness, pyrexia, chills, myalgia, arthralgia, malaise or fatigue.

ADVERSE REACTIONS
The most commonly reported adverse reactions (incidence ≥ 10% and greater than placebo) are injection site reactions, flu-like symptoms, nausea, headache, and elevations in serum transaminases, specifically ALT.
 
USE IN SPECIFIC POPULATIONS\
  • Nursing mothers: Discontinue drug or nursing. 
  • Pediatric Patients: Safety and effectiveness not established. 


Comments

Popular posts from this blog

Carbohydrate Metabolism: MCQs and answers on Glycolysis & Gluconeogenesis

                                      MCQ on Glycolysis & Gluconeogenesis 1) Which of the following enzyme is not involved in galactose metabolism? a) Glucokinase b) Galactokinase c) Galactose-1-Phosphate Uridyl transferase d) UDP-Galactose 4- epimerase 2) Which of the following enzyme is defective in galactosemia (type I) - a fatal genetic disorder in infants? a) Glucokinase b) Galactokinase c) Galactose-1-Phosphate Uridyl transferase d) UDP-Galactose 4- epimerase 3) In the liver, the accumulation of which of the following metabolite attenuates the inhibitory of ATP on phosphofructokinase? a) Glucose-6-Phosphate b) Citrate c) Fructose-1,6-Bisphosphate d) Fructose-2,6-Bisphosphate 4) Mutation in which of the following enzymes leads to a glycogen storage disease known as "Tarui’s disease"? a) Glucokinase b) Phosphofructokinase c) Phosphoglucomutase d) Pyruvate Kinase 5) E...

MCQs and Answers on cultivation (culture/incubation), Isolation and Identification of microorganisms: Medical Microbiology

40 plus questions - Multiple Choice Questions on Classification, Culture, and Identification of the microorganisms 1. Which of the following microorganism has the cocci cell shapes and sizes arranged usually in tetrad structures? a)  Streptococcus pneumoniae b)  Staphylococcus aureus c)  Chlamydia trachomatis d)  Neisseria meningitidis 2. What are the different growth morphology and cell structures used for the classification of fungi? Select all the correct answers: a) Yeast b) Mold c) Mycelia d) Protozoa 3. Which of the following media is formulated with additional nutrients to support the growth of fastidious or nutritionally demanding bacteria that may not grow well on basic media? a) Differential media b) Enriched media c) Nutrient agar (media) d) Selective media 4. Which of the following metabolic characteristic is a distinguishing characteristic and identification of colonies of  E. coli ? a) Hydrogen sulfide formation b) Indole Formation c) Lactose fe...

MCQs on Bacterial Pathogenesis: Medical Microbiology

Key aspects of Bacterial pathogenesis/ General steps in bacterial pathogenesis Adherence and Colonization  Invasion Immune Evasion Toxin Production Nutrient Acquisition Host Cell Manipulation Inflammation and Tissue Damage                         Multiple Choice Questions on Bacterial Pathogenesis       Figure 1: Phagocyte activity and possible outcomes of phagocyte-bacterial interactions                                     (Source/Reference: Bailey & Scott’s Diagnostic  Microbiology) 1) Which of the following microorganism is the major inhabitant of the human skin? a) Escherichia coli b) Staphylococcus epidermidis c) Staphylococcus aureus d) Streptococcus pyogenes 2) Select all the medically important bacteria which are frequently isolated pathogen  human infections? a) Enteric ba...