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(mipomersen sodium) Injection
RISK OF HEPATOTOXICITY
KYNAMRO can cause elevations in transaminases. In the KYNAMRO clinical trial in patients with HoFH, 4 (12%) of the 34 patients treated with KYNAMRO compared with 0% of the 17 patients treated with placebo had at least one elevation in alanine aminotransferase (ALT) ≥ 3x upper limit of normal (ULN). There were no concomitant clinically meaningful elevations of total bilirubin, international normalized ratio (INR) or partial thromboplastin time (PTT) [see WARNINGS AND PRECAUTIONS].
KYNAMRO also increases hepatic fat, with or without concomitant increases in transaminases. In the trials in patients with heterozygous familial hypercholesterolemia (HeFH) and hyperlipidemia, the median absolute increase in hepatic fat was 10% after 26 weeks of treatment, from 0% at baseline, measured by magnetic resonance imaging (MRI). Hepatic steatosis is a risk factor for advanced liver disease; including steatohepatitis and cirrhosis [see WARNINGS AND PRECAUTIONS].
Measure ALT, AST, alkaline phosphatase, and total bilirubin before initiating treatment and then ALT, AST regularly as recommended. During treatment, withhold the dose of KYNAMRO if the ALT or AST are ≥ 3 x ULN. Discontinue KYNAMRO for clinically significant liver toxicity [see DOSAGE AND ADMINISTRATION and WARNINGS AND PRECAUTIONS].
Because of the risk of hepatotoxicity, KYNAMRO is available only through a restricted program under a Risk Evaluation and Mitigation Strategy (REMS) called the KYNAMRO REMS [see WARNINGS AND PRECAUTIONS].
KYNAMRO (mipomersen sodium) Injection is a sterile, preservative-free, clear, colorless to slightly yellow, aqueous solution for subcutaneous injection. KYNAMRO is supplied in single-use, 2 mL, clear glass vials or single-use, 1 mL, clear glass pre-filled syringes filled to deliver 1 mL of solution containing 200 mg of mipomersen sodium (200 mg per 1 mL). KYNAMRO is formulated in water for injection and may include hydrochloric acid and/or sodium hydroxide for pH adjustment to 7.5 – 8.5.
Mipomersen sodium is an oligonucleotide inhibitor of apo B-100 synthesis. ApoB is the principal apolipoprotein of LDL and its metabolic precursor, very low density lipoprotein (VLDL). Mipomersen inhibits synthesis of apoB by sequence-specific binding to its messenger ribonucleic acid (mRNA) resulting in degradation of the mRNA through enzyme-mediated pathways or disruption of mRNA function through binding alone.
Mipomersen sodium is a synthetic phosphorothioate oligonucleotide sodium salt, 20 nucleotides in length, with the following sequence:
5'-GMeCMeCMeUMeC AGTMeCTGMeCTTMeC GMeCAMeCMeC- 3'
where the underlined residues are 2'-O-(2-methoxyethyl) nucleosides; all other residues are 2'-deoxynucleosides. Substitution at the 5-position of the cytosine (C) and uracil (U) bases with a methyl group is indicated by Me.
Mipomersen sodium is represented by the following structural formula:
The molecular formula of mipomersen sodium is C230H305N67O122P19S19Na19 and the molecular weight is 7594.9 g/mol.
Last reviewed on RxList: 2/8/2013
This monograph has been modified to include the generic and brand name in many instances.
Additional Kynamro Information
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