NEXLETOL Film-coated tablet (2020)

Βιβλιογραφική αναφορά

Συγγραφείς

Esperion Therapeutics, Inc.

Λέξεις κλειδιά

72426-118

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1. Indications and Usage

NEXLETOL is indicated as an adjunct to diet and maximally tolerated statin therapy for the treatment of adults with heterozygous familial hypercholesterolemia or established atherosclerotic cardiovascular ...

2. Dosage and Administration

2.1 Recommended Dosage The recommended dosage of NEXLETOL, in combination with maximally tolerated statin therapy, is 180 mg administered orally once daily. NEXLETOL can be taken with or without food. ...

3. Dosage Forms and Strengths

NEXLETOL is available as: Tablets: 180 mg, white to off-white, oval shaped, debossed with 180 on one side and ESP on the other side.

4. Contraindications

None.

5. Warnings and Precautions

5.1 Hyperuricemia NEXLETOL inhibits renal tubular OAT2 and may increase blood uric acid levels [see Clinical Pharmacology (12.3)]. In clinical trials, 26% of NEXLETOL-treated patients with normal ...

6. Adverse Reactions

The following clinically significant adverse reactions are described elsewhere in the labeling: Hyperuricemia [see Warnings and Precautions (5.1)] Tendon Rupture [see Warnings and Precautions ...

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 ...

7. Drug Interactions

Simvastatin Clinical Impact: Concomitant use of NEXLETOL with simvastatin causes an increase in simvastatin concentration and may increase the risk of simvastatin-related myopathy [see Clinical Pharmacology ...

8.1. Pregnancy

Risk Summary Discontinue NEXLETOL when pregnancy is recognized unless the benefits of therapy outweigh the potential risks to the fetus. There are no available data on NEXLETOL use in pregnant women to ...

8.2. Lactation

Risk Summary There is no information regarding the presence of NEXLETOL in human or animal milk, the effects of the drug on the breastfed infant, or the effects of the drug on milk production. NEXLETOL ...

8.4. Pediatric Use

The safety and effectiveness of NEXLETOL have not been established in pediatric patients.

8.5. Geriatric Use

Of the 3009 patients in clinical trials of NEXLETOL, 1753 (58%) were 65 years and older, while 478 (16%) were 75 years and older. No overall differences in safety or effectiveness were observed between ...

8.6. Renal Impairment

No dosage adjustment is necessary in patients with mild or moderate renal impairment. There is limited experience with NEXLETOL in patients with severe renal impairment (eGFR <30 mL/min/1.73 m²), and NEXLETOL ...

8.7. Hepatic Impairment

No dosage adjustment is necessary in patients with mild or moderate hepatic impairment (Child-Pugh A or B) [see Clinical Pharmacology (12.3)]. Patients with severe hepatic impairment (Child-Pugh ...

10. Overdosage

There is no clinical experience with NEXLETOL overdose. In the event of an overdosage, contact Poison Control (1-800-222-1222) for latest recommendations.

11. Description

NEXLETOL tablets, for oral use, contain bempedoic acid, an adenosine triphosphate-citrate lyase (ACL) inhibitor. The chemical name for bempedoic acid is 8-hydroxy-2,2,14,14-tetramethyl-pentadecanedioic ...

12.1. Mechanism of Action

Bempedoic acid is an adenosine triphosphate-citrate lyase (ACL) inhibitor that lowers low-density lipoprotein cholesterol (LDL-C) by inhibition of cholesterol synthesis in the liver. ACL is an enzyme upstream ...

12.2. Pharmacodynamics

Administration of bempedoic acid in combination with maximally tolerated statins, with or without other lipid modifying agents, decreases LDL-C, non-high density lipoprotein cholesterol (non-HDL-C), apolipoprotein ...

12.3. Pharmacokinetics

Bempedoic acid pharmacokinetic parameters are presented as the mean [standard deviation ± (SD)] unless otherwise specified. The steady-state maximum plasma concentration (Cmax) and area under ...

13.1. Carcinogenesis, Mutagenesis, Impairment of Fertility

Bempedoic acid was negative for mutagenicity in an in vitro Ames assay and negative for clastogenicity in the vitro human lymphocyte chromosome aberration assay. Bempedoic acid was negative in both in ...

14. Clinical Studies

The efficacy of NEXLETOL was investigated in two multi-center, randomized, double-blind, placebo-controlled trials that enrolled 3009 adult patients with heterozygous familial hypercholesterolemia or established ...

16.1. How Supplied

NEXLETOL (bempedoic acid) tablets are supplied as follows: Tablet Strength Description Package Configuration NDC No. 180 mg White to off white and oval, debossed with 180 on one side and ESP on the ...

16.2. Storage and Handling

Store at 68°F to 77°F (20°C to 25°C); excursions permitted to 59°F to 86°F (15°C to 30°C) [see USP Controlled Room Temperature]. Store and dispense in the original package. Do not discard desiccant. ...

17. Patient Counseling Information

Advise patients to read the FDA-approved patient labeling. Risk of Hyperuricemia Advise patients of the risk of elevated serum uric acid levels, including development of gout. Inform patients that serum ...