Nexletol Generic Name & Formulations
Nexletol tablets are supplied as 180 mg strength tablets in 30- and 90-count bottles. Each tablet is white to off white and oval, debossed with “180” on one side and “ESP” on the other side.
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.
Mechanism of Action
Limitations of Use
Nexletol Dosage and Administration
Nexletol Boxed Warnings
Nexletol may increase blood uric acid levels, which typically occurred within the first 4 weeks of initiating treatment and persisted during treatment.
Elevated blood uric acid may result in gout. Patients with a history of gout have an increased risk for gout events.
Assess serum uric acid as clinically indicated. Monitor for signs/symptoms of hyperuricemia, and initiate treatment appropriately.
Increased risk for tendon rupture or injury especially in patients >60 years of age, in those taking corticosteroid or fluoroquinolone drugs, in those with renal failure, and in those with previous tendon disorders.
Discontinue immediately if tendon rupture occurs. Consider discontinuing if joint pain, swelling, or inflammation develop.
Advise patients to rest at the first sign of tendinitis or tendon rupture. Consider alternative therapy if history of tendon disorders or tendon rupture.
Discontinue Nexletol if pregnancy is recognized unless the benefits of therapy outweigh the potential risks to the fetus.
If Nexletol is administered during pregnancy, healthcare providers should report Nexletol exposure by contacting Esperion at 1-833-377-7633.
Nursing Mother Considerations
Advise patients that breastfeeding is not recommended during treatment.
The safety and efficacy of Nexletol have not been established in pediatric patients.
Renal Impairment Considerations
There is limited experience with Nexletol in patients with severe renal impairment (eGFR < 30 mL/min/1.73 m2), and Nexletol has not been studied in patients with end-stage renal disease (ESRD) receiving dialysis.
Hepatic Impairment Considerations
Patients with severe hepatic impairment (Child-Pugh C) have not been studied.
Median time to maximum concentration: 3.5 hours.
Apparent volume of distribution: 18 L. Plasma protein bound: 99.3%.
Renal (~70%), fecal (~30%). Steady-state clearance: 11.2 mL/min. Half-life: 21 ± 11 hours.
Nexletol Adverse Reactions
Nexletol Clinical Trials
The approval was based on data from two phase 3, multicenter, double-blind, placebo-controlled studies (CLEAR Harmony [NCT02666664] and CLEAR Wisdom [NCT02991118]) that evaluated the efficacy and safety of Nexletol in 3009 adult patients with HeFH and/or ASCVD as an add on to a maximally tolerated statin therapy for 52 weeks.
Results demonstrated that Nexletol provided a statistically significant lowering of LDL-C from baseline with a placebo-adjusted difference of -18% (95% CI, -20 to -16; P <.001) in CLEAR Harmony and -17% (95% CI, -21 to -14; P <.001) in CLEAR Wisdom; in both trials, the maximum LDL-C lowering effects occurred at week 4.
Nexletol Patient Counseling
Risk of Hyperuricemia
Advise patients of the risk of elevated serum uric acid levels, including development of gout. Inform patients that serum uric acid levels may be monitored during treatment with Nexletol. Contact your healthcare provider if signs or symptoms of hyperuricemia occur.
Risk of Tendon Rupture
Inform patients of the risk of tendon rupture. Advise patients to rest at the first sign of tendinitis or tendon rupture and to immediately contact their healthcare provider if tendinitis or tendon rupture symptoms occur.
Risk of Myopathy with Concomitant Use of Simvastatin or Pravastatin
Advise patients to notify their healthcare provider(s) if they are taking, or plan to take simvastatin or pravastatin. The risk of myopathy occurring with the use of simvastatin or pravastatin may be increased when taken with Nexletol.
Advise pregnant women of the potential risk to a fetus based on Nexletol’s mechanism of action. Advise females to inform their healthcare provider of a known or suspected pregnancy. Advise women who are exposed to Nexletol during pregnancy that there is a pregnancy surveillance study. Encourage these patients to report their pregnancy to Esperion at 1-833-377- 7633.