Repatha by Amgen Inc

ON AUGUST 27, 2015, the FDA approved Repatha (evolocumab) for the treatment of primary hyperlipidemia in combination with dietary measures and maximally tolerated doses of statins. Use of Repatha is indicated in patients with heterozygous familial hypercholesterolemia (HeFH), patients with homozygous familial hypercholesterolemia (HoFH), and patients with clinical atherosclerotic cardiovascular disease who require additional low-density lipoprotein cholesterol (LDL-C) reduction.

Although Repatha has been shown to lower LDL-C, its effect on cardiovascular morbidity and mortality remains undetermined.1,2

Mechanism of Action
Repatha contains a monoclonal immunoglobulin G2 antibody that binds to circulating protein known as proprotein convertase subtilisin kexin 9 (PCSK9). Normally, PCKS9 binds to and inhibits the activity of the LDL receptor (LDLR) on the surface of hepatocytes. By binding to PCSK9, Repatha prevents PCSK9 from inhibiting LDLR activity.

As a result, more LDLRs are available on hepatocytes to capture LDL-C from the blood, resulting in lower LDL-C levels.2

Pharmacology and Pharmacokinetics
After administration of a single dose of Repatha, maximal PCSK9 inhibition occurs within approximately 4 hours, with peak levels reached within 3 to 4 days. With multiple doses, Repatha trough concentrations accumulate 2- to 3-fold and steady-state trough levels are reached within approximately 12 weeks. Repatha has an effective half-life estimated at 11 to 17 days.2

Age, gender, race, creatinine clearance, and bodyweight had no clinically meaningful effects on the pharmacokinetics of Repatha. Although Repatha has not been studied in patients with severe renal impairment, because monoclonal antibodies are not eliminated renally, severe renal impairment should not affect Repatha exposure.

The dose of Repatha should not be adjusted in patients with mild to moderate hepatic impairment, although it is notable that exposure and maximum concentrations of Repatha were lower in these patients than in healthy patients.2

Dosage and Administration
Prefilled syringes of Repatha contain 1 mL of medication at a concentration of 140 mg/mL. Syringes are supplied either as ordinary prefilled syringes (1 per box) or as SureClick autoinjectors (1 to 3 per box).

Injections of Repatha are administered at a dose of either 140 mg every 2 weeks or 420 mg monthly (3 consecutive injections of 140 mg each administered over a 30-minute period) in patients with HeFH or clinical atherosclerotic cardiovascular disease.

However, only the monthly dosage regimen should be used in patients with HoFH.2 Instruct patients to either store Repatha under refrigeration or to keep Repatha in its original carton at room temperature (no higher than 77°F) for up to 1 month.

If Repatha is refrigerated, it should be kept at room temperature for a minimum of 30 minutes before administration. After inspecting the solution for discoloration and particulates, the medication may be injected subcutaneously into the abdomen, thigh, or upper arm.

Patients should rotate the injection site with each injection. If a dose is missed, the missed dose may be administered late as long as consecutive doses are administered more than 7 days apart.2



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