Dyslipidemia: Blockbuster Therapies Are on the Horizon

Abstract

Potential blockbuster therapies, such as proprotein convertase subtilisin/kexin type 9 inhibitors, are expected to revolutionize dyslipidemia treatment and raise global sales.

Dyslipidemia is recognized as a prominent risk factor for cardiovascular disease (CVD); every 1% decrease in cholesterol levels is linked to a 2% decrease in coronary heart disease risk.^1,2 This disease continues to present a large economic burden in the U.S., with approximately 1.33 million patients diagnosed in 2013.^1,3 Given that the number of patients is expected to rise in the coming years, the acute coronary syndrome market is projected to expand globally from $12.3 billion to $43.4 billion in sales by 2023.³

Dyslipidemia is defined by elevations in low-density lipoprotein-cholesterol (LDL-C) and triglyceride concentrations, in addition to low levels of high-density lipoprotein-cholesterol (HDL-C).⁴ Statins are a universally established therapy due to their ability to dramatically reduce LDL-C levels and lower CVD risk. However, there is a gap in clinical practice when it comes to achieving LDL-C goals for many patients, and 5% to 10% of people cannot tolerate statin treatment.^1,2 Specifically, patients with familial hypercholesterolemia are more likely to suffer from statin resistance and require additional effective therapies.²

Future therapies include the proprotein convertase subtilisin/kexin type 9 (PCSK9) inhibitors, a new class of agents with blockbuster potential that are expected to launch this year and may address the needs unmet by statins. These self-injectable monoclonal antibodies work by increasing the liver’s ability to filter LDL-C from circulation.² Additional novel cholesterol-lowering therapies with specific effects on LDL-C and/or HDL-C levels are also on the horizon. These agents are expected to revolutionize the dyslipidemia market.

Future Therapies

Drug Manufacturer	Status	Regimen Information	Pivotal Studies	Expected Approval	Anticipated Peak Year Sales/Pricing
PCSK9 Inhibitors
Repatha (evolocumab) Amgen	Phase 3	140 mg once every two weeks via SC injection or 420 mg once every four weeks via SC injection	PROFICIO	2015	$10.2 billion by 2023; using the once-every-four-weeks regimen, it is expected that one dose of evolocumab will cost twice as much as one dose of Humira, which is used every two weeks
Praluent (alirocumab) Sanofi/Regeneron	Phase 3	150 mg once every two weeks via SC injection	ODYSSEY	2016	$5.2 billion by 2023; expected to be about 5% lower than current pricing for Humira, which costs $1,921 per 40-mg injection
Bococizumab Pfizer	Phase 2/3	One dose once every two weeks via SC injection	SPIRE	2018	$2.2 billion by 2023; expected to be about 10% lower than current pricing for Humira
Cholesteryl Ester Transfer Protein Inhibitors
Evacetrapib Eli Lilly	Phase 3	130 mg once daily orally	ACCELERATE	2017	$1.1 billion by 2023; expected to be about 30% higher than current cost of Crestor
Anacetrapib Merck	Phase 3	100 mg once daily orally	DEFINE REVEAL	2018	$538.3 million by 2023; expected to be priced about 25% higher than Crestor’s current cost of about $8.23 per pill

SC = subcutaneous

Sources: FDA; GlobalData; company websites; ClinicalTrials.gov

Current Therapies^a

Drug Manufacturer	Approval Date	Indicationb	Regimen Informationc	Cost of Course of Therapy per Yeard
3-Hydroxy-3-Methylglutaryl Coenzyme A Reductase Inhibitors
Livalo (pitavastatin) Kowa Pharmaceuticals	2009	Hyperlipidemia; mixed dyslipidemia	1 mg to 4 mg daily	$2,606
Crestor (rosuvastatin) AstraZeneca	2003	Hyperlipidemia; mixed dyslipidemia; pediatric HeFH; HoFH (adjunct therapy)	5 mg to 40 mg daily	$3,004
Altoprev (lovastatin) Shionogi	2002	Primary prevention of CAD; CAD; hyperlipidemia	20 mg to 60 mg daily	$6,764
Lipitor (atorvastatin) Pfizer	1997	Prevention of CV disease; hyperlipidemia	10 mg to 80 mg daily	$2,652–$3,783 (generic, $134–$702)
Lescol (fluvastatin) Novartis	1993	Hypercholesterolemia; mixed dyslipidemia; secondary prevention of CV disease	20 mg to 80 mg daily	$2,230–$4,460 (generic, $1,377–$2,759)
Zocor (simvastatin) Merck	1992	Hyperlipidemia; HeFH; reductions in risk of CHD mortality and CV events	5 mg to 40 mg daily	$1,235–$2,888 (generic, $1,028–$1,814)
Pravachol (pravastatin) Bristol-Myers Squibb	1991	Prevention of CV disease; hyperlipidemia	40 mg daily	$2,478 (generic, $1,206)
Selective Cholesterol Absorption Inhibitor
Zetia (ezetimibe) Merck	2002	Hyperlipidemia; HoFH; homozygous sitosterolemia	10 mg daily	$3,142
Niacin/Nicotinic Acid
Niaspan (niacin) AbbVie	1997	Primary hyperlipidemia; mixed hyperlipidemia	500 mg	$1,981 (generic, $1,546)
Fibrates
Fibricor (fenofibric acid) Mutual Pharmaceutical	2009	Hyperlipidemia; mixed dyslipidemia; severe hypertriglyceridemia	105 mg daily	$1,503 (generic, $1,096)
Trilipix (fenofibric acid) AbbVie	2008	Mixed dyslipidemia; severe hypertriglyceridemia; hypercholesterolemia	135 mg daily	$3,084 (generic, $1,947)
Triglide (fenofibrate) Shionogi	2005	Hypercholesterolemia; mixed dyslipid- emia; severe hypertriglyceridemia	160 mg daily	$2,916 (generic, $867)
Tricor (fenofibrate) AbbVie	2004	Hypercholesterolemia; mixed dyslipidemia; severe hypertriglyceridemia	145 mg daily	$3,235 (generic, $2,091)
Lopid (gemfibrozil) Pfizer	1981	Hyperlipidemia; reduction in risk of developing CHD	1,200 mg daily	$3,473 (generic, $798)
Combination Therapies
Liptruzet (ezetimibe/atorvastatin) Merck	2013	Hyperlipidemia; HoFH	10/10 mg to 10/80 mg daily	$2,409
Simcor (niacin ER/simvastatin) AbbVie	2008	Hypercholesterolemia	500/20 mg daily	$1,981
Caduet (amlodipine/atorvastatin) Pfizer	2004	Hypertension; CAD; prevention of CV disease; hyperlipidemia	5/10 mg to 10/80 mg daily	$3,602–$4,927
Vytorin (ezetimibe/simvastatin) Merck	2004	Primary hyperlipidemia; HoFH (adjunct therapy)	10/10 mg to 10/40 mg daily	$3,113
Advicor (niacin ER/lovastatin) AbbVie	2001	Hypercholesterolemia	500/20 mg daily	$2,831

^aThis list is not all-inclusive; additional therapies may be available for this disease state.

^bAbbreviated indication provided; for full indication, please refer to prescribing information.

^cRegimens based on the recommended dosage and maintenance phases from prescribing information; typical doses and titration schedules may vary based on patient-specific requirements.

^dCosts calculated using average wholesale price and regimen provided and rounded to the nearest dollar.

Sources: Red Book; Drugs@FDA; and prescribing information for all medications

CAD = coronary artery disease; CHD = coronary heart disease; CV = cardiovascular; ER = extended release; HeFH = heterozygous familial hypercholesterolemia; HoFH = homozygous familial hypercholesterolemia