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New Therapeutic Agents Marketed in 2015: Part 4 Amy M CPE New therapeutic agents marketed in 2015: Part 4 Amy M. Lugo and Brian Park Amy M. Lugo, PharmD, BCPS, BC-ADM, Abstract FAPhA, Clinical Pharmacy Specialist, Pharmacy Operations Division, Formu- lary Management Branch, Defense Health Objective: To provide information about the most important properties of new Agency, San Antonio therapeutic agents approved by FDA and first marketed in 2015. Brian Park, PharmD candidate, University of Data sources: Product labeling supplemented selectively with published stud- New England College of Pharmacy, Portland, ies and drug information reference sources. ME Data synthesis: This review covers 11 new therapeutic agents approved by FDA Correspondence: Amy M. Lugo, 7800 and first marketed in the United States in 2015: selexipag, cobimetinib, osimertinib, IH-10 W, Ste. 335, San Antonio, TX 78230; necitumumab, alectinib, insulin degludec, lesinurad, mepolizumab, brexpiprazole, [email protected] cariprazine, and flibanserin. Indications and information on dosage and adminis- Disclosure: The authors declare no conflicts tration for these agents are reviewed, as well as efficacy, safety, the most important of interest or financial interests in any product or service mentioned in this article. pharmacokinetic properties, drug interactions, and other precautions. Practical considerations for use of these new agents also are discussed. Whenever possible, Department of Defense (DoD) disclaimer: The information discussed here represents properties of the new drugs are compared with those of older agents marketed for the views of the author and does not neces- the same indications. sarily reflect the views of DoD or the Depart- Summary: Selexipag is the second oral prostacyclin agonist for the treatment ments of the Army, Navy, or Air Force. of pulmonary arterial hypertension. Cobimetinib is a new agent indicated for un- resectable or metastatic melanoma. Three new drugs (osimertinib, necitumumab, and alectinib) have been approved for the treatment of various types of non–small cell lung cancer. Insulin degludec is a new long-acting basal insulin for diabetes. Lesinurad is a novel agent approved for the treatment of hyperuricemia in gout. Mepolizumab is a monoclonal antibody for adolescents and adults with severe eosinophilic asthma. Brexpiprazole and cariprazine are two new atypical antipsy- chotics indicated for schizophrenia. Brexpiprazole is also approved as an adjunct to antidepressant therapy for major depressive disorder, and cariprazine is also approved for bipolar disorders. Flibanserin is the first drug approved for women with hypoactive sexual desire disorder. Pharm Today. 2016;22(4):59–76 Accreditation information Provider: American Pharmacists Association ACPE number: 0202-0000-16-103-H01-P Target audience: Pharmacists CPE credit: 2 hours (0.2 CEUs) Release date: April 1, 2016 Fee: There is no fee associated with this activity Expiration date: April 1, 2019 for members of the American Pharmacists Learning level: 2 Association. There is a $25 fee for nonmembers. Learning objectives The American Pharmacists Association is accredited by the Accreditation Council ■ List new therapeutic agents approved for Pharmacy Education as a provider of continuing pharmacy education (CPE). The by FDA and first marketed in 2015. ACPE Universal Activity Number assigned to this activity by the accredited provider is ■ Describe the mechanisms of action and 0202-0000-16-103-H01-P. indications for these new therapeutic Advisory Board: Mark S. Johnson, PharmD, BCPS, Professor and Vice Chair, Department of agents. Pharmacy Practice and Director of Postgraduate Education, Bernard J. Dunn School of Pharmacy, ■ Compare and contrast the new thera- Shenandoah University, Winchester, VA. peutic agents with products available Disclosures: Mark S. Johnson, PharmD, BCPS, declares that he and his spouse hold stock in with similar indications. Merck & Co. Amy M. Lugo, PharmD, BCPS, BC-ADM, FAPhA; Brian Park; and APhA’s editorial staff ■ Summarize adverse effects and patient declare no conflicts of interest or financial interests in any product or service mentioned in this activ- safety considerations for the new ity, including grants, employment, gifts, stock holdings, and honoraria. For complete staff disclo- therapeutic agents. sures, please see the APhA Accreditation Information section at www.pharmacist.com/education. ■ Discuss important patient education Development: This home-study CPE activity was developed by the American Pharmacists and therapeutic monitoring parameters Association. for the new therapeutic agents. www.pharmacist.com APRIL 2016 • PharmacyToday 59 CPE NEW THERAPEUTIC AGENTS MARKETED IN 2015: PART 4 enous prostacyclin, it has its own distinct mechanism of Preassessment questions action as a selective prostacyclin IP receptor agonist, which Before participating in this activity, test your knowledge by answering the following questions. These questions will also be part of the CPE could theoretically decrease adverse gastrointestinal drug exam. reactions (nausea and vomiting) in comparison with other prostacyclin agonists.2 1. Which of the following drugs is administered subcutaneously? a. Lesinurad c. Alectinib Selexipag has rapid absorption and is highly protein b. Necitumumab d. Mepolizumab bound (~99%) to albumin and alpha-1 acid glycoprotein. With hepatic metabolism, selexipag is converted to an active 2. With use of which of the following agents is bradycardia the most metabolite via the isoenzymes cytochrome P450 (CYP) 3A4, important risk? CYP2C8, uridine 5'-diphosphate-glucuronosyltransferase a. Alectinib (UGT) 1A3, and UGT2B7. The active metabolite has a half-life b. Osimertinib of 6.2 to 13.5 hours, and absorption of the drug is delayed c. Mepolizumab 2 d. Necitumumab with food. Excretion is primarily in the feces (~93%). Selexipag is dosed 200 mcg orally twice daily, then in- 3. Which of the following statements is correct about brexpiprazole? creased by 200 mcg twice daily, typically at weekly intervals, a. The most common adverse effect is weight loss. to the highest tolerated dose. See additional dosing informa- b. It is safe to use in pregnant woman. c. Warnings include blood dyscrasias, central nervous system tion in Table 2. A missed dose should be taken as soon as effects, and dyslipidemia. possible unless the next dose is within the next 6 hours. If 3 d. It is safe to use in older adult patients. or more days of treatment are missed, restart at a lower dose and then retitrate.2 No dose adjustments are necessary in renal impairment Objective or mild hepatic impairment, although the label recommends The fourth and final part of this four-part series on new ther- once-daily instead of twice-daily dosing for moderate hepat- apeutic agents approved in the United States in 2015 covers ic impairment (Child-Pugh Class B). Use should be avoided 11 new drugs: selexipag, cobimetinib, osimertinib, necitu- in severe hepatic impairment. Selexipag has not been studied mumab, alectinib, insulin degludec, lesinurad, mepolizumab, in patients with a glomerular filtration rate (GFR) of less than brexpiprazole, cariprazine, and flibanserin. Tables 1 through 15 mL/min or in hemodialysis. 5 provide additional information on these newly approved Efficacy of selexipag was evaluated in the GRIPHON agents, including detailed dosing, pharmacology, pregnancy study, a randomized, double-blind, placebo-controlled tri- and lactation information, and related abbreviations. al in 1,156 patients with symptomatic PAH (mostly WHO Group II or III) who were treatment naive or already on treat- New cardiology agent: Selexipag ment. Patients were randomized to receive either selexipag Pulmonary arterial hypertension (PAH) is an uncommon 200 mcg orally twice daily or placebo and continue therapy disease. Patients with PAH have a dysregulation in the endo- until a prespecified number of primary endpoints was thelin, nitric oxide, and/or prostacyclin metabolic pathways reached. The dose was increased weekly by increments of that leads to constriction of the pulmonary arteries and an 200 mcg twice daily to the highest tolerated dose up to 1,600 enlarged right ventricle. Right heart failure and pulmonary mcg twice daily. The primary endpoint was time to a com- edema are the principal consequences of PAH.1 posite endpoint of death or a complication related to PAH, Multiple classes of drugs are used in the treatment of whichever occurred first. Disease progression was defined PAH, such as endothelin receptor antagonists (ambrisen- as a decrease from baseline of at least 15% in the 6-minute tan, bosentan, and macitentan); drugs that work in the ni- walk distance (6MWD).3 tric oxide pathway, including phosphodiesterase-5 inhibitors Results of the GRIPHON study showed a 40% reduction (tadalafil and sildenafil) and guanylate cyclase stimulators in the primary composite endpoint in the selexipag arm com- (riociguat); and prostacyclin receptor agonists (epoprostenol, pared with the placebo arm. Of note, there was no significant treprostinil, and iloprost). Until recently, use of a prostacyclin difference in mortality between the selexipag and placebo agonist was limited to I.V. and inhaled therapies. Treprostinil groups. The secondary endpoint of 6MWD showed an in- became available in an oral dosage form in 2013 with the ap- crease of 4.0 m in the selexipag group and a decrease of 9.0 m proval of Orenitram (United Therapeutics). Prostacylins are in the placebo group from baseline to week 26. The median typically not used
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