• Long-term data analysis suggests that REXULTI was associated with a sustained, clinically meaningful response over 24 weeks with a consistent rate of improvement.1
  • Patients who received REXULTI showed a reduction in frequency of the most common agitation behaviors compared to those who received a placebo, including restlessness, pacing and cursing.2
  • Among the behaviors rated by caregivers as the “most bothersome,” patients who received REXULTI had a greater reduction in frequency of those behaviors compared to those who received a placebo.3
  • REXULTI is the first and only treatment approved by the U.S. Food and Drug Administration (FDA) for agitation associated with dementia due to Alzheimer’s disease.4

Otsuka Pharmaceutical Development & Commercialization, Inc. (Otsuka) and Lundbeck Pharmaceuticals LLC (Lundbeck) presented new post hoc pooled analyses of Phase 3 trials evaluating the safety and efficacy of REXULTI® (brexpiprazole) in patients with agitation associated with dementia due to Alzheimer’s disease.1-3 These data analyses were presented in three posters at the 2024 Alzheimer’s Association International Conference (AAIC), taking place July 28 to Aug. 2 in Philadelphia, USA.1-3

This press release features multimedia. View the full release here: https://www.businesswire.com/news/home/20240731398299/en/

New analysis from an extension trial confirmed the efficacy of REXULTI in treating patients with agitation associated with dementia due to Alzheimer’s disease. The analysis explored clinically meaningful response (CMR) among patients over 12 and 24 weeks (NCT03548584 and NCT03594123), defined by a 20-point score reduction from baseline in Cohen-Mansfield Agitation Inventory (CMAI) total score. Over the initial 12-week Phase 3 trial period, approximately 62 percent of patients who received REXULTI achieved a CMR versus approximately 45 percent of patients who received placebo. Following this, patients enrolled in a 12-week extension trial, during which efficacy was an exploratory endpoint. Over the full 24-week period, approximately 82 percent of patients previously on REXULTI achieved a CMR while approximately 73 percent of patients who were switched to REXULTI from placebo also achieved a CMR.1

The second analysis focused specifically on patients (n=610) who most frequently exhibited agitation symptoms at baseline in two Phase 3 trials (NCT03548584 and NCT01862640). Efficacy was measured using the CMAI, which gauges the frequency of 29 agitation behaviors, including restlessness, pacing/aimless wandering, and cursing or verbal aggression, each scoring 1 (never) to 7 (a few times an hour). Patients taking REXULTI showed a reduction in frequency of the most common agitation behaviors, with a numerically greater reduction of the least squares mean CMAI score in 24 out of the 29 agitation behaviors versus placebo from baseline to Week 12.2

A further analysis of the same group of patients (n=610) specifically examined the efficacy of REXULTI in agitation behaviors that had been identified by unpaid caregivers as “most bothersome” and which may influence their decision to transfer the patient to long-term care. The survey highlighted agitation behaviors such as excessive motor activity, verbal aggression and physical aggression. In patients frequently exhibiting these bothersome behaviors, fixed-dosed (2 or 3 mg/day) REXULTI was associated with a greater reduction in frequency of these behaviors than placebo.3

“Agitation is a complex and stressful aspect of caring for people living with Alzheimer’s dementia,”5 said John Kraus, M.D., Ph.D., executive vice president and chief medical officer, Otsuka. “This is the first time REXULTI was associated with a sustained clinically meaningful response over 24 weeks, providing clinicians with longer term data to inform clinical practice.”1

“These new data analyses underscore the efficacy of REXULTI in addressing the most frequent forms of agitation behaviors in patients,” said Johan Luthman, DDS, Ph.D., executive vice president, Lundbeck Research & Development. “Collectively, the analyses presented add to a substantial body of clinical evidence showing the potential of REXULTI to address the many ways agitation presents itself, which can impact patients’ and their caregivers’ lives.”

About Agitation Associated with Dementia Due to Alzheimer’s Disease

Agitation associated with dementia due to Alzheimer’s disease is a common neuropsychiatric symptom that is reported in approximately half of all patients with dementia due to Alzheimer’s disease.5 The condition has a large impact on patients, family members and caregivers.5,6

Agitation associated with dementia due to Alzheimer’s disease covers a large group of behaviors occurring in patients with this condition, such as pacing, gesturing, profanity, shouting, shoving and hitting.7 Symptoms of agitation are also a consistent predictor of nursing home admission in patients with dementia, including those with Alzheimer’s disease.8-9

About REXULTI (brexpiprazole)

Brexpiprazole was approved in the U.S. in 2015, as an adjunctive therapy to antidepressants in adults with major depressive disorder (MDD) and as a treatment for schizophrenia in adults. Most recently, brexpiprazole was approved in the U.S. for the treatment of agitation associated with dementia due to Alzheimer's disease, in May 2023. Brexpiprazole was also approved by Health Canada for schizophrenia and adjunctive treatment of MDD in 2017 and 2019, respectively, and for agitation associated with dementia due to Alzheimer's disease in 2024. It was approved by the European Medicines Agency in 2018 for the treatment of schizophrenia and the Ministry of Health, Labour and Welfare in Japan for the treatment of schizophrenia and MDD in 2018 and 2023, respectively.

Brexpiprazole was discovered by Otsuka and is being co-developed by Otsuka and Lundbeck. The mechanism of action of brexpiprazole is unknown. Brexpiprazole has high receptor binding affinity to norepinephrine, serotonin and dopamine receptors. It is an antagonist at norepinephrine α1B and α2C receptors and serotonin 5-HT2A receptors, as well as a partial agonist at serotonin 5-HT1A and dopamine D2 receptors.10-12

INDICATION and IMPORTANT SAFETY INFORMATION for REXULTI® (brexpiprazole)

INDICATION: REXULTI is a prescription medicine used to treat agitation that may happen with dementia due to Alzheimer’s disease. REXULTI should not be used as an “as needed” treatment for agitation that may happen with dementia due to Alzheimer’s disease.

IMPORTANT SAFETY INFORMATION:

Increased risk of death in elderly people with dementia-related psychosis. Medicines like REXULTI can raise the risk of death in elderly people who have lost touch with reality (psychosis) due to confusion and memory loss (dementia). REXULTI is not approved for the treatment of people with dementia-related psychosis without agitation that may happen with dementia due to Alzheimer’s disease.

Do not take REXULTI if you are allergic to brexpiprazole or any of the ingredients in REXULTI.

REXULTI may cause serious side effects, including:

  • Cerebrovascular problems, including stroke, in elderly people with dementia-related psychosis that can lead to death.
  • Neuroleptic malignant syndrome (NMS) is a serious condition that can lead to death. Call your healthcare provider or go to the nearest hospital emergency room right away if you have some or all of the following signs and symptoms of NMS: high fever; changes in your pulse, blood pressure, heart rate, and breathing; stiff muscles; confusion; increased sweating.
  • Uncontrolled body movements (tardive dyskinesia). REXULTI may cause movements that you cannot control in your face, tongue, or other body parts. Tardive dyskinesia may not go away, even if you stop taking REXULTI. Tardive dyskinesia may also start after you stop taking REXULTI.
  • Problems with your metabolism such as:
    • high blood sugar (hyperglycemia) and diabetes. Increases in blood sugar can happen in some people who take REXULTI. Extremely high blood sugar can lead to coma or death. Your healthcare provider should check your blood sugar before you start, or soon after you start REXULTI and then regularly during long term treatment with REXULTI. Call your healthcare provider if you have any of these symptoms of high blood sugar during treatment with REXULTI:
      • feel very thirsty
      • feel very hungry
      • feel sick to your stomach
      • need to urinate more than usual
      • feel weak or tired
      • feel confused, or
      • your breath smells fruity
  • increased fat levels (cholesterol and triglycerides) in your blood. Your healthcare provider should check the fat levels in your blood before you start, or soon after you start REXULTI, and then periodically during treatment with REXULTI.
    • weight gain. You and your healthcare provider should check your weight before you start and often during treatment with REXULTI.
  • Unusual and uncontrollable (compulsive) urges. Some people taking REXULTI have had strong unusual urges to gamble and gambling that cannot be controlled (compulsive gambling). Other compulsive urges include sexual urges, shopping, and eating or binge eating. If you or your family members notice that you are having new or unusual strong urges or behaviors, talk to your healthcare provider.
  • Low white blood cell count. Your healthcare provider may do blood tests during the first few months of treatment with REXULTI.
  • Decreased blood pressure (orthostatic hypotension) and fainting. You may feel dizzy, lightheaded or pass out (faint) when you rise too quickly from a sitting or lying position.
  • Falls. REXULTI may make you sleepy or dizzy, may cause a decrease in your blood pressure when changing position (orthostatic hypotension), and can slow your thinking and motor skills which may lead to falls that can cause fractures or other injuries.
  • Seizures (convulsions).
  • Problems controlling your body temperature so that you feel too warm. Do not become too hot or dehydrated during treatment with REXULTI. Do not exercise too much. In hot weather, stay inside in a cool place if possible. Stay out of the sun. Do not wear too much clothing or heavy clothing. Drink plenty of water.
  • Difficulty swallowing that can cause food or liquid to get into your lungs.
  • Sleepiness, drowsiness, feeling tired, difficulty thinking and doing normal activities. Do not drive a car, operate machinery, or do other dangerous activities until you know how REXULTI affects you. REXULTI may make you feel drowsy.

Before taking REXULTI, tell your healthcare provider about all of your medical conditions, including if you:

  • have or have had heart problems or a stroke
  • have or have had low or high blood pressure
  • have or have had diabetes or high blood sugar or a family history of diabetes or high blood sugar.
  • have or have had high levels of total cholesterol, LDL cholesterol, or triglycerides, or low levels of HDL cholesterol
  • have or have had seizures (convulsions)
  • have or have had kidney or liver problems
  • have or have had a low white blood cell count
  • are pregnant or plan to become pregnant. REXULTI may harm your unborn baby. Taking REXULTI during your third trimester of pregnancy may cause your baby to have abnormal muscle movements or withdrawal symptoms after birth. Talk to your healthcare provider about the risk to your unborn baby if you take REXULTI during pregnancy.
    • Tell your healthcare provider if you become pregnant or think you are pregnant during treatment with REXULTI.
    • There is a pregnancy exposure registry for women who are exposed to REXULTI during pregnancy. If you become pregnant during treatment with REXULTI, talk to your healthcare provider about registering with the National Pregnancy Registry for Psychiatric Medications. You can register by calling 1-866-961-2388 or visit http://womensmentalhealth.org/clinical-and-research-programs/pregnancyregistry/.
  • are breastfeeding or plan to breastfeed. It is not known if REXULTI passes into your breast milk. Talk to your healthcare provider about the best way to feed your baby during treatment with REXULTI.

Tell your healthcare provider about all the medicines you take, including prescription and over-the-counter medicines, vitamins, and herbal supplements. REXULTI and other medicines may affect each other causing possible serious side effects. REXULTI may affect the way other medicines work, and other medicines may affect how REXULTI works. Your healthcare provider can tell you if it is safe to take REXULTI with your other medicines. Do not start or stop any medicines during treatment with REXULTI without first talking to your healthcare provider.

The most common side effects of REXULTI include weight gain, sleepiness, dizziness, common cold symptoms, and restlessness or feeling like you need to move (akathisia).

These are not all the possible side effects of REXULTI. For more information, ask your healthcare provider or pharmacist.

You are encouraged to report side effects of REXULTI (brexpiprazole). Please contact Otsuka America Pharmaceutical, Inc. at 1-800-438-9927 or FDA at 1-800-FDA-1088 (www.fda.gov/medwatch).

Please read FULL PRESCRIBING INFORMATION, including BOXED WARNING, and MEDICATION GUIDE for REXULTI.

About Otsuka Otsuka Pharmaceutical Co., Ltd. is a global healthcare company with the corporate philosophy: Otsuka–people creating new products for better health worldwide. Otsuka researches, develops, manufactures, and markets innovative products, with a focus on pharmaceutical products to meet unmet medical needs and nutraceutical products for the maintenance of everyday health.

In pharmaceuticals, Otsuka is a leader in the challenging areas of mental, renal, and cardiovascular health and has additional research programs in oncology and on several under-addressed diseases including tuberculosis, a significant global public health issue. These commitments illustrate how Otsuka is a “big venture” company at heart, applying a youthful spirit of creativity in everything it does.

Otsuka established a presence in the U.S. in 1973 and today its U.S. affiliates include Otsuka Pharmaceutical Development & Commercialization, Inc. (OPDC) and Otsuka America Pharmaceutical, Inc. (OAPI). These two companies’ 2,250 employees in the U.S. develop and commercialize medicines in the areas of mental health and nephrology, using cutting-edge technology to address unmet healthcare needs.

OPDC and OAPI are indirect subsidiaries of Otsuka Pharmaceutical Co., Ltd., which is a subsidiary of Otsuka Holdings Co., Ltd. headquartered in Tokyo, Japan. The Otsuka group of companies employed 34,400 people worldwide and had consolidated sales of approximately USD 14.2 billion in 2023.

All Otsuka stories start by taking the road less traveled. Learn more about Otsuka in the U.S. at www.otsuka-us.com and connect with us on LinkedIn and Twitter at @OtsukaUS. Otsuka Pharmaceutical Co., Ltd.’s global website is accessible at https://www.otsuka.co.jp/en/.

About Lundbeck Lundbeck Pharmaceuticals LLC is a wholly owned US subsidiary of H. Lundbeck A/S (HLUNa/ HLUNb, HLUNA DC/HLUNB DC), a global biopharmaceutical company focused exclusively on neuroscience, with more than 70 years of experience in improving the lives of people with neurological and psychiatric diseases.

As a focused innovator, we strive for our research and development programs to tackle some of the most complex challenges. We develop transformative medicines targeting people for whom there are few, if any, treatment options. Our goal is to create long term value and make a positive contribution to people and societies, everywhere we operate. We are committed to fighting stigma and discrimination, and we act to improve health equity for the people we serve and the communities we are part of.

Too many people worldwide live with brain diseases – complex conditions often invisible to others that nonetheless take a tremendous toll on individuals, families and societies. We are committed to fighting stigma and discrimination against people living with brain diseases and advocating for broader social acceptance of people with brain health conditions. Every day, we strive for improved treatment and a better life for people living with brain disease.

We have approximately 5,700 employees, and our products are available in more than 100 countries. Our research programs tackle some of the most complex challenges in neuroscience, and our pipeline is focused on bringing forward transformative treatments for brain diseases for which there are few, if any, therapeutic options. We have research facilities in Denmark and the United States, and our production facilities are located in Denmark, France, and Italy.

Lundbeck US comprises the wholly owned US subsidiaries of H. Lundbeck A/S, including Lundbeck LLC and Lundbeck Pharmaceuticals LLC. With a workforce of more than 1,000 colleagues, Lundbeck US is deeply committed to enhancing the lives of patients, families, and caregivers through focused innovation in neuroscience. For additional information, please visit Lundbeck.com/us and connect with us on LinkedIn and X at @LundbeckUS.

References

  1. Brubaker M, Wang D, Chumki SR, et al. Sustained clinically meaningful response in patients with agitation associated with dementia due to Alzheimer’s disease treated with brexpiprazole: post hoc analysis. Presented at AAIC (July 28–Aug. 2).
  2. Brubaker M, Wang D, Chumki SR, et al. Efficacy of brexpiprazole on frequently occurring agitation behaviors in patients with dementia due to Alzheimer’s disease: post hoc pooled analysis of two randomized controlled trials. Presented at AAIC (July 28–Aug. 2).
  3. Brubaker M, Wang D, Chumki SR, et al. Efficacy of brexpiprazole on agitation in patients with dementia due to Alzheimer’s disease exhibiting behaviors most bothersome to caregivers: post hoc pooled analysis of two randomized controlled trials. Presented at AAIC (July 28–Aug. 2).
  4. FDA News Release. FDA Approves First Drug to Treat Agitation Symptoms Associated with Dementia due to Alzheimer’s Disease. Published: May 11, 2023. Last accessed: Feb. 20, 2024. Available at: https://www.fda.gov/news-events/press-announcements/fda-approves-first-drug-treat-agitation-symptoms-associated-dementia-due-alzheimers-disease
  5. Halpern R, Seare J, Tong J, Hartry A, Olaoye A, Aigbogun MS. Using electronic health records to estimate the prevalence of agitation in Alzheimer disease/dementia. Int J Geriatr Psychiatry. 2019;34(3):420-431.
  6. Fillit H, Aigbogun MS, Gagnon-Sanschagrin P, et al. Impact of agitation in long-term care residents with dementia in the United States. Int J Geriatr Psychiatry. 2021;36(12):1959-1969.
  7. Sano M, Cummings J, Auer S, et al. Agitation in cognitive disorders: Progress in the International Psychogeriatric Association consensus clinical and research definition. Int Psychogeriatr. 2024 April;36(4):238-250
  8. Kales HC, Gitlin LN, Lyketsos CG. Assessment and management of behavioral and psychological symptoms of dementia. BMJ. 2015;350:h369.
  9. Yaffe K, Fox P, Newcomer R, et al. Patient and caregiver characteristics and nursing home placement in patients with dementia. JAMA. 2002;287(16):2090-2097.
  10. Maeda K, Sugino H, Akazawa H, et al. Brexpiprazole I: in vitro and in vivo characterization of a novel serotonin-dopamine activity modulator. J Pharmacol Exp Ther. 2014;350(3):589-604.
  11. Otsuka. Otsuka Pharmaceutical and Lundbeck Announce Topline Results from Two Phase 3 Trials of Brexpiprazole as Combination Therapy with Sertraline for the Treatment of Post-Traumatic Stress Disorder in Adults. Release date: Sept. 07, 2023. Last accessed: July 02, 2024. Available at: https://www.otsuka-us.com/news/otsuka-pharmaceutical-and-lundbeck-announce-topline-results-two-phase-3-trials-brexpiprazole
  12. REXULTI® (brexpiprazole). Prescribing Information. FDA. Reference ID: 4911319. May 2024.

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Otsuka in the U.S. Robert Murphy Corporate Communications Otsuka America Pharmaceutical, Inc. robert.murphy@otsuka-us.com +1 609 249 7262

Otsuka outside the U.S. Jeffrey Gilbert Leader, Pharmaceutical PR Otsuka Pharmaceutical Co., Ltd. Gilbert.jeffrey.a@otsuka.co.jp

Lundbeck in the U.S. Dyana Lescohier Corporate Communications Lundbeck U.S. dyle@lundbeck.com +1 847 894 3586