Fabre-Kramer Pharmaceuticals Announces FDA Approval of EXXUA™, the First and Only Oral Selective 5HT1a Receptor Agonist for the Treatment of Major Depressive Disorder in Adults

EXXUA is the first new chemical entity (NCE) utilizing this single mechanism approved for the treatment of major depressive disorder.

EXXUA's approved labeling does not list sexual dysfunction as an adverse reaction.

HOUSTON, Sept. 28, 2023 /PRNewswire/ -- Fabre-Kramer Pharmaceuticals Inc. (Fabre-Kramer), a biopharmaceutical company committed to developing novel therapies to address unmet needs in psychiatry and neurology, is pleased to announce that the U.S. Food and Drug Administration (FDA) has approved Exxua™ (gepirone hydrochloride extended-release tablets) for the treatment of major depressive disorder (MDD) in adults. Exxua represents a new class of antidepressant; the first and only approved antidepressant with a novel mechanism of action that selectively targets the serotonin 1A receptor, a key regulator of mood and emotion. Exxua has been shown to effectively relieve depressive symptoms, and its approved labeling does not contain Warnings or Adverse Reactions regarding causing sexual dysfunction or weight gain vs. placebo. Exxua is expected to be available in pharmacies in early 2024.

Studied in over 5,000 patients, EXXUA's unique mechanism of targeted single serotonin (5HT) 1a receptor agonism relieves depressive symptoms with an acceptable side effect profile. Sexual side effects experienced with EXXUA treatment in clinical trials were comparable to placebo and did not meet the incidence criteria for inclusion in the Adverse Reaction section of EXXUA's label. EXXUA also showed an overall acceptable safety profile, with no significant adverse effect on weight, blood pressure, heart rate or liver function. The most frequent adverse events seen in clinical trials were dizziness and nausea, which generally were mild, of short duration, related to dose escalations and did not require discontinuation of treatment.

Anita H. Clayton, MD, Chair, Department of Psychiatry & Neurobehavioral Sciences, University of Virginia School of Medicine, a renowned clinician and researcher of sexual dysfunction issues in MDD treatment commented "I am thrilled for our patients that EXXUA (gepirone ER) is now FDA approved for the treatment of major depressive disorder (MDD). EXXUA is the first 5-HT1a agonist with superior efficacy vs. placebo as MDD monotherapy, yet did not differ from placebo in rates of sexual dysfunction in clinical trials. This provides an important new treatment option for patients."

"EXXUA represents an important milestone in the treatment of MDD, a serious and debilitating condition that affects millions of people worldwide," said Stephen Kramer, M.D., CEO of Fabre-Kramer. "There is value in providing prescribers and patients with a wide range of effective options for use in clinical practice. We are proud to bring this innovative therapy to patients who need a new option to manage their depression and improve their quality of life."

Michael Pollack, Chief Executive Officer of the Depression and Bipolar Support Alliance (DBSA), a leading national patient advocacy organization said "The mental health crisis in the United States is one of the most pressing health issues facing our country today. Over 20 million American adults experienced major depressive disorder each year prior to the COVID-19 pandemic. These numbers increased dramatically during the pandemic with approximately 30% of adults in the US or more than 80 million Americans experiencing elevated symptoms of depression. The need for new treatment options, particularly those with new mechanisms of action, could not be clearer and more urgent for those living with, or impacted by, major depressive disorder."

The mechanism of the antidepressant effect of EXXUA is not fully understood but is believed to be related to its modulation of serotonin activity in the CNS through selective agonist activity at 5HT1a receptors. EXXUA and its active metabolite exhibit exclusive and strong binding affinity for 5HT1a receptors. Dr. Stephen Stahl, Professor of Psychiatry, University of California and founder of the Neuroscience Education Institute, a recognized expert neuropsychopharmacologist said "EXXUA is the first truly selective agonist of the serotonin 1a receptor that has been consistently linked to mediation of mood disorders and suicide risk. It's an important addition to the armamentarium to treat depression."

About EXXUA

EXXUA is a novel oral selective serotonin (5HT) 1a receptor agonist indicated for the treatment of major depressive disorder (MDD) in adults. Exxua is also being developed for other psychiatric disorders.

INDICATIONS and IMPORTANT SAFETY INFORMATION for EXXUA (gepirone) extended-release tablets

 INDICATIONS

EXXUA is indicated for the treatment of major depressive disorder (MDD) in adults.

 IMPORTANT SAFETY INFORMATION

• Antidepressants increased the risk of suicidal thoughts and behaviors in pediatric and young adult patients in short-term studies. Closely monitor all antidepressant-treated patients for clinical worsening and emergence of suicidal thoughts and behaviors.
• EXXUA is not approved for use in pediatric patients.

Do not take EXXUA if you:

• are allergic to EXXUA or any of the ingredients in EXXUA. See the end of this Medication Guide for a complete list of ingredients in EXXUA.
• have a prolonged QTc interval greater than 450 msec or congenital long QT syndrome.
• are taking medicines known as strong CYP3A4 inhibitors. Ask your healthcare provider if you are not sure if you are taking one of these medicines.
• have severe liver problems.
• are taking, or have stopped taking within the last 14 days, a medicine called a monoamine oxidase inhibitor (MAOI), including the antibiotic linezolid or intravenous methylene blue. Ask your healthcare provider or pharmacist if you are not sure if you take an MAOI, including the antibiotic linezolid or intravenous methylene blue.
• Do not start taking an MAOI for at least 14 days after you have stopped treatment with EXXUA.

EXXUA may cause serious side effects, including:

• Changes in the electrical activity of your heart called QT prolongation. QT prolongation can cause irregular heartbeats that can be life-threatening or lead to death. Your healthcare provider will check the electrical activity of your heart with a test called an electrocardiogram (ECG) and will also do blood tests to check your levels of body salts (electrolytes) before and during treatment with EXXUA. Your healthcare provider may check your electrolytes more often during treatment if you have heart failure, a slow heart rate, abnormal levels of electrolytes in your blood, or if you take a medicine that can prolong the QT interval of your heartbeat. Tell your healthcare provider right away if you have an irregular heartbeat or feel dizzy, lightheaded, or faint during treatment with EXXUA.
• Serotonin syndrome. A potentially life-threatening problem called serotonin syndrome can happen when EXXUA is taken with certain other medicines.
• Manic episodes. Manic episodes may happen in people with bipolar disorder who take EXXUA.

 Please read FULL PRESCRIBING INFORMATION and MEDICATION GUIDE for EXXUA.

About Fabre-Kramer

Fabre-Kramer is committed to developing and bringing to market advanced new medications to help physicians treat their patients' unmet medical needs in the therapeutic areas of psychiatry and neurology. The Company focuses on compounds to license-in, develop for global registration, and license-out to commercial partners.

Follow us on social media - LinkedIn
Visit our website at www.fabrekramer.com
Contact – [email protected]

SOURCE Fabre-Kramer Pharmaceuticals, Inc.