FDA approves first-in-class antidepressant

The US Food and Drug Administration (FDA) has approved Exxua™ (gepirone hydrochloride extended-release tablets) for adults with major depressive disorder (MDD). Oral selective serotonin (5HT) 1a receptor agonist Exxua is the first approved antidepressant with a novel mechanism of action that selectively targets the serotonin 1A receptor, a key regulator of mood and emotion.

Dr Stephen Kramer, CEO of Fabre-Kramer Pharmaceuticals declared that the approval of Exxua “represents an important milestone in the treatment of MDD”. According to the company’s website, the medicine offers the first truly novel mechanism for MDD in over 30 years.

Exxua: representing a new class of antidepressants

“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 is an important addition to the armamentarium to treat depression,” shared Dr Stephen Stahl, Professor of Psychiatry, University of California and founder of the Neuroscience Education Institute.

The mechanism of the antidepressant effect of Exxua is believed to be related to how it modulates 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, according to Fabre-Kramer .

Clinical efficacy of the serotonin 1a receptor antagonist for major depressive disorder

Studied in over 5,000 patients, Exxua has demonstrated an overall acceptable safety profile, with no significant adverse effect on weight, blood pressure, heart rate or liver function.

“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,” urged Michael Pollack, Chief Executive Officer of the Depression and Bipolar Support Alliance (DBSA).

“Exxua is the first 5-HT1a agonist with superior efficacy versus 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,” commented Dr Anita Clayton, Chair of the Department of Psychiatry & Neurobehavioral Sciences at the University of Virginia’s School of Medicine.

The major depressive disorder treatment is expected to be available for patients in early 2024.