General Information

Exxua (gepirone) selectively targets the serotonin 1A receptor.

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

Dosing/Administration

Exxua is an extended release capsule. 

Correct electrolyte abnormalities and perform electrocardiogram (ECG) prior to initiating treatment with Exxua. Do not initiate Exxua if QTc is > 450 msec. Perform ECGs during dosage titration and periodically during treatment.

The recommended starting dose is 18.2 mg administered orally once daily with food at approximately the same time each day.

Depending on clinical response and tolerability, the dosage may be increased to 36.3 mg once daily on Day 4. Dosage may be further titrated to 54.5 mg once daily after Day 7 and to 72.6 mg once daily after an additional week.

Mechanism of Action

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.

Side Effects

Adverse effects associated with the use of Exxua may include, but are not limited to, the following:

• dizziness
• nausea
• insomnia
• abdominal pain
• dyspepsia

The Exxua drug label comes with the following Black Box Warning: Increased risk of suicidal thinking and behavior in pediatric and young adult patients taking antidepressants. Closely monitor for worsening and emergence of suicidal thoughts and behaviors. Exxua is not approved for use in pediatric patients.

Clinical Trial Results

The efficacy of EXXUA for the treatment for major depressive disorder (MDD) in adults was evaluated in two eight-week randomized, double-blind, placebo-controlled, flexible-dose studies in adults (age 18 to 69 years) meeting Diagnostic and Statistical Manual of Mental Disorders (DSM-IV) criteria for MDD.

In Study 1 and Study 2, the primary efficacy measure was the change from baseline in the Hamilton Depression Rating Scale (HAMD-17) total score at Week 8. In both studies, patients in the Exxua groups experienced statistically significantly greater improvement on the primary endpoint compared to patients in the placebo groups