Combination of | |
---|---|
Tianeptine | Atypical μ-opioid receptor agonist |
Naloxone | Orally inactive μ-opioid receptor antagonist |
Clinical data | |
Other names | Naloxone/tianeptine; Tianeptine oxalate/naloxone; Naloxone/tianeptine oxalate; Tianeptine hemioxalate/naloxone; Naloxone/tianeptine hemioxalate; TNX-601; TNX601; TNX-601 CR; TNX-601-CR; TNX-601 ER; TNX-601-ER |
Routes of administration | Oral |
Tianeptine/naloxone (developmental code names TNX-601, TNX-601-CR, TNX-601-ER), or naloxone/tianeptine, is an extended-release combination of tianeptine, an atypical μ-opioid receptor agonist, and naloxone, an orally inactive μ-opioid receptor antagonist, which was under development for the treatment of major depressive disorder, post-traumatic stress disorder (PTSD), and neurocognitive dysfunction associated with corticosteroid use but was never marketed.[1][2][3][4][5]
Whereas tianeptine is marketed widely throughout Europe, Asia, and Latin America but is not available in the United States or the United Kingdom, tianeptine/naloxone was under development for registration in the United States and other countries.[1][3][4] In addition, whereas tianeptine has a short duration of action and requires administration three times per day, tianeptine/naloxone was developed as an extended-release formulation with enhanced pharmacokinetics suitable for once-daily administration.[3][1] The combination formulation employs tianeptine as the oxalate salt, which is said to have improved physicochemical properties for use in the extended-release formulation compared to the amorphous tianeptine sodium that is used in immediate-release tianeptine-only formulations.[3][1] Naloxone is used in misuse-resistant oral drug formulations as it is inactive if taken orally but becomes active if oral tablets are crushed and administered parenterally, such as by injection.[6][4]
Tianeptine/naloxone reached phase 2 clinical trials for major depressive disorder and phase 1 clinical trials for post-traumatic stress disorders and cognition dysfunction related to corticosteroid use prior to the discontinuation of its development.[1][2] Its development was discontinued for all indications in October 2023 due to lack of effectiveness for major depressive disorder in a phase 2 clinical trial.[1][7]