Drug intelligence / Profile preview

amitriptyline + clovoxamine + fluvoxamine

Development stage
Preclinical
Lead developer
Merck
Modality
Small Molecules
Administration
Oral
01

Overview

This is a combination of three antidepressant drugs: - **Amitriptyline** is a tricyclic antidepressant (TCA) that inhibits the reuptake of serotonin and norepinephrine, increasing their levels in the central nervous system. It is primarily used for major depressive disorder, neuropathic pain, migraine prophylaxis, and other off-label uses[8]. - **Clovoxamine** is an antidepressant with both selective serotonin reuptake inhibitor (SSRI) and some noradrenergic activity. It has been used in some countries for depression and anxiety disorders. - **Fluvoxamine** is a selective serotonin reuptake inhibitor (SSRI), mainly indicated for obsessive-compulsive disorder but also used off-label for depression[5]. Fluvoxamine increases synaptic serotonin by inhibiting its reuptake. Combining these agents may theoretically enhance antidepressant efficacy due to complementary mechanisms on serotonergic and noradrenergic neurotransmission. However, such combinations are rarely standard practice due to significant risks of pharmacokinetic interactions—especially between fluvoxamine and amitriptyline—and increased risk of adverse effects including serotonin syndrome[1][2][3][4][6][7][9].

02

Targets

HRH1 (Histamine H1 Receptor)SERT (Sodium-dependent serotonin transporter)SIGMAR1 (Sigma non-opioid intracellular receptor 1)NET (Norepinephrine Transporter)M1 (Muscarinic acetylcholine receptor M1)

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