Drug intelligence / Profile preview

gemfibrozil + sertraline

Development stage
Unknown
Lead developer
Pfizer
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules, Irreversible Covalent Inhibitors → Covalent Small Molecules → Small Molecules
Administration
Oral
01

Overview

Gemfibrozil + sertraline is a combination of two small molecule drugs, each with distinct mechanisms and primary indications. Gemfibrozil is a lipid-regulating agent primarily used to lower serum triglyceride levels in patients with hyperlipidemia and to reduce the risk of coronary heart disease. It acts mainly by activating peroxisome proliferator-activated receptor alpha (PPARα), which increases the oxidation of fatty acids and reduces triglyceride levels[3][6]. Sertraline is a selective serotonin reuptake inhibitor (SSRI) antidepressant, commonly prescribed for major depressive disorder (MDD), anxiety disorders, and related conditions. It works by inhibiting the sodium-dependent serotonin transporter, increasing serotonin availability in synaptic clefts[1]. Recent clinical research has explored gemfibrozil as an adjunctive treatment to sertraline for MDD; one randomized controlled trial found that adding gemfibrozil to sertraline improved depression outcomes compared to sertraline alone[2].

02

Targets

SLCO1B3 (Organic anion transporting polypeptide 1B3)SIGMAR1 (Sigma non-opioid intracellular receptor 1)CYP2C19 (Cytochrome P450 2C19)PPARA (Peroxisome proliferator-activated receptor alpha)SERT (Sodium-dependent serotonin transporter)CYP2C8 (Cytochrome P450 2C8)

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