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zonisamide + bupropion
- Development stage
- Discontinued
- Lead developer
- Orexigen Therapeutics, Inc
- Modality
- Small Molecules
- Administration
- Oral
01
Overview
Empatic is a fixed-dose combination of zonisamide and bupropion, both in sustained-release (SR) formulations, developed by Orexigen Therapeutics for the treatment of obesity. The combination targets the hypothalamus, specifically the pro-opiomelanocortin (POMC) neurons, to regulate appetite and energy expenditure. Bupropion acts as a norepinephrine-dopamine reuptake inhibitor (NDRI), stimulating POMC neurons to release alpha-melanocyte-stimulating hormone (α-MSH), while zonisamide, an anticonvulsant, is believed to enhance this effect and prevent the inhibitory feedback that typically limits weight loss. Although Phase IIb trials demonstrated significant weight loss compared to placebo, Orexigen discontinued development of Empatic to focus on its other obesity drug, Contrave (naltrexone/bupropion).
- Brand names
- Empatic
- Other names
- zonisamide SR + bupropion SRzonisamide CR + bupropion SR
02
Targets
Nicotinic Acetylcholine ReceptorNaV (Voltage-gated sodium channels)DAT (Dopamine plasma membrane transport protein)NET (Norepinephrine Transporter)CA2 (Carbonic Anhydrase 2)CaV3 (Caveolin-3)
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