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OREX-003
- Development stage
- Discontinued
- Lead developer
- Orexigen Therapeutics, Inc
- Modality
- Small Molecules
- Administration
- Oral
01
Overview
OREX-003 is a proprietary combination therapy developed by Orexigen Therapeutics, consisting of a sustained-release formulation of the anticonvulsant zonisamide and the atypical antipsychotic olanzapine. It was primarily investigated for the treatment of schizophrenia, with a specific focus on mitigating the significant weight gain and metabolic side effects typically associated with olanzapine (Zyprexa) treatment. The mechanism involves the antipsychotic efficacy of olanzapine coupled with the weight-modulating effects of zonisamide, which is thought to involve carbonic anhydrase inhibition and modulation of dopaminergic and serotonergic neurotransmission. Development reached Phase 2a (trial OZ-101) before being discontinued in 2008 as Orexigen Therapeutics refocused its efforts on its primary obesity drug programs, such as Contrave.
- Other names
- zonisamide SR + olanzapine
02
Targets
NaV (Voltage-gated sodium channels)HRH1 (Histamine H1 Receptor)M1 (Muscarinic acetylcholine receptor M1)HTR2A (Serotonin receptor 5-HT2A)CA (Carbonic anhydrase)HTR2C (5-hydroxytryptamine 2C receptor)DRD2 (Dopamine D2 Receptor)CaV3 (Caveolin-3)
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