SB-773812 + ketoconazole

SB-773812 + ketoconazole is an experimental combination of two drugs: SB-773812, a novel small molecule antipsychotic in development for schizophrenia, and ketoconazole, a potent CYP3A4 inhibitor. SB-773812 was designed to antagonize dopamine D2, D3, serotonin 5-HT2A, 5-HT2C, and 5-HT6 receptors, while minimizing activity at receptor sites linked to the side effects seen with current antipsychotics. Ketoconazole is co-administered primarily to assess potential pharmacokinetic drug-drug interactions, as SB-773812 is predominantly metabolized by the CYP3A4 pathway. The rationale for this combination in studies is to investigate how co-administration with a CYP3A4 inhibitor like ketoconazole affects the metabolism and exposure of SB-773812 in healthy volunteers or patients.