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basmisanil + itraconazole
- Development stage
- Unknown
- Lead developer
- Roche
- Modality
- Small Molecules
- Administration
- Oral
01
Overview
**Basmisanil + itraconazole** is a **combination drug** of basmisanil and itraconazole.\nBasmisanil (RG1662, RO5186582) is a highly selective negative allosteric modulator (NAM) of the GABA\(_A\) receptor α5 subunit, investigated for cognitive impairment in Down syndrome and schizophrenia. It acts by selectively inhibiting GABA\(_A\) receptor α5 subunits, potentially enhancing cognition by reducing excessive GABAergic inhibition, particularly in Down syndrome[5][3][9].\nItraconazole is a triazole-class antifungal agent. It functions by inhibiting 14-α-demethylase (a cytochrome P450 enzyme), leading to impaired ergosterol synthesis and disruption of fungal cell membrane integrity, thereby inhibiting the growth of susceptible fungi[2].\nThe combination is non-standard; no clinical evidence of "RG1662 + itraconazole" being a marketed or studied combination was found. The description reflects the pharmacology of each component.
- Other names
- basmisanil + itraconazole
02
Targets
σR (Sigma receptors)GABRA5 (Gamma-aminobutyric acid type A receptor subunit alpha-5)OSBP2 (Oxysterol-binding protein 1)CYP51A1 (Sterol 14α-demethylase)
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