Drug intelligence / Profile preview

VH4524184 + itraconazole

Development stage
Unknown
Lead developer
ViiV Healthcare
Modality
Small Molecules
Administration
Oral
01

Overview

VH4524184 + itraconazole is a combination of the investigational antiretroviral drug VH4524184, a third-generation integrase strand transfer inhibitor (INSTI) in development for HIV-1 infection, with itraconazole, a broadly used triazole antifungal agent. - VH4524184 acts by inhibiting HIV-1 integrase, preventing the insertion of viral DNA into the host genome, and is notable for its long-acting potential and activity against second-generation INSTI-resistant HIV-1 strains. Its mechanism distinguishes it as an advanced antiretroviral therapy with possible use in long-acting regimens for treatment or prevention of HIV-1 infection[2][4][5][7]. - Itraconazole inhibits fungal cytochrome P450 14α-demethylase, blocking ergosterol synthesis and fungal cell membrane formation. It is primarily indicated for management of systemic and superficial fungal infections. - The combination is likely under consideration for managing HIV-1 infection in settings where fungal co-infection is a risk, or to study pharmacokinetic or drug interaction effects, as both agents are metabolized via hepatic pathways (notably, VH4524184 does not significantly affect CYP3A4)[5].

02

Targets

CYP51A1 (Sterol 14α-demethylase)Integrase allosteric pocket (HIV)

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