Delavirdine mesylate (U-90152) is a non-nucleoside reverse transcriptase inhibitor (NNRTI) used as part of highly active antiretroviral therapy (HAART) for the treatment of human immunodeficiency virus (HIV) type 1. Delavirdine mesylate selectively inhibits HIV-1 reverse transcriptase (RNA-dependent DNA polymerase) over other cellular polymerases with IC50 values of 0.26, 440 and >550 μM for HIV-1 reverse transcriptase, DNA polymerase α and DNA polymerase δ. U-90152 (Delavirdine mesylate) blocked the replication in peripheral blood lymphocytes of 25 primary HIV-1 isolates with a mean 50% effective dose of 0.066 +/- 0.137 microM.
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
U-90152, a potent inhibitor of human immunodeficiency virus type 1 replication.
Dueweke TJ, et al. Antimicrob Agents Chemother. 1993 May;37(5):1127-31. PMID: 7685995.
In vitro inhibition of human immunodeficiency virus type 1 by a combination of delavirdine (U-90152) with protease inhibitor U-75875 or interferon-alpha.
Pagano PJ, et al. J Infect Dis. 1995 Jan;171(1):61-7. PMID: 7528253.
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