Lersivirine is a potent enzyme inducer in rodents capable of inducing a number of hepatic enzymes including those involved in its own metabolism. Preclinically lersivirine has been associated with hepatocellular hypertrophy and thyroid gland follicular cell hypertrophy in rats, mice, and dogs. Lersivirine has therapeutic potential for HIV-infected individuals with viral strains resistant against first-line NNRTIs. However, no large, well-powered studies have been conducted so far, which assess noninferiority against established antiretroviral agents. Lersivirine 750 mg and 1,000 mg qd was associated with lower rates of viral suppression at week 24 and week 48 versus etravirine in patients with prior NNRTI use and evidence of NNRTI resistance. No new safety signals were detected.
|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.
Efficacy and safety of lersivirine versus etravirine for the treatment of HIV-1 infection in patients with prior non-nucleoside reverse transcriptase inhibitor (NNRTI) use and evidence of NNRTI resistance: a randomized phase 2B trial.
DeJesus E, et al. HIV Clin Trials. 2014 Sep-Oct;15(5):209-17. PMID: 25350959.
Effects of Lersivirine on Canine and Rodent Thyroid Function.
Houle CD, et al. Toxicol Pathol. 2013 Oct 16;42(5):897-912. PMID: 24135463.
Lersivirine - a new drug for HIV infection therapy.
Platten M, et al. Expert Opin Investig Drugs. 2013 Dec;22(12):1687-94. PMID: 24128277.
Effect of lersivirine co-administration on pharmacokinetics of methadone in healthy volunteers.
Vourvahis M, et al. Drug Alcohol Depend. 2012 Nov 1;126(1-2):183-8. PMID: 22682979.
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