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Nelfinavir mesylate: a protease inhibitor
1College of Pharmacy, Ohio State University, Columbus 43210, USA.
The Annals of Pharmacotherapy
|April 14, 1999
Summary
Nelfinavir mesylate is an effective HIV protease inhibitor, reducing viral load and increasing CD4+ cell counts when used with other antiretrovirals. Dosage guidelines are established for adults and children, with ongoing studies for improved regimens.
Area of Science:
- Pharmacology
- Virology
- Infectious Diseases
Background:
- HIV protease inhibitors are crucial in managing HIV infection.
- Nelfinavir mesylate (AG1343) is a protease inhibitor investigated for its therapeutic potential.
Purpose of the Study:
- To comprehensively review the clinical pharmacology, pharmacokinetics, efficacy, adverse effects, drug interactions, and dosage guidelines of nelfinavir mesylate.
Main Methods:
- Literature search of MEDLINE and journal reviews (1966-1998).
- Inclusion of FDA data and meeting abstracts.
- Data synthesis from in vitro studies, open-label, and controlled trials.
Main Results:
- Nelfinavir inhibits HIV protease, producing noninfectious virions.
- Combination therapy with nucleoside reverse transcriptase inhibitors significantly reduces viral load and increases CD4+ cell counts.
- Nelfinavir exhibits bioavailability of 20-80%, increased with food; steady-state concentrations are 3-4 mcg/mL (max) and 1-3 mcg/mL (min).
- Elimination half-life is 3-5 hours; metabolism is hepatic via CYP450, excretion is fecal.
- Common adverse events include diarrhea, nausea, vomiting, and abdominal pain.
Conclusions:
- Nelfinavir is FDA-approved for combination therapy in HIV treatment.
- Antiretroviral regimen selection requires consideration of disease progression, patient history, and drug interactions.