Capravirine update? In play or old news?
Jun 3, 2004
Good day to you sir. In this site, below I found some information on Capravirine. Not much has been heard on this agent in 2004, do you think it will ever hit the market or it is old news?
Capravirine Phase 1 trials suggest that capravirine is ten times more potent than current NNRTIs. A dosing study reported that 2,100 mg capravirine twice daily produced a 1.69 log reduction in viral load after 10 days of treatment. This was equivalent to the viral load reduction in the triple therapy control arm.
Capravirine is active against HIV variants with single mutations at codons K103N or V106A or L100I which confer resistance to NNRTIs. Capravirine is likely to be active against viruses with resistance to efavirenz. Resistance to nevirapine (usually characterized by a mutation at codon Y181C) would render capravirine useless. However, a mutation at codon 181 or a dual mutation at codons 103 and 100 will confer high level resistance to this compound, calling into question its usefulness.
Clinical trials of capravirine were suspended pending safety checks following the discovery that the drug causes vasculitis (inflammation of the blood vessels) in dogs. Vasculitis may cause severe damage to the tissue supplied by inflamed blood vessels because blood cannot adequately reach the tissue. Development has now resumed. In a phase II study, a higher rate of nausea, vomiting and diarrhea was seen in the 2,100 mg group, and so the 1,400 mg dose has now been selected for further development. Capravirine is currently being tested in two international studies. One is testing the drug in treatment-naive patients, and the other is testing the drug in combination with nelfinavir and two new NRTIs in patients who have failed or did not respond to an NNRTI-containing regimen.
Capravirine is also being tested in studies where it is combined with drugs that are p450 cytochrome inhibitors, because these have been shown to boost plasma levels of the drug. Taking the drug with food also increases blood levels. A study in healthy volunteers showed that capravirine reduced lopinavir levels somewhat, but that lopinavir increased capravirine levels substantially.
Response from Dr. Pierone
Yes, capravirene is back in clinical development and moving forward. Hopefully it will be successful and become available for patients that have developed resistance to agents like Sustiva and Viramune.
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