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Kaletra once daily?
Mar 27, 2002

I have read that at the confrence in Seattle they suggested that a once daily regime of Kaletra(six tablets), epriv,and zerit may be as effective as the normal Kaletra BID(3pills twice daily)currently used? When can we expect to see Kaletra available for once daily dosing and is it possible to make the pills larger to cut the number from 6 pills once a day to maybe 3 or 2? Also could you tell me what the current status of CRCX4 and CCRX5 recepter attachment inhibitors are currently? If we could effectly block both receptor cites would this be better than current thearpy?

Response from Dr. Boyle

In the study presented at the Conference on Retroviruses and Opportunistic Infections in Seattle (abstract 409), at the end of 48 weeks of therapy patients given Kaletra (lopinavir/ritonavir) once-daily (6 capsules once daily) did just as well as patients given Kaletra twice daily (3 capsules twice daily). However, there were lower lopinavir trough levels overall and much greater variability in trough levels in the patients on once daily therapy. While the levels appeared adequate against wild-type virus in all of the patients, these data raise some concerns about lopinavir levels being too low in some patients when it is dosed once daily. Kaletra dosed once-daily may be relatively safe in protease inhibitor-naive patients, but based upon these data I would still prefer to dose it twice daily. If I was going to use Kaletra once daily, and I may in certain PI-naive patients who have problems with a twice daily regimen, I would check a lopinavir trough level to assure that an adequate safety margin exists. Also, since lopinavir levels may fall relatively rapidly when given once daily (as the ritonavir component is metabolized), patients should be advised to stick very closely to taking it every 24 hours, and try not to be late with doses. Data on entry inhibitors (including R5 and X4 inhibitors)show that they are steadily making progress and many are now in clinical studies.



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