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Abstract
ANTIVIRAL ACTIVITY, SAFETY AND PHAMACOKINETICS OF MOZENAVIR (DMP 450), A NOVEL CYCLIC UREA PROTEASE INHIBITOR, IN COMBINATION WITH d4T AND 3TC IN TREATMENT-NAÏVE HIV-1 INFECTED PATIENTS (STUDY DMP-102)
SIERRA-MADERO J
OBJECT OF STUDY:
Primary: To evaluate the safety, tolerance and pharmacokinetics of multiple, repeat doses of mozenavir in combination with d4T and 3TC.
Secondary: To evaluate the antiviral activity of mozenavir as defined by the percentage of patients who achieve and maintain plasma HIV-1 RNA < 400 copies/mL and <50 copies/mL at 24 and 48 weeks.
MATERIALS:
Mozenavir (DMP 450) is a non-peptidomimetic, water soluable, cyclic urea that is a selective inhibitor of HIV-1 protease. Background medications are d4T and 3TC.
METHODS:
Antiretroviral naïve patients with HIV-1 RNA > 10,000 copies/mL and unrestricted CD4 counts were randomized to receive either mozenavir at one of three doses or indinavir in background combination with d4T and 3TC. Fifty patients were enrolled in the following dose regimens: A)12 patients received mozenavir 750 mg TID, B)15 patients received mozenavir 1250 mg BID, C)13 patients received mozenavir1250 mg TID and D)10 patients received indinvavir 800 mg TID.
RESULTS:
Enrollment has been completed and the on-treatment period ranges from 40 to72 weeks. The median log10 viral load at baseline was A) 4.61, B) 4.99, C) 5.25 and D) 4.93. The percentage of patients at Week 24, intent to treat, with HIV-1 viral load < 50 copies/mL was A) 75, B) 80, C) 77 and D) 70. Mozenavir has been well tolerated, with no significant laboratory toxicities noted. Most adverse events have been mild to moderate and self-limited. In particular, careful analysis of cardiac repolarization during the first 24 weeks of the study showed no difference between the 3 mozenavir groups and indinavir. The study is ongoing and 48 week data, to include pharmacokinetics, will be presented.
CONCLUSION:
The 24 Week data show that all three doses of mozenavir produced significant antiviral activity comparable to that of indinavir. The safety analyses show good tolerability and safety for all doses tested with no difference noted in regards to effects on cardiac repolarization.
The 1st. IAS Conference on HIV Pathogenesis and Treatment
Abstract no.
2
Suggested Citation
"SIERRA-MADERO J
ANTIVIRAL ACTIVITY, SAFETY AND PHAMACOKINETICS OF MOZENAVIR (DMP 450), A NOVEL CYCLIC UREA PROTEASE INHIBITOR, IN COMBINATION WITH d4T AND 3TC IN TREATMENT-NAÏVE HIV-1 INFECTED PATIENTS (STUDY DMP-102).
Oral Presentation:
The 1st. IAS Conference on HIV Pathogenesis and Treatment
:
Abstract no.
2"
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