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Experimental HIV Drugs

Elvitegravir 'Quad' Single-tablet Regimen Shows Continued HIV Suppression at 48 Weeks

Gilead Science's experimental "Quad" pill -- a once-daily single-tablet coformulation containing the new integrase inhibitor elvitegravir, the novel boosting agent cobicistat (GS 9350), and tenofovir plus emtricitabine (the drugs in the Truvada pill) -- continued to demonstrate potent antiviral activity and good tolerability at 48 weeks, according to data presented this week at the 50th Interscience Conference on Antimicrobial Agents and Chemotherapy (ICAAC 2010). In a second comparison, cobicistat worked as well as ritonavir as a booster for atazanavir, with similar changes in kidney function.

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New NRTI Festinavir Exhibits Good Anti-HIV Activity and Safety in Phase 1b/2a Study

The new nucleoside reverse transcriptase inhibitor (NRTI) festinavir, or OBP-601, demonstrated good antiviral activity, lowering HIV viral load by more than 1 log over 10 days, researchers reported this week at the 50th Interscience Conference on Antimicrobial Agents and Chemotherapy (ICAAC 2010) in Boston. The new drug, which is related to stavudine (d4T, Zerit), was associated with few serious drug-related adverse events in this short-term study, but longer clinical trials are needed.

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More Promising Data on GSK572 Integrase Inhibitor, Phase 3 Studies to Begin Soon

S/GSK1349572 (better known as GSK572), the second-generation integrase inhibitor being developed jointly by Shionogi and ViiV Healthcare, continues to show potent antiviral activity with good tolerability, according to 2 studies presented at the XVIII International AIDS Conference (AIDS 2010) this week in Vienna. GSK572 worked against HIV with some raltegravir resistance mutations and has a high genetic barrier to resistance itself. Based on these findings, the companies announced the drug would soon enter Phase 3 trials.

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AIDS 2010: Investigational HIV Drug TBR-652 Reduces Viral Replication and May Dampen Inflammation

Tobira Pharmaceuticals' TBR-652, an experimental drug that blocks both the CCR5 and CCR2 cell surface receptors, has the dual effect of inhibiting HIV and affecting a biomarker associated with inflammation, according to data presented at the XVIII International AIDS Conference (AIDS 2010) last month in Vienna. TBR-652 was generally well-tolerated and a Phase 2b clinical trial is planned for early next year.

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Monoclonal Antibody PRO 140 Suppresses HIV Viral Load with Once-weekly Dosing

Subcutaneous injections of PRO 140, a humanized monoclonal antibody that blocks the CCR5 co-receptor and inhibits HIV entry into cells, reduced viral load significantly more than placebo, according to a study described in the May 15, 2010 Journal of Infectious Diseases. PRO 140 worked well when administered once-weekly, offering proof-of-concept for an antiretroviral therapy that can be taken less often than current drugs.

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