The XVII International AIDS Conference (AIDS 2008)

TMC278 Nanosuspension Found Long-Acting, Well-Tolerated in First Trial in HIV-Uninfected Subjects

August 5, 2008

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This is Dr. Gerald Pierone from the AIDS Research and Treatment Center of the Treasure Coast, and I'm at the International AIDS Conference in Mexico City. I'm here at a poster presentation, which is titled "TMC278 Long Acting - A Parenteral Nanosuspension Formulation That Provides Sustained Clinically Relevant Plasma Concentrations in HIV-Negative Volunteers."1 I'm here with one of the investigators of this study, Dr. Peter Williams. I'd like to thank you for agreeing to speak with me today. Can you tell me what a nanosuspension is?

Peter Williams, Ph.D.
Peter Williams, Ph.D.
In this case, a nanosuspension is a formulation which, in an aqueous formulation, has small crystals, very small crystals, of TMC278, an investigational non-nucleoside reverse transcriptase inhibitor. These crystals are made small by a milling process, which reduces them to approximately twice the diameter of an HIV particle.

Can you tell me about the research that you presented at this meeting?

What we present here is the first study in which this formulation has been given to HIV seronegative subjects in single doses. We studied the tolerability of the formulation and the plasma concentrations of TMC278 over time, after each single dose.

What did you find?

We found really good tolerability, in comparison to the placebo injections. There were no systemic adverse events, just some injection site reactions around the point at which the injection was given. We also found very long, sustained plasma concentrations of TMC278 out to 12 weeks after the single doses.

And these studies were done in about how many individuals?

In total, about 50 individuals in the study.

This is a very innovative thing that you have done. What prompted you to do this line of work?

We feel that this sort of depot formulation could be useful in maintenance therapy of HIV infections, as long as we can find a companion drug to go with TMC278 long-acting. We also speculate that it may have some utility in pre-exposure prophylaxis.

So if successful -- and this is very early with this compound, of course -- this might be the first agent for a new paradigm of HIV treatment.

Yes, as long as it is with companion antiretroviral drugs, which are also injectable.

I can't tell you how many times in the clinic I have a patient or an adolescent that is nonadherent, and I just think, gosh, if I just had a once-a-month shot. It's exciting that you are at least taking one step down this road.


What future studies do you have planned?

We plan to study a more concentrated formulation. The current one has 100 mg of 278 per ml in formulation. We have now developed, or at least got ready for, our first human trial, a more concentrated 300 mg per ml formulation.

OK, so that's the next step. Then?

Then we would need to give multiple doses and study the safety and tolerability of that formulation.

I wish you good luck, and thank you for agreeing to speak with me today.



  1. Verloes R, van't Klooster G, Baert L, et al. TMC278 long acting - a parenteral nanosuspension formulation that provides sustained clinically relevant plasma concentrations in HIV-negative volunteers. In: Program and abstracts of the XVII International AIDS Conference; August 3-8, 2008; Mexico City, Mexico. Abstract TUPE0042.

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