Investigational NNRTI TMC278 swiftly cuts viral load in treatment-naive patients

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TMC278, an investigational nonnucleoside reverse transcriptase inhibitor (NNRTI) reputed to have a high barrier to resistance, passed a crucial step in clinical development—a seven day monotherapy test in treatment-naive patients. The median viral load drop measured 1.2 log10 copies/mL (more than 10-fold), reported Frank Goebel, MD, from Munich’s Ludwig Maximilians University, at the Twelfth Conference on Retroviruses and Opportunistic Infections held in Boston, Massachusetts (Goebel 2005).

With activity against some NNRTI-resistant virus (de Bethune 2005), TMC278 is the second of two NNRTIs under development at Tibotec in Mechelen, Belgium. The drug’s lengthy 38-hour half-life could make once-daily dosing possible.

Dr. Goebel and colleagues in Russia and the United Kingdom randomised 47 treatment-naive individuals to placebo or 25mg, 50mg, 100mg, or 150mg TMC278 given once daily for seven days as an oral solution. Study participants began treatment with a median viral load of 4.5 log10 copies/ml (range 3.5-5.9 log10 copies/ml) and a median CD4+ cell count of 292 cells/mm3 (range, 29-590 cells/ mm3).

Glossary

placebo

A pill or liquid which looks and tastes exactly like a real drug, but contains no active substance.

treatment-naive

A person who has never taken treatment for a condition.

naive

In HIV, an individual who is ‘treatment naive’ has never taken anti-HIV treatment before.

oral

Refers to the mouth, for example a medicine taken by mouth.

investigational

In medicine, a drug that is approved by the regulatory authorities (Food and Drug Administration, European Medicines Agency) for testing in clinical trials, but not yet approved for commercial marketing and sale. Also called experimental drug, investigational agent, and investigational new drug (IND).

After seven days, the median HIV-1 load dropped 1.29 logs with TMC278 25mg, 1.23 logs with 50mg, 1.07 logs with 100mg, and 1.17 logs with 150mg , with no change in the placebo group (P value vs placebo

No one stopped treatment because of toxicity in this brief study, and no serious side effects were reported. The median CD4+ cell count climbed 55 cells/mm3 in seven days.

A multinational phase 2b dose-finding study begins in March 2005.

This content licensed to aidsmap by iMedOptions, publishers of http://clinicaloptions.com. Copyright iMedOptions, LLC, 2005

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References

Goebel F et al. TMC278: potent anti-HIV activity in antiretroviral therapy-naive patients. Twelfth Conference on Retroviruses and Opportunistic Infections, Boston, abstract 160, 2005.

de Bethune MP et al. TMC278, a new potent NNRTI with an increased barrier to resistance and good pharmacokinetic profile. Twelfth Conference on Retroviruses and Opportunistic Infections, Boston, abstract 556, 2005.