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Photo not available due to experimental status
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Brand Name: Not yet established
Common Name: etravirine or TMC-125
Class: experimental non-nucleoside analog (also called non-nucleoside reverse transcriptase inhibitor, NNRTI or non-nuke)
Standard Dose: Two 100 mg tablets twice a day being used in the EAP (Expanded Access Program); the smaller and more bioavailable reformulation created during development.
Manufacturer contact: Tibotec, 1 (866) 889–2074, www.tibotec.com
AIDSInfo:1 (800) HIV–0440 (448–0440), www.aidsinfo.nih.gov
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| Potential side effects and toxicity: |
Diarrhea seen in approximately 28% of patients in studies. Other common side effects were rash and pyrexia (increased body temperature).
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| Potential drug interactions: |
| Norvir reduces TMC-125 levels by 75%. Aptivus significantly reduces levels of TMC-125, and Aptivus and Norvir levels are increased with TMC-125 and therefore not recommended together. No interaction with Prezista (TMC-114), a protease inhibitor, in clinical studies. When TMC-125 was given with Kaletra and Invirase, there was a decrease in the lopinavir component of Kaletra, but the clinical revelance is not known at this time. No interaction was found with the acid suppressants ranitidine (Zantac and others) or Prilosec (omeprazole) when given with TMC-125. There was also no interaction with methadone and TMC-125. |
| Tips: |
Available through expanded access (free drug before FDA approval for people in medical need. Call 1–866–889–2074, e-mail TMC125EAP@i3research.com, or visit www.tibotec-eap-usa.com. TMC-125 is a badly needed drug in the non-nuke class. The non-nukes can develop resistance quickly, and with only one mutation in the virus. The second-generation (it’s new and improved, but still being proven) TMC-125 was developed to have a higher genetic barrier to drug resistance. It has shown effectiveness in people for whom Sustiva or Viramune has failed, although it may work better for Sustiva failure (people with the HIV mutation K103N). Sustiva and Viramune are known for potency and tolerability compared to the protease inhibitors, although they have the potential for very negative side effects. Remember also that Sustiva should not be taken during pregnancy and that Viramune may lead to liver damage or life-threatening rash. TMC-125 is likewise generally tolerable, but then it has the diarrhea of the PIs—experienced by almost a third of the people who’ve taken TMC-125. One Phase II study was stopped, however, when TMC-125 didn’t perform as well as the protease inhibitors in the comparator group of people, but a similar study found that it had superior results to protease inhibitors. TMC-125 showed a 1.99 log drop in viral load in a 7-day monotherapy study with people taking HIV meds for the first time, evidence of tremendous potency. In a Phase IIb study presented at the 2006 International AIDS Society meeting, 199 individuals with documented NNRTI resistance were randomized to receive either TMC-125 or another type of drug regimen (a comparator). The viral load reduction in people receiving a TMC-125 regimen was significantly greater than in the comparator group with optimized therapy. These are encouraging results. It also has efficacy against HIV-2 strains, the kind most commonly found in developing countries (not all the HIV drugs do this). It is important to remember that as the clinical studies are being completed, we will find out more information about this new drug. Tibotec is also developing another non-nuke, TMC-278, which seems to have pharmacologic advantages over 125, including greater potency and the potential for once-a-day dosing.
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| Doctor |
| Etravirine (TMC-125) is a 2nd generation NNRTI developed for activity against HIV strains resistant to the currently available NNRTIs (i.e., efavirenz). Etravirine should be very active in treatment naïve patients with no underlying NNRTI-resistant mutations, but its initial niche will be in patients with NNRTI-resistant HIV. Results available to date are quite limited regarding efficacy when etravirine is substituted for a failing NNRTI-based regimen, though preliminary results have noted reasonable short term efficacy in that setting. Results of a safety analysis of a TORO-style trial (etravirine plus optimized background therapy versus OBT) noted no significant side effect differences between the two arms. The most common reported side effects have been diarrhea, nausea, rash, and central nervous system effects. An expanded access program is now open for etravirine.—Keith Henry, MD |
| Activist |
| Etravirine is a new NNRTI which is scheduled to hit the market sometime in 2007 (assuming all goes well with its last compulsory studies, which we can say with a fair level of confidence will be just fine). Etravirine competes directly against Sustiva and Viramune, and is said to have activity against NNRTI–resistant strains of virus. The most notable side effects from this drug were diarrhea and headache. At the writing of this review, etravirine is currently available via expanded access to people who need a new drug to create a viable regimen. The maker of this drug, Tibotec Pharmaceuticals, was the first company to put two experimental agents together in a clinical trial (the now approved PI called Prezista, i.e., TMC 114, and etravirine). Etravirine has not been shown to have the same side effect profile as the competitors in its class, which is good news. But with all drugs, sometimes these things reveal themselves later. We will just have to wait and see, but in the meantime, this is a welcome addition to our arsenal of medications.—Cathy Olufs |
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