Intelence (etravirine, TMC-125)

August 2009     View PDF     En español
Reprinted from www.aidsmeds.com, US

What is Intelence?
Intelence is a non-nucleoside reverse transcriptase inhibitor (NNRTI) manufactured by Tibotec Therapeutics, a division of Centocor Ortho Biotech products, LP. It was approved by the US Food and Drug Administration (FDA) in January 2008. Intelence is approved for treatment-experienced patients who have HIV strains that are resistant to an NNRTI and other HIV drugs. It is not yet approved for people starting antiretroviral therapy for the first time.

Intelence works by blocking HIV's reverse transcriptase enzyme. After HIV's genetic material is deposited inside a cell, its RNA must be converted (reverse transcribed) into DNA. NNRTIs stop this process and prevent HIV from infecting the CD4 cell and producing new virus particles.

Intelence must be used in combination with other HIV drugs.

Tibotec Therapeutics has established a patient assistance program (PAP) for people living with HIV who do not have private or public health insurance and are unable to afford Intelence. To learn more about the PAP for Intelence, call 866-836-0114 or refer to Tibotec's website for more information. For those with private health insurance, Tibotec has established a program to help cover up to 80 percent of the amount of each Intelence co-payment, up to $100 every month. To learn more about this co-pay program, call 866-961-7169.

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What is already known about Intelence?
The Intelence dose is two 100 mg tablets taken by mouth twice a day. It should be taken following a meal (e.g., breakfast and dinner).

The tablets should be swallowed whole, with liquid such as water. The tablets should not be chewed. If you are unable to swallow the tablets whole, you can dilute the tablets in a glass of water. Stir the water well, until it looks milky, then drink the mixture immediately. Make sure that there's no medication residue remaining in the glass (add additional water and then mix and swallow again).

Intelence is active against HIV strains resistant to other antiretrovirals, including many strains that are resistant to the NNRTIs Sustiva (efavirenz), Viramune (nevirapine) and Rescriptor (delavirdine). Drug-resistance testing can be used to determine how effective Intelence will be against HIV, if other NNRTIs have been used in the past.

Intelence is not approved for people with HIV that have no resistance to other available antiretroviral drugs. This includes HIV-positive people beginning treatment for the first time.

Intelence is not yet approved for use in HIV-positive children.

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What about drug interactions?
Because of the way Intelence is metabolized (broken down) in the body, it can interact with many other medications used to treat HIV, AIDS-related complications and other diseases. Intelence may cause blood levels of other medications to become too low (which can decrease their effectiveness) or high (which can increase the risk of side effects). Similarly, other medications may cause blood levels of Intelence to become too low or high.

At the time of Intelence's approval in January 2008, there were no known "contraindications," meaning that there were no known medications that must be avoided while taking Intelence. However, there are a number of medications that are not yet recommended for use in combination with Intelence.

Intelence can interact with several HIV medications. Intelence should not be combined with the following: Norvir (ritonavir)-boosted Aptivus (tipranavir), Norvir-boosted Lexiva (fosamprenavir) or Norvir-boosted Reyataz (atazanavir); any protease inhibitors given without a boosting dose of Norvir; or any of the other approved NNRTIs.

Intelence can be combined with any of the approved nucleoside reverse transcriptase inhibitors (NRTIs). It can also be combined with Norvir-boosted Prezista (darunavir) or Norvir-boosted Invirase (saquinavir) without having to adjust the doses of any of the drugs being used. Intelence can also be combined with the integrase inhibitor Isentress (raltegravir), without requiring dose adjustments.

Kaletra (lopinavir plus ritonavir) should be used cautiously with Intelence, given that it can raise Intelence blood levels 85 percent and potentially increase the risk of Intelence side effects. While it is possible that Intelence can be combined with Selzentry (maraviroc), official dosing recommendations have not yet been made (if using Intelence without a Norvir-boosted protease inhibitor, the Selzentry dose will likely be 600 mg, taken twice a day; if using Intelence with a Norvir-boosted protease inhibitor, the Selzentry dose will likely be 150 mg, taken twice a day).

Intelence can interact with Biaxin (clarithromycin), Rifadin (rifampin), Priftin (rifapentine) and Mycobutin (rifabutin) — medications used to treat TB, MAC, and other bacterial infections. Zithromax (azithromycin) should be used as an alternative to Biaxin. Because Rifadin and Priftin can greatly reduce levels of Intelence in the bloodstream, they should not be used at the same time. If Intelence is being used with a Norvir-boosted protease inhibitor, Mycobutin should not be used. If Intelence is being used without a Norvir-boosted protease inhibitor, a Mycobutin dose of 300 mg once a day is recommended.

Intelence can interact with several medications used to treat thrush (candidiasis) and other fungal infections, including Diflucan (fluconazole), Sporanox (itraconazole), Nizoral (ketoconazole), Noxafil (posaconazole) and Vfend (voriconazole). Dose adjustments of antifungal medications may need to be made if used in combination with Intelence.

Methadone, commonly used to treat drug addiction, can be taken with Intelence.

Intelence can interact with a number of heart medications, including Vascor (bepridil), Tambocor (flecainide) and Rythmol (propafenone). Intelence can reduce levels of these medications in the bloodstream, potentially making them less effective. Monitoring blood levels of these heart medications is recommended if using them in combination with Intelence.

The anticonvulsants Tegretol (carbamazepine), Luminal (phenobarbital) and Dilantin (phenytoin) should not be used in combination with Intelence.

Cholesterol-lowering drugs, also known as "statins," can interact with Intelence. Intelence may decrease blood levels of Zocor (simvastatin) and Mevacor (lovastatin). Lescol (fluvastatin) levels may be increased in the blood stream. Intelence can be given with Lipitor (atorvastatin), although it may be necessary to adjust the dose of Lipitor if cholesterol levels do not improve. It is not expected that Intelence will interact with Pravachol (pravastatin) or Crestor (rosuvastatin).

Viagra (sildenafil), Levitra (vardenafil) and Cialis® (tadalafil) levels in the bloodstream may decrease when combined with Intelence. Doses of these medications may need to be adjusted.

Herbal products can also interact with Intelence. St. John's wort should not be used with Intelence, since it can reduce the amount of Intelence in the bloodstream.

Other drug interactions are possible. Be sure to tell your doctor about all the medications you are taking (or plan to take), including those you buy over the counter at your pharmacy or health-food store, while taking Intelence.

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What is known about side effects?
The most common side effects reported in clinical trials using Intelence were rash (16.9 percent) and nausea (13.9 percent). Some severe rashes have been reported, including a life-threatening condition called Stevens-Johnson syndrome. Other possible hypersensitivity reactions include fever, generally ill feeling, extreme tiredness, muscle or joint aches, blisters, oral lesions, eye inflammation, facial swelling and/or signs and symptoms of liver problems. Notify your health care provider immediately if you develop a rash or other severe side effect while taking Intelence.

Other possible side effects of Intelence include diarrhea, nausea, vomiting, abdominal pain, tiredness, tingling or pain in hands or feet, numbness, headache and high blood pressure.

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Can pregnant women take Intelence?
Intelence is classified by the FDA as a "pregnancy category B" drug. Pregnancy category B means that animal studies have failed to demonstrate a risk to the fetus, but there have not been adequate, well-controlled studies involving pregnant women. HIV-positive women who become pregnant should discuss the benefits and possible side effects of anti-HIV treatment to help protect their babies from HIV.

It is not known whether Intelence passes into breast milk and what effect it may have on a nursing baby. To prevent transmission of the virus to uninfected babies, it is recommended that HIV-positive mothers not breast-feed.

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Where can I learn more about clinical trials of Intelence?
If you would like to find out if you are eligible for any clinical trials that include Intelence, there is an interactive web site run by ACRIA, the AIDS Community Research Initiative of America.

Another useful service for finding clinical trials is AIDSinfo.nih.gov, a site run by the US National Institutes of Health. NIH has "health information specialists" you can talk to at their toll-free number, 800.HIV.0440 (800.448.0440).

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