Gene/Protein Disease Symptom Drug Enzyme Compound
Pivot Concepts:   Target Concepts:
Query: EC:2.7.7.49 (reverse transcriptase)
 31,746 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

As many as 25 to 45 percent of patients using triple therapy with protease inhibitors will develop resistance due to a change in the genetic HIV code. However, patients who develop resistance may still benefit clinically when protease inhibitors are used in combination with other antiretrovirals. These patients may not have undetectable viral loads although they may have stable T4-cell counts. Resistance does not always lead to disease progression. Newer drugs under development or available through compassionate track programs may benefit people with resistance. DMP-266 (Sustiva) is a non-nucleoside reverse transcriptase inhibitor that shows promise for these patients. Other drugs in development include Compound 141, 1592, and adefovir.
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PMID:Understanding and managing resistance. 1136 97

Studies of efavirenz (Sustiva, formerly DMP-266) in monkeys have shown newborn monkeys with abnormalities. Dupont Merck, the manufacturer of the non-nucleoside reverse transcriptase inhibitor, presented the information to the Food and Drug Administration (FDA). Although it is unknown if the risk exists in humans, the FDA warns that pregnant women should not use DMP-266.
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PMID:Safety alert issued on efavirenz (Sustiva). 1136 72

Phase III data show that efavirenz (Sustiva, formerly DMP-266) is effective in suppressing viral load when used in combination with other treatments. A head-to-head comparison trial in volunteers with little or no previous antiretroviral experience shows that efavirenz may suppress viral load as well as Indinavir (Crixivan). Efavirenz is an experimental non-nucleoside reverse transcriptase inhibitor (NNRTI), and widespread consensus seems to accept it as a valid treatment for AIDS. The most noteworthy trial result showed that using it in combination with AZT plus 3TC suppressed viral load to below 400 copies in a significant number of volunteers, with few patients dropping out. Viral load remains low at 72 weeks, but not much information is available on those patients who were more heavily pre-treated. Other combinations also appear effective. DuPont Pharmaceuticals, the manufacturer, says common side effects include rash, nausea, diarrhea, headache, and insomnia, and cautions against widespread use in pregnant women. Efavirenz is unlikely to work in patients who have developed resistance to either Nevirapine or Delavirdine, two other NNRTI drugs.
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PMID:Efavirenz (Sustiva) may equal or exceed protease inhibitor in initial antiretroviral combination. 1136 99

Antiviral drugs, like any trend, may be in demand one year but passe the next. Saquinavir is an example of this trendiness. Initially, it was in great demand, but within 2 years the side effects had reduced the demand. Efavirenz (Sustiva), a non-nucleoside reverse transcriptase inhibitor, is the new trend. The Geneva Conference provided study results showing that a regimen containing efavirenz plus AZT plus 3TC helped 95 percent of the patients reduce their viral load to below detectable levels after 24 weeks of therapy. Efavirenz also requires only one dose per day, and it can be taken with or without food.
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PMID:Dressing up your virus: a new outfit for HIV. 1136 10

Treatment activists are circulating a letter opposing drug-pricing strategies for abacavir (Ziagen) and efavirenz (Sustiva). The groups are concerned that these drugs will be priced significantly higher than other nucleoside analogs and non-nucleoside reverse transcriptase inhibitors. The statement notes that higher survival rates should insure drug manufacturers of a steady supply of patients, allowing them to lower prices and still make a profit. Both drugs are appropriate for treatment-naive and treatment-experienced patients, making the potential market for them large. The letter is sponsored by the Fair Price Working Group, which includes members from Project Inform, ACT UP/New York, the San Francisco AIDS Foundation, GMHC Treatment Issues, Foundation for AIDS and Immune Research, and AIDS Treatment News. Contact information is included.
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PMID:New drug pricing consensus letter, sign-ons requested. 1136 62

Efavirenz (Sustiva), a non-nucleoside reverse transcriptase inhibitor (NNRTI) developed by DuPont Pharmaceuticals, was approved by the Food and Drug Administration. DuPont has promoted the once-daily efavirenz as being as equally effective as a protease inhibitor, and has priced it accordingly. The results from Study 006, the central trial for efavirenz, reported high antiviral activity, but had a significant dropout rate. This made it difficult to extrapolate the findings for those individuals remaining. The results of other key studies, such as Study 020 and ACTG 364, are discussed. Efavirenz is most effective when combined with protease inhibitors or nucleoside analogs. Some of the side effects of efavirenz are higher cholesterol levels, dizziness, and skin rashes. The possibility of birth defects has prompted DuPont to advise patients to use two types of birth control while taking efavirenz. A contact number is provided for physicians to register pregnant patients for follow-up if they have been exposed to efavirenz. Other protease-sparing options besides efavirenz are discussed, such as Nevirapine and Delavirdine.
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PMID:Another expensive drug for your cocktail. 1136 6

The U.S. Food and Drug Administration (FDA) has approved Sustiva (efavirenz) as the first HIV drug to have a once-daily dosing schedule. The drug, developed by DuPont Pharmaceuticals, is a non-nucleoside reverse transcriptase inhibitor (NNRTI) and will be used in combination with other anti-HIV drugs for both adult and pediatric patients. Results from clinical trials show that Sustiva reduces plasma viral loads to below quantifiable levels in a majority of treatment naive and experienced individuals in two, three, and four drug combinations. It can be taken with or without food, although high fat meals may interfere with absorption and should be avoided. The drug is generally well tolerated, with the most significant side effects being nervous system related, such as insomnia and dizziness. Mild to moderate skin rashes were also reported in one out of four patients. Women should not become pregnant while taking Sustiva because birth defects have been noted in animal studies. Contact information is provided.
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PMID:FDA approves Sustiva (efavirenz) capsules, first once-daily anti-HIV drug. Food and Drug Administration. 1136 15

Sustiva (efavirenz), a drug developed by DuPont Pharmaceuticals, is a non-nucleoside reverse transcriptase inhibitor that is used in combination therapy and is taken once a day. Clinical trial results indicate that the low dosage and efficacy of Sustiva make it a good treatment option for many patients. AIDS advocates have asked the company to consider lowering the price of the drug.
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PMID:New drug approved. 1136 34

Efavirenz (Sustiva) is the first once-daily dosing anti-HIV drug approved by the Food and Drug Administration. The non-nucleoside reverse transcriptase inhibitor (NNRTI) is highly potent and more convenient than other therapies, and is used to treat HIV-1 in both adults and pediatric patients. It is effective in combination therapy, and patients on efavirenz had fewer side effects than patients on other triple combinations therapies. It remains to be seen if efavirenz will be used in first-line therapy. Some reports show that patients who are taking other drugs that affect the central nervous system suffer additional central nervous system side effects from efavirenz. There are reports of cross-resistance with other drugs in the same class, and limited data that is available on fetal toxicity suggests that women of childbearing age need to be counseled carefully before taking this drug.
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PMID:First once-daily drug simplifies dosing, offers new options in HIV-1 treatment. 1136 67

The Food and Drug Administration (FDA) approved DuPont Pharma's new non-nucleoside reverse transcriptase inhibitor (NNRTI) efavirenz (Sustiva, DMP-266). Efavirenz has shown promise in trials with over 2000 participants for up to 24 weeks, and early data suggests it may be as effective as protease inhibitors when used in a combination regimen. It is the first anti-HIV drug approved for once-daily dosing. Efavirenz is well tolerated, and the main side effects reported are dizziness, insomnia, abnormal dreams, and skin rash. Efavirenz has been approved for adults and children, but should not be used by pregnant women. Contact information is provided.
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PMID:FDA approves efavirenz. Food and Drug Administration. 1136 87


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