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)

Nevirapine, a non-nucleoside reverse transcriptase inhibitor, is related to Delavirdine and efavirenz, and was given a conditional Notice of Compliance by Canada's Health Protection Branch. This conditional approval requires that additional data from continuing studies be submitted by the drug manufacturer, Boehringer Ingelheim. Participants in the expanded access program will receive Nevirapine through the end of the year.
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PMID:Nevirapine receives green light from Health Protection Branch. 1136 78

Recent progress in treatment methods and medicines has made HIV more manageable. Factors contributing to this progress include advances in testing; the use and approval of protease inhibitors, non-nucleoside reverse transcriptase inhibitors, and other nucleosides; and the success of highly active antiretroviral regimens (HAART) and combination therapy. Nucleoside reverse transcriptase inhibitors, such as Zidovudine and Didanosine, and non-nucleoside reverse transcriptase inhibitors (NNRTIs) such as Nevirapine (Viramune) and Delavirdine (Rescriptor), are recommended for use in combination therapy. The pharmacology, side effects, and contraindications of these types of drugs are provided. Dosages and common side effects are also mentioned.
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PMID:Understanding the reverse transcriptase inhibitors in HIV. 1136 42

The Food and Drug Administration recently approved efavirenz (Sustiva), a non-nucleoside reverse transcriptase inhibitor (NNRTI), for use in treatment of adults and children. When used in combination therapy, efavirenz has shown to be very effective in suppressing viral loads for a minimum of 24 weeks. People taking efavirenz should be aware of potential cross-resistance with the other two approved NNRTIs, Nevirapine and Delavirdine, as well as possible drug interactions. Common side effects and dosing information are described. Because of the high cost, efavirenz may not be covered under some States' AIDS Drug Assistance Programs (ADAPs). The Access Project can provide the numbers of State ADAP coordinators for further information, or individuals may contact Dupont Pharma's Patient Assistance Program at the number provided.
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PMID:Efavirenz (Sustiva) receives FDA approval. Food and Drug Administration. 1136 87

Protease-sparing regimens are sometimes considered the best initial therapy because they can effectively reduce viral load, while allowing the individual to reserve potent protease inhibitor therapy for later treatment. Others contend that the more potent therapy should be used first, to give a patient the best shot at long-term viral suppression. The debate continues with the promotion of efavirenz (Sustiva), a non-nucleoside reverse transcriptase inhibitor (NNRTI), sometimes prescribed as the initial course of therapy. Several reasons are explored for re-evaluating this decision, which is largely based on limited information from one trial with significant results. A table compares efavirenz with Nevirapine and Delavirdine, two other NNRTIs. There are still not enough data to support a recommendation about the use of protease-sparing treatment or the comparative value of the three NNRTIs listed.
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PMID:Strategy update: protease-sparing regimens. 1136 90

New anti-HIV drugs that are expected to become available in the future are discussed. The potent protease inhibitor amprenavir (Agenerase) is expected to be available in pharmacies by early 1999. Results of a study of treatment-naive, HIV-positive people showed that those taking amprenavir as part of a three-drug combination therapy, with AZT and 3TC, had better viral reduction than those using AZT and 3TC alone. In a French study of the non-nucleoside reverse transcriptase inhibitor Nevirapine, and a similar study of Delavirdine, a majority of participants had HIV RNA levels below the limit of detection. Further comparative studies are needed between Nevirapine, Delavirdine and the more costly, highly publicized competitor, efavirenz. Several studies of regimens that include protease inhibitors compare dosing twice daily to three times a day. A Canadian study describes salvage therapies, for people who have failed previous treatment with protease inhibitors, that can include up to nine drugs. Because there is a shortage in the development of new types of HIV drugs, people are encouraged to carefully consider when to begin treatment and what medical options are available.
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PMID:Antivirals update. 1136 1

Five heavily pretreated HIV-infected children were put on amprenavir and delavirdine plus two nucleoside inhibitors to reverse transcriptase to boost amprenavir levels and to use the antiretroviral activity of a non-nucleoside reverse transcriptase inhibitor. No data are available about this combination in children. It w;as well tolerated, and the median reduction in viral load was 1.5 log after 18 months. Delavirdine boosted amprenavir trough levels more than 10-fold, and delavirdine trough levels remained i several fold above susceptible HIV strains.
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PMID:Long-term pharmacokinetics of amprenavir in combination with delavirdine in HIV-infected children. 1519 27

A novel series of piperidine-substituted triazine derivatives have been synthesized and evaluated for anti-HIV activities in MT-4 cells. Most compounds displayed extremely promising activity against wild-type HIV-1 with EC(50) values in low nanomolar concentration, better than that of Nevirapine, Delavirdine, Zidovudine and Dideoxycitidine, and higher potency towards the resistant mutant strain K103N/Y181C than that of Nevirapine and Delavirdine. Selected compounds were also assayed against reverse transcriptase with lower IC(50) values than that of Nevirapine. The structure-activity relationship (SAR) of these novel structural congeners was also discussed.
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PMID:Synthesis and biological evaluation of piperidine-substituted triazine derivatives as HIV-1 non-nucleoside reverse transcriptase inhibitors. 2240 88


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