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| | SF AIDS Fdn: BETA 9/97 -- Protease Inhibitor Drug Interactions |
 | | Stopping a protease inhibitor may result in the development of drug resistance and may preclude later use of that drug. | | | Much is already known about protease inhibitors and the ways they affect and are affected by other drugs. | | | Ketoconazole (Nizoral) and related drugs block the breakdown of saquinavir, indinavir and perhaps other protease inhibitors, with a resulting increase in protease inhibitor levels. |
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http://www.sfaf.org/treatment/beta/b34/b34piint.html
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| | StereoGraphics Success Stories - SmithGlaxoKline |
| | Eric Furfine, GSK's protease research project leader, sought to show the investigators conducting the clinical trials the biochemical and structural characteristics of the HIV protease inhibitor as it bound to wild-type (WT) and drug-resistant HIV protease. | | | Specifically, Eric Furfine, director of Biomedical and Analytical Pharmacology at GlaxoSmithKline, has been leading the search for new protease inhibitor drugs that can be used in conjunction with other medications. | | | For years, researchers at GlaxoSmithKline's vast research complex in Research Triangle Park, N.C. have been designing new drugs for the treatment of AIDS. |
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http://www.stereographics.com/news_about_us/success_stories/smithg.html
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| | Update on HIV Pharmacology and Therapeutic Drug Monitoring |
| | For therapeutic drug monitoring to have a role in antiretroviral therapy, active drug levels must be quantifiable, there must be a quantitative relationship between drug level and outcome of interest (eg, anti-HIV effect or toxicity, for example), and the information should translate into ability to modulate therapy to the patient's benefit. | | | For reliable inhibitory quotients, comparative data for the different protease inhibitor combinations and other drugs need to be generated under identical experimental conditions. | | | Further, therapeutic drug monitoring may not be necessary if drug pharmacokinetic profiles can be optimized in other ways - eg, by exploiting beneficial pharmacokinetic interactions such as those used to maintain increased blood levels of protease inhibitors. |
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http://hivinsite.ucsf.edu/InSite.jsp?page=md-04-01-15
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| | FDA Approves LEXIVA (fosamprenavir): study results for teatment naive & experienced, safety, adverse events, ... |
| | Because the potential for HIV cross-resistance among protease inhibitors has not been fully explored, it is unknown what effect therapy with LEXIVA will have on the activity of subsequently administered protease inhibitors. | | | Particular caution should be used when prescribing phosphodiesterase (PDE5) inhibitors for erectile dysfunction (e.g., sildenafil or vardenafil) in patients receiving protease inhibitors, including LEXIVA. | | | In 2 clinical studies of LEXIVA plus low-dose ritonavir, rash occurred in 8 of 50 patients (16%) with a history of sulfonamide allergy compared with 50 of 412 patients (12%) with no history of sulfonamide allergy. |
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http://www.natap.org/2003/oct/102303_1.htm
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| | HIV Patients May Be At Risk Of Heart Problems When Taking Protease Inhibitor Drugs |
| | They investigated the hypothesis that the widely-used protease inhibitors may, in fact, be linked to the development of heart rhythm problems through the mechanism of blocking a channel. | | | After hearing of a case of heart rhythm disturbances in a patient taking protease inhibitors, the researchers looked for evidence of other patients with similar experiences. | | | They encourage physicians to be especially thorough when performing medical exams, and in taking patient histories to be alert for signs of heart rhythm disturbances. |
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http://www.sciencedaily.com/releases/2005/02/050218161626.htm
(809 words)
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| | Introduction |
| | Testimony to the great mutability of HIV is recent research that have found protease inhibitor resistant strains of HIV in patients who have never received protease inhibitor therapy before. | | | Recent research suggests that HIV gains resistance at substantial cost to protease functionality and that increased selective pressure from more protease inhibitors may lead to less virulent strains of HIV. | | | However, after the sequence of available protease inhibitors are exhausted by HIV resistance development, there are no other effective therapy options available, and the patient's CD4 |
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http://www.stanford.edu/~siegelr/philhsu.htm
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| | CROI: Doubling Up on Protease Inhibitor Helps Control Viral Infection in HIV Patients in Virologic Failure |
| | The researchers concluded that patients with virologic failure on their first PI have better virologic and immunologic responses when they receive a NNRTI-containing salvage regimen with 2 protease inhibitors rather than with 1 protease inhibitor. | | | The CPCRA is a community-based clinical trials network aimed at informing healthcare providers and people living with HIV on the most appropriate use of available HIV therapies in diverse populations across the spectrum of HIV diseases. | | | "In patients with virologic failure on their first protease inhibitor, the non-nucleoside reverse transcriptase inhibitor [NNRTI]-containing salvage regimens with 2 protease inhibitors provided better virologic and immunologic responses than the regimens with 1 protease inhibitor," reported Jay Kostman, MD, Chief, Division of Infectious Diseases, Presbyterian Medical Center, Philadelphia, Pennsylvania. |
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http://www.pslgroup.com/dg/242e86.htm
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| | The Management of HIV-1 Protease Inhibitor Pharmacokinetic Interactions |
| | The HIV-1 protease inhibitors (PIs) are widely used in combination antiretroviral therapy for the management of HIV-1 infection. | | | Guidelines for the treatment of HIV infection suggest that alternative antiretroviral therapy (ARV) be considered for patients requiring treatment for both HIV and Mycobacterium tuberculosis, specifically the option of replacing the PI with a non-nucleoside reverse-transcriptase inhibitor.2 This is of particular importance in limited resource countries, in which rifabutin may not be available. | | | In: Program and Abstracts of the Sixth International Workshop on Clinical Pharmacology of HIV Therapy, Quebec City, 2005. |
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http://www.hivdent.org/drugs1/drugTMHP0705.htm
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| | Antiretroviral Pharmacology: An Expert Interview With David M. Burger, PharmD, PhD |
| | With the large number of antiretroviral regimens now available for the treatment of HIV, clinical pharmacology has become one of the most critical areas of AIDS research. | | | Disclosure: Mark Wainberg, PhD, has disclosed that he has received grants for clinical research from GlaxoSmithKline and Bristol-Myers Squibb.
Disclosure: David M. Burger, PharmD, PhD, has disclosed that he has received grants for clinical research and educational activities from Gilead (Viread and Emtriva). | | | We're not quite sure if the interaction is as it was presented today, but if people are going to use this, they should be monitoring for nevirapine toxicity and a possible drug interaction. Dr. Wainberg: What about half-life of nevirapine as it pertains to this? |
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http://www.medscape.com/content/2004/00/48/37/483721/483721.xml
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| | The Body Pro: Pharmacokinetics in HIV/AIDS |
| | Protease Inhibitor Drug Interactions and Non-Nucleoside RT Inhibitor Drug Interactions — November 2004 | | | Maintained by the University of Liverpool and geared toward healthcare professionals; features interactive charts for assessing the risks of interaction between protease inhibitors, NNRTIs and other drugs. | | | Drug Interactions of Protease Inhibitors and Psychiatric Medications &; January 2001 |
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http://www.thebodypro.com/treat/interactions.html
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| | Four Studies Examine Tolerability and Antiviral Activity of Once-Daily Fortovase Plus Ritonavir |
| | Efficacy data are not yet available; the data presented focused on a pharmacokinetic substudy of the FOCUS Trial evaluating a cohort of 49 patients. | | | Concomitant use with lovastatin or simvastatin is also not recommended; caution should be exercised with other HMG-CoA reductase inhibitors metabolized by the CYP 3A4 pathway. | | | inhibitors and that the cause and long-term health effects of these conditions are not known at this time. |
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http://www.rocheusa.com/newsroom/current/2001/pr2001041801.html
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| | 6th Conference - Session 79 |
| | A Syndrome of Lipodystrophy in Patients Receiving a Stable Nucleoside-Analogue Therapy. | | | Effects of Protease Inhibitor Use on Hyperglycemia and Hyperlipidemia: A Five Year Analysis. | | | Prevalence and Risk Factors for Hyperglycemia, Dyslipidemia, and Coronary Disease Among HIV-Infected Patients on Initial Protease Inhibitor Therapy. |
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http://www.retroconference.org/1999/posters/session79.htm
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| | L-chicoric acid, an inhibitor of human immunodeficiency virus type 1 (HIV-1) integrase, improves on the in vitro ... |
| | The improved anti-HIV activity was observed with a tissue culture adapted strain of HIV (HIV(LAI)) and with limited passage clinical isolates of HIV (HIV(R19) and HIV(R45)). | | | Combinations of anti-human immunodeficiency virus (HIV) drugs, including reverse transcriptase inhibitors and protease inhibitors, have proven immensely potent in the therapy of acquired immune deficiency syndrome (AIDS). | | | To determine whether HIV integrase is a suitable target for combination therapy, the ability of an HIV integrase inhibitor, L-chicoric acid, to work in combination with a protease inhibitor and Zidovudine was tested in vitro. |
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http://www.aegis.com/aidsline/1999/mar/A9930490.html
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| | protomed, protease inhibitor in soybeans |
| | and Therapeutics (June issue) that a protease inhibitor | | | revealed in a paper to be published in Pharmacology |
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http://www.ag.uiuc.edu/archives/experts/health/1998a/0403.html
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| | 614 - Abstract (11th CROI) |
| | 3-Way Pharmacokinetic Interaction among Amprenavir, Efavirenz, and a Second Protease Inhibitor | | | Interestingly, NFV and IDV increased the APV AUC in the presence of EFV in a manner not predicted from prior isoform and 2-way clinical interaction studies. |
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http://www.retroconference.org/2004/cd/Abstract/614.htm
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| | British Journal of Pharmacology - YD-3, a novel inhibitor of protease-induced platelet activation |
| | Our results showed that pretreatment of human platelets with chymotrypsin selectively enhanced the inhibitory effect of YD-3 on thrombin-, but not U46619-induced platelet aggregation. | | | Therefore, development of thrombin inhibitors or receptor antagonists would be of therapeutic interest in preventing these pathological events. | | | Thrombin is a trypsin-like serine protease playing a central role in both haemostasis and thrombosis (Hemker, 1994). |
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http://www.nature.com/bjp/journal/v130/n6/full/0703437a.html
(4356 words)
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| | ABT-378: a second generation protease inhibitor. |
| | Keywords: NEWSLETTER ARTICLE Clinical Trials Drug Interactions Drug Therapy, Combination Drugs, Investigational HIV Protease Inhibitors/ADMINISTRATION and DOSAGE/*PHARMACOLOGY/ PHARMACOKINETICS Human Pyrimidinones/ADMINISTRATION and DOSAGE/*PHARMACOLOGY/ PHARMACOKINETICS Ritonavir/ADMINISTRATION and DOSAGE/PHARMACOLOGY/PHARMACOKINETICS | | | ABT-378 was engineered to overcome some of the problems associated with the protease inhibitors currently on the market. | | | Early results show it to be about 10 times more potent than Abbott's already-approved drug, Ritonavir. |
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http://www.aegis.com/aidsline/1999/dec/A99C0632.html
(315 words)
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| | Protease inhibitor (biology) - Wikipedia, the free encyclopedia |
| | For the drugs used in AIDS, please refer to protease inhibitor (pharmacology) | | | A1AT is indeed the protease inhibitor most often involved in disease, namely in alpha 1-antitrypsin deficiency. | | | In medicine, protease inhibitor is often used interchangeably with alpha 1-antitrypsin (A1AT, which is abbreviated P |
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http://en.wikipedia.org/wiki/Protease_inhibitor_(biology)
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| | Amprenavir or Fosamprenavir Plus Ritonavir in HIV Infection: Pharmacology, Efficacy and Tolerability Profile |
| | Amprenavir (Agenerase) is an HIV-1 protease inhibitor, the first in vitro activity studies of which were published in 1995. | | | During in vivo development, it became clear that the pharmacokinetics of the drug would result in patients taking a large number of pills daily. | | | The pharmacokinetic properties of fosamprenavir and the first clinical trials in treatment-naive and treatment-experienced patients should allow it to be considered as a better alternative to amprenavir in countries where fosamprenavir is already available. |
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http://www.hivandhepatitis.com/recent/pibosted/031605_a.html
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| | HIVresistanceWeb.com- Bibliography - Abstract |
| | Antiviral Therapy 1999; 4 (Supplement 1): Abstract 18 | | | Taken together, the data suggest that BMS 232,632 is a new generation of HIV protease inhibitor that should be a valuable addition to our anti-HIV armamentarium. | | | Resistance profile of BMS 232,632, a new inhibitor of HIV protease |
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http://www.hivresistanceweb.com/protected/biblio/99-seplin.shtml
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| | Abstract 80 - Fourth HIV DRP Symposium: Antiviral Drug Resistance |
| | THE STRUCTURAL AND THERMODYNAMIC BASIS FOR THE BINDING OF TMC114, A NEXT-GENERATION HIV-1 PROTEASE INHIBITOR | | | To examine the basis for this potency, we solved the following crystal structures: TMC114 complexed with wt HIV-1 protease, and TMCl14 and APV complexed with a multi-drug-resistant (MDR; L63P, V82T, I84V) protease variant. | | | However, TMC114 binding to the triple-mutant HIV-1 protease is reduced by a factor of 13.3. |
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http://www.ncifcrf.gov/campus/symposium/abstract_80.html
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| | Achillion Pharmaceuticals, Inc. |
| | Genetic resistance studies have demonstrated that the compound is compatible with HCV protease and polymerase inhibitors. | | | The compound has demonstrated good oral bioavailability and safety pharmacology, and is currently undergoing pre-IND testing with an expectation to begin human testing in the second half of 2005. | | | In an attempt to address these treatment issues and limitations, Achillion has an ongoing effort to discover novel small molecule inhibitors of HCV that can be administered orally. |
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http://www.achillion.com/hepatitisc.php
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