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07-SEPTEMBER-2008 03:17:44 - pharmacology For natural protease inhibitors, please see protease inhibitor biology Protease inhibitors PIs are a class of medications used to treat or prevent infection by viruses, including HIV and Hepatitis C. PIs prevents viral replication by inhibiting the activity of HIV-1 protease, an enzyme used by the viruses to cleave nascent proteins for final assembly of new virons. Protease inhibitors have been developed or are presently undergoing testing for treating various viruses: HIV/AIDS: antiretroviral protease inhibitors saquinavir, ritonavir, indinavir, nelfinavir etc. Hepatitis C: experimental agents: BILN 2061 All clinical trials of BILN 2061 have been suspended due to cardiac issues, VX 950 trade name Telaprevir, or SCH 5030341 Given the specificity of the target of these drugs there is the risk, as in antibiotics, of the development of drug-resistant mutated viruses. To reduce this risk it is common to use several different drugs together that are each aimed at different targets. Contents 1 Antiretrovirals 2 Antiprotozoal Activity 3 Anticancer Activity 4 References Antiretrovirals Protease inhibitors were the second class of antiretroviral drugs developed. In all cases, patents remain in force until 2010 or beyond. Name Trade name Company Patent Notes Saquinavir Fortovase, Invirase Hoffmann-La Roche U.S. Patent 5,196,438 It was the first protease inhibitor approved by the FDA December 6, 1995. Ritonavir Norvir Abbott Laboratories U.S. Patent 5,541,206 - Indinavir Crixivan Merck Co. U.S. Patent 5,413,999 - Nelfinavir Viracept Japan Tobacco U.S. Patent 5,484,926 - Amprenavir Agenerase GlaxoSmithKline U.S. Patent 5,585,397 The FDA approved it April 15, 1999, making it the sixteenth FDA-approved antiretroviral. It was the first protease inhibitor approved for twice-a-day dosing instead of needing to be taken every eight hours. The convenient dosing came at a price, as the dose required is 1,200mg, delivered in eight very large gel capsules. Production was discontinued by the manufacturer December 31, 2004, as it has been superseded by fosamprenavir. Lopinavir Kaletra Abbott - Is only marketed as a combination, with ritonavir. Atazanavir Reyataz - - - Fosamprenavir Lexiva GlaxoSmithKline - Is a pro-drug of amprenavir. The FDA approved it October 20, 2003. The human body metabolizes fosamprenavir in order to form amprenavir, which is the active ingredient. That metabolization increases the duration that amprenavir is available, making fosamprenavir a slow-release version of amprenavir and thus reduces the number of pills required versus standard amprenavir. Tipranavir Aptivus Boehringer-Ingelheim - Also known as tipranavir disodium Darunavir Prezista Tibotec - It was approved by the Food and Drug Administration FDA on June 23, 2006. Several ongoing phase III trials are showing a high efficiency for the PREZISTA/rtv combination being superior to the lopinavir/rtv combination for first-line therapy.2 Darunavir is the first drug in a long time that didn't come with a price increase. It leapfrogged two other approved drugs of its type, and is matching the price of a third3.45 Antiprotozoal Activity Researchers are investigating the use of protease inhibitors developed for HIV treatment as anti-protozoals for use against malaria and gastrointestinal protozoal infections: A combination of ritonavir and lopinavir was found to have some effectiveness against Giardia infection.6 The drugs saquinavir, ritonavir, and lopinavir have been found to have anti-malarial properties.7 A cysteine protease inhibitor drug was found to cure Chagas disease in mice.8 Anticancer Activity Researchers are investigating whether protease inhibitors could possibly be used to treat cancer. For example, nelfinavir and atazanavir are able to kill tumor cells in culture in a Petri dish.910 This effect has not yet been examined in humans; but studies in laboratory mice have shown that nelfinavir is able to suppress the growth of tumors in these animals, which represents a promising lead towards testing this drug in humans as well.10 References ^ FDA Grants Fast Track Designation To Oral HCV Protease Inhibitor SCH 503034 1 ^ Darunavir-ritonavir more effective than Lopinavir-ritonavir in HIV infected, treatment-experienced patients,The Lancet, Volume 370, Number 9581, 7 July 2007, http://www.thelancet.com/journals/lancet/issue?volume=370issue=9581 ^ Liz Highleyman, Patient Advocates Commend Pricing of New PI Darunavir, http://www.hivandhepatitis.com/recent/2006/ad1/063006_a.html ^ Darunavir - first molecule to treat drug-resistant HIV, http://www.news-medical.net/?id=19211 ^ Retaining Efficacy Against Evasive HIV, http://pubs.acs.org/cen/news/84/i34/8434drugdesign.html ^ Dunn LA, Andrews KT, McCarthy JS, et al 2007. The activity of protease inhibitors against Giardia duodenalis and metronidazole-resistant Trichomonas vaginalis. Int. J. Antimicrob. Agents 29 1: 98-102. doi:10.1016/j.ijantimicag.2006.08.026. PMID 17137752. ^ Andrews KT, Fairlie DP, Madala PK, et al 2006. Potencies of human immunodeficiency virus protease inhibitors in vitro against Plasmodium falciparum and in vivo against murine malaria. Antimicrob. Agents Chemother. 50 2: 639-48. doi:10.1128/AAC.50.2.639-648.2006. PMID 16436721. ^ Doyle PS, Zhou YM, Engel JC, McKerrow JH 2007. A Cysteine Protease Inhibitor Cures Chagas' Disease in an, Immunodeficient Murine Model of Infection. Antimicrobial Agents and Chemotherapy 51: 3932. doi:10.1128/AAC.00436-07. PMID 17698625. ^ J.J. Gills et al. 2007. Nelfinavir, A Lead HIV Protease Inhibitor, Is a Broad-Spectrum, Anticancer Agent that Induces Endoplasmic Reticulum Stress, Autophagy, and Apoptosis In vitro and In vivo. Clinical Cancer Research 13: 5183-5194. doi:10.1158/1078-0432.CCR-07-0161. PMID 17785575. ^ a b Pyrko, P. 2007. HIV-1 protease inhibitors nelfinavir and atazanavir induce malignant glioma death by triggering endoplasmic reticulum stress. Cancer Research 67: 10920-10928. doi:10.1158/0008-5472.CAN-07-0796. PMID 18006837. A brief history of the development of protease inhibitors by Hoffman La Roche, Abbott, and Merck v d e Antivirals used against HIV HAART primarily J05 Nucleoside Nucleotide Reverse Transcriptase Inhibitors NRTI Abacavir ABC° Dexelvucitabine§ Emtricitabine° Lamivudine 3TC° Tenofovir° Didanosine Zidovudine AZT Apricitabine† Stampidine† Elvucitabine† Racivir† Amdoxovir† Stavudine‡ Zalcitabine‡ Non-Nucleoside Reverse Transcriptase Inhibitors NNRTI Ateviridine§ Capravirine§ Efavirenz° Emivirine§ Lodenosine§ Nevirapine Etravirine Rilpivirine† Loviride‡ Delavirdine‡ Quinotaline§ Protease Inhibitors PI Atazanavir° Brecanavir§ Fosamprenavir° Lopinavir° Darunavir Nelfinavir Ritonavir Saquinavir Tipranavir Amprenavir‡ Indinavir‡ Entry/fusion inhibitors Aplaviroc§ Enfuvirtide Maraviroc Vicriviroc† PRO 140† Ibalizumab† Integrase inhibitors Raltegravir Elvitegravir† Maturation inhibitors Bevirimat† Vivecon† Combined formulations Combivir Atripla Trizivir Truvada Kaletra Epzicom Other experimental agents Foscarnet Hydroxyurea Synergistic enhancers Epigallocatechin gallate Portmanteau inhibitors Globoidnan A Griffithsin Diarylpyrimidines Calanolide A Cyanovirin-N Miltefosine R-roscovitine† °DHHS preferred first-line agent. †Undergoing clinical trials, not FDA approved. ‡Formerly or rarely used agent. §Development terminated. v d e Pharmacology: enzyme inhibition Class Competitive inhibition - Uncompetitive inhibition - Non-competitive inhibition - Suicide inhibition - Mixed inhibition Substrate Oxidoreductase EC 1: Aromatase inhibitors - Lipoxygenase inhibitor - Monoamine oxidase inhibitors - COX-2 inhibitor Transferase EC 2: Integrase inhibitor - Protein kinase inhibitors - Reverse transcriptase inhibitors - COMT inhibitors Hydrolase EC 3: Acetylcholinesterase inhibitors - Phosphodiesterase inhibitors - Protease inhibitors ACE inhibitor, Trypsin inhibitor - Histone deacetylase inhibitor Lyase EC 4: Carbonic anhydrase inhibitors Retrieved from http://en..org/wiki/Protease_inhibitor_pharmacology Categories: Antivirals | Antiretroviral drugs | Antiprotozoal agents Views Article Discussion this page History Personal tools Log in / create account Navigation Main page Contents Featured content Current events Random article Search Go Search Interaction Community portal Recent changes Contact Donate to Help Toolbox What links here Related changes Upload file Special pages Printable version Permanent link Cite this page Languages Deutsch Français Bahasa Indonesia This page was last modified on 9 July 2008, at 23:03
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