Retroviral Integrase: Difference between revisions

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==Mechanism for strand-transfer inhibition action==

==Antiretrovirals==

{| class="wikitable"

| '''Name''' || '''Trade name''' || '''Company''' || '''Patent''' || '''Notes'''

|-

| [[Atazanavir]] || Reyataz || [[Bristol-Myers Squibb]] || - || The FDA approved it on June 20, 2003. Atazanavir was the first PI approved for once-daily dosing. It appears to be less likely to cause lipodystrophy and elevated cholesterol as side effects. It may also not be cross-resistant with other PIs.

|-

| [[Amprenavir]] || Agenerase || [[GlaxoSmithKline]] || {{US patent|5585397}} || 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 1,200 mg, delivered in eight very large gel capsules. Production was discontinued by the manufacturer December 31, 2004, as it has been superseded by fosamprenavir.

|-

| [[Darunavir]] || Prezista || [[Tibotec]] || - || It was approved by the [[Food and Drug Administration]] (FDA) on June 23, 2006. Prezista is an [[OARAC]] recommended treatment option for treatment-naïve and treatment-experienced adults and adolescents<ref name="oarac">Guidelines for the Use of Antiretroviral Agents in HIV-1-Infected Adults and Adolescents, November 3, 2008, Developed by the DHHS Panel on Antiretroviral Guidelines for Adults and Adolescents – A Working Group of the Office of AIDS Research Advisory Council (OARAC). [http://www.aidsinfo.nih.gov/ContentFiles/AdultandAdolescentGL.pdf full guidelines].</ref>. Several ongoing [[Clinical trial#Phase III|phase III]] trials are showing a high efficiency for the PREZISTA/[[ritonavir|rtv]] combination being superior to the [[lopinavir]]/[[ritonavir|rtv]] combination for first-line therapy.<ref>{{cite journal |author=Madruga JV, Berger D, McMurchie M, ''et al.'' |title=Efficacy and safety of darunavir-ritonavir compared with that of lopinavir-ritonavir at 48 weeks in treatment-experienced, HIV-infected patients in TITAN: a randomised controlled phase III trial |journal=Lancet |volume=370 |issue=9581 |pages=49–58 |year=2007 |month=Jul |pmid=17617272 |doi=10.1016/S0140-6736(07)61049-6 |url=}}</ref> Darunavir is the first drug in a long time that didn't come with a price increase. It [[leapfrogging|leapfrogged]] two other approved drugs of its type, and is matching the price of a third.<ref>Liz Highleyman, Patient Advocates Commend Pricing of New PI Darunavir, http://www.hivandhepatitis.com/recent/2006/ad1/063006_a.html</ref><ref>[Darunavir - first molecule to treat drug-resistant HIV, http://www.news-medical.net/?id=19211]</ref><ref>{{cite journal |author=Borman S |title=Retaining Efficacy Against Evasive HIV: Darunavir analog to AIDS-virus shapeshifters: Resistance may be futile |journal=Chemical & Engineering News |volume=84 |issue=34 |pages=9 |year=2006 |url=http://pubs.acs.org/cen/news/84/i34/8434drugdesign.html }}</ref>

|}

|-

| [[Fosamprenavir]]|| Lexiva, Telzir || [[GlaxoSmithKline]] || - || Is a [[prodrug]] 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.

|-

| [[Indinavir]] || Crixivan || [[Merck & Co.]] || {{US patent|5413999}} || -

|-

| [[Lopinavir]] || Kaletra || [[Abbott Laboratories|Abbott]] || - || Is only marketed as a combination, with [[ritonavir]].

|-

| [[Nelfinavir]] || Viracept || [[Agouron Pharmaceuticals]] || {{US patent|5484926}} || -

|-

| [[Ritonavir]] || Norvir || [[Abbott Laboratories]] || {{US patent|5541206}} || -

|-

| [[Saquinavir]] || Fortovase, Invirase || [[Hoffmann–La Roche]] || {{US patent|5196438}} || It was the first protease inhibitor approved by the [[Food and Drug Administration|FDA]] (December 6, 1995).

|-

| [[Tipranavir]] || Aptivus || [[Boehringer-Ingelheim]] || - || Also known as tipranavir disodium

|-

==References==

Retroviral Integrase: Difference between revisions

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@@ Line 21: / Line 21: @@
 ==Mechanism for strand-transfer inhibition action==
+==Antiretrovirals==
+{| class="wikitable"
+| '''Name''' || '''Trade name''' || '''Company''' || '''Patent''' || '''Notes'''
+ |-
+ | [[Atazanavir]]  || Reyataz  || [[Bristol-Myers Squibb]] || - || The FDA approved it on June 20, 2003. Atazanavir was the first PI approved for once-daily dosing. It appears to be less likely to cause lipodystrophy and elevated cholesterol as side effects. It may also not be cross-resistant with other PIs.
+ |-
+ | [[Amprenavir]]  || Agenerase  || [[GlaxoSmithKline]] || {{US patent|5585397}} || 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 1,200&nbsp;mg, delivered in eight very large gel capsules. Production was discontinued by the manufacturer December 31, 2004, as it has been superseded by fosamprenavir.
+ |-
+| [[Darunavir]]  || Prezista  || [[Tibotec]] || - ||  It was approved by the [[Food and Drug Administration]] (FDA) on June 23, 2006. Prezista is an [[OARAC]] recommended treatment option for treatment-naïve and  treatment-experienced adults and adolescents<ref name="oarac">Guidelines for the Use of Antiretroviral Agents in HIV-1-Infected Adults and Adolescents, November 3, 2008, Developed by the DHHS Panel on Antiretroviral Guidelines for Adults and Adolescents – A Working Group of the Office of AIDS Research Advisory Council (OARAC). [http://www.aidsinfo.nih.gov/ContentFiles/AdultandAdolescentGL.pdf full guidelines].</ref>. Several ongoing [[Clinical trial#Phase III|phase III]] trials are showing a high efficiency for the PREZISTA/[[ritonavir|rtv]] combination being superior to the [[lopinavir]]/[[ritonavir|rtv]] combination for first-line therapy.<ref>{{cite journal |author=Madruga JV, Berger D, McMurchie M, ''et al.'' |title=Efficacy and safety of darunavir-ritonavir compared with that of lopinavir-ritonavir at 48 weeks in treatment-experienced, HIV-infected patients in TITAN: a randomised controlled phase III trial |journal=Lancet |volume=370 |issue=9581 |pages=49–58 |year=2007 |month=Jul |pmid=17617272 |doi=10.1016/S0140-6736(07)61049-6 |url=}}</ref> Darunavir is the first drug in a long time that didn't come with a price increase. It  [[leapfrogging|leapfrogged]] two other approved drugs of its type, and is matching the price of a third.<ref>Liz Highleyman, Patient Advocates Commend Pricing of New PI Darunavir, http://www.hivandhepatitis.com/recent/2006/ad1/063006_a.html</ref><ref>[Darunavir - first molecule to treat drug-resistant HIV, http://www.news-medical.net/?id=19211]</ref><ref>{{cite journal |author=Borman S |title=Retaining Efficacy Against Evasive HIV: Darunavir analog to AIDS-virus shapeshifters: Resistance may be futile |journal=Chemical & Engineering News |volume=84 |issue=34 |pages=9 |year=2006 |url=http://pubs.acs.org/cen/news/84/i34/8434drugdesign.html }}</ref>
+|}
+ |-
+ |  [[Fosamprenavir]]|| Lexiva, Telzir || [[GlaxoSmithKline]] || - || Is a [[prodrug]] 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.
+ |-
+ | [[Indinavir]]  || Crixivan  || [[Merck & Co.]] || {{US patent|5413999}} || -
+ |-
+ | [[Lopinavir]]  || Kaletra || [[Abbott Laboratories|Abbott]] || - || Is only marketed as a combination, with [[ritonavir]].
+ |-
+ | [[Nelfinavir]]  || Viracept  || [[Agouron Pharmaceuticals]] || {{US patent|5484926}} || -
+ |-
+ | [[Ritonavir]] || Norvir || [[Abbott Laboratories]] || {{US patent|5541206}} || -
+ |-
+ | [[Saquinavir]]  || Fortovase, Invirase || [[Hoffmann–La Roche]] || {{US patent|5196438}} || It was the first protease inhibitor approved by the [[Food and Drug Administration|FDA]] (December 6, 1995).
+ |-
+ | [[Tipranavir]]  || Aptivus  || [[Boehringer-Ingelheim]] || - || Also known as tipranavir disodium
+ |-
 ==References==