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__NOTOC__
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{{Darunavir}}
{{Darunavir}}
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{{CMG}}; {{AE}} {{AZ}}


==Overview==
==Overview==
''Darunavir''' is a [[drug]] used to treat [[HIV]] infection.  It is in the [[protease inhibitor]] class. PDarunavir 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> Developed by pharmaceutical company [[Tibotec]], darunavir is named after [http://www.chem.purdue.edu/people/faculty/faculty.asp?itemID=76 Arun K. Ghosh], the chemist who discovered the molecule at the [[University of Illinois at Chicago]]. It was approved by the [[Food and Drug Administration]] (FDA) on June 23, 2006.<ref>Rodger D MacArthura, Darunavir: promising initial results, {{doi|10.1016/S0140-6736(07)60499-1}}</ref>
Darunavir is a second-generation protease inhibitor (PIs), designed specifically to overcome problems with the older agents in this class, such as[[indinavir]].  Early PIs often have severe side effects and drug toxicities, require a  high therapeutic dose, are costly to manufacture, and show a disturbing susceptibility to drug resistant mutations. Such mutations can develop in as little as a year of use, and effectively render the drugs useless.
Darunavir was designed to form robust interactions with the [[protease]] enzyme from many strains of HIV, including strains from treatment-experienced patients with multiple resistance mutations to PIs.<ref name="pmid17900913">{{cite journal
| author = Ghosh AK, Dawson ZL, Mitsuya H
| title = Darunavir, a conceptually new HIV-1 protease inhibitor for the treatment of drug-resistant HIV
| journal = Bioorg. Med. Chem.
| volume = 15
| issue = 24
| pages = 7576–80
| year = 2007
| pmid = 17900913
| doi = 10.1016/j.bmc.2007.09.010
| url = http://linkinghub.elsevier.com/retrieve/pii/S0968-0896(07)00783-3
| accessdate = 2007-12-22
| pmc = 2112938
}}</ref><ref>''Darunavir-ritonavir more effective than Lopinavir-ritonavir in HIV infected, treatment-experienced patients'', The Lancet, '''2007''', 370,[http://www.thelancet.com/journals/lancet/issue?volume=370&issue=9581 article URL]</ref>
Darunavir received much attention at the time of its release, as it represents an important treatment option for patients with drug-resistant HIV.  Patient advocacy groups pressured developer Tibotec not to follow the previous trend of releasing new drugs at prices higher than existing drugs in the same class. Darunavir was priced to match other common PIs already in use, such as the [[Fixed-dose combination (antiretroviral)|fixed-dose combination]]drug [[lopinavir/ritonavir]]. <!-- The drug costs around $9,000 for a one year supply.<ref>Liz Highleyman, Patient Advocates Commend Pricing of New PI Darunavir, [http://www.hivandhepatitis.com/recent/2006/ad1/063006_a.html HIV and HCV news]</ref><ref>Darunavir - first molecule to treat drug-resistant HIV, [http://www.news-medical.net/?id=19211 Medical news]</ref><ref>Retaining Efficacy Against Evasive HIV, [http://pubs.acs.org/cen/news/84/i34/8434drugdesign.html Chemical and engineering news]</ref> -->


==Category==
==Category==
Antiretroviral


==US Brand Names==
==US Brand Names==
PREZISTA<sup>®</sup>


==FDA Package Insert==
==FDA Package Insert==
Line 26: Line 51:


==Mechanism of Action==
==Mechanism of Action==
[[Darunavir (patient information)]]


==References==
==References==

Revision as of 16:01, 31 December 2013

Darunavir
PREZISTA® FDA Package Insert
Description
Clinical Pharmacology
Microbiology
Indications and Usage
Contraindications
Warnings and Precautions
Adverse Reactions
Overdosage
Clinical Studies
Dosage and Administration
How Supplied
Labels and Packages

Editor-In-Chief: C. Michael Gibson, M.S., M.D. [1]; Associate Editor(s)-in-Chief: Ahmed Zaghw, M.D. [2]

Overview

Darunavir' is a drug used to treat HIV infection. It is in the protease inhibitor class. PDarunavir is an OARAC recommended treatment option for treatment-naïve and treatment-experienced adults and adolescents.[1] Developed by pharmaceutical company Tibotec, darunavir is named after Arun K. Ghosh, the chemist who discovered the molecule at the University of Illinois at Chicago. It was approved by the Food and Drug Administration (FDA) on June 23, 2006.[2]

Darunavir is a second-generation protease inhibitor (PIs), designed specifically to overcome problems with the older agents in this class, such asindinavir. Early PIs often have severe side effects and drug toxicities, require a high therapeutic dose, are costly to manufacture, and show a disturbing susceptibility to drug resistant mutations. Such mutations can develop in as little as a year of use, and effectively render the drugs useless.

Darunavir was designed to form robust interactions with the protease enzyme from many strains of HIV, including strains from treatment-experienced patients with multiple resistance mutations to PIs.[3][4]

Darunavir received much attention at the time of its release, as it represents an important treatment option for patients with drug-resistant HIV. Patient advocacy groups pressured developer Tibotec not to follow the previous trend of releasing new drugs at prices higher than existing drugs in the same class. Darunavir was priced to match other common PIs already in use, such as the fixed-dose combinationdrug lopinavir/ritonavir.

Category

Antiretroviral

US Brand Names

PREZISTA®

FDA Package Insert

Description | Clinical Pharmacology | Microbiology | Indications and Usage | Contraindications | Warnings and Precautions | Adverse Reactions | Overdosage | Clinical Studies | Dosage and Administration | Compatibility, Reconstitution, and Stability | Directions For Use | How Supplied | Labels and Packages

Mechanism of Action

References

  1. 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).full guidelines.
  2. Rodger D MacArthura, Darunavir: promising initial results, doi:10.1016/S0140-6736(07)60499-1
  3. Ghosh AK, Dawson ZL, Mitsuya H (2007). "Darunavir, a conceptually new HIV-1 protease inhibitor for the treatment of drug-resistant HIV". Bioorg. Med. Chem. 15 (24): 7576–80. doi:10.1016/j.bmc.2007.09.010. PMC 2112938. PMID 17900913. Retrieved 2007-12-22.
  4. Darunavir-ritonavir more effective than Lopinavir-ritonavir in HIV infected, treatment-experienced patients, The Lancet, 2007, 370,article URL