Darunavir
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 | How Supplied | Labels and Packages
Mechanism of Action
References
- ↑ 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.
- ↑ Rodger D MacArthura, Darunavir: promising initial results, doi:10.1016/S0140-6736(07)60499-1
- ↑ 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.
- ↑ Darunavir-ritonavir more effective than Lopinavir-ritonavir in HIV infected, treatment-experienced patients, The Lancet, 2007, 370,article URL