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Darunavir (Prezista) is a drug used to treat HIV infection. It is in the protease inhibitor class. Developed by pharmaceutical company Tibotec, darunavir is named after Arun K. Ghosh, the chemist who discovered the molecule at the University of Illinois in Chicago. It was approved by the Food and Drug Administration (FDA) on June 23, 2006.
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.
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 kaletra. The drug is still costly, at around $9000 for a one year supply.
Additional recommended knowledge
Darunavir showed superiority to lopinavir and other protease inhibitors in the POWER trials. The POWER 1 and POWER 2 are designed for treatment-experienced patients, together with supportive data from the POWER 3 analysis . The patients eligible for these studies had experience with at least one protease inhibitor, one non-nucleoside reverse transcriptase inhibitor (NNRTI) and two nucleoside reverse transcriptase inhibitors (NRTI), and had one or more primary protease inhibitor mutations.
Darunavir also showed superior results to lopinavir in the TITAN trials (pre-planned, secondary endpoint, week 48), which was designed for patients with less advanced HIV disease compared to the POWER trials.
Analysis of 595 treatment-experienced patients being lopinavir/r-naïve, HIV-1 infected adults with a viral load of >1000 HIV-1 RNA copies/mL. Pre-planned secondary endpoint findings include:
Development of resistance also was studied. Findings include:
POWER 1 and POWER 2 trials
A pooled analysis of results from POWER 1 and POWER 2 demonstrated that after 24 weeks:
The efficacy results of POWER 1 and POWER 2 are confirmed by data from a large, non-randomized, open-label analysis known as POWER 3. After 24 weeks:
As other antivirals, DARUNAVIR does not cure HIV infection or AIDS, and does not prevent passing HIV to others.
In studies, DARUNAVIR was generally well tolerated. Mild to moderate rash was seen in 7% of patients. Some patients developed severe rash. In clinical studies, 0.3% of patients discontinued due to rash. The most common moderate to severe side effects associated with DARUNAVIR include diarrhea (2.3%), headache (3.8%), abdominal pain (2.3%), constipation (2.3%), and vomiting (1.5%). Four percent of patients discontinued treatment due to adverse events. People who are allergic to DARUNAVIR or any of its ingredients, or ritonavir (NORVIR) should not take DARUNAVIR.
There were few relevant drug-drug interactions with other medications commonly used in HIV patient populations, such as other antiretroviral medications, proton pump inhibitors, and H2 receptor antagonists. Patients should talk to their healthcare provider about all the medicines they are taking or plan to take, including prescription and nonprescription medicines, vitamins, and herbal supplements.
Before taking DARUNAVIR, patients should tell their healthcare provider if they have any medical conditions, including diabetes, liver problems, hemophilia, or allergy to sulfa medicines and should tell their doctor if they are pregnant or planning to become pregnant, or are nursing. DARUNAVIR should be used with caution in patients with hepatic impairment.
High blood sugar, diabetes or worsening of diabetes, muscle pain, tenderness or weakness, and increased bleeding in people with hemophilia have been reported in patients taking protease inhibitor medicines like DARUNAVIR ™ . Changes in body fat have been seen in some patients taking anti-HIV medicines, including loss of fat from legs, arms and face, increased fat in the abdomen and other internal organs, breast enlargement and fatty lumps on the back of the neck. The cause and long-term health effects of these conditions are not known at this time.
Clinical laboratory safety observed in the DARUNAVIR group was comparable to the control group. (Product Monograph, Darunavir)
Dosing and Administration
The recommended oral dose of DARUNAVIR tablets is 600 mg (two 300 mg tablets) twice daily (BID) taken with ritonavir 100mg BID and with food. The drug can be taken with any type of food.
Additional Studies Involving DARUNAVIR
|This article is licensed under the GNU Free Documentation License. It uses material from the Wikipedia article "Darunavir". A list of authors is available in Wikipedia.|