Atazanavir
Encyclopedia
Atazanavir, marketed under the trade name Reyataz by Bristol Myers
, (formerly known as BMS-232632) is an antiretroviral drug
of the protease inhibitor
(PI) class. Like other antiretrovirals, it is used to treat infection of human immunodeficiency virus (HIV
).
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Atazanavir is distinguished from other PIs in that it can be given once-daily (rather than requiring multiple doses per day) and has lesser effects on the patient's lipid profile (the amounts of cholesterol
and other fatty substances in the blood). Like other protease inhibitors, it is used only in combination with other HIV medications.
The U.S. Food and Drug Administration
(FDA) approved atazanavir on June 20, 2003. Atazanavir is the first PI approved for once-daily dosing, and also appears to be less likely to cause lipodystrophy
and elevated cholesterol
as side effects. It may also not be cross-resistant with other PIs. When boosted with ritonavir
it is of equivalent potency to lopinavir
for use in salvage therapy in patients with a degree of drug resistance; although boosting with ritonavir reduces the metabolic advantages of atazanavir.
On October 20, 2006, the FDA approved a new formulation of atazanavir (300 mg capsules) to be taken as part of combination drug therapy. This formulation should reduce pill burden, as one 300 mg capsule may replace two 150 mg capsules.
Newer research has been investigating the potential anticancer effects of atazanavir. For example, laboratory studies have found that this drug can inhibit the growth of brain tumor cells in culture.
levels in the blood are normally asymptomatically raised with atazanavir. A single case of torsades de pointes
attributable to atazanavir therapy has been described.
CONTRAINDICATIONS: In April 2009, the FDA issued a warning: Atazanavir should not be used with proton pump inhibitors, such as omeprazole (Prilosec), esomeprazole (Nexium), or rabeprazole (Aciphex). According to the FDA, "A 76% reduction in atazanavir area under the concentration-time curve (AUC) and a 78% reduction in atazanavir trough plasma concentration (Cmin) were observed when REYATAZ/ritonavir [a protease inhibitor, the same class as Azatanavir] 300/100 mg was coadministered with omeprazole 40 mg." In other words, proton pump inhibitors reduce the effects of atazanavir.
For more information, visit: http://www.fda.gov/ForConsumers/ByAudience/ForPatientAdvocates/HIVandAIDSActivities/ucm124940.htm
Bristol-Myers Squibb
Bristol-Myers Squibb , often referred to as BMS, is a pharmaceutical company, headquartered in New York City. The company was formed in 1989, following the merger of its predecessors Bristol-Myers and the Squibb Corporation...
, (formerly known as BMS-232632) is an antiretroviral drug
Antiretroviral drug
Antiretroviral drugs are medications for the treatment of infection by retroviruses, primarily HIV. When several such drugs, typically three or four, are taken in combination, the approach is known as Highly Active Antiretroviral Therapy, or HAART...
of the protease inhibitor
Protease inhibitor (pharmacology)
Protease inhibitors are a class of drugs used to treat or prevent infection by viruses, including HIV and Hepatitis C. PIs prevent viral replication by inhibiting the activity of proteases, e.g.HIV-1 protease, enzymes used by the viruses to cleave nascent proteins for final assembly of new...
(PI) class. Like other antiretrovirals, it is used to treat infection of human immunodeficiency virus (HIV
HIV
Human immunodeficiency virus is a lentivirus that causes acquired immunodeficiency syndrome , a condition in humans in which progressive failure of the immune system allows life-threatening opportunistic infections and cancers to thrive...
).
Cholesterol
Cholesterol is a complex isoprenoid. Specifically, it is a waxy steroid of fat that is produced in the liver or intestines. It is used to produce hormones and cell membranes and is transported in the blood plasma of all mammals. It is an essential structural component of mammalian cell membranes...
and other fatty substances in the blood). Like other protease inhibitors, it is used only in combination with other HIV medications.
The U.S. Food and Drug Administration
Food and Drug Administration
The Food and Drug Administration is an agency of the United States Department of Health and Human Services, one of the United States federal executive departments...
(FDA) approved atazanavir on June 20, 2003. Atazanavir is the first PI approved for once-daily dosing, and also appears to be less likely to cause lipodystrophy
Lipodystrophy
Lipodystrophy is a medical condition characterized by abnormal or degenerative conditions of the body's adipose tissue. A more specific term, lipoatrophy is used when describing the loss of fat from one area...
and elevated cholesterol
Cholesterol
Cholesterol is a complex isoprenoid. Specifically, it is a waxy steroid of fat that is produced in the liver or intestines. It is used to produce hormones and cell membranes and is transported in the blood plasma of all mammals. It is an essential structural component of mammalian cell membranes...
as side effects. It may also not be cross-resistant with other PIs. When boosted with ritonavir
Ritonavir
Ritonavir, with trade name Norvir , is an antiretroviral drug from the protease inhibitor class used to treat HIV infection and AIDS....
it is of equivalent potency to lopinavir
Lopinavir
Lopinavir is an antiretroviral of the protease inhibitor class. It is used as a fixed-dose combination with another protease inhibitor, ritonavir, under the trade names Kaletra and Aluvia ....
for use in salvage therapy in patients with a degree of drug resistance; although boosting with ritonavir reduces the metabolic advantages of atazanavir.
On October 20, 2006, the FDA approved a new formulation of atazanavir (300 mg capsules) to be taken as part of combination drug therapy. This formulation should reduce pill burden, as one 300 mg capsule may replace two 150 mg capsules.
Newer research has been investigating the potential anticancer effects of atazanavir. For example, laboratory studies have found that this drug can inhibit the growth of brain tumor cells in culture.
Therapeutic Efficacy
The efficacy of atazanavir has been assessed in a number of well designed trials in ART-naive and ART-experienced adults.Adverse effects
BilirubinBilirubin
Bilirubin is the yellow breakdown product of normal heme catabolism. Heme is found in hemoglobin, a principal component of red blood cells. Bilirubin is excreted in bile and urine, and elevated levels may indicate certain diseases...
levels in the blood are normally asymptomatically raised with atazanavir. A single case of torsades de pointes
Torsades de pointes
Torsades de pointes, or simply torsades, is a French term that literally means "twisting of the points". It was first described by Dessertenne in 1966 and refers to a specific, rare variety of ventricular tachycardia that exhibits distinct characteristics on the electrocardiogram .- Presentation...
attributable to atazanavir therapy has been described.
CONTRAINDICATIONS: In April 2009, the FDA issued a warning: Atazanavir should not be used with proton pump inhibitors, such as omeprazole (Prilosec), esomeprazole (Nexium), or rabeprazole (Aciphex). According to the FDA, "A 76% reduction in atazanavir area under the concentration-time curve (AUC) and a 78% reduction in atazanavir trough plasma concentration (Cmin) were observed when REYATAZ/ritonavir [a protease inhibitor, the same class as Azatanavir] 300/100 mg was coadministered with omeprazole 40 mg." In other words, proton pump inhibitors reduce the effects of atazanavir.
For more information, visit: http://www.fda.gov/ForConsumers/ByAudience/ForPatientAdvocates/HIVandAIDSActivities/ucm124940.htm