Antiretrovirals
Protease inhibitors were the second class of antiretroviral drugs developed. In all cases, patents remain in force until 2010 or beyond.
Name | Trade name | Company | Patent | Notes |
Saquinavir | Fortovase, Invirase | Hoffmann–La Roche | U.S. Patent 5,196,438 | It was the first protease inhibitor approved by the FDA (December 6, 1995). |
Ritonavir | Norvir | Abbott Laboratories | U.S. Patent 5,541,206 | - |
Indinavir | Crixivan | Merck & Co. | U.S. Patent 5,413,999 | - |
Nelfinavir | Viracept | Agouron Pharmaceuticals | U.S. Patent 5,484,926 | - |
Amprenavir | Agenerase | GlaxoSmithKline | U.S. Patent 5,585,397 | 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 Production was discontinued by the manufacturer December 31, 2004, as it has been superseded by fosamprenavir. |
Lopinavir | Kaletra | Abbott | - | Is only marketed as a combination, with ritonavir. |
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. |
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. |
Tipranavir | Aptivus | Boehringer-Ingelheim | - | Also known as tipranavir disodium |
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. Several ongoing phase III trials are showing a high efficiency for the PREZISTA/rtv combination being superior to the lopinavir/rtv combination for first-line therapy. Darunavir is the first drug in a long time that didn't come with a price increase. It leapfrogged two other approved drugs of its type, and is matching the price of a third. |
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