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Potent Small Molecule Inhibitors for HIV-1 Protease

Summary: The researchers have also developed a new generation of protease inhibitors that are exceedingly potent and maintain potency against multidrug resistant HIV-1 variants. Dr. Ghosh's laboratory has designed, synthesized, and evaluated several different series of compounds. These novel protease inhibitors show potent enzyme inhibitory, antiviral activity, and exceptional broad spectrum activity against highly cross-resistant mutant.

Technology Benefits: Decreased adverse side effectsEffective against multidrug resistant HIV-1 variants Improved bioavailabilitySuperior pharmacokinetic properties

Technology Application: Medical/HealthcarePharmaceuticalsHIV/AIDS TreatmentDrug Development

Detailed Technology Description: Arun GhoshGhosh GroupPurdue Chemistry

Countries: United States

Application No.: None

*Abstract

*Background: Advances in the treatment of HIV/AIDS with HIV-1 protease inhibitors in combination with reverse transcriptase inhibitors, known as highly active antiretroviral therapy (HAART), has resulted in improved life expectancy and significantly reduced HIV/AIDS-related mortality in the developed world. Unfortunately, HAART suffers from adverse drug side effects, poor oral bioavailability, and drug interactions. Also, drug-resistant HIV-1 variants have begun to emerge. Development of antiretroviral therapy with broad-spectrum activity and minimal side effects is needed for current and future HIV/AIDS treatment. Purdue University researchers have developed Darunavir, brand name Prezista, a drug used to treat HIV infection. Prezista was developed by the pharmaceutical company Tibotec and is an OARAC recommended treatment option for treatment-naive and -experienced adults and adolescents. It is also used in patients with drug-resistant HIV.

*IP Issue Date: None

*IP Type: Divisional

*Stage of Development: Concept Developed

*Web Links: Purdue Office of Technology CommercializationPurdueInnovation and EntrepreneurshipArun GhoshGhosh GroupPurdue Chemistry

Country/Region: USA

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