Lopinavir

Better Known as: Kaletra

• Marketed By: Abbott Laboratories
  
• Major Indication: Human Immunodeficiency Virus Infection
  
• Drug Class: HIV Protease Inhibitor
• Date of FDA Approval (Patent Expiration): 2000 (2016)
  
• 2007 Sales: $1.1 Billion
• Importance: Forms part of the Lopinavir & Ritonavir first-line therapy for HIV infections. Due to its low bioavilbility, it is sold as a co-formulation with Ritonavir, which is a potent CYP3A4 inhibitor.
• See Pharmaceutical Drugs for more information about other drugs and diseases.

Mechanism of Action

When HIV infects an individuals body, it directs the synthesis of several polyproteins. The maturation of the virus to its infectious form requires that these polyproteins be cleaved to their component proteins by HIV Protease. The subunits of come together to form a catalytic tunnel capable of binding the nascent peptides and cleaving them into their mature form. Within this tunnel lies , which contain the . These catalytic Asp residues carry out the hydrolytic cleavage of the polyprotein. Indinavir to these conserved sequences within the HIV Protease tunnel, preventing the nascent polyproteins from entering. Unable to cleave the nascent proteins into their appropriate form, HIV is unable to mature and proliferate, allowing the patients immune system to fight off the infection more easily.^[1][2]

Drug Resistance

The biggest difficulty with treating HIV is the rapidity at which it mutates and becomes resistant to treatments. To view a comprehensive and interactive analysis of the mutations which confer drug resistance to HIV Protease, See: HIV Protease Inhibitor Resistance Profile

For Pharmacokinetic Data References, See: References