Lopinavir (ABT-378) is an antiretroviral of the protease inhibitor class. It is marketed by Abbott as Kaletra®, a co-formulation with a sub-therapeutic dose of ritonavir, as a component of combination therapy to treat HIV/AIDS.

As of 2006, lopinavir/ritonavir forms part of the preferred combination for first-line therapy recommended by the US DHHS.DHHS panel. Guidelines for the use of antiretroviral agents in HIV-1-infected adults and adolescents (May 4, 2006). (Available for download from AIDSInfo) It is available as capsules, tablets and oral solution.

History

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Lopinavir was developed by Abbott in an attempt to improve on the HIV resistance and serum protein-binding properties of the company's earlier protease inhibitor, ritonavir.Sham HL, Kempf DJ, Molla A, et al. (1998) ABT-378, a highly potent inhibitor of the human immunodeficiency virus protease. Antimicrob. Agents Chemother. 42: 3218-24 Administered alone, lopinavir has insufficient bioavailability; however, like several HIV protease inhibitors, its blood levels are greatly increased by low doses of ritonavir, a potent inhibitor of cytochrome P450 3A4. Abbott therefore pursued a strategy of co-administering lopinavir with sub-therapeutic doses of ritonavir, and lopinavir is only marketed as a co-formulation with ritonavir.

Lopinavir/ritonavir was approved by the US FDA on 15 September 2000, and in Europe in April 2001.

Adverse effects

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The most common adverse effects observed with lopinavir/ritonavir are diarrhoea and nausea. In key clinical trials, moderate or severe diarrhoea occurred in up to 27% of patients, and moderate/severe nausea in up to 16%.KALETRA® (lopinavir/ritonavir) capsules; (lopinavir/ritonavir) oral solution. Prescribing information. April 2005 Other common adverse effects include abdominal pain, asthenia, headache, vomiting and, particularly in children, rash.

Raised liver enzymes and hyperlipidemia (both hypertriglyceridemia and hypercholesterolemia) are also commonly observed during lopinavir/ritonavir treatment.

References

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External link

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• Company website

HIV/AIDS | Antivirals