Why Lopinavir and Hydroxychloroquine do not work on COVID-19
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Lopinavir is a drug against HIV; hydroxychloroquine is used to treat malaria and rheumatism. Until recently, both drugs were regarded as potential agents in the fight against the coronavirus SARS-CoV-2. A research group from the University of Basel and the University Hospital has now discovered that the concentration of the two drugs in the lungs of COVID-19 patients is not sufficient to fight the virus.

The authors included 92 patients in their study. Professor Parham Sendi, who is the co-leader of this study, summarizes the main findings as follows:
- First, lopinavir plasma levels were more than two to threefold higher than typically observed in HIV patients. Hydroxychloroquine levels were with normal range.
- Second, there was a significant correlation between the inflammation marker levels in the blood and lopinavir plasma levels.
- Third, when the inflammation was blocked with the Interleukin-6 inhibitor Tocilizumab, lopinavir plasma levels were significantly lower than the ones in patients without Tozulizumab treatment.

These results clearly indicate that drug metabolism enzymes (cytochrome P450 3A) are inhibited by systemic inflammation. The authors write, "Caution is advised when prescribing CYP3A4 substrates such as Lopinavir/ritonavir or any other drug with a narrow therapeutic index to COVID-19 patients because of the risk of elevated drug levels and related toxicities."

Importantly, from the lopinavir and hydroxychloroquine concentrations in the plasma, the study group calculated the corresponding concentration in the lung compartment—the anatomic site of SARS-CoV-2 infection. The results strongly suggest that it is unlikely that either drug reaches sufficient concentrations to inhibit virus replication in the lung.

Source: https://aac.asm.org/content/early/2020/07/07/AAC.01177-20
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