12 Facts About Ritonavir

1.

Ritonavir is a protease inhibitor and is used with other protease inhibitors.

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2.

Ritonavir was patented in 1989 and came into medical use in 1996.

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3.

Ritonavir capsules were approved as a generic medication in the United States in 2020.

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4.

Ritonavir is indicated in combination with other antiretroviral agents for the treatment of HIV-1-infected patients.

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5.

Ritonavir induces CYP1A2 and inhibits the major P450 isoforms 3A4 and 2D6.

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6.

Ritonavir was originally developed as an inhibitor of HIV protease, one of a family of pseudo-C2-symmetric small molecule inhibitors.

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7.

Ritonavir is rarely used for its own antiviral activity but remains widely used as a booster of other protease inhibitors.

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8.

Ritonavir was demonstrated to have an in vitro potency of EC50=0.

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9.

Ritonavir was initially derived from a moderately potent and orally bioavailable small molecule, A-80987.

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10.

Ritonavir serves to slow down metabolism of nirmatrelvir by cytochrome enzymes to maintain higher circulating concentrations of the main drug.

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11.

Ritonavir was originally dispensed as a capsule that did not require refrigeration.

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12.

Ritonavir produced in a solid dispersion by melt-extrusion was found to remain in form I, and was re-introduced commercially in 2010.

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