Ritonavir is an HIV protease inhibitor that interferes with the reproductive cycle of HIV. Although it was initially developed as an independent antiviral agent, it has been shown to possess advantageous properties in combination regimens with low-dose ritonavir and other protease inhibitors. It is now more commonly used as a booster of other protease inhibitors and is available in both liquid formulations and as capsules. While ritonavir is not an active antiviral agent against hepatitis C virus (HCV) infection, it is added in combination therapies indicated for the treatment of HCV infections as a booster. Ritonavir is a potent CYP3A inhibitor that increases peak and trough plasma drug concentrations of other protease inhibitors such as [DB09297] and overall drug exposure. American Association for the Study of Liver Diseases (AASLD) and the Infectious Diseases Society of America (IDSA) guidelines recommend ritonavir-boosted combination therapies as first-line therapy for HCV Genotype 1a/b and 4 treatment-naïve patients with or without cirrhosis. Ritonavir is found in a fixed-dose combination product with [DB09296], [DB09183], and [DB09297] as the FDA-approved product Viekira Pak. First approved in December 2014, Viekira Pak is indicated for the treatment of HCV genotype 1b without cirrhosis or with compensated cirrhosis, and when combined with Ribavirin for the treatment of HCV genotype 1a without cirrhosis or with compensated cirrhosis. Ritonavir is also available as a fixed-dose combination product with [DB09296] and [DB09297] as the FDA- and Health Canada-approved product Technivie. First approved in July 2015, Technivie is indicated in combination with Ribavirin for the treatment of patients with genotype 4 chronic hepatitis C virus (HCV) infection without cirrhosis or with compensated cirrhosis. In Canada, ritonavir is also available as a fixed-dose combination product with [DB09296], [DB09183], and [DB09297] as the Health Canada-approved, commercially available product Holkira Pak. First approved in January 2015, Holkira Pak is indicated for the treatment of HCV genotype 1b with or without cirrhosis, and when combined with Ribavirin for the treatment of HCV genotype 1a with or without cirrhosis. The inclusion of ritonavir can select for HIV-1 protease inhibitor resistance-associated substitutions. Any HCV/HIV-1 co-infected patients treated with ritonavir-containing combination therapies should also be on a suppressive antiretroviral drug regimen to reduce the risk of HIV-1 protease inhibitor drug resistance. Ritonavir is combined with other drugs to treat coronavirus disease 2019 (COVID-19) in patients at risk for progressing into a severe form of the disease, such as [nirmatrelvir].[L40094]
Synonyms
Ritonavir
Ritonavirum
Brand Names
Lopinavir and Ritonavir
Ritonavir film coated
Kaletra
Lopinavir-Ritonavir
Viekira Pak
Viekirax
Ritonavir
Paxlovid
Lopinavir/ritonavir Mylan
Technivie
Norvir Sec
Holkira Pak
Norvir
Viekira XR
Ritonavir Mylan
Lopinavir and ritonavir
Auro-ritonavir
Indication
Ritonavir is indicated in combination with other antiretroviral agents for the treatment of HIV-1 infection.[L3513, L12357, L11163, L13443] In the US, Europe, and Canada, ritonavir, in combination with [nirmatrelvir], is indicated for the treatment of mild-to-moderate coronavirus disease 2019 (COVID-19) in adults who are at high risk for progression to severe COVID-19, including hospitalization or death.[L46586, L39840] In Europe, this therapeutic indication is approved under conditional marketing authorization.[L40089]
Categories
Acids, Acyclic
Agents Causing Muscle Toxicity
Anti-HIV Agents
Anti-Infective Agents
Anti-Retroviral Agents
Antiinfectives for Systemic Use
Antiviral Agents
Antivirals for Systemic Use
Antivirals for treatment of HCV infections
Antivirals used in combination for the treatment of HIV infections
Drug Info/Drug Targets: DrugBank 3.0: a comprehensive resource for 'omics' research on drugs. Knox C, Law V, Jewison
T, Liu P, Ly S, Frolkis A, Pon A, Banco K, Mak C, Neveu V, Djoumbou Y, Eisner R, Guo AC, Wishart DS.
Nucleic Acids Res. 2011 Jan; 39 (Database issue):D1035-41. | PMID:21059682
