Darunavir | HIV-1 protease inhibitor

Darunavir (206361-99-1) is a very potent (IC₅₀ = 3 nM against lab HIV-1 strains and clinical isolates) HIV-1 protease inhibitor that is in clinical use.^1,2 Also potent against multi-PI-resistant HIV-1 strains from patient samples.  Darunavir has been investigated as a potential anti-SARS-CoV2 therapeutic with mixed results.^3-6

References:

1. Koh et al. (2003), Novel bis-tetrahydrofuranylurethane-containing nonpeptidic protease inhibitor (PI UIC-94017 (YMC114) with potent activity against multi-PI-resistant human immunodeficiency virus in vitro; Antimicrob. Agents Chemother., 47 2123
2. Surleraux et al. (2005), Discovery and selection of TMC114, a next generation HIV-1 protease inhibitor; J. Med. Chem., 48 1813
3. Beck et al. (2020), Predicting commercially available antiviral drugs that may act on the novel coronavirus (SARS-CoV-2) through a drug-target interaction deep learning model; Comput. Struct. Biotechnol. J, 18 784
4. Khan et al. (2020), Identification of chymotrypsin-like protease inhibitors of SARS-VCoV-2 via integrated computational approach; J. Biomol.Struct. Dyn., 39 2607
5. De Meyers et al. (2020), Lack of antiviral activity of darunavir against SARS-CoV-2; J. Infect. Dis, 97 7
6. Kim et al. (2020), Use of Darunavir-Cobicistat as a Treatment Option for Critically Ill Patients with SARS-CoV-2 Infection; Yonsei Med. J., 61 826