Darunavir for the Treatment of SARS-CoV-2

With a solid pharmacological background, deep experience in drug discovery and leading technology platforms, Creative Biolabs has highly qualified for providing comprehensive and efficient as well as economic darunavir inhibitor study services for the treatment of SARS-CoV-2.

Introduction of Darunavir

Darunavir is an oral nonpeptidic HIV-1 protease inhibitor that is used to selectively inhibit the cleavage of HIV polyproteins, thereby preventing viral maturation, proteolytic activity, and HIV-1 replication. Darunavir binds to HIV-1 protease with high affinity, potent antiviral activity against both wild-type and multidrug-resistant HIV-1. The drug is currently valuable used as part of an antiretroviral therapy regimen for HIV-1 infection in treatment-experienced patients with limited therapeutic options.

Recently, two protease inhibitors, lopinavir and ritonavir have been used in clinical for efficacy tests, with results showing some clinical effects. Darunavir designed to target viral proteinases, researchers have processed drug-target interaction (DTI) prediction of antiviral drugs available on markets against SARS-CoV-2 helicase, among darunavir predicted to have a K_d of 90.38 nM against SARS-CoV-2’s helicase. Moreover, the DTI prediction results of anti-viral drugs available against a novel coronavirus (SARS-CoV-2) 3'-to-5' exonuclease show that darunavir has a K_d of 195.73 nM (Beck, 2020). Although there was no current supporting literature found for darunavir to be used as a CoV therapeutic, lopinavir is possible as a potent drug against coronavirus infection in further research.

Fig.1 Screen for potential 2019-nCoV inhibitors from commercial medicines. (Liu, 2020)

Our Service of Darunavir Protease Inhibitor

Creative Biolabs can provide a variety of darunavir protease inhibitor services to help our customers for further researches of the SARS-CoV-2, including but not limited to:

• The catalytic mechanism, the structure, and dynamic behaviors study and antiviral activity assays
• In vitro/in vivo pharmacodynamics studies to assess pharmacodynamics (PD) for therapeutic compounds
• In vitro ADME to evaluate drug absorption, distribution, metabolism, excretion, and toxicology
• In vivo PK studies for all aspects of in vivo pharmacokinetic support
• Prophylactic in vivo efficacy studies to determine if drug regimens could affect virus replication and/or disease progression
• Pharmacology studies and various animal models to describe the effect in response to drug dose
• Toxicity study and safety evaluation for preclinical trial
• Pre-formulation and formulation development, dose prediction and drug abuse tests

With our vast experience and leading technology platforms, experts in Creative Biolabs are pleased to introduce our impeccable service of darunavir protease inhibitors to support drug discovery and development for the treatment of SARS-CoV-2. Please feel free to contact us for more information about drug discovery for SARS-CoV-2.

References

1. Liu, X.; Wang, X. J. Potential inhibitors for 2019-nCoV coronavirus M protease from clinically approved medicines. bioRxiv. 2020.
2. Beck, B. R.; et al. Predicting commercially available antiviral drugs that may act on the novel coronavirus (2019-nCoV), Wuhan, China through a drug-target interaction deep learning model. bioRxiv. 2020.

For Research Use Only. We do not provide direct services or products for patients.