Other substances

Nilotinib

A tyrosine kinase inhibitor.

Phase of research

Potential treatment - pre-clinical evidence

How it helps

Antiviral

Drug status

Used to treat other disease

Supporting references

Contradictory references

AI-suggested references

Clinical trials

General information

Nilotinib stabilizes the kinase domain of the Abl protein in its inactive form, which inhibits the Bcr-Abl-mediated proliferation of certain chronic myeloid leukemia cells. Nilotinib also inhibits tyrosine kinases, that are constitutively active in most gastrointestinal stromal tumours (NCIt). It was shown to have anti-SARS-CoV-2 properties in vitro, which are likely to root from its ability to bind and perturb DDX42 helicase, a host RNA-binding protein predicted to interact with SARS-CoV-2 RNA (Sun et al., 2021).

Nilotinib on DrugBank
Nilotinib on PubChem
Nilotinib on Wikipedia

Marketed as

TASIGNA (NILOTINIB HYDROCHLORIDE)

CC1=C(C=C(C=C1)C(=O)NC2=CC(=CC(=C2)C(F)(F)F)N3C=C(N=C3)C)NC4=NC=CC(=N4)C5=CN=CC=C5

Supporting references

Link	Tested on	Impact factor	Notes	Publication date
Antiviral Drug Screen of Kinase inhibitors Identifies Cellular Signaling Pathways Critical for SARS-CoV-2 Replication Preprint Screening	VERO E6 cell cultures			Jun/25/2020
Identification of Potent and Safe Antiviral Therapeutic Candidates Against SARS-CoV-2 Small molecule In vitro Screening	Vero cells	5.09		Nov/25/2020
Systemic in Silico Screening in Drug Discovery for Coronavirus Disease (COVID-19) with an Online Interactive Web Server	in silico	4.55	Predicted to bind a SARS-CoV-2 protein structural feature.	Aug/11/2020
The tyrosine kinase inhibitor nilotinib inhibits SARS‐CoV‐2 In Vitro Small molecule In vitro	Vero E6 cells; Calu-3 cells	2.65	Inhibits SARS-CoV-2 replication in vitro at EC50 values below the cited mean peak concentration of the drug in patient plasma in 400 mg BID dosing.	Nov/24/2020
In vivo structural characterization of the SARS-CoV-2 RNA genome identifies host proteins vulnerable to repurposed drugs RNA Biophysical assay In vitro Mechanism In silico	in silico; in vitro biophysical assay; Caco-2 cells; Huh7.5.1 cells; Calu-3 cells; A549-ACE2 cells	38.64	Inhibited SARS-CoV-2 infection in Huh7.5.1 cells with low cytotoxicity. Antiviral activity was observed in Caco-2, Calu-3, and A549-ACE2 cells, as well. Its activity is likely to root from its ability to bind and perturb DDX42 helicase, which is a host RNA-binding protein predicted to interact with SARS-CoV-2 RNA.	Feb/09/2021

AI-suggested references

Link	Publication date
Discovery of Potent SARS-CoV-2 Inhibitors from Approved Antiviral Drugs via Docking and Virtual Screening.	Mar/10/2022
Searching for target-specific and multi-targeting organics for Covid-19 in the Drugbank database with a double scoring approach.	Nov/05/2020
A Repurposed Drug Screen Identifies Compounds That Inhibit the Binding of the COVID-19 Spike Protein to ACE2	Sep/01/2020
SARS-CoV-2 and SARS-CoV: Virtual screening of potential inhibitors targeting RNA-dependent RNA polymerase activity (NSP12)	Jul/09/2020
Drug Repurposing to Identify Nilotinib as a Potential SARS-CoV-2 Main Protease Inhibitor: Insights from a Computational and In Vitro Study	Jul/08/2021
In silico identification of available drugs targeting cell surface BiP to disrupt SARS-CoV-2 binding and replication: Drug repurposing approach	Feb/04/2020
The tyrosine kinase inhibitor nilotinib inhibits SARS-CoV-2 in vitro	Dec/04/2020
Small Molecule Therapeutics to Destabilize the ACE2-RBD Complex: a Molecular Dynamics Study	Jan/29/2021
Identification of FDA approved drugs against SARS-CoV-2 RNA dependent RNA polymerase (RdRp) and 3-chymotrypsin-like protease (3CLpro), drug repurposing approach.	Mar/31/2021
Tyrosine Kinase Inhibitors Play an Antiviral Action in Patients Affected by Chronic Myeloid Leukemia: A Possible Model Supporting Their Use in the Fight Against SARS-CoV-2.	Sep/02/2020
Structure-Based Virtual Screening Identifies Multiple Stable Binding Sites at the RecA Domains of SARS-CoV-2 Helicase Enzyme.	Mar/07/2021
Proposition of a new allosteric binding site for potential SARS-CoV-2 3CL protease inhibitors by utilizing molecular dynamics simulations and ensemble docking	Oct/28/2021

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