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Enpatoran

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Identification

Generic Name
Enpatoran
DrugBank Accession Number
DB16501
Background

Enpatoran (M5049) was under investigation in clinical trials for various conditions. It was investigated for systemic lupus erythematosus and cutaneous lupus erythematosus in completed trials (NCT04647708 and NCT05162586) and in a recruiting trial (NCT05540327). Additionally, M5049 was studied for COVID-19 pneumonia in a completed trial with results (NCT04448756) and is currently being recruited for a trial involving participants with dermatomyositis and polymyositis (NCT05650567).

Type
Small Molecule
Groups
Investigational
Structure
3D
Similar Structures
Weight
Average: 320.319
Monoisotopic: 320.124880988
Chemical Formula
C16H15F3N4
Synonyms
  • 5-((3R,5S)-3-AMINO-5-TRIFLUOROMETHYLPIPERIDIN-1-YL)QUINOLINE-8-CARBONITRILE
External IDs
  • M-5049
  • M5049
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Pharmacology

Indication

Not Available

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Pharmacodynamics

Not Available

Mechanism of action

M5049 is a small molecule Toll-like receptor (TLR)7 and TLR8 inhibitor. The drug blocks activation of TLR7/8, thereby stopping immune cell activation, inflammation, and the progression into a cyotkine storm. The drug is currently being investigated against COVID-19.

Absorption

Not Available

Volume of distribution

Not Available

Protein binding

Not Available

Metabolism
Not Available
Route of elimination

Not Available

Half-life

Not Available

Clearance

Not Available

Adverse Effects
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Toxicity

Not Available

Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
Not Available
Food Interactions
Not Available

Categories

Drug Categories
Classification
Not classified
Affected organisms
Not Available

Chemical Identifiers

UNII
7CZ390V26X
CAS number
2101938-42-3
InChI Key
BJXYHBKEQFQVES-NWDGAFQWSA-N
InChI
InChI=1S/C16H15F3N4/c17-16(18,19)11-6-12(21)9-23(8-11)14-4-3-10(7-20)15-13(14)2-1-5-22-15/h1-5,11-12H,6,8-9,21H2/t11-,12+/m0/s1
IUPAC Name
SMILES
N[C@@H]1C[C@@H](CN(C1)C1=CC=C(C#N)C2=C1C=CC=N2)C(F)(F)F

References

General References
  1. Patra R, Chandra Das N, Mukherjee S: Targeting human TLRs to combat COVID-19: A solution? J Med Virol. 2021 Feb;93(2):615-617. doi: 10.1002/jmv.26387. Epub 2020 Aug 13. [Article]
  2. External Link [Link]
ChemSpider
115009403
ChEMBL
CHEMBL4802159
PDBe Ligand
QLH
PDB Entries
6zjz

Clinical Trials

Clinical Trials
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PhaseStatusPurposeConditionsCountStart DateWhy Stopped100+ additional columns
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2Active Not RecruitingTreatmentSystemic Lupus Erythematosus1somestatusstop reasonjust information to hide
2CompletedTreatmentCoronavirus Disease 2019 (COVID‑19)1somestatusstop reasonjust information to hide
2RecruitingTreatmentSystemic Lupus Erythematosus1somestatusstop reasonjust information to hide
1CompletedOtherHealthy Volunteers (HV)2somestatusstop reasonjust information to hide
1CompletedTreatmentHealthy Volunteers (HV)1somestatusstop reasonjust information to hide

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not Available
Dosage Forms
Not Available
Prices
Not Available
Patents
Not Available

Properties

State
Not Available
Experimental Properties
Not Available
Predicted Properties
PropertyValueSource
Predicted ADMET Features
Not Available

Spectra

Mass Spec (NIST)
Not Available
Spectra
Not Available
Chromatographic Properties
Collision Cross Sections (CCS)
Not Available

Drug created at January 21, 2021 02:01 / Updated at July 13, 2024 15:36