Identification

Generic Name
MB07811
DrugBank Accession Number
DB05192
Background

MB07811 is the first of a novel class of product candidates discovered by Metabasis designed to lower serum cholesterol and triglycerides. MB07811, a small molecule that is administered orally, has been extensively studied preclinically and is currently undergoing clinical testing. MB07811 combines a novel thyroid hormone receptor agonist with the Company's novel HepDirect liver targeting prodrug technology. The combination of selectivity for the beta form of the receptor, liver targeting and other structural characteristics that limit extra-hepatic activity is designed to provide significant efficacy while avoiding side effects associated with activation of thyroid hormone receptors outside the liver.

Type
Small Molecule
Groups
Investigational
Synonyms
Not Available

Pharmacology

Indication

Investigated for use/treatment in hyperlipidemia.

Pharmacology
Reduce drug development failure rates
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Contraindications & Blackbox Warnings
Contraindications
Avoid life-threatening adverse drug events
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Pharmacodynamics

MB07811's TR beta receptor selectivity and liver targeting could harness the efficacy of the approach, while avoiding extra-hepatic activation of TR alpha and TR beta receptors that may lead to therapy limiting side effects. These benefits may include: reduction of LDL and total cholesterol, Reduced liver and serum triglycerides, reduced Lp(a) and enhanced clearance of liver fat.

Mechanism of action

Studies indicate that targeting TR agonists to the liver has the potential to lower both LDL-cholesterol (the "bad" cholesterol) and both hepatic and plasma triglyceride levels.

TargetActionsOrganism
UThyroid hormone receptor betaNot AvailableHumans
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
Adverseeffects
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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
Not Available
CAS number
Not Available
InChI Key
Not Available
InChI
Not Available
IUPAC Name
Not Available
SMILES
Not Available

References

General References
  1. Erion MD, Cable EE, Ito BR, Jiang H, Fujitaki JM, Finn PD, Zhang BH, Hou J, Boyer SH, van Poelje PD, Linemeyer DL: Targeting thyroid hormone receptor-beta agonists to the liver reduces cholesterol and triglycerides and improves the therapeutic index. Proc Natl Acad Sci U S A. 2007 Sep 25;104(39):15490-5. Epub 2007 Sep 18. [Article]
PubChem Substance
347910014

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
2WithdrawnTreatmentHigh Cholesterol1

Pharmacoeconomics

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

Properties

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

Spectra

Mass Spec (NIST)
Not Available
Spectra
Not Available

Targets

Drugtargets2
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Kind
Protein
Organism
Humans
Pharmacological action
Unknown
General Function
Zinc ion binding
Specific Function
Nuclear hormone receptor that can act as a repressor or activator of transcription. High affinity receptor for thyroid hormones, including triiodothyronine and thyroxine.
Gene Name
THRB
Uniprot ID
P10828
Uniprot Name
Thyroid hormone receptor beta
Molecular Weight
52787.16 Da
References
  1. Berman HM, Westbrook J, Feng Z, Gilliland G, Bhat TN, Weissig H, Shindyalov IN, Bourne PE: The Protein Data Bank. Nucleic Acids Res. 2000 Jan 1;28(1):235-42. [Article]

Drug created at October 21, 2007 22:24 / Updated at June 12, 2020 16:52