Neovastat

Identification

Generic Name
Neovastat
DrugBank Accession Number
DB05387
Background

Neovastat is a naturally occurring anti-angiogenic compound, extracted from cartilage, with multiple anti-angiogenic mechanisms of action that provide broad therapeutic potential for a number of diseases. It is currently in international Phase III trials for renal cell carcinoma and non-small-cell lung cancer.

Type
Small Molecule
Groups
Investigational
Synonyms
Not Available
External IDs
  • AE 941
  • AE-941
  • AE941

Pharmacology

Indication

Investigated for use/treatment in kidney cancer, lung cancer, macular degeneration, multiple myeloma, prostate cancer, and psoriasis and psoriatic disorders.

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Contraindications & Blackbox Warnings
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Pharmacodynamics

Not Available

Mechanism of action

AE-941(Neovastat) contains a component that specifically prevents the binding of VEGF (Vascular Endothelial Growth Factor) to its receptors. It inhibits gelatinolytic and elastinolytic activities for MMP-2, MMP-9, and MMP-12. The MMP's are often over expressed in tumors and play an important role in the degradation of the matrix that surrounds the cell (extracellular matrix), which allows tumor growth and invasion (metastasis). It also induces apoptosis (programmed cell death) which is an additional Anti angiogenic activity found in Neovastat.

TargetActionsOrganism
U72 kDa type IV collagenaseNot AvailableHumans
UMatrix metalloproteinase-9Not AvailableHumans
UMacrophage metalloelastaseNot 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
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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

Products

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International/Other Brands
Neovastat

Categories

Drug Categories
Classification
Not classified
Affected organisms
Not Available

Chemical Identifiers

UNII
D2YCN1I522
CAS number
Not Available
InChI Key
Not Available
InChI
Not Available
IUPAC Name
Not Available
SMILES
Not Available

References

General References
  1. Lee SY, Chung SM: Neovastat (AE-941) inhibits the airway inflammation via VEGF and HIF-2 alpha suppression. Vascul Pharmacol. 2007 Nov-Dec;47(5-6):313-8. Epub 2007 Sep 18. [Article]
PubChem Substance
347910112
Wikipedia
Shark_cartilage

Clinical Trials

Clinical Trials
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PhaseStatusPurposeConditionsCountStart DateWhy Stopped100+ additional columns
3CompletedTreatmentAdenocarcinoma of the Lung / Adenosquamous Lung Carcinoma / Lung Cancer, Nonsmall Cell, Stage IIIA / Lung Large Cell Carcinoma / Squamous Cell Lung Cancer / Stage IIIB Non-Small Cell Lung Cancer1somestatusstop reasonjust information to hide
3CompletedTreatmentRenal Cancer1somestatusstop reasonjust information to hide
2CompletedTreatmentMultiple Myeloma and Plasma Cell Neoplasm1somestatusstop reasonjust information to hide

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
Chromatographic Properties
Collision Cross Sections (CCS)
Not Available

Targets

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Kind
Protein
Organism
Humans
Pharmacological action
Unknown
General Function
Ubiquitinous metalloproteinase that is involved in diverse functions such as remodeling of the vasculature, angiogenesis, tissue repair, tumor invasion, inflammation, and atherosclerotic plaque rupture. As well as degrading extracellular matrix proteins, can also act on several nonmatrix proteins such as big endothelial 1 and beta-type CGRP promoting vasoconstriction. Also cleaves KISS at a Gly-|-Leu bond. Appears to have a role in myocardial cell death pathways. Contributes to myocardial oxidative stress by regulating the activity of GSK3beta. Cleaves GSK3beta in vitro. Involved in the formation of the fibrovascular tissues in association with MMP14
Specific Function
endopeptidase activity
Gene Name
MMP2
Uniprot ID
P08253
Uniprot Name
72 kDa type IV collagenase
Molecular Weight
73881.695 Da
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
General Function
Matrix metalloproteinase that plays an essential role in local proteolysis of the extracellular matrix and in leukocyte migration (PubMed:12879005, PubMed:1480034, PubMed:2551898). Could play a role in bone osteoclastic resorption (By similarity). Cleaves KiSS1 at a Gly-|-Leu bond (PubMed:12879005). Cleaves NINJ1 to generate the Secreted ninjurin-1 form (PubMed:32883094). Cleaves type IV and type V collagen into large C-terminal three quarter fragments and shorter N-terminal one quarter fragments (PubMed:1480034). Degrades fibronectin but not laminin or Pz-peptide
Specific Function
collagen binding
Gene Name
MMP9
Uniprot ID
P14780
Uniprot Name
Matrix metalloproteinase-9
Molecular Weight
78457.51 Da
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
General Function
May be involved in tissue injury and remodeling. Has significant elastolytic activity. Can accept large and small amino acids at the P1' site, but has a preference for leucine. Aromatic or hydrophobic residues are preferred at the P1 site, with small hydrophobic residues (preferably alanine) occupying P3
Specific Function
calcium ion binding
Gene Name
MMP12
Uniprot ID
P39900
Uniprot Name
Macrophage metalloelastase
Molecular Weight
54001.175 Da

Drug created at November 18, 2007 18:24 / Updated at July 18, 2023 22:56