This drug entry is a stub and has not been fully annotated. It is scheduled to be annotated soon.

Identification

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Name
Endostatin
Accession Number
DB06423
Type
Biotech
Groups
Investigational
Biologic Classification
Protein Based Therapies
Other protein based therapies
Description
Not Available
Protein chemical formula
Not Available
Protein average weight
Not Available
Sequences
Not Available
Synonyms
  • Endostatins
  • Recombinant human endostatin
External IDs
YH 16 / YH-16
International/Other Brands
Endostar
Categories
UNII
67RHC0R671
CAS number
187888-07-9

Pharmacology

Indication

Investigated for use/treatment in cancer/tumors (unspecified), macular degeneration, and diabetic retinopathy.

Pharmacodynamics
Not Available
Mechanism of action

Endostatin is an endogenous antitumor protein. Endostatin is a 20-kDa C-terminal fragment derived from type XVIII collagen which inhibits cell proliferation and migration, and induces endothelial cell apoptosis and cell cycle arrest. It is proposed that endostatin's effects are due to inhibition of vascular endothelial growth factor (VEGF) tyrosine phosphorylation of KDR/F1k-1 (VEGF receptor 2), the cell surface receptor for VEGF. VEGF is an important mediator of angiogensis. Endostatin additionally blocks activation of extracellular signal related kinases, or ERK, protein 38 mitogen activated protein kinase, or p38 MAPK (signal transduction pathways involving kinases that couple growth factors to cell surface receptors), as well as focal adhesion kinase (p125FAK). Studies are being done to determine if endostatin has possible impact on other pathways, and may also target E-selectin and block activity of metalloproteinases 2, 9 and 13. There is further research into a possible mechanistic link involving endostatin's angiogenic and zinc binding ability.

TargetActionsOrganism
U72 kDa type IV collagenaseNot AvailableHumans
UMatrix metalloproteinase-9Not AvailableHumans
UCollagenase 3Not AvailableHumans
UFocal adhesion kinase 1Not AvailableHumans
UE-selectinNot 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
Toxicity
Not Available
Affected organisms
Not Available
Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
DrugInteraction
Alendronic acidThe risk or severity of jaw osteonecrosis and anti-angiogenesis can be increased when Endostatin is combined with Alendronic acid.
Clodronic acidThe risk or severity of jaw osteonecrosis and anti-angiogenesis can be increased when Endostatin is combined with Clodronic acid.
Etidronic acidThe risk or severity of jaw osteonecrosis and anti-angiogenesis can be increased when Endostatin is combined with Etidronic acid.
IbandronateThe risk or severity of jaw osteonecrosis and anti-angiogenesis can be increased when Endostatin is combined with Ibandronate.
Incadronic acidThe risk or severity of jaw osteonecrosis and anti-angiogenesis can be increased when Endostatin is combined with Incadronic acid.
Pamidronic acidThe risk or severity of jaw osteonecrosis and anti-angiogenesis can be increased when Endostatin is combined with Pamidronic acid.
Risedronic acidThe risk or severity of jaw osteonecrosis and anti-angiogenesis can be increased when Endostatin is combined with Risedronic acid.
Tiludronic acidThe risk or severity of jaw osteonecrosis and anti-angiogenesis can be increased when Endostatin is combined with Tiludronic acid.
Zoledronic acidThe risk or severity of jaw osteonecrosis and anti-angiogenesis can be increased when Endostatin is combined with Zoledronic acid.
Additional Data Available
  • Extended Description
    Extended Description

    Extended description of the mechanism of action and particular properties of each drug interaction.

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  • Severity
    Severity

    A severity rating for each drug interaction, from minor to major.

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  • Evidence Level
    Evidence Level

    A rating for the strength of the evidence supporting each drug interaction.

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  • Action
    Action

    An effect category for each drug interaction. Know how this interaction affects the subject drug.

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Food Interactions
Not Available

References

General References
  1. Folkman J: Antiangiogenesis in cancer therapy--endostatin and its mechanisms of action. Exp Cell Res. 2006 Mar 10;312(5):594-607. Epub 2005 Dec 22. [PubMed:16376330]
  2. Ling Y, Yang Y, Lu N, You QD, Wang S, Gao Y, Chen Y, Guo QL: Endostar, a novel recombinant human endostatin, exerts antiangiogenic effect via blocking VEGF-induced tyrosine phosphorylation of KDR/Flk-1 of endothelial cells. Biochem Biophys Res Commun. 2007 Sep 14;361(1):79-84. Epub 2007 Jul 10. [PubMed:17644065]
External Links
Wikipedia
Endostatin

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
1CompletedTreatmentUnspecified Adult Solid Tumor, Protocol Specific2
1, 2CompletedTreatmentStage III Non-small-Cell Lung Cancer1
2CompletedTreatmentNeurofibromatosis Type 2 / Vestibular Schwannomas1
2Not Yet RecruitingTreatmentNasopharyngeal Carcinoma1
2RecruitingTreatmentAdvanced Melanoma1
2RecruitingTreatmentEndostatin / Esophageal Cancers1
2RecruitingTreatmentHepatocellular,Carcinoma1
2RecruitingTreatmentNeoplasms, Breast1
2Unknown StatusTreatmentLiver Metastasis / Lung Cancer Non-Small Cell Cancer (NSCLC) / Malignant Neoplasm of Nasopharynx1
2Unknown StatusTreatmentLung Cancer Non-Small Cell Cancer (NSCLC)2
2Unknown StatusTreatmentNasopharyngeal Carcinoma1
2Unknown StatusTreatmentT Cell Lymphomas1
3Not Yet RecruitingTreatmentCancer, Advanced / Lung Cancer Non-Small Cell Cancer (NSCLC)1
3RecruitingTreatmentNeoplasms, Head and Neck1
3Unknown StatusTreatmentCancer, Breast1
4CompletedTreatmentLung Cancer Non-Small Cell Cancer (NSCLC)1

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not Available
Dosage forms
Not Available
Prices
Not Available
Patents
Not Available

Properties

State
Solid
Experimental Properties
Not Available

Taxonomy

Description
Not Available
Kingdom
Organic Compounds
Super Class
Organic Acids
Class
Carboxylic Acids and Derivatives
Sub Class
Amino Acids, Peptides, and Analogues
Direct Parent
Peptides
Alternative Parents
Not Available
Substituents
Not Available
Molecular Framework
Not Available
External Descriptors
Not Available

Targets

Kind
Protein
Organism
Humans
Pharmacological action
Unknown
General Function
Zinc ion binding
Specific Function
Ubiquitinous metalloproteinase that is involved in diverse functions such as remodeling of the vasculature, angiogenesis, tissue repair, tumor invasion, inflammation, and atherosclerotic plaque rup...
Gene Name
MMP2
Uniprot ID
P08253
Uniprot Name
72 kDa type IV collagenase
Molecular Weight
73881.695 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. [PubMed:10592235]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
General Function
Zinc ion binding
Specific Function
May play an essential role in local proteolysis of the extracellular matrix and in leukocyte migration. Could play a role in bone osteoclastic resorption. Cleaves KiSS1 at a Gly-|-Leu bond. Cleaves...
Gene Name
MMP9
Uniprot ID
P14780
Uniprot Name
Matrix metalloproteinase-9
Molecular Weight
78457.51 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. [PubMed:10592235]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
General Function
Zinc ion binding
Specific Function
Plays a role in the degradation of extracellular matrix proteins including fibrillar collagen, fibronectin, TNC and ACAN. Cleaves triple helical collagens, including type I, type II and type III co...
Gene Name
MMP13
Uniprot ID
P45452
Uniprot Name
Collagenase 3
Molecular Weight
53819.32 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. [PubMed:10592235]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
General Function
Signal transducer activity
Specific Function
Non-receptor protein-tyrosine kinase that plays an essential role in regulating cell migration, adhesion, spreading, reorganization of the actin cytoskeleton, formation and disassembly of focal adh...
Gene Name
PTK2
Uniprot ID
Q05397
Uniprot Name
Focal adhesion kinase 1
Molecular Weight
119232.025 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. [PubMed:10592235]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
General Function
Transmembrane signaling receptor activity
Specific Function
Cell-surface glycoprotein having a role in immunoadhesion. Mediates in the adhesion of blood neutrophils in cytokine-activated endothelium through interaction with PSGL1/SELPLG. May have a role in ...
Gene Name
SELE
Uniprot ID
P16581
Uniprot Name
E-selectin
Molecular Weight
66654.575 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. [PubMed:10592235]

Enzymes

Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
Oxygen binding
Specific Function
Catalyzes the formation of aromatic C18 estrogens from C19 androgens.
Gene Name
CYP19A1
Uniprot ID
P11511
Uniprot Name
Aromatase
Molecular Weight
57882.48 Da
References
  1. Holmes CE, Huang JC, Pace TR, Howard AB, Muss HB: Tamoxifen and aromatase inhibitors differentially affect vascular endothelial growth factor and endostatin levels in women with breast cancer. Clin Cancer Res. 2008 May 15;14(10):3070-6. doi: 10.1158/1078-0432.CCR-07-4640. [PubMed:18483373]

Drug created on March 19, 2008 10:33 / Updated on June 04, 2019 06:23