This drug entry is a stub and has not been fully annotated. It is scheduled to be annotated soon.
Identification
- Generic Name
- Endostatin
- DrugBank Accession Number
- DB06423
- Background
Not Available
- Type
- Biotech
- Groups
- Investigational
- Biologic Classification
- Protein Based Therapies
Other protein based therapies - Protein Chemical Formula
- Not Available
- Protein Average Weight
- Not Available
- Sequences
- Not Available
- Synonyms
- Endostatins
- Recombinant human endostatin
- External IDs
- YH 16
- YH-16
Pharmacology
- Indication
Investigated for use/treatment in cancer/tumors (unspecified), macular degeneration, and diabetic retinopathy.
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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.
Target Actions Organism U72 kDa type IV collagenase Not Available Humans UMatrix metalloproteinase-9 Not Available Humans UCollagenase 3 Not Available Humans UFocal adhesion kinase 1 Not Available Humans UE-selectin Not Available Humans - 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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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.
Drug Interaction Integrate drug-drug
interactions in your softwareAlendronic acid The risk or severity of jaw osteonecrosis and anti-angiogenesis can be increased when Endostatin is combined with Alendronic acid. Ambroxol The risk or severity of methemoglobinemia can be increased when Endostatin is combined with Ambroxol. Articaine The risk or severity of methemoglobinemia can be increased when Endostatin is combined with Articaine. Benzocaine The risk or severity of methemoglobinemia can be increased when Endostatin is combined with Benzocaine. Benzyl alcohol The risk or severity of methemoglobinemia can be increased when Endostatin is combined with Benzyl alcohol. Bupivacaine The risk or severity of methemoglobinemia can be increased when Endostatin is combined with Bupivacaine. Butacaine The risk or severity of methemoglobinemia can be increased when Endostatin is combined with Butacaine. Butamben The risk or severity of methemoglobinemia can be increased when Endostatin is combined with Butamben. Capsaicin The risk or severity of methemoglobinemia can be increased when Endostatin is combined with Capsaicin. Chloroprocaine The risk or severity of methemoglobinemia can be increased when Endostatin is combined with Chloroprocaine. 
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- Not Available
Products
Drug product information from 10+ global regionsOur datasets provide approved product information including:dosage, form, labeller, route of administration, and marketing period.Access drug product information from over 10 global regions.- International/Other Brands
- Endostar
Categories
- Drug Categories
- Amino Acids, Peptides, and Proteins
- Angiogenesis Inhibitors
- Angiogenesis Modulating Agents
- Angiogenic Proteins
- Angiostatic Proteins
- Antineoplastic Agents
- Biological Factors
- Collagen
- Collagen Type XVIII
- Compounds used in a research, industrial, or household setting
- Extracellular Matrix Proteins
- Growth Inhibitors
- Growth Substances
- Intercellular Signaling Peptides and Proteins
- Non-Fibrillar Collagens
- Peptides
- Proteins
- Scleroproteins
- Chemical TaxonomyProvided by Classyfire
- 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
- Affected organisms
- Not Available
Chemical Identifiers
- UNII
- 67RHC0R671
- CAS number
- 187888-07-9
References
- General References
- 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. [Article]
- 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. [Article]
- External Links
- Wikipedia
- Endostatin
Clinical Trials
- Clinical Trials
Phase Status Purpose Conditions Count 4 Completed Treatment Non-Small Cell Lung Cancer (NSCLC) 1 4 Not Yet Recruiting Treatment Lung Cancer 1 4 Not Yet Recruiting Treatment Metastatic Malignant Neoplasm to the Leptomeninges 1 4 Recruiting Treatment Squamous Cell Carcinoma of the Lung 1 4 Unknown Status Treatment Adenocarcinoma of the Lung 1 4 Unknown Status Treatment Advanced Lung Squamous Carcinoma 1 4 Unknown Status Treatment Advanced Non-Small Cell Lung Cancer (NSCLC) / NSCLC, Recurrent 1 4 Unknown Status Treatment Non-Small Cell Lung Cancer (NSCLC) 3 4 Unknown Status Treatment Patients With Esophageal Cancer(Ⅱ-Ⅲ) 1 3 Completed Treatment Advanced Non-Small Cell Lung 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
Targets
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- 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
- 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]
- 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
- 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]
- 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
- 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]
- 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
- 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]
- 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
- 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]
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
- 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. [Article]
Drug created at March 19, 2008 16:33 / Updated at January 14, 2023 19:04