Endostatin
Also known as: COL18A1 C-terminal fragment, Collagen XVIII fragment, Endostar, Endostatin, rh-Endostatin, YH-16
Source Endostatin at Peptiology
Save 10% with code PEPTI-BOSSRABBIT-10
Affiliate link: we earn a commission on purchases made through this link, at no extra cost to you.
Tapping Shop Now & Save 10% copies your 10% off code PEPTI-BOSSRABBIT-10 to your clipboard. Paste it at the Peptiology checkout to claim the discount.
Summary
Endostatin is a naturally occurring, collagen‑derived peptide that acts as an endogenous inhibitor of angiogenesis. It is investigated primarily as an anti‑angiogenic agent for cancer, ocular neovascular disorders, and obesity‑related vascular changes. The compound is not approved for therapeutic use and is employed in research settings via intravenous or subcutaneous administration of recombinant protein or labelled variants.
Mechanism of Action
Endostatin interferes with endothelial cell proliferation and new‑vessel formation by binding to specific endostatin receptors on endothelial cells, thereby antagonising pro‑angiogenic signals such as VEGF and basic fibroblast growth factor. This interaction reduces endothelial migration, tube formation, and matrix degradation, leading to suppression of angiogenesis in tumours and other tissues.
What the Research Shows
Preclinical studies have labelled endostatin with radionuclides (99mTc‑EC‑endostatin) or near‑infrared dyes (Cy5.5‑endostatin) to image receptor density in tumour‑bearing rodents, demonstrating its utility as a molecular imaging probe for angiogenesis. Review articles cite endostatin among anti‑angiogenic molecules that maintain corneal avascularity and propose its use to counteract obesity‑driven vascular expansion. No human clinical trials are reported; the evidence is limited to animal models, imaging feasibility studies, and conceptual reviews of its anti‑angiogenic role.
Reported Benefits
Animal experiments suggest endostatin can inhibit tumour‑associated angiogenesis, potentially slowing cancer growth. Imaging studies indicate it may serve as a tracer to identify patients who could benefit from anti‑angiogenic therapy. Reviews propose that endostatin, together with other angiostatic agents, could mitigate pathological neovascularisation in the eye and limit adipose‑tissue vascularisation linked to obesity.
Limitations of the Evidence
All reported data are preclinical; no human efficacy or safety trials have been published. The imaging studies focus on tracer development rather than therapeutic outcomes. The precise receptor mechanisms and optimal dosing regimens remain undefined, and the translational relevance of animal findings to clinical practice is uncertain.
Safety Considerations
No adverse‑event information is provided in the cited literature. Because endostatin has only been studied in animals and in vitro, its safety profile in humans is unknown. Potential immunogenicity, off‑target effects, or vascular complications have not been documented, underscoring the need for formal toxicology and clinical safety assessments before therapeutic use.
How It Is Administered
In research protocols, endostatin is administered intravenously or subcutaneously as a recombinant protein. Formulations may include radiolabelled (99mTc) or fluorescent (Cy5.5) conjugates for imaging purposes. Dosing schedules, concentrations, and vehicle composition vary across studies and are not standardized.
Routes of Administration
Goals & Uses
- Ocular neovascularization (wet AMD)OphthalmologyLow
- Cancer therapyOncologyModerate
- Colorectal cancer treatmentOncologyLow
- Non-small cell lung cancer treatmentOncologyModerate
- Breast cancer treatmentOncologyLow
- Anti‑angiogenic researchResearchHigh
- Anti-tumor angiogenesis inhibitionOncologyModerate
Contraindications
- Active hemorrhage or coagulopathyHematologicModerate
- Severe hepatic impairmentOrganModerateLiver function concerns
- PregnancyPopulationHighPotential fetal risk or insufficient safety data
- Hypersensitivity to endostatin or excipientsAllergy / ImmunologyHigh
Adverse Effects
- Nausea / VomitingGastrointestinalUncommon
- HypertensionCardiovascularUncommonHigh blood pressure
- Injection site reactionsLocalCommon
- HypotensionCardiovascularUnknownLow blood pressure
- FatigueGeneralUnknownLow energy or tiredness
- Elevated liver enzymes (transaminases)HepaticUncommon
- ThromboembolismCardiovascularRare
Drug Interactions
- Other anti-angiogenic agents (bevacizumab, sunitinib)Moderate
- Anticoagulants (warfarin, heparin)Moderate
- Vinorelbine / Cisplatin (NP regimen)Moderate
Population Constraints
- Pediatric patientsAgeRelative
- Breastfeeding womenReproductiveRelative
- Patients with active bleeding disordersHematologicRelative
- Pregnant womenReproductiveAbsolute
Regulatory Status
- European UnionUnapprovedNo EMA marketing authorization.
- United StatesUnapprovedInvestigational only; no FDA approval.
- United KingdomUnapprovedNot licensed by MHRA.
Not approved for clinical use in any major jurisdiction; investigated in pre‑clinical and early‑phase clinical trials.
Evidence & Sources
- Journal ArticleModerateLeung K2004-01-01T00:00:00.000000Z
- Journal ArticleModerateChang JH, et al.2001-01-01T00:00:00.000000Z
- Journal ArticleModerateNijhawans P, Behl T, Bhardwaj S2020-01-01T00:00:00.000000Z
- Journal ArticleModerateLeung K2004-01-01T00:00:00.000000Z
- Journal ArticleModerateLeung K2004-01-01T00:00:00.000000Z
Frequently Asked Questions
What is the primary biological role of endostatin?
Endostatin is an endogenous inhibitor of angiogenesis; it binds to receptors on endothelial cells and suppresses the signals that drive new blood‑vessel formation, thereby limiting tissue vascularisation.
Has endostatin been approved as a drug for any disease?
No. Endostatin is classified as an investigational compound used only in research settings; it has not received regulatory approval for therapeutic indications.
Can endostatin be used to image tumours?
Preclinical work shows that radiolabelled or fluorescently tagged endostatin can highlight endostatin‑receptor‑rich tumours in animal models, suggesting a potential role as an imaging tracer, but clinical validation is lacking.
Is there any evidence that endostatin works in humans?
The cited literature contains no human clinical trial data; all efficacy and mechanistic observations are derived from animal experiments or review articles.
What are the known safety concerns with endostatin?
Safety data are absent from the available abstracts. Because it has only been tested in preclinical models, potential adverse effects, immunogenicity, or toxicity in humans remain undefined.
What is Endostatin used for?
Endostatin is educationally associated with: Ocular neovascularization (wet AMD), Cancer therapy, Colorectal cancer treatment, Non-small cell lung cancer treatment, Breast cancer treatment, Anti‑angiogenic research, Anti-tumor angiogenesis inhibition. Educational only — not medical advice.
How is Endostatin administered?
Recorded routes of administration: Intravenous, Subcutaneous.
What are the potential side effects of Endostatin?
Reported adverse effects include: Nausea / Vomiting, Hypertension, Injection site reactions, Hypotension, Fatigue, Elevated liver enzymes (transaminases), Thromboembolism. This list is not exhaustive — consult a qualified clinician.
Who should avoid Endostatin?
Recorded contraindications: Active hemorrhage or coagulopathy, Severe hepatic impairment, Pregnancy, Hypersensitivity to endostatin or excipients. Consult a qualified clinician before use.