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| Targets |
The primary targets of Anecortave are multiple angiogenic factors. Unlike anti-VEGF agents that target a single angiogenic pathway, anecortave inhibits neovascularization induced by multiple angiogenic factors including VEGF, FGF2, PDGF, and IGF1. The compound displays glucocorticoid and mineralocorticoid receptor binding activities, which are useful for studies involving steroid receptor pathways. However, the compound was specifically modified to eliminate glucocorticoid receptor-mediated activity while retaining anti-angiogenic efficacy. Anecortave's broad-spectrum anti-angiogenic activity makes it a valuable tool for studying neovascular disorders.
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| ln Vitro |
In vitro, Anecortave exhibits broad-spectrum anti-angiogenic activity. The compound inhibits neovascularization induced by multiple angiogenic factors including VEGF, FGF2, PDGF, and IGF1. Unlike anti-VEGF agents that target a single angiogenic pathway, anecortave's multi-target approach may offer advantages in treating complex neovascular disorders. The compound's effects can be evaluated in endothelial cell proliferation, migration, and tube formation assays. Anecortave also displays glucocorticoid and mineralocorticoid receptor binding activities, which can be assessed in receptor binding studies. These in vitro activities support its investigation for ocular neovascular conditions.
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| ln Vivo |
In vivo, Anecortave has been investigated clinically (as the acetate prodrug) for exudative age-related macular degeneration and for steroid-induced intraocular pressure elevation. The compound inhibits angiogenesis in various in vivo models of neovascularization. Its unique structure facilitates studies on steroid metabolism and drug development, providing a robust tool for exploring novel treatments and understanding steroid-related pathways in pharmaceutical research. The compound's anti-angiogenic activity is retained while glucocorticoid receptor-mediated activity is eliminated, making it a potentially safer alternative for long-term use. Further in vivo studies are needed to fully characterize its therapeutic potential.
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| Enzyme Assay |
In vitro enzyme/receptor binding studies for Anecortave focus on its interactions with steroid receptors and angiogenic factors. Glucocorticoid receptor binding can be assessed using radioligand competition assays with [³H]-dexamethasone. Mineralocorticoid receptor binding can be evaluated using similar techniques. The compound's anti-angiogenic activity can be assessed in vitro by measuring its ability to inhibit VEGF-induced endothelial cell proliferation, migration, and tube formation. Binding to angiogenic factors can be evaluated using surface plasmon resonance or ELISA-based assays. These methods are for research purposes only.
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| Cell Assay |
In vitro cell-based assays for Anecortave evaluate its anti-angiogenic and steroid receptor activities. Endothelial cells (e.g., HUVEC, HMEC-1) are treated with Anecortave at various concentrations (typically 0.1-100 µM) and stimulated with angiogenic factors (VEGF, FGF2, PDGF, IGF1). Cell proliferation is measured using MTT or BrdU incorporation assays. Cell migration is assessed using scratch wound or Boyden chamber assays. Tube formation is evaluated on Matrigel or collagen gels. Steroid receptor activity can be assessed using reporter cell lines transfected with glucocorticoid or mineralocorticoid response element-driven luciferase constructs. Standard cell culture conditions are used.
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| Animal Protocol |
In vivo animal studies for Anecortave utilize models of ocular neovascularization. Laser-induced choroidal neovascularization models in mice or rats are commonly used to evaluate anti-angiogenic efficacy. Anecortave is administered via periocular injection or topical application. The extent of neovascularization is assessed by fluorescein angiography, histology, or choroidal flat-mount analysis. Steroid-induced intraocular pressure models can be used to evaluate effects on ocular pressure. All procedures must comply with institutional animal care guidelines. Clinical studies have been conducted in patients with age-related macular degeneration.
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| ADME/Pharmacokinetics |
The pharmacokinetic properties of Anecortave are related to its use as an ocular therapeutic. As the acetate prodrug, anecortave acetate is administered via periocular injection for sustained drug delivery to the eye. The prodrug is hydrolyzed to the active metabolite anecortave. The compound has a molecular weight of 344.4 g/mol and is soluble in DMSO. The compound's unique structure facilitates studies on steroid metabolism. Detailed pharmacokinetic parameters (half-life, Cmax, AUC) are available from published preclinical and clinical studies. The compound is for research use only.
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| Toxicity/Toxicokinetics |
The toxicity profile of Anecortave has been evaluated in preclinical and clinical studies. The compound was purposefully modified to eliminate glucocorticoid receptor-mediated activity while retaining anti-angiogenic efficacy, potentially reducing steroid-related side effects. The compound has been investigated clinically for age-related macular degeneration, indicating an acceptable safety profile. Common adverse effects may include injection-site reactions or transient increases in intraocular pressure. The compound is for research use only and is not approved for clinical use. Standard safety precautions for handling pharmaceutical compounds apply.
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| References | |
| Additional Infomation |
Anecortave is a 21-hydroxysteroid. Anecortave is being investigated in the clinical trial NCT00691717 (Safety of Anecortave acetate in patients with open-angle glaucoma or ocular hypertension).
Additional information: Anecortave is also known as AL-4940. It is a 21-hydroxy steroid and the desacetylated, pharmacologically active metabolite of anecortave acetate. The compound has the molecular formula C₂₁H₂₈O₄ and molecular weight 344.4 g/mol. Anecortave was chemically derived from cortisol and modified to eliminate glucocorticoid receptor-mediated activity while retaining anti-angiogenic efficacy. The compound inhibits neovascularization induced by multiple angiogenic factors including VEGF, FGF2, PDGF, and IGF1. Anecortave has been investigated clinically (as the acetate prodrug) for exudative age-related macular degeneration and steroid-induced intraocular pressure elevation. The product is for research use only and is not approved for clinical or therapeutic applications. |
| Molecular Formula |
C21H28O4
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| Molecular Weight |
344.44462
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| Exact Mass |
344.199
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| CAS # |
10184-70-0
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| PubChem CID |
7074810
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| Appearance |
White to off-white solid powder
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| LogP |
2.73
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
25
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| Complexity |
705
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| Defined Atom Stereocenter Count |
5
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| SMILES |
C[C@]12CCC(=O)C=C1CC[C@@H]3C2=CC[C@]4([C@H]3CC[C@@]4(C(=O)CO)O)C
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| InChi Key |
BCFCRXOJOFDUMZ-ONKRVSLGSA-N
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| InChi Code |
InChI=1S/C21H28O4/c1-19-8-5-14(23)11-13(19)3-4-15-16(19)6-9-20(2)17(15)7-10-21(20,25)18(24)12-22/h6,11,15,17,22,25H,3-5,7-10,12H2,1-2H3/t15-,17+,19+,20+,21+/m1/s1
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| Chemical Name |
(8S,10S,13S,14S,17R)-17-hydroxy-17-(2-hydroxyacetyl)-10,13-dimethyl-2,6,7,8,12,14,15,16-octahydro-1H-cyclopenta[a]phenanthren-3-one
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~50 mg/mL (~145.16 mM)
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.9033 mL | 14.5163 mL | 29.0326 mL | |
| 5 mM | 0.5807 mL | 2.9033 mL | 5.8065 mL | |
| 10 mM | 0.2903 mL | 1.4516 mL | 2.9033 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT00299507 | Completed | Drug: Anecortave Acetate Sterile Suspension, 30 mg/mL Drug: Anecortave Acetate Sterile Suspension, 60 mg/mL Other: Anecortave Acetate Vehicle |
Macular Degeneration | Alcon Research | 2005-03 | Phase 3 |
| NCT00570479 | Completed | Drug: anecortave acetate | Glaucoma Uveitis, Posterior |
Texas Retina Associates | 2006-09 | Phase 1 |
| NCT00333216 | Terminated | Drug: Anecortave Acetate Sterile Suspension, 30 mg/mL Drug: Anecortave Acetate Sterile Suspension, 60 mg/ML Other: Anecortave Acetate Vehicle |
AMD | Alcon Research | 2005-05 | Phase 3 |
| NCT00489840 | Completed | Drug: Anecortave Acetate Sterile suspension 15 mg
Drug: Anecortave Acetate |
Chronic Central Serous Chorioretinopathy | Manhattan Eye, Ear & Throat Hospital | 2007-05 | Phase 1 Phase 2 |
| NCT00332657 | Terminated | Drug: Anecortave Acetate Sterile Suspension, 30 mg/mL Drug: Anecortave Acetate Sterile Suspension, 60 mg/mL Other: Anecortave Acetate Vehicle |
AMD | Alcon Research | 2006-09 | Phase 3 |
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