anecortave acetate: derived from cortisone (11 OH replaced by 9-11 double bond) [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]
| ID Source | ID |
|---|---|
| PubMed CID | 111332 |
| CHEMBL ID | 2106613 |
| CHEBI ID | 31215 |
| SCHEMBL ID | 94110 |
| MeSH ID | M0376255 |
| Synonym |
|---|
| nsc-24345 |
| nsc24345 |
| anecortave acetate |
| al-3789 |
| retaane |
| 7753-60-8 |
| nsc-15475 |
| nsc15475 |
| anecortave acetate (jan/usan) |
| D01733 |
| [2-[(8s,10s,13s,14s,17r)-17-hydroxy-10,13-dimethyl-3-oxo-2,6,7,8,12,14,15,16-octahydro-1h-cyclopenta[a]phenanthren-17-yl]-2-oxoethyl] acetate |
| NCGC00181018-01 |
| dtxsid5046805 , |
| dtxcid3026805 |
| cas-7753-60-8 |
| tox21_112668 |
| AKOS015917580 |
| CHEMBL2106613 |
| nsc 24345 |
| 21-(acetyloxy)-17-hydroxypregna-4,9(11)-diene-3,20-dione |
| nsc 15475 |
| al 3789 |
| y0pc411k4t , |
| pregna-4,9(11)-diene-3,20-dione, 21-(acetyloxy)-17-hydroxy- |
| unii-y0pc411k4t |
| retaane suspension |
| 17-alpha,21-dihydroxypregna-4,9(11)-diene-3,20-dione 21-acetate |
| 17,21-dihydroxypregna-4,9(11)-diene-3,20-dione 21-acetate |
| anecortave [inn] |
| 4,9(11)-pregnadien-17alpha,21-diol-3,20-dione-21-acetate |
| anecortave acetate [usan] |
| einecs 231-812-5 |
| 17-hydroxy-3,20-dioxopregna-4,9(11)-dien-21-yl acetate |
| anecortave acetate [mi] |
| al3789 |
| anecortave acetate [jan] |
| anecortave [mart.] |
| hydrocortisone acetate impurity e [ep impurity] |
| DB05288 |
| SCHEMBL94110 |
| 17alpha-hydroxy-21 -acetoxy-pregna-4,9(11)-diene-3,20-dione |
| 17alpha-hydroxy-21-acetoxypregna-4,9(11)-diene-3,20-dione |
| 21-acetoxy-17-hydroxy-4,9(11)-pregnadiene-3,20-dione |
| 17-hydroxy-3,20-dioxopregna-4,9(11)-dien-21-yl acetate # |
| pregn-4,9(11)-dien-17,21-diol-3,20-dione, acetate(ester) |
| CHEBI:31215 |
| EX-A5253 |
| Q4761567 |
| anecortave acetate (200 mg)f0e2980.997mg/mg(ai) |
| anecortave-acetate |
| CS-0066714 |
| HY-116868 |
Anecortave acetate is an angiostatic steroid which shows distinct mechanism of action in inhibiting neovascularization. It is a synthetic derivative of cortisol, but very specific and irreversible chemical modifications to the cortisol structure have resulted in the creation of a potent inhibitor of blood vessel growth.
| Excerpt | Reference | Relevance |
|---|---|---|
| "Anecortave acetate is an angiostatic steroid which shows distinct mechanism of action in inhibiting neovascularization, making it different from the anti-VEGF agents (Pegaptanib, Ranibizumab and Bevacizumab)." | ( [Present status of studies on the treatment of choroidal neovascularization by Anecortave acetate]. Li, X; Wang, YS, 2008) | 1.29 |
| "Anecortave acetate is a synthetic derivative of cortisol, but very specific and irreversible chemical modifications to the cortisol structure have resulted in the creation of a potent inhibitor of blood vessel growth with no evidence non-clinically or clinically of glucocorticoid receptor-mediated bioactivity. " | ( Safety of posterior juxtascleral depot administration of the angiostatic cortisene anecortave acetate for treatment of subfoveal choroidal neovascularization in patients with age-related macular degeneration. Augustin, AJ; Beasley, C; D'Amico, DJ; Mieler, WF; Schneebaum, C, 2005) | 2 |
| "Anecortave acetate is a novel angiostatic cortisene being evaluated clinically for treatment of exudative age-related macular degeneration (ARMD). " | ( Anecortave acetate for the treatment of subfoveal choroidal neovascularization secondary to age-related macular degeneration. Aue, A; Michels, R; Michels, S; Schmidt-Erfurth, U, ) | 3.02 |
| "Anecortave acetate is a unique angiostatic agent. " | ( Mechanism of action of the angiostatic cortisene anecortave acetate. Clark, AF, 2007) | 2.04 |
| "Anecortave acetate is a unique ocular angiostatic cortisene that has broad-based anti-angiogenic activity in 14 different preclinical models of neovascularization, across multiple species and inducers of neovascularization. " | ( Preclinical efficacy of anecortave acetate. Clark, AF, 2007) | 2.09 |
| "Anecortave acetate is an angiostatic cortisene which is injected as a posterior juxtascleral depot and has been shown to be effective in the treatment of exudative age-related macular degeneration (AMD). " | ( First clinical experience with anecortave acetate (Retaane). Barthelmes, D; Fleischhauer, JC; Hayek, S; Helbig, H; Kurz-Levin, MM; Menghini, M; Scherrer, M; Sutter, FK, 2007) | 2.07 |
| Excerpt | Reference | Relevance |
|---|---|---|
| "Anecortave acetate has broad based angiostatic activity, inhibiting neovascularization at multiple steps." | ( Mechanism of action of the angiostatic cortisene anecortave acetate. Clark, AF, 2007) | 1.32 |
| Excerpt | Reference | Relevance |
|---|---|---|
| "Eyes treated with anecortave acetate showed a 28% (P < 0.001) increase in hypoxic regions in comparison with the saline-treated control group 1 day after injection and a 17% (P < 0.001) increase 1 week after injection." | ( Increased hypoxia following vessel targeting in a murine model of retinoblastoma. Boutrid, H; Cebulla, CM; Feuer, WJ; Jockovich, ME; Lampidis, TJ; Murray, TG; Piña, Y, 2009) | 0.68 |
Anecortave acetate 15 mg is safe and well-tolerated when administered as a posterior juxtascleral depot at 6-month intervals.
| Excerpt | Reference | Relevance |
|---|---|---|
| "The ocular delivery of anecortave acetate was tested in preclinical and clinical pharmacokinetic and metabolism studies." | ( Pharmacokinetics and metabolism of anecortave acetate in animals and humans. Dahlin, DC; Rahimy, MH, 2007) | 0.93 |
| Excerpt | Reference | Relevance |
|---|---|---|
| "42 h (dogs), and bioavailability of 74." | ( VBP15: preclinical characterization of a novel anti-inflammatory delta 9,11 steroid. Damsker, JM; Hoffman, EP; McCall, JM; Nagaraju, K; Reeves, EKM, 2013) | 0.39 |
| "The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs." | ( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019) | 0.51 |
| Excerpt | Relevance | Reference |
|---|---|---|
| " The reduction of tumor burden followed a U-shaped dose-response curve." | ( Anecortave acetate as single and adjuvant therapy in the treatment of retinal tumors of LH(BETA)T(AG) mice. Escalona-Benz, E; Feuer, W; Hernandez, E; Jockovich, ME; Murray, TG, 2006) | 1.78 |
| " Additional studies are required to establish better their efficacy and safety, optimal dosing frequency, mechanism of action, and potential additivity to other IOP-lowering therapies." | ( Anterior juxtascleral delivery of anecortave acetate in eyes with primary open-angle glaucoma: a pilot investigation. Bergamini, MV; Cagle, GD; Clark, AF; Covert, DW; Defaller, JM; Dickerson, JE; Krueger, S; Landry, TA; Realini, T; Robin, AL; Scheib, SA, 2009) | 0.63 |
| Class | Description |
|---|---|
| organic molecular entity | Any molecular entity that contains carbon. |
| [compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res] | |
| Protein | Taxonomy | Measurement | Average (µ) | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| AR protein | Homo sapiens (human) | Potency | 2.9319 | 0.0002 | 21.2231 | 8,912.5098 | AID743036; AID743040; AID743042; AID743053; AID743054 |
| glucocorticoid receptor [Homo sapiens] | Homo sapiens (human) | Potency | 6.7400 | 0.0002 | 14.3764 | 60.0339 | AID720692 |
| estrogen nuclear receptor alpha | Homo sapiens (human) | Potency | 17.0282 | 0.0002 | 29.3054 | 16,493.5996 | AID743069; AID743075; AID743079 |
| cytochrome P450, family 19, subfamily A, polypeptide 1, isoform CRA_a | Homo sapiens (human) | Potency | 26.6032 | 0.0017 | 23.8393 | 78.1014 | AID743083 |
| thyroid hormone receptor beta isoform 2 | Rattus norvegicus (Norway rat) | Potency | 6.1143 | 0.0003 | 23.4451 | 159.6830 | AID743065; AID743067 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
| Assay ID | Title | Year | Journal | Article |
|---|---|---|---|---|
| AID1296008 | Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening | 2020 | SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1 | Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening. |
| AID1346986 | P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular pharmacology, 11, Volume: 96, Issue:5 | A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
| AID1346987 | P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular pharmacology, 11, Volume: 96, Issue:5 | A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
| AID740555 | Transactivation of glucocorticoid receptor in HEK293 cells co-transfected with GRE assessed as induction of GRE-dependent gene expression at 100 ug/ml after 6 hrs by luciferase reporter gene assay | 2013 | Bioorganic & medicinal chemistry, Apr-15, Volume: 21, Issue:8 | VBP15: preclinical characterization of a novel anti-inflammatory delta 9,11 steroid. |
| AID740557 | Inhibition of TNFalpha-induced NFkappaB activation in mouse C2C12 cells incubated for 24 hrs prior to TNFalpha induction measured after 24 hrs by luciferase reporter gene assay | 2013 | Bioorganic & medicinal chemistry, Apr-15, Volume: 21, Issue:8 | VBP15: preclinical characterization of a novel anti-inflammatory delta 9,11 steroid. |
| AID740556 | Induction of glucocorticoid receptor nuclear translocation in mouse C2C12 cells at 1 x 10'-5 to 1.69 x 10'-10 M by chemiluminescence assay relative to control | 2013 | Bioorganic & medicinal chemistry, Apr-15, Volume: 21, Issue:8 | VBP15: preclinical characterization of a novel anti-inflammatory delta 9,11 steroid. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||||
| Timeframe | Studies, This Drug (%) | All Drugs % |
|---|---|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 3 (4.48) | 18.2507 |
| 2000's | 52 (77.61) | 29.6817 |
| 2010's | 11 (16.42) | 24.3611 |
| 2020's | 1 (1.49) | 2.80 |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||
According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be moderate demand-to-supply ratio for research on this compound.
| This Compound (23.15) All Compounds (24.57) |
| Publication Type | This drug (%) | All Drugs (%) |
|---|---|---|
| Trials | 9 (13.24%) | 5.53% |
| Reviews | 22 (32.35%) | 6.00% |
| Case Studies | 2 (2.94%) | 4.05% |
| Observational | 0 (0.00%) | 0.25% |
| Other | 35 (51.47%) | 84.16% |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||