Page last updated: 2024-10-15
abarelix
Description
abarelix: RN & structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]
abarelix : A polypeptide compound composed of ten natural and non-natural amino acid resiudes in a linear sequence. [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]
Cross-References
| ID Source | ID |
|---|---|
| PubMed CID | 16131215 |
| CHEMBL ID | 1252 |
| CHEBI ID | 337298 |
| SCHEMBL ID | 9533 |
| SCHEMBL ID | 19712245 |
| MeSH ID | M0412551 |
Synonyms (49)
| Synonym |
|---|
| gtpl1188 |
| abarelix-depot-m |
| abarelix |
| r-3827 |
| ppi-149 |
| plenaxis |
| D02738 |
| plenaxis (tn) |
| 183552-38-7 |
| abarelix (usan/inn) |
| DB00106 |
| ppi 149 |
| n-acetyl-3-(2-naphthyl)-d-alanyl-4-chloro-d-phenylalanyl-3-(3-pyridyl)-d-alanyl-l-seryl-n-methyl-l-tyrosyl-d-asparginyl-l-leucyl-n6-isopropyl-l-lysyl-l-prolyl-d-alaninamide |
| n-acetyl-3-(2-naphthyl)-d-alanyl-4-chloro-d-phenylalanyl-3-(3-pyridyl)-d-alanyl-l-seryl-n-methyl-l-tyrosyl-d-asparaginyl-l-leucyl-n(sup 6)-isopropyl-l-lysyl-l-prolyl-d-alaninamide |
| r 3827 |
| plenaxis depot |
| d-alaninamide, n-acetyl-3-(2-naphthalenyl)-d-alanyl-4-chloro-d-phenylalanyl-3-(3-pyridinyl)-d-alanyl-l-seryl-n-methyl-l-tyrosyl-d-asparaginyl-l-leucyl-n6-(1-methylethyl)-l-lysyl-l-prolyl- 10 |
| R382 , |
| r-382 |
| CHEMBL1252 , |
| R3827 , |
| ac-d-nal-[d-(pcl)phe]-d-pal-ser-[nalpha-me-tyr]-d-asn-leu-ilys-pro-dala-nh2 |
| bdbm50102442 |
| chebi:337298 , |
| n-acetyl-3-(2-naphthyl)-d-alanyl-4-chloro-d-phenylalanyl-3-(pyridin-3-yl)-d-alanyl-l-seryl-n-methyl-l-tyrosyl-d-asparginyl-l-leucyl-n(6)-isopropyl-l-lysyl-l-prolyl-d-alaninamide |
| abarelix [usan:inn] |
| w486sj5824 , |
| unii-w486sj5824 |
| SCHEMBL9533 |
| d-alaninamide, n-acetyl-3-(2-naphthalenyl)-d-alanyl-4-chloro-d-phenylalanyl-3-(3-pyridinyl)-d-alanyl-l-seryl-n-methyl-l-tyrosyl-d-asparaginyl-l-leucyl-n6-(1-methylethyl)-l-lysyl-l-prolyl-10 |
| DTXSID20171443 , |
| HY-13534 |
| AIWRTTMUVOZGPW-HSPKUQOVSA-N |
| CS-5873 |
| n-acetyl-3-(2-naphthyl)-d-alanyl-4-chloro-d-phenylalanyl-3-(3-pyridyl)-d-alanyl-l-seryl-n-methyl-l-tyrosyl-d-asparagyl-l-leucyl-n6-isopropyl-l-lysyl-l-prolyl-d-alaninamide |
| SCHEMBL19712245 |
| Q305555 |
| d-alaninamide, n-acetyl-3-(2-naphthalenyl)-d-alanyl-4-chloro-d-phenylalanyl-3-(3-pyridinyl)-d-alanyl-l-seryl-n-methyl-l-tyrosyl-d-asparaginyl-l-leucyl-n6-(1-methylethyl)-l-lysyl-l-prolyl- |
| AT36700 |
| MS-32159 |
| ppi 149r3827 |
| ppi149 |
| EN300-20605823 |
| r3827;ppi 149 |
| abarelixum |
| n-acetyl-3-(2-naphthalenyl)-d-alanyl-4-chloro-d-phenylalanyl-3-(3-pyridinyl)-d-alanyl-l-seryl-n-methyl-l-tyrosyl-d-asparaginyl-l-leucyl-n(6)-(1-methylethyl)-l-lysyl-l-prolyl-d-alaninamide |
| dtxcid4093934 |
| l02xb01 |
| AKOS040732360 |
Research Excerpts
Overview
Abarelix (PPI-149) is a luteinizing hormone-releasing hormone (LHRH) receptor antagonist. It is under development by Praecis, Amgen and Sanofi-Synthelabo for the potential treatment of prostate cancer, breast cancer and hormone-related disorders.
| Excerpt | Reference |
|---|---|
| "Abarelix (PPI-149) is a luteinizing hormone-releasing hormone (LHRH) receptor antagonist under development by Praecis, Amgen and Sanofi-Synthelabo for the potential treatment of prostate cancer, breast cancer and hormone-related disorders [285672,328910]. " | ( Technology evaluation: Abarelix, Praecis pharmaceuticals. Doehn, C; Jocham, D, 2000) |
Treatment
Treatment with abarelix in patients with androgen-independent prostate cancer after orchiectomy results in marked reduction in circulating FSH. Treatment produced a higher percentage of patients who avoided a testosterone surge and a more rapid time to testosterone suppression.
| Excerpt | Reference |
|---|---|
| "Treatment with abarelix in patients with androgen-independent prostate cancer after orchiectomy results in marked reduction in circulating FSH. " | ( Targeting FSH in androgen-independent prostate cancer: abarelix for prostate cancer progressing after orchiectomy. Beer, TM; Eilers, KM; Garzotto, M; Lemmon, D; Wersinger, EM, 2004) |
| "Treatment with abarelix produced a higher percentage of patients who avoided a testosterone surge and had a more rapid time to testosterone suppression with a higher rate of medical castration 1 day after treatment and greater reductions in testosterone, luteinizing hormone, follicle-stimulating hormone, and dihydrotestosterone during the first 2 weeks of treatment compared with leuprolide acetate. " | ( A phase 3, multicenter, open-label, randomized study of abarelix versus leuprolide acetate in men with prostate cancer. Campion, M; Fotheringham, N; Garnick, MB; Gleason, D; McLeod, D; Tomera, K; Zinner, N, 2001) |
Pharmacokinetics
Abarelix concentrations peaked with the median observed time to reach peak concentration at approximately 28 days. The pharmacokinetic characteristics and the pharmacologic activities of abarelix were measured.
| Excerpt | Reference |
|---|---|
| "Our objective was to evaluate the pharmacokinetic and pharmacodynamic characteristics of abarelix after continuous subcutaneous infusion of 50 microg x kg(-1) x d(-1) in patients with prostate cancer and to identify a plasma concentration of abarelix that may provide a sustained pharmacodynamic effect." | ( Pharmacokinetics and pharmacodynamics of abarelix, a gonadotropin-releasing hormone antagonist, after subcutaneous continuous infusion in patients with prostate cancer. Baughman, SA; Garnick, MB; Lau, DT; Menchaca, D; Wong, SL, 2003) |
| " The pharmacokinetic characteristics and the pharmacologic activities of abarelix on testosterone, prostate-specific antigen, dihydrotestosterone, follicle-stimulating hormone, and luteinizing hormone during and after treatment with abarelix were measured." | ( Pharmacokinetics and pharmacodynamics of abarelix, a gonadotropin-releasing hormone antagonist, after subcutaneous continuous infusion in patients with prostate cancer. Baughman, SA; Garnick, MB; Lau, DT; Menchaca, D; Wong, SL, 2003) |
| "After a continuous subcutaneous infusion of 50 microg x kg(-1) x d(-1), abarelix concentrations peaked with the median observed time to reach peak concentration at approximately 28 days." | ( Pharmacokinetics and pharmacodynamics of abarelix, a gonadotropin-releasing hormone antagonist, after subcutaneous continuous infusion in patients with prostate cancer. Baughman, SA; Garnick, MB; Lau, DT; Menchaca, D; Wong, SL, 2003) |
Dosage Studied
| Excerpt | Reference |
|---|---|
| " All patients were treated at a dosage of 50 microg x kg(-1) x d(-1) for at least 28 days (4 weeks)." | ( Pharmacokinetics and pharmacodynamics of abarelix, a gonadotropin-releasing hormone antagonist, after subcutaneous continuous infusion in patients with prostate cancer. Baughman, SA; Garnick, MB; Lau, DT; Menchaca, D; Wong, SL, 2003) |
| "8%, respectively, were achieved by study day 15 (14 days after dosing started), and inhibition continued to be maintained until the last dosing day." | ( Pharmacokinetics and pharmacodynamics of abarelix, a gonadotropin-releasing hormone antagonist, after subcutaneous continuous infusion in patients with prostate cancer. Baughman, SA; Garnick, MB; Lau, DT; Menchaca, D; Wong, SL, 2003) |
| " Consequently, we evaluated the safety of more frequent (biweekly) dosing of abarelix and characterized the effect of this dosing schedule on serum follicle-stimulating hormone levels in men with prostate cancer that is progressing despite luteinizing hormone-releasing hormone agonist therapy." | ( Dose-escalated abarelix in androgen-independent prostate cancer: a phase I study. Beer, TM; Bhat, G; Garnick, M; Ryan, C, 2006) |
| " The main disadvantage of degarelix compared to the LHRH agonists is the monthly dosing and the inconvenience for some patients and practices." | ( Utility of LHRH antagonists for advanced prostate cancer. Moul, JW, 2014) |
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
Roles (2)
| Role | Description |
|---|---|
| hormone antagonist | A chemical substance which inhibits the function of the endocrine glands, the biosynthesis of their secreted hormones, or the action of hormones upon their specific sites. |
| antineoplastic agent | A substance that inhibits or prevents the proliferation of neoplasms. |
| [role 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] | |
Drug Classes (1)
| Class | Description |
|---|---|
| polypeptide | A peptide containing ten or more amino acid residues. |
| [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 Targets (1)
Inhibition Measurements
| Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| Gonadotropin-releasing hormone receptor | Homo sapiens (human) | IC50 (µMol) | 0.0035 | 0.0001 | 0.1289 | 5.2000 | AID74279 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
Activation Measurements
| Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| Gonadotropin-releasing hormone receptor | Homo sapiens (human) | Kd | 0.0008 | 0.0001 | 0.0009 | 0.0025 | AID74429 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
Biological Processes (4)
| Process | via Protein(s) | Taxonomy |
|---|---|---|
| gonadotropin secretion | Gonadotropin-releasing hormone receptor | Homo sapiens (human) |
| cellular response to gonadotropin-releasing hormone | Gonadotropin-releasing hormone receptor | Homo sapiens (human) |
| G protein-coupled receptor signaling pathway | Gonadotropin-releasing hormone receptor | Homo sapiens (human) |
| cellular response to hormone stimulus | Gonadotropin-releasing hormone receptor | Homo sapiens (human) |
| [Information is prepared from geneontology information from the June-17-2024 release] | ||
Molecular Functions (2)
| Process | via Protein(s) | Taxonomy |
|---|---|---|
| peptide binding | Gonadotropin-releasing hormone receptor | Homo sapiens (human) |
| gonadotropin-releasing hormone receptor activity | Gonadotropin-releasing hormone receptor | Homo sapiens (human) |
| [Information is prepared from geneontology information from the June-17-2024 release] | ||
Ceullar Components (2)
| Process | via Protein(s) | Taxonomy |
|---|---|---|
| plasma membrane | Gonadotropin-releasing hormone receptor | Homo sapiens (human) |
| membrane | Gonadotropin-releasing hormone receptor | Homo sapiens (human) |
| plasma membrane | Gonadotropin-releasing hormone receptor | Homo sapiens (human) |
| [Information is prepared from geneontology information from the June-17-2024 release] | ||
Bioassays (4)
| Assay ID | Title | Year | Journal | Article |
|---|---|---|---|---|
| AID74279 | Antagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cells | 2001 | Journal of medicinal chemistry, Feb-01, Volume: 44, Issue:3 | GnRH antagonists: a new generation of long acting analogues incorporating p-ureido-phenylalanines at positions 5 and 6. |
| AID74429 | Competitive antagonism of GnRH-induced response in the reporter gene assay | 2001 | Journal of medicinal chemistry, Feb-01, Volume: 44, Issue:3 | GnRH antagonists: a new generation of long acting analogues incorporating p-ureido-phenylalanines at positions 5 and 6. |
| AID104503 | Compound was tested for inhibition of Leutenizing hormone release at 24 hours (very short duration) in castrated male rat assay | 2001 | Journal of medicinal chemistry, Feb-01, Volume: 44, Issue:3 | GnRH antagonists: a new generation of long acting analogues incorporating p-ureido-phenylalanines at positions 5 and 6. |
| AID1346002 | Human GnRH1 receptor (Gonadotrophin-releasing hormone receptors) | 2007 | Endocrinology, Feb, Volume: 148, Issue:2 | Pharmacological characterization of a novel nonpeptide antagonist of the human gonadotropin-releasing hormone receptor, NBI-42902. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||||
Research
Studies (39)
| Timeframe | Studies, This Drug (%) | All Drugs % |
|---|---|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 0 (0.00) | 18.2507 |
| 2000's | 31 (79.49) | 29.6817 |
| 2010's | 7 (17.95) | 24.3611 |
| 2020's | 1 (2.56) | 2.80 |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||
Study Types
| Publication Type | This drug (%) | All Drugs (%) |
|---|---|---|
| Trials | 9 (22.50%) | 5.53% |
| Reviews | 16 (40.00%) | 6.00% |
| Case Studies | 1 (2.50%) | 4.05% |
| Observational | 0 (0.00%) | 0.25% |
| Other | 14 (35.00%) | 84.16% |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||
Clinical Trials (3)
Trial Overview
| Trial | Phase | Enrollment | Study Type | Start Date | Status | ||
|---|---|---|---|---|---|---|---|
| Phase III Study of the Comparison of Abarelix Versus Goserelin Plus Bicalutamide in Patients With Advanced or Metastatic Prostate Cancer. A One Year Randomised, Open Label, Multi-Centre Phase III Trial.[NCT00841113] | Phase 3 | 177 participants (Actual) | Interventional | 1999-01-31 | Completed | ||
| Incidence of Immediate Onset Systemic Allergic Reactions in Patients Treated With Plenaxis®[NCT00103623] | Phase 4 | 2,000 participants | Interventional | 2004-06-30 | Suspended | ||
| Phase 2 Study of Abarelix in Androgen-Independent Prostate Cancer Progressing After Agonist Therapy[NCT00100243] | Phase 2 | 22 participants | Interventional | 2004-05-31 | Completed | ||
| [information is prepared from clinicaltrials.gov, extracted Sep-2024] | |||||||