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buserelin

Trade name: receptal

Small moleculeexperimental

Buserelin, sold under the brand name Suprefact among others, is a medication which is used primarily in the treatment of prostate cancer and endometriosis. It is also used for other indications such as the treatment of premenopausal breast cancer, uterine fibroids, and early puberty, in assisted reproduction for female infertility, and as a part of transgender hormone therapy. In addition, buserelin is used in veterinary medicine. The medication is typically used as a nasal spray three times per day, but is also available for use as a solution or implant for injection into fat. — Wikipedia

Clinical trial activity

23 trials · 33 clinical orgs · 0 marketing orgs

Phase 1
4
Phase 2
15
Phase 3
12
Phase 4
6

Earliest trial started Mar 1, 1995 (NCT00002633)

Timeline

1990s

  1. Jan 1, 1995

    Earliest Phase 3 Sponsor(trial)

2000s

  1. Jan 1, 2002

    Earliest Phase 1 Sponsor(trial)

2010s

  1. Jan 1, 2014

    Earliest Phase 2 Sponsor(trial)

Indications

Approved for

Studied for

Mechanism of action

  • Gonadotropin-releasing hormone receptorAGONIST

    GNRHR agonist

    Buserelin, a gonadotropin-releasing hormone (GnRH) agonist, is a therapeutic drug suppressing the release of Luteinizing hormone (LH) and Follicle-stimulating hormone (FSH). Initial interaction of buserelin with the GnRH receptor induces release of FSH and LH by gonadotrophes. Long-term exposure to constant levels of buserelin, rather than endogenous pulses, leads to downregulation of the GnRH receptors and subsequent suppression of the pituitary release of LH and FSH.

Chemistry & pharmacology

Loading structure…

SMILES

CCNC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](COC(C)(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@@H]1CCC(=O)N1
Mol. weight
1239.45 g/mol
Chirality
Single Stereoisomer
Inorganic
No
Polymer
No

Oral

No

Parenteral

No

Topical

No

Sources

Also known as

  • buserelin
  • buserelin
  • buserelin
  • buserelin
  • buserelin
  • buserelin
  • buserelin
  • buserelin
  • buserelin acetate
  • buserelin acetate
  • (des-gly10,d-ser(tbu)6,pro-nhet9)-lhrh
  • (des-gly10,d-ser(tbu)6,pro-nhet9)-lhrh
  • d-ser(tbu)6ea10lhrh
  • d-ser(tbu)6ea10lhrh
  • etilamide
  • etilamide
  • etilamide
  • receptal
  • suprecur
  • suprecur
  • suprefact
  • suprefact
  • suprefact

Clinical trials

NCT IDPhaseStart dateSponsor(s)
NCT05050084Phase 3Nov 11, 2021National Cancer Institute (NCI), NRG Oncology
NCT04513717Phase 3Dec 15, 2020National Cancer Institute (NCI), NRG Oncology
NCT02703584Phase 4Mar 1, 2016University of Toronto
NCT02487823Phase 1Oct 1, 2014Institut Paoli-Calmettes, Novartis
NCT01989780Phase 2Jan 1, 2014Chugai, Fukushima Medical University, Japan Breast Cancer Research Group, Kyoto University
NCT01816789Phase 4Mar 1, 2013Andros Day Surgery Clinic
NCT01636505Phase 3Sep 1, 2012European Hospital
NCT01546987Phase 3May 1, 2012Harvard University, National Cancer Institute (NCI), NRG Oncology, Radiation Therapy Oncology Group
NCT01492972Phase 3Jan 1, 2012Proton Collaborative Group
NCT00936390Phase 3Sep 1, 200921st Century Oncology, National Cancer Institute (NCI), NRG Oncology, Radiation Therapy Oncology Group
NCT01213147Phase 4Apr 1, 2009Shahid Sadoughi University of Medical Science, Yazd Research & Clinical Center for Infertility
NCT00627406Phase 4Jan 1, 2009Hospitalsenhed Midt
NCT00823121Phase 1/Phase 2 (Phase 2)Aug 1, 2008Shahid Sadoughi University of Medical Science
NCT00823004Phase 1/Phase 2 (Phase 2)Jun 1, 2008Shahid Sadoughi University of Medical Science, Yazd Research & Clinical Center for Infertility
NCT00651326Phase 3Mar 1, 2008British Columbia Cancer Agency, Canadian Cancer Trials Group
NCT00823602Phase 3Mar 1, 2008Shahid Sadoughi University of Medical Science, Yazd Research & Clinical Center for Infertility
NCT00830492Phase 4Jan 1, 2008Shahid Sadoughi University of Medical Science
NCT00329797Phase 3Mar 1, 2006Harvard University, Medical College of Wisconsin, National Cancer Institute (NCI), Radiation Therapy Oncology Group, University of North Carolina, Charlotte
NCT00461916Phase 4May 1, 2005Isfahan University
NCT00054106Phase 1Dec 1, 2002British Columbia Cancer Agency, Canadian Cancer Trials Group
Showing 20 of 23 trials
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Organizations

Research & Development (33)

OrganizationOrg typeTrialsAs lead sponsorPhasesEarliest year
National Cancer Institute (NCI)Government7011995
Shahid Sadoughi University of Medical ScienceAcademic/Hospital5532008
Canadian Cancer Trials GroupAcademic/Hospital4421995
NRG OncologyAcademic/Hospital4212009
Radiation Therapy Oncology GroupAcademic/Hospital3312006
University of TorontoAcademic/Hospital3121995
Yazd Research & Clinical Center for InfertilityAcademic/Hospital3032008
British Columbia Cancer AgencyAcademic/Hospital2022002
Harvard UniversityAcademic/Hospital2012006
Southwest Oncology GroupAcademic/Hospital2011995
21st Century OncologyAcademic/Hospital1012009
Andros Day Surgery ClinicAcademic/Hospital1112013
ChugaiFor profit1012014
Eastern Cooperative Oncology GroupAcademic/Hospital1011995
European HospitalAcademic/Hospital1112012
Fukushima Medical UniversityAcademic/Hospital1012014
Hospitalsenhed MidtAcademic/Hospital1112009
Institut Gustave RoussyAcademic/Hospital1012002
Institut Paoli-CalmettesAcademic/Hospital1112014
Isfahan UniversityAcademic/Hospital1112005
33 organizations
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