Identification

Name
Buserelin
Accession Number
DB06719
Description

Buserelin is a synthetic peptide analog of the luteinizing hormone-releasing hormone (LHRH) agonist, which stimulates the pituitary gland's gonadotrophin-releasing hormone receptor (GnRHR). It is used in prostate cancer treatment.

Type
Biotech
Groups
Approved, Investigational
Biologic Classification
Protein Based Therapies
Hormones
Protein Structure
Db06719
Protein Chemical Formula
C62H90N16O15
Protein Average Weight
Not Available
Sequences
Not Available
Synonyms
  • (Des-Gly10,D-Ser(tBu)6,Pro-NHEt9)-LHRH
  • Buserelina
  • D-Ser(Tbu)6EA10LHRH
  • Etilamide
  • Tiloryth

Pharmacology

Indication

Buserelin may be used in the treatment of hormone-responsive cancers such as prostate cancer or breast cancer, estrogen-dependent conditions (such as endometriosis or uterine fibroids), and in assisted reproduction.

Associated Conditions
Contraindications & Blackbox Warnings
Learn about our commercial Contraindications & Blackbox Warnings data.
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Pharmacodynamics

The substitution of glycine in position 6 by D-serine, and that of glycinamide in position 10 by ethylamide, leads to a nonapeptide with a greatly enhanced LHRH effect. The effects of buserelin on FSH and LH release are 20 to 170 times greater than those of LHRH. Buserelin also has a longer duration of action than natural LHRH. Investigations in healthy adult males and females have demonstrated that the increase in plasma LH and FSH levels persist for at least 7 hours and that a return to basal values requires about 24 hours. Clinical inhibition of gonadotropin release, and subsequent reduction of serum testosterone or estradiol to castration level, was found when large pharmacologic doses (50-500 mcg SC/day or 300-1200 mcg IN/day) were administered for periods greater than 1 to 3 months. Chronic administration of such doses of buserelin results in sustained inhibition of gonadotropin production, suppression of ovarian and testicular steroidogenesis and, ultimately, reduced circulating levels of gonadotropin and gonadal steroids. These effects form the basis for buserelin use in patients with hormone-dependent metastatic carcinoma of the prostate gland as well as in patients with endometriosis.

Mechanism of action

Buserelin stimulates the pituitary gland's gonadotrophin-releasing hormone receptor (GnRHR). Buserelin desensitizes the GnRH receptor, reducing the amount of gonadotropin. In males, this results in a reduction in the synthesis and release of testosterone. In females, estrogen secretion is inhibited. While initially, there is a rise in FSH and LH levels, chronic administration of Buserelin results in a sustained suppression of these hormones.

TargetActionsOrganism
ALutropin-choriogonadotropic hormone receptorNot AvailableHumans
AGonadotropin-releasing hormone receptorNot AvailableHumans
Absorption

Buserelin is water soluble and readily absorbed after subcutaneous injection (70% bioavailable). However, bioavailability after oral absorption. When administered correctly via the nasal route, it may be absorbed in the nasal mucosa to achieve sufficient plasma levels.

Volume of distribution

Buserelin circulates in serum predominantly in intact active form. Preferred accumulation is preferentially in the liver and kidneys as well as in the anterior pituitary lobe, the biological target organ.

Protein binding

15%

Metabolism

It is metabolized and subsequently inactivated by peptidase (pyroglutamyl peptidase and chymotrypsin-like endopeptidase) in the liver and kidneys as well as in the gastrointestinal tract. In the pituitary gland, it is inactivated by membrane-located enzymes.

Route of elimination

Buserelin and its inactive metabolites are excreted via the renal and biliary routes. In man it is excreted in urine at 50% in its intact form.

Half-life

The elimination half-life is approximately 50 to 80 minutes following intravenous administration, 80 minutes after subcutaneous administration and approximately 1 to 2 hours after intranasal administration.

Clearance
Not Available
Adverse Effects
Learn about our commercial Adverse Effects data.
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Toxicity

Buserelin may induce early, transient increase in serum testosterone or estradiol which can lead in the exacerbation of signs and symptoms of metastatic prostate cancer or endometriosis. Adverse reactions reported at more than 10% occurrence include headache, loss of libido in patients with prostate cancer, hot flashes, hypermenorrhea, decreased libido in prostate cancer and endometriosis, flatulence, impotence, vaginal dryness, back pain and nasal mucosa irritation.

Affected organisms
  • Humans and other mammals
Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
DrugInteraction
AcarboseThe therapeutic efficacy of Acarbose can be decreased when used in combination with Buserelin.
AcebutololThe risk or severity of QTc prolongation can be increased when Buserelin is combined with Acebutolol.
AcetohexamideThe therapeutic efficacy of Acetohexamide can be decreased when used in combination with Buserelin.
AcrivastineThe risk or severity of QTc prolongation can be increased when Buserelin is combined with Acrivastine.
AdenosineThe risk or severity of QTc prolongation can be increased when Buserelin is combined with Adenosine.
AjmalineThe risk or severity of QTc prolongation can be increased when Ajmaline is combined with Buserelin.
AlbiglutideThe therapeutic efficacy of Albiglutide can be decreased when used in combination with Buserelin.
AlfuzosinThe risk or severity of QTc prolongation can be increased when Alfuzosin is combined with Buserelin.
AlimemazineThe risk or severity of QTc prolongation can be increased when Alimemazine is combined with Buserelin.
AlogliptinThe therapeutic efficacy of Alogliptin can be decreased when used in combination with Buserelin.
Additional Data Available
  • Extended Description
    Extended Description

    Extended description of the mechanism of action and particular properties of each drug interaction.

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  • Severity
    Severity

    A severity rating for each drug interaction, from minor to major.

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  • Evidence Level
    Evidence Level

    A rating for the strength of the evidence supporting each drug interaction.

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  • Action
    Action

    An effect category for each drug interaction. Know how this interaction affects the subject drug.

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Food Interactions
Not Available

Products

Product Ingredients
IngredientUNIICASInChI Key
Buserelin acetate13U86G7YSP68630-75-1PYMDEDHDQYLBRT-DRIHCAFSSA-N
International/Other Brands
Cinnafact (Cinnagen)
Brand Name Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
SuprefactSolutionSubcutaneousCheplapharm Arzneimittel Gmbh1998-05-05Not applicableCanada flag
SuprefactSolutionNasalCheplapharm Arzneimittel Gmbh1998-02-03Not applicableCanada flag
Suprefact Depot 2 MonthsImplantSubcutaneousCheplapharm Arzneimittel Gmbh1997-02-10Not applicableCanada flag
Suprefact Depot 3 MonthsImplantSubcutaneousCheplapharm Arzneimittel Gmbh2000-02-24Not applicableCanada flag
Suprefact Inj 1mg/mlLiquidSubcutaneousHoechst Canada Inc.1988-12-311998-08-25Canada flag
Suprefact Intranasal Solution 1mg/mlSprayNasalHoechst Canada Inc.1988-12-311996-08-29Canada flag
Suprefact Liq 1mg/mlLiquidNasalHoechst Roussel Canada Inc.1993-12-312000-07-28Canada flag
Additional Data Available
  • Application Number
    Application Number

    A unique ID assigned by the FDA when a product is submitted for approval by the labeller.

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  • Product Code
    Product Code

    A governmentally-recognized ID which uniquely identifies the product within its regulatory market.

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Categories

ATC Codes
L02AE01 — Buserelin
Drug Categories
Chemical TaxonomyProvided by Classyfire
Description
Not Available
Kingdom
Organic Compounds
Super Class
Organic Acids
Class
Carboxylic Acids and Derivatives
Sub Class
Amino Acids, Peptides, and Analogues
Direct Parent
Peptides
Alternative Parents
Not Available
Substituents
Not Available
Molecular Framework
Not Available
External Descriptors
Not Available

Chemical Identifiers

UNII
PXW8U3YXDV
CAS number
57982-77-1

References

General References
  1. Link [Link]
KEGG Drug
D01831
PubChem Substance
347910362
RxNav
1825
ChEMBL
CHEMBL1909304
Wikipedia
Buserelin
AHFS Codes
  • 10:00.00 — Antineoplastic Agents
  • 92:00.00 — Miscellaneous Therapeutic Agents

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
4CompletedTreatmentFertility / Optimal Stimulation Protocol / Reproductive Endocrinology1
4CompletedTreatmentInfertility1
4CompletedTreatmentOHSS (Ovarian Hyperstimulation)1
4CompletedTreatmentOvarian Stimulation1
4CompletedTreatmentPregnancy1
4RecruitingTreatmentInfertility1
4TerminatedTreatmentAssisted Reproductive Technology therapy / Ovarian Stimulation1
3Active Not RecruitingTreatmentProstate Cancer3
3CompletedTreatmentProstate Cancer2
3Not Yet RecruitingTreatmentAdenocarcinoma, Prostate / Metastatic Malignant Neoplasm in the Bone / Stage III Prostate Cancer AJCC v8 / Stage IIIA Prostate Cancer AJCC v8 / Stage IIIB Prostate Cancer AJCC v8 / Stage IIIC Prostate Cancer AJCC v8 / Stage IVA Prostate Cancer AJCC v81

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not Available
Dosage Forms
FormRouteStrength
Implant6.3 MG
Implant9.45 MG
Injection, solution1 MG/ML
SolutionNasal
SolutionSubcutaneous
ImplantSubcutaneous
LiquidSubcutaneous
SprayNasal
LiquidNasal
Prices
Not Available
Patents
Not Available

Properties

State
Liquid
Experimental Properties
Not Available

Targets

Kind
Protein
Organism
Humans
Pharmacological action
Yes
General Function
Luteinizing hormone receptor activity
Specific Function
Receptor for lutropin-choriogonadotropic hormone. The activity of this receptor is mediated by G proteins which activate adenylate cyclase.
Gene Name
LHCGR
Uniprot ID
P22888
Uniprot Name
Lutropin-choriogonadotropic hormone receptor
Molecular Weight
78642.01 Da
References
  1. Kirby RS, Fitzpatrick JM, Clarke N: Abarelix and other gonadotrophin-releasing hormone antagonists in prostate cancer. BJU Int. 2009 Dec;104(11):1580-4. doi: 10.1111/j.1464-410X.2009.08924.x. [PubMed:20053189]
Kind
Protein
Organism
Humans
Pharmacological action
Yes
General Function
Peptide binding
Specific Function
Receptor for gonadotropin releasing hormone (GnRH) that mediates the action of GnRH to stimulate the secretion of the gonadotropic hormones luteinizing hormone (LH) and follicle-stimulating hormone...
Gene Name
GNRHR
Uniprot ID
P30968
Uniprot Name
Gonadotropin-releasing hormone receptor
Molecular Weight
37730.355 Da
References
  1. Kirby RS, Fitzpatrick JM, Clarke N: Abarelix and other gonadotrophin-releasing hormone antagonists in prostate cancer. BJU Int. 2009 Dec;104(11):1580-4. doi: 10.1111/j.1464-410X.2009.08924.x. [PubMed:20053189]

Enzymes

Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Inducer
General Function
Oxygen binding
Specific Function
Catalyzes the formation of aromatic C18 estrogens from C19 androgens.
Gene Name
CYP19A1
Uniprot ID
P11511
Uniprot Name
Aromatase
Molecular Weight
57882.48 Da
References
  1. Maeda K, Kitawaki J, Yokota K, Noguchi T, Urabe M, Yamamoto T, Honjo H: [Effects of gonadotropin-releasing hormone and its analogue (buserelin) on aromatase in cultured human granulosa cells]. Nihon Sanka Fujinka Gakkai Zasshi. 1996 Feb;48(2):89-95. [PubMed:8718543]

Drug created on June 07, 2010 16:44 / Updated on September 17, 2020 23:28

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