==== Reference: Usmani SS, Bedi G, Samuel JS, Singh S, Kalra S, Kumar P, et al. (2017) THPdb: Database of FDA-approved peptide and protein therapeutics. PLoS ONE 12(7) e0181748.====

Detailed description page of THPdb

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1601 details
Primary information
ThPP IDTh1127
Therapeutic Peptide/Protein NameBuserelin
SequencepGlu-His-Trp-Ser-Tyr-D-Ser(tBu)-Leu-Arg-Pro-NHEt view full sequnce in fasta
Functional ClassificationIIIc
Molecular WeightN.A.
Chemical FormulaC62H90N16O15
Isoelectric PointN.A.
HydrophobicityN.A.
Melting Point (℃)N.A.
Half Life50-80 minutes by IV dose, 80 mins. By SC dose, 1-2 hrs by Intranasal dose
DescriptionBuserelin is a luteinizing hormone-releasing hormone (LHRH) agonist. It is a synthetic hormone which stimulates the pituitary gland's gonadotrophin-releasing hormone receptor (GnRHR) and is used in prostate cancer treatment.
Indication/DiseaseBuserelin 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.
PharmacodynamicsN.A.
Mechanism of ActionBuserelin stimulates the pituitary gland's gonadotrophin-releasing hormone receptor (GnRHR). Buserelin desensitizes the GnRH receptor, reducing the amount of LH and testosterone. However, there is a concomitant surge in LH and testosterone levels with the decrease in androgens, so antiandrogens must administered.
ToxicityN.A.
MetabolismN.A.
AbsorptionN.A.
Volume of DistributionN.A.
ClearanceN.A.
CategoriesN.A.
Patents NumberN.A.
Date of IssueN.A.
Date of ExpiryN.A.
Drug InteractionN.A.
TargetN.A.
Information of corresponding available drug in the market
Brand NameSuprecur (injection)
CompanySanofi-Aventis
Brand DiscriptionSuprecur 1mg/ml Injection (called Suprecur Injection throughout this leaflet). It contains a medicine called buserelin acetate. This belongs to a group of medicines called gonadotropin releasing hormone analogues. This is a synthetic version of a hormone that occurs naturally in the body. It works by lowering the production of sex hormones. It can be used to treat infertility. It works by stopping the natural production of hormones that control ovulation. Synthetic hormones are then used to artificially stimulate ovulation. Your doctor should give you more information about how your treatment works.
Prescribed for infertility
Chemical NameN.A.
FormulationEach 1ml of solution contains 1 milligram of the active substance, buserelin as buserelin acetate. The other ingredients are, sodium chloride, sodium dihydrogen phosphate, sodium hydroxide, benzyl alcohol and water for injections
Physcial Appearnce1mg/ml Injection
Route of AdministrationSubcutaneous
Recommended DosageTreatment starts on day 1 or day 21 of menstrual cycle. Daily dose is: 200 to 500 micrograms given as a single daily injection or 500 micrograms twice a day; Daily injections until blood tests show that levels of sex hormones are lowered. This usually takes one to three weeks; After this other hormones along with Suprecur Injection;Doctor determines the treatment time
ContraindicationDo not have this medicine and tell your doctor if: Allergy (hypersensitive) to buserelin or other similar medicines such as goserelin, or any of the other ingredients of Suprecur Injection. Abnormal menstrual bleeding Pregnancy or breast-feeding A tumour that is not affected by changes in hormone levels. This medicine is for use in women only. However there is another form of this medicine that can be used in men. Men should not use either form of this medicine if they have had their testicles removed.
Side EffectsN.A.
Useful Linkhttp://www.drugs.com/uk/pdf/leaflet/468557.pdf
PubMed ID25496312, 25293536, 25276180, 24690459, 24657556
3-D StructureN.A.