==== 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


Details of Th1007 which contains 11 entries.


Entry 1
(1) Primary information
ID1038
ThPP IDTh1007
Therapeutic Peptide/Protein NameLeuprolide
SequencePHWSYLLR view full sequnce in fasta
Functional ClassificationIIa
Molecular Weight1209.3983
Chemical FormulaC59H84N16O12
Isoelectric PointN.A.
Hydrophobicity0.1
Melting Point (℃)N.A.
Half LifeApproximately 3 hours
DescriptionLeuprolide is a synthetic 9 residue peptide analog of gonadotropin releasing hormone belonging to the class of drugs called hormones or hormone antagonists. It is used to treat advanced prostate cancer, uterine fibroids and endometriosis (under investigation for possible use in the treatment of mild to moderate Alzheimer's disease).
Indication/DiseaseTo treat prostate cancer, endometriosis, uterine fibroids and premature puberty.
PharmacodynamicsLeuprolide is a luteinizing hormone agonist that results in suppression of testicular or follicular steroidogenesis thus used in the palliative treatment of advanced prostate cancer.
Mechanism of ActionLeuprolide binds to the gonadotropin releasing hormone receptor and acts as an efficient inhibitor of gonadotropin secretion.
ToxicitySubcutaneous administration of 250 to 500 times the recommended human dose in rats, expressed on a per body weight basis, resulted in dyspnea, decreased activity, and local irritation at the injection site. There is no evidence at present that there is a
MetabolismPrimarily degraded by peptidase (instead of cytochrome P450 enzymes).
AbsorptionBioavailability by subcutaneous administration is comparable to that by intravenous administration.
Volume of Distribution27 L [intravenous bolus administration to healthy male volunteers]
ClearanceExcretion in urine, 8.34 L/hour [healthy male receiving a 1-mg IV bolus]
CategoriesAntineoplastic Agents
Patents NumberN.A.
Date of IssueN.A.
Date of ExpiryN.A.
Drug InteractionN.A.
TargetGonadotropin-releasing hormone receptor
Information of corresponding available drug in the market
Brand NameEligard
CompanyAtrix Labs/QLT In
Brand DiscriptionELIGARD is a sterile polymeric matrix formulation of leuprolide acetate, a GnRH agonist, for subcutaneous injection, designed to deliver leuprolide acetate at a controlled rate over a one-, three-, four- or six-month therapeutic period.
Prescribed forEligard is used to treat the symptoms of prostate cancer in men.
Chemical Name5-oxo-L-prolyl-L-histidyl-L-tryptophyl-L-seryl-L-tyrosyl-D-leucyl-L-arginyl-N-ethyl-L-prolinamide acetate
FormulationELIGARD is prefilled and supplied in two separate, sterile syringes whose contents are mixed immediately prior to administration. The two syringes are joined and the single dose product is mixed until it is homogenous. One syringe contains the ATRIGEL De
Physcial AppearanceSuspension
Route of AdministrationSubcutaneous Injection
Recommended Dosage7.5mg-1 injection/month, 22.5mg-1 injection per 3 month, 30mg-1 injection per 4 month, 45 mg- 1 injection every 6 month.
ContraindicationHypersensitivity and pregnancy
Side EffectsRare pain or unusual sensations in your back; numbness, weakness, or tingly feeling in your legs or feet; muscle weakness or loss of use; loss of bowel or bladder control; or liver problems - nausea, upper stomach pain, itching, tired feeling, loss of apetite.
Useful LinkSequence Information Link:http://www.freepatentsonline.com/EP1790656.html# RxMed:http://www.rxmed.com/b.main/b2.pharmaceutical/b2.1.monographs/CPS-%20Monographs/CPS-%20(General%20Monographs-%20L)/LUPRON%20DEPOT.html
PubMed ID16370917, 15568711
3-D StructureTh1007 (View) or (Download)


Entry 2
(2) Primary information
ID1039
ThPP IDTh1007
Therapeutic Peptide/Protein NameLeuprolide
SequencePHWSYLLR view full sequnce in fasta
Functional ClassificationIIa
Molecular Weight1209.3983
Chemical FormulaC59H84N16O12
Isoelectric PointN.A.
Hydrophobicity0.1
Melting Point (℃)N.A.
Half LifeApproximately 3 hours
DescriptionLeuprolide is a synthetic 9 residue peptide analog of gonadotropin releasing hormone belonging to the class of drugs called hormones or hormone antagonists. It is used to treat advanced prostate cancer, uterine fibroids and endometriosis (under investigation for possible use in the treatment of mild to moderate Alzheimer's disease).
Indication/DiseaseTo treat prostate cancer, endometriosis, uterine fibroids and premature puberty
PharmacodynamicsLeuprolide is a luteinizing hormone agonist that results in suppression of testicular or follicular steroidogenesis thus used in the palliative treatment of advanced prostate cancer.
Mechanism of ActionLeuprolide binds to the gonadotropin releasing hormone receptor and acts as an efficient inhibitor of gonadotropin secretion.
ToxicitySubcutaneous administration of 250 to 500 times the recommended human dose in rats, expressed on a per body weight basis, resulted in dyspnea, decreased activity, and local irritation at the injection site. There is no evidence at present that there is a
MetabolismPrimarily degraded by peptidase (instead of cytochrome P450 enzymes).
AbsorptionBioavailability by subcutaneous administration is comparable to that by intravenous administration.
Volume of Distribution27 L [intravenous bolus administration to healthy male volunteers]
ClearanceExcretion in urine, 8.34 L/hour [healthy male receiving a 1-mg IV bolus]
CategoriesHormonal and Fertility Agents
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 NameEnantone
CompanyTakeda
Brand DiscriptionN.A.
Prescribed forN.A.
Chemical NameN.A.
FormulationN.A.
Physcial AppearanceSolution
Route of AdministrationInjection
Recommended DosageOne3.75 mg DPS mnthly or one 11.25 mg DPS every 3 month as a single SC/IM injection.
ContraindicationHypersensitivity, undiagnosed abnormal vag bleeding, pregnancy, lactation
Side EffectsWeightloss, Parosmia (distortion of the sense of smell, as in smelling odours that are not present), Nausea (feeling of having an urge to vomit), Musculoskeletal Stiffness (stiffness of the body's muscles, joints, tendons, ligaments and nerves), Mood Swinng.
Useful Linkhttp://www.eligard.com
PubMed ID16370917, 15568711
3-D StructureTh1007 (View) or (Download)


Entry 3
(3) Primary information
ID1040
ThPP IDTh1007
Therapeutic Peptide/Protein NameLeuprolide
SequencePHWSYLLR view full sequnce in fasta
Functional ClassificationIIa
Molecular Weight1209.3983
Chemical FormulaC59H84N16O12
Isoelectric PointN.A.
Hydrophobicity0.1
Melting Point (℃)N.A.
Half LifeApproximately 3 hours
DescriptionLeuprolide is a synthetic 9 residue peptide analog of gonadotropin releasing hormone belonging to the class of drugs called hormones or hormone antagonists. It is used to treat advanced prostate cancer, uterine fibroids and endometriosis (under investigation for possible use in the treatment of mild to moderate Alzheimer's disease).
Indication/DiseaseTo treat prostate cancer, endometriosis, uterine fibroids and premature puberty
PharmacodynamicsLeuprolide is a luteinizing hormone agonist that results in suppression of testicular or follicular steroidogenesis thus used in the palliative treatment of advanced prostate cancer.
Mechanism of ActionLeuprolide binds to the gonadotropin releasing hormone receptor and acts as an efficient inhibitor of gonadotropin secretion.
ToxicitySubcutaneous administration of 250 to 500 times the recommended human dose in rats, expressed on a per body weight basis, resulted in dyspnea, decreased activity, and local irritation at the injection site. There is no evidence at present that there is a
MetabolismPrimarily degraded by peptidase (instead of cytochrome P450 enzymes).
AbsorptionBioavailability by subcutaneous administration is comparable to that by intravenous administration.
Volume of Distribution27 L [intravenous bolus administration to healthy male volunteers]
ClearanceExcretion in urine, 8.34 L/hour [healthy male receiving a 1-mg IV bolus]
CategoriesFemale and Estrogen Antagonists
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 NameLeuplin
CompanyTakeda
Brand DiscriptionN.A.
Prescribed forN.A.
Chemical NameN.A.
FormulationN.A.
Physcial AppearanceN.A.
Route of AdministrationInjection
Recommended DosageN.A.
ContraindicationN.A.
Side EffectsN.A.
Useful Linkhttp://www.drugs.com/drug-interactions/leuprolide,eligard-index.html
PubMed ID16370917, 15568711
3-D StructureTh1007 (View) or (Download)


Entry 4
(4) Primary information
ID1041
ThPP IDTh1007
Therapeutic Peptide/Protein NameLeuprolide
SequencePHWSYLLR view full sequnce in fasta
Functional ClassificationIIa
Molecular Weight1209.3983
Chemical FormulaC59H84N16O12
Isoelectric PointN.A.
Hydrophobicity0.1
Melting Point (℃)N.A.
Half LifeApproximately 3 hours
DescriptionLeuprolide is a synthetic 9 residue peptide analog of gonadotropin releasing hormone belonging to the class of drugs called hormones or hormone antagonists. It is used to treat advanced prostate cancer, uterine fibroids and endometriosis (under investigation for possible use in the treatment of mild to moderate Alzheimer's disease).
Indication/DiseaseTo treat prostate cancer, endometriosis, uterine fibroids and premature puberty
PharmacodynamicsLeuprolide is a luteinizing hormone agonist that results in suppression of testicular or follicular steroidogenesis thus used in the palliative treatment of advanced prostate cancer.
Mechanism of ActionLeuprolide binds to the gonadotropin releasing hormone receptor and acts as an efficient inhibitor of gonadotropin secretion.
ToxicitySubcutaneous administration of 250 to 500 times the recommended human dose in rats, expressed on a per body weight basis, resulted in dyspnea, decreased activity, and local irritation at the injection site. There is no evidence at present that there is a
MetabolismPrimarily degraded by peptidase (instead of cytochrome P450 enzymes).
AbsorptionBioavailability by subcutaneous administration is comparable to that by intravenous administration.
Volume of Distribution27 L [intravenous bolus administration to healthy male volunteers]
ClearanceExcretion in urine, 8.34 L/hour [healthy male receiving a 1-mg IV bolus]
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 NameLeuProMaxx
CompanyBaxter/Teva
Brand DiscriptionN.A.
Prescribed forN.A.
Chemical NameN.A.
FormulationN.A.
Physcial AppearanceN.A.
Route of AdministrationN.A.
Recommended DosageN.A.
ContraindicationN.A.
Side EffectsN.A.
Useful Linkhttp://www.mims.com/THAILAND/drug/info/Enantone%20L-P-
PubMed ID16370917, 15568711
3-D StructureTh1007 (View) or (Download)


Entry 5
(5) Primary information
ID1042
ThPP IDTh1007
Therapeutic Peptide/Protein NameLeuprolide
SequencePHWSYLLR view full sequnce in fasta
Functional ClassificationIIa
Molecular Weight1209.3983
Chemical FormulaC59H84N16O12
Isoelectric PointN.A.
Hydrophobicity0.1
Melting Point (℃)N.A.
Half LifeApproximately 3 hours
DescriptionLeuprolide is a synthetic 9 residue peptide analog of gonadotropin releasing hormone belonging to the class of drugs called hormones or hormone antagonists. It is used to treat advanced prostate cancer, uterine fibroids and endometriosis (under investigation for possible use in the treatment of mild to moderate Alzheimer's disease).
Indication/DiseaseTo treat prostate cancer, endometriosis, uterine fibroids and premature puberty
PharmacodynamicsLeuprolide is a luteinizing hormone agonist that results in suppression of testicular or follicular steroidogenesis thus used in the palliative treatment of advanced prostate cancer.
Mechanism of ActionLeuprolide binds to the gonadotropin releasing hormone receptor and acts as an efficient inhibitor of gonadotropin secretion.
ToxicitySubcutaneous administration of 250 to 500 times the recommended human dose in rats, expressed on a per body weight basis, resulted in dyspnea, decreased activity, and local irritation at the injection site. There is no evidence at present that there is a
MetabolismPrimarily degraded by peptidase (instead of cytochrome P450 enzymes).
AbsorptionBioavailability by subcutaneous administration is comparable to that by intravenous administration.
Volume of Distribution27 L [intravenous bolus administration to healthy male volunteers]
ClearanceExcretion in urine, 8.34 L/hour [healthy male receiving a 1-mg IV bolus]
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 NameLeupromer
CompanyN.A.
Brand DiscriptionN.A.
Prescribed forN.A.
Chemical NameN.A.
FormulationN.A.
Physcial AppearanceN.A.
Route of AdministrationInjection
Recommended DosageN.A.
ContraindicationN.A.
Side EffectsN.A.
Useful Linkhttps://www.takeda.com/news/2014/20140905_6740.html
PubMed ID16370917, 15568711
3-D StructureTh1007 (View) or (Download)


Entry 6
(6) Primary information
ID1043
ThPP IDTh1007
Therapeutic Peptide/Protein NameLeuprolide
SequencePHWSYLLR view full sequnce in fasta
Functional ClassificationIIa
Molecular Weight1209.3983
Chemical FormulaC59H84N16O12
Isoelectric PointN.A.
Hydrophobicity0.1
Melting Point (℃)N.A.
Half LifeApproximately 3 hours
DescriptionLeuprolide is a synthetic 9 residue peptide analog of gonadotropin releasing hormone belonging to the class of drugs called hormones or hormone antagonists. It is used to treat advanced prostate cancer, uterine fibroids and endometriosis (under investigation for possible use in the treatment of mild to moderate Alzheimer's disease).
Indication/DiseaseTo treat prostate cancer, endometriosis, uterine fibroids and premature puberty
PharmacodynamicsLeuprolide is a luteinizing hormone agonist that results in suppression of testicular or follicular steroidogenesis thus used in the palliative treatment of advanced prostate cancer.
Mechanism of ActionLeuprolide binds to the gonadotropin releasing hormone receptor and acts as an efficient inhibitor of gonadotropin secretion.
ToxicitySubcutaneous administration of 250 to 500 times the recommended human dose in rats, expressed on a per body weight basis, resulted in dyspnea, decreased activity, and local irritation at the injection site. There is no evidence at present that there is a
MetabolismPrimarily degraded by peptidase (instead of cytochrome P450 enzymes).
AbsorptionBioavailability by subcutaneous administration is comparable to that by intravenous administration.
Volume of Distribution27 L [intravenous bolus administration to healthy male volunteers]
ClearanceExcretion in urine, 8.34 L/hour [healthy male receiving a 1-mg IV bolus]
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 NameLupron
CompanyAbbott/TAP Pharmaceuticals
Brand DiscriptionN.A.
Prescribed forN.A.
Chemical NameN.A.
FormulationN.A.
Physcial AppearanceN.A.
Route of AdministrationInjection
Recommended Dosage7.5 mg for 1-month, 22.5 mg for 3-month, 30 mg for 4-month, and 45 mg for 6-month administration are prescribed for the palliative treatment of advanced prostate cancer, 3.75 mg for 1-month and 11.25 mg for 3-month administration are used for the manageme.
ContraindicationAllergic, pregnancy, lactation
Side EffectsN.A.
Useful Linkhttp://trademarks.justia.com/761/06/leupromaxx-76106691.html
PubMed ID16370917, 15568711
3-D StructureTh1007 (View) or (Download)


Entry 7
(7) Primary information
ID1044
ThPP IDTh1007
Therapeutic Peptide/Protein NameLeuprolide
SequencePHWSYLLR view full sequnce in fasta
Functional ClassificationIIa
Molecular Weight1209.3983
Chemical FormulaC59H84N16O12
Isoelectric PointN.A.
Hydrophobicity0.1
Melting Point (℃)N.A.
Half LifeApproximately 3 hours
DescriptionLeuprolide is a synthetic 9 residue peptide analog of gonadotropin releasing hormone belonging to the class of drugs called hormones or hormone antagonists. It is used to treat advanced prostate cancer, uterine fibroids and endometriosis (under investigation for possible use in the treatment of mild to moderate Alzheimer's disease).
Indication/DiseaseTo treat prostate cancer, endometriosis, uterine fibroids and premature puberty
PharmacodynamicsLeuprolide is a luteinizing hormone agonist that results in suppression of testicular or follicular steroidogenesis thus used in the palliative treatment of advanced prostate cancer.
Mechanism of ActionLeuprolide binds to the gonadotropin releasing hormone receptor and acts as an efficient inhibitor of gonadotropin secretion.
ToxicitySubcutaneous administration of 250 to 500 times the recommended human dose in rats, expressed on a per body weight basis, resulted in dyspnea, decreased activity, and local irritation at the injection site. There is no evidence at present that there is a
MetabolismPrimarily degraded by peptidase (instead of cytochrome P450 enzymes).
AbsorptionBioavailability by subcutaneous administration is comparable to that by intravenous administration.
Volume of Distribution27 L [intravenous bolus administration to healthy male volunteers]
ClearanceExcretion in urine, 8.34 L/hour [healthy male receiving a 1-mg IV bolus]
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 NameLutrate
CompanyN.A.
Brand DiscriptionN.A.
Prescribed forN.A.
Chemical NameN.A.
FormulationN.A.
Physcial AppearanceN.A.
Route of AdministrationN.A.
Recommended DosageN.A.
ContraindicationN.A.
Side EffectsN.A.
Useful Linkhttp://www.lupron.com/ http://www.drugs.com/lupron.html
PubMed ID16370917, 15568711
3-D StructureTh1007 (View) or (Download)


Entry 8
(8) Primary information
ID1045
ThPP IDTh1007
Therapeutic Peptide/Protein NameLeuprolide
SequencePHWSYLLR view full sequnce in fasta
Functional ClassificationIIa
Molecular Weight1209.3983
Chemical FormulaC59H84N16O12
Isoelectric PointN.A.
Hydrophobicity0.1
Melting Point (℃)N.A.
Half LifeApproximately 3 hours
DescriptionLeuprolide is a synthetic 9 residue peptide analog of gonadotropin releasing hormone belonging to the class of drugs called hormones or hormone antagonists. It is used to treat advanced prostate cancer, uterine fibroids and endometriosis (under investigation for possible use in the treatment of mild to moderate Alzheimer's disease).
Indication/DiseaseTo treat prostate cancer, endometriosis, uterine fibroids and premature puberty
PharmacodynamicsLeuprolide is a luteinizing hormone agonist that results in suppression of testicular or follicular steroidogenesis thus used in the palliative treatment of advanced prostate cancer.
Mechanism of ActionLeuprolide binds to the gonadotropin releasing hormone receptor and acts as an efficient inhibitor of gonadotropin secretion.
ToxicitySubcutaneous administration of 250 to 500 times the recommended human dose in rats, expressed on a per body weight basis, resulted in dyspnea, decreased activity, and local irritation at the injection site. There is no evidence at present that there is a
MetabolismPrimarily degraded by peptidase (instead of cytochrome P450 enzymes).
AbsorptionBioavailability by subcutaneous administration is comparable to that by intravenous administration.
Volume of Distribution27 L [intravenous bolus administration to healthy male volunteers]
ClearanceExcretion in urine, 8.34 L/hour [healthy male receiving a 1-mg IV bolus]
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 NameMemryte
CompanyCuraxis
Brand DiscriptionN.A.
Prescribed forN.A.
Chemical NameN.A.
FormulationN.A.
Physcial AppearanceN.A.
Route of AdministrationN.A.
Recommended DosageN.A.
ContraindicationN.A.
Side EffectsN.A.
Useful Linkhttps://www.takeda.com/news/2012/20120229_3944.html
PubMed ID16370917, 15568711
3-D StructureTh1007 (View) or (Download)


Entry 9
(9) Primary information
ID1046
ThPP IDTh1007
Therapeutic Peptide/Protein NameLeuprolide
SequencePHWSYLLR view full sequnce in fasta
Functional ClassificationIIa
Molecular Weight1209.3983
Chemical FormulaC59H84N16O12
Isoelectric PointN.A.
Hydrophobicity0.1
Melting Point (℃)N.A.
Half LifeApproximately 3 hours
DescriptionLeuprolide is a synthetic 9 residue peptide analog of gonadotropin releasing hormone belonging to the class of drugs called hormones or hormone antagonists. It is used to treat advanced prostate cancer, uterine fibroids and endometriosis (under investigation for possible use in the treatment of mild to moderate Alzheimer's disease).
Indication/DiseaseTo treat prostate cancer, endometriosis, uterine fibroids and premature puberty
PharmacodynamicsLeuprolide is a luteinizing hormone agonist that results in suppression of testicular or follicular steroidogenesis thus used in the palliative treatment of advanced prostate cancer.
Mechanism of ActionLeuprolide binds to the gonadotropin releasing hormone receptor and acts as an efficient inhibitor of gonadotropin secretion.
ToxicitySubcutaneous administration of 250 to 500 times the recommended human dose in rats, expressed on a per body weight basis, resulted in dyspnea, decreased activity, and local irritation at the injection site. There is no evidence at present that there is a
MetabolismPrimarily degraded by peptidase (instead of cytochrome P450 enzymes).
AbsorptionBioavailability by subcutaneous administration is comparable to that by intravenous administration.
Volume of Distribution27 L [intravenous bolus administration to healthy male volunteers]
ClearanceExcretion in urine, 8.34 L/hour [healthy male receiving a 1-mg IV bolus]
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 NameProstap 3
CompanyTakeda UK Limited
Brand DiscriptionN.A.
Prescribed forN.A.
Chemical NameN.A.
FormulationN.A.
Physcial AppearanceN.A.
Route of AdministrationN.A.
Recommended DosageN.A.
ContraindicationN.A.
Side EffectsN.A.
Useful Linkhttp://www.rxlist.com/eligard-drug.htm
PubMed ID16370917, 15568711
3-D StructureTh1007 (View) or (Download)


Entry 10
(10) Primary information
ID1047
ThPP IDTh1007
Therapeutic Peptide/Protein NameLeuprolide
SequencePHWSYLLR view full sequnce in fasta
Functional ClassificationIIa
Molecular Weight1209.3983
Chemical FormulaC59H84N16O12
Isoelectric PointN.A.
Hydrophobicity0.1
Melting Point (℃)N.A.
Half LifeApproximately 3 hours
DescriptionLeuprolide is a synthetic 9 residue peptide analog of gonadotropin releasing hormone belonging to the class of drugs called hormones or hormone antagonists. It is used to treat advanced prostate cancer, uterine fibroids and endometriosis (under investigation for possible use in the treatment of mild to moderate Alzheimer's disease).
Indication/DiseaseTo treat prostate cancer, endometriosis, uterine fibroids and premature puberty
PharmacodynamicsLeuprolide is a luteinizing hormone agonist that results in suppression of testicular or follicular steroidogenesis thus used in the palliative treatment of advanced prostate cancer.
Mechanism of ActionLeuprolide binds to the gonadotropin releasing hormone receptor and acts as an efficient inhibitor of gonadotropin secretion.
ToxicitySubcutaneous administration of 250 to 500 times the recommended human dose in rats, expressed on a per body weight basis, resulted in dyspnea, decreased activity, and local irritation at the injection site. There is no evidence at present that there is a
MetabolismPrimarily degraded by peptidase (instead of cytochrome P450 enzymes).
AbsorptionBioavailability by subcutaneous administration is comparable to that by intravenous administration.
Volume of Distribution27 L [intravenous bolus administration to healthy male volunteers]
ClearanceExcretion in urine, 8.34 L/hour [healthy male receiving a 1-mg IV bolus]
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 NameProstap SR
CompanyTakeda UK Limited
Brand DiscriptionN.A.
Prescribed forN.A.
Chemical NameN.A.
FormulationN.A.
Physcial AppearanceN.A.
Route of AdministrationN.A.
Recommended DosageN.A.
ContraindicationN.A.
Side EffectsN.A.
Useful Linkhttp://clinicaltrials.gov/ct2/show/record/NCT02167893
PubMed ID16370917, 15568711
3-D StructureTh1007 (View) or (Download)


Entry 11
(11) Primary information
ID1048
ThPP IDTh1007
Therapeutic Peptide/Protein NameLeuprolide
SequencePHWSYLLR view full sequnce in fasta
Functional ClassificationIIa
Molecular Weight1209.3983
Chemical FormulaC59H84N16O12
Isoelectric PointN.A.
Hydrophobicity0.1
Melting Point (℃)N.A.
Half LifeApproximately 3 hours
DescriptionLeuprolide is a synthetic 9 residue peptide analog of gonadotropin releasing hormone belonging to the class of drugs called hormones or hormone antagonists. It is used to treat advanced prostate cancer, uterine fibroids and endometriosis (under investigation for possible use in the treatment of mild to moderate Alzheimer's disease).
Indication/DiseaseTo treat prostate cancer, endometriosis, uterine fibroids and premature puberty
PharmacodynamicsLeuprolide is a luteinizing hormone agonist that results in suppression of testicular or follicular steroidogenesis thus used in the palliative treatment of advanced prostate cancer.
Mechanism of ActionLeuprolide binds to the gonadotropin releasing hormone receptor and acts as an efficient inhibitor of gonadotropin secretion.
ToxicitySubcutaneous administration of 250 to 500 times the recommended human dose in rats, expressed on a per body weight basis, resulted in dyspnea, decreased activity, and local irritation at the injection site. There is no evidence at present that there is a
MetabolismPrimarily degraded by peptidase (instead of cytochrome P450 enzymes).
AbsorptionBioavailability by subcutaneous administration is comparable to that by intravenous administration.
Volume of Distribution27 L [intravenous bolus administration to healthy male volunteers]
ClearanceExcretion in urine, 8.34 L/hour [healthy male receiving a 1-mg IV bolus]
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 NameViadur
CompanyBayer AG
Brand DiscriptionN.A.
Prescribed forN.A.
Chemical Name5-Oxo-L-prolyl-L-histidyl-L-tryptophyl-L-seryl-L-tyrosyl-D-leucyl-Lleucyl-L-arginyl-N-ethyl-L-prolinamide acetate
FormulationN.A.
Physcial AppearanceN.A.
Route of AdministrationN.A.
Recommended DosageN.A.
ContraindicationN.A.
Side EffectsN.A.
Useful Linkhttp://www.varianpharmed.com/en/products/gnrh/leupromer
PubMed ID16370917, 15568711
3-D StructureTh1007 (View) or (Download)