| Primary information |
|---|
| ThPP ID | Th1007 |
| Therapeutic Peptide/Protein Name | Leuprolide |
| Sequence | PHWSYLLR view full sequnce in fasta |
| Functional Classification | IIa |
| Molecular Weight | 1209.3983 |
| Chemical Formula | C59H84N16O12 |
| Isoelectric Point | N.A. |
| Hydrophobicity | 0.1 |
| Melting Point (℃) | N.A. |
| Half Life | Approximately 3 hours |
| Description | Leuprolide 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/Disease | To treat prostate cancer, endometriosis, uterine fibroids and premature puberty |
| Pharmacodynamics | Leuprolide 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 Action | Leuprolide binds to the gonadotropin releasing hormone receptor and acts as an efficient inhibitor of gonadotropin secretion. |
| Toxicity | Subcutaneous 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 |
| Metabolism | Primarily degraded by peptidase (instead of cytochrome P450 enzymes). |
| Absorption | Bioavailability by subcutaneous administration is comparable to that by intravenous administration. |
| Volume of Distribution | 27 L [intravenous bolus administration to healthy male volunteers] |
| Clearance | Excretion in urine, 8.34 L/hour [healthy male receiving a 1-mg IV bolus] |
| Categories | N.A. |
| Patents Number | N.A. |
| Date of Issue | N.A. |
| Date of Expiry | N.A. |
| Drug Interaction | N.A. |
| Target | N.A. |
| Information of corresponding available drug in the market |
|---|
| Brand Name | Lupron |
| Company | Abbott/TAP Pharmaceuticals |
| Brand Discription | N.A. |
| Prescribed for | N.A. |
| Chemical Name | N.A. |
| Formulation | N.A. |
| Physcial Appearnce | N.A. |
| Route of Administration | Injection |
| Recommended Dosage | 7.5 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. |
| Contraindication | Allergic, pregnancy, lactation |
| Side Effects | N.A. |
| Useful Link | http://trademarks.justia.com/761/06/leupromaxx-76106691.html |
| PubMed ID | 16370917, 15568711 |
| 3-D Structure | Th1007 (View) or (Download) |