| 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 | Antineoplastic Agents |
| Patents Number | N.A. |
| Date of Issue | N.A. |
| Date of Expiry | N.A. |
| Drug Interaction | N.A. |
| Target | Gonadotropin-releasing hormone receptor |
| Information of corresponding available drug in the market |
|---|
| Brand Name | Eligard |
| Company | Atrix Labs/QLT In |
| Brand Discription | ELIGARD 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 for | Eligard is used to treat the symptoms of prostate cancer in men. |
| Chemical Name | 5-oxo-L-prolyl-L-histidyl-L-tryptophyl-L-seryl-L-tyrosyl-D-leucyl-L-arginyl-N-ethyl-L-prolinamide acetate |
| Formulation | ELIGARD 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 Appearnce | Suspension |
| Route of Administration | Subcutaneous Injection |
| Recommended Dosage | 7.5mg-1 injection/month, 22.5mg-1 injection per 3 month, 30mg-1 injection per 4 month, 45 mg- 1 injection every 6 month. |
| Contraindication | Hypersensitivity and pregnancy |
| Side Effects | Rare 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 Link | Sequence 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 ID | 16370917, 15568711 |
| 3-D Structure | Th1007 (View) or (Download) |