Leuprorelin - CAS 53714-56-0
Catalog number:
53714-56-0
Category:
Inhibitor
Not Intended for Therapeutic Use. For research use only.
Molecular Formula:
C59H84N16O12
Molecular Weight:
1209.41
COA:
Inquire
Targets:
GNRH Receptor
Description:
Leuprorelin is a gonadotropin-releasing hormone (GnRH) analogue used to treat prostate cancer and breast cancer.
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Purity:
≥95%
Appearance:
Lyophilised solid
Synonyms:
Leuprolide; Eligard; H-Pyr-His-Trp-Ser-Tyr-D-Leu-Leu-Arg-Pro-NHEt;
Solubility:
Soluble in DMSO
Storage:
Store at -20 °C
MSDS:
Inquire
Application:
An agonist at pituitary GnRH receptors
Quality Standard:
Enterprise Standard
Shelf Life:
As supplied, 2 years from the QC date provided on the Certificate of Analysis, when stored properly
Quantity:
Milligrams-Grams
Density:
1.44 g/cm3
InChIKey:
GFIJNRVAKGFPGQ-LIJARHBVSA-N
InChI:
1S/C59H84N16O12/c1-6-63-57(86)48-14-10-22-75(48)58(87)41(13-9-21-64-59(60)61)68-51(80)42(23-32(2)3)69-52(81)43(24-33(4)5)70-53(82)44(25-34-15-17-37(77)18-16-34)71-56(85)47(30-76)74-54(83)45(26-35-28-65-39-12-8-7-11-38(35)39)72-55(84)46(27-36-29-62-31-66-3
Canonical SMILES:
CCNC(=O)C1CCCN1C(=O)C(CCCN=C(N)N)NC(=O)C(CC(C)C)NC(=O)C(CC(C)C)NC(=O)C(CC2=CC=C(C=C2)O)NC(=O)C(CO)NC(=O)C(CC3=CNC4=CC=CC=C43)NC(=O)C(CC5=CN=CN5)NC(=O)C6CCC(=O)N6
Current Developer:
Tolmar
1.Efficacy and safety of leuprorelin acetate 6-month depot, TAP-144-SR (6M), in combination with tamoxifen in postoperative, premenopausal patients with hormone receptor-positive breast cancer: a phas
Kurebayashi J1, Toyama T2, Sumino S3, Miyajima E3, Fujimoto T3. Breast Cancer. 2016 Mar 26. [Epub ahead of print]
BACKGROUND: Leuprorelin acetate, a luteinizing hormone-releasing hormone agonist, is used worldwide in premenopausal women with hormone receptor-positive breast cancer. This study was conducted to assess the non-inferiority of the 6-month depot formulation, TAP-144-SR (6M) 22.5 mg to the 3-month depot formulation, TAP-144-SR (3M) 11.25 mg in postoperative, premenopausal patients with hormone receptor-positive breast cancer.
2.A RANKL Wrinkle: Denosumab-Induced Hypocalcemia.
Laskowski LK1, Goldfarb DS2, Howland MA3,4, Kavcsak K5, Lugassy DM3, Smith SW3. J Med Toxicol. 2016 Mar 17. [Epub ahead of print]
The human monoclonal antibody denosumab inhibits osteoclast-mediated bone resorption by binding to receptor activator of nuclear factor κB ligand (RANKL), which is upregulated by tumor cells. Denosumab is indicated to prevent skeletal-related events (SREs) from osteoporosis and metastatic bone disease. We report a case of denosumab-induced hypocalcemia to highlight potential toxicity and treatment considerations. A 66-year-old man with prostate cancer, small cell lung cancer, and bone metastases presented with fatigue, weakness, and muscle spasm. Sixteen days prior, he received cycle 6 of cisplatin and etoposide, leuprolide, and denosumab (120 mg subcutaneously). His examination demonstrated a slight resting tremor, normal strength, and negative Chvostek sign. Laboratory analysis revealed hemoglobin, 8.0 g/dL; total calcium, 5.2 mg/dL (pre-denosumab, 8.9 mg/dL); and magnesium, 0.7 mg/dL. He initially received two units packed red blood cells, intravenous calcium and magnesium, and vitamin D.
3.Simultaneous Measurement of Serum Chemical Castration Agents and Testosterone Levels Using Ultra-Performance Liquid Chromatography-Tandem Mass Spectrometry.
Ko DH1, Lee K2, Jeon SH3, Song SH4, Yun YM5, Chun S1, Kim HS6, Kim JY6, In MK6, Song J7. J Anal Toxicol. 2016 Mar 17. pii: bkw017. [Epub ahead of print]
Chemical castration involves administration of drugs to prevent pathological sexual behavior, reduce abnormal sexual drive and treat hormone-dependent cancers. Various drugs have been used for chemical castration; however, substantial interindividual variability and side effects are often observed. In this study, we proposed a useful monitoring method for the application of chemical castration agents using ultra-performance liquid chromatography-tandem mass spectrometry (UPLC-MS-MS). Testosterone, cyproterone acetate, medroxyprogesterone, goserelin acetate, leuprolide acetate and triptorelin acetate were analyzed by UPLC-MS-MS. The target drugs were extracted from serum samples by double protein precipitation using methanol. Testosterone-1,2-d2 and buserelin acetate were used as internal standards. Parameters of analytical performance were evaluated, including imprecision, linearity, ion suppression and detection capabilities. Testosterone measurements were compared with the results of immunoassays.
4.Interstitial pneumonitis secondary to leuprorelin acetate for prostate cancer.
Tan HE1, Lake F1. Respirol Case Rep. 2016 Mar 31;4(2):e00146. doi: 10.1002/rcr2.146. eCollection 2016.
Androgen blockade is standard treatment for advanced prostate cancer. We report an uncommon case of interstitial pneumonitis induced by leuprorelin acetate.
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