Details
| Stereochemistry | ABSOLUTE |
| Molecular Formula | C72H96ClN17O14.C2H4O2 |
| Molecular Weight | 1519.1459 |
| Optical Activity | UNSPECIFIED |
| Defined Stereocenters | 10 / 10 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
CC(O)=O.CCCC[C@H](NC(=O)[C@@H](CCCCNC(N)=O)NC(=O)[C@H](CC1=CC=C(O)C=C1)N(C)C(=O)[C@H](CO)NC(=O)[C@@H](CC2=CN=CC=C2)NC(=O)[C@@H](CC3=CC=C(Cl)C=C3)NC(=O)[C@@H](CC4=CC5=CC=CC=C5C=C4)NC(C)=O)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N6CCC[C@H]6C(=O)N[C@H](C)C(N)=O
InChI
InChIKey=WMTZITCJULQSAS-FDIISDFSSA-N
InChI=1S/C72H96ClN17O14.C2H4O2/c1-5-6-17-52(63(96)85-54(19-12-33-79-71(75)76)70(103)90-34-13-20-59(90)67(100)81-42(2)61(74)94)83-62(95)53(18-9-10-32-80-72(77)104)84-68(101)60(39-45-24-29-51(93)30-25-45)89(4)69(102)58(41-91)88-66(99)57(38-47-14-11-31-78-40-47)87-65(98)56(36-44-22-27-50(73)28-23-44)86-64(97)55(82-43(3)92)37-46-21-26-48-15-7-8-16-49(48)35-46;1-2(3)4/h7-8,11,14-16,21-31,35,40,42,52-60,91,93H,5-6,9-10,12-13,17-20,32-34,36-39,41H2,1-4H3,(H2,74,94)(H,81,100)(H,82,92)(H,83,95)(H,84,101)(H,85,96)(H,86,97)(H,87,98)(H,88,99)(H4,75,76,79)(H3,77,80,104);1H3,(H,3,4)/t42-,52+,53-,54+,55-,56-,57-,58+,59+,60+;/m1./s1
Ozarelix is a luteinizing hormone-releasing hormone (LHRH) antagonist. It is known that LHRH antagonist exerts rapid inhibition of luteinizing hormone and follicle stimulating hormone with an accompanying rapid decrease in sex hormones. Thus this inhibitor can be effective in a variety of hormonally dependent disease including prostate cancer, benign prostatic hyperplasia (BPH), and endometriosis. Ozarelix was developed for the treatment of all these diseases including Alzheimer's disease. However, in January 2010 Spectrum Pharmaceuticals announced that it was discontinuing development of ozarelix in BPH. Because the low-dose intermittent therapy was disappointing in the treatment of lower urinary tract symptoms in men with BPH. The development of the drug for Alzheimer's disease was also discontinued. Ozarelix completed phase II trials for the treatment of prostate cancer and is in preclinical trials for the treatment of endometriosis and ovarian cancer.
Approval Year
PubMed
| Title | Date | PubMed |
|---|---|---|
| The impact of polyelectrolyte structure on the shape of nanoassemblies with cationic peptides. | 2013-08 |
|
| Fluorescence spectroscopic determination of the critical aggregation concentration of the GnRH antagonists Cetrorelix, Teverelix and Ozarelix. | 2010-11 |
|
| Ozarelix, a fourth generation GnRH antagonist, induces apoptosis in hormone refractory androgen receptor negative prostate cancer cells modulating expression and activity of death receptors. | 2010-09-01 |
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DTXSID20237851
Created by
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896710-46-6
Created by
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NON-SPECIFIC STOICHIOMETRY | |||
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05D1DCL744
Created by
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71587850
Created by
admin on Mon Mar 31 21:15:43 GMT 2025 , Edited by admin on Mon Mar 31 21:15:43 GMT 2025
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PRIMARY |
ACTIVE MOIETY
SUBSTANCE RECORD