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| ln Vitro |
Degarelix exhibits only very weak histamine-releasing properties and has the lowest histamine-releasing capacity among LHRH antagonists, including Cetrorelix, Abarelix, and Ganirelix [1]. Degarelix (1 nM-10 μM, 0-72 hours) reduces cell viability in all prostate cell lines (WPE1-NA22, WPMY-1, BPH-1, VCaP cells), except PC-3 cells [2] . Degarelix (10 μM, 0-72 hours) exerts a direct effect on prostate cell growth through apoptosis [2]. Cell viability assay[2] Cell lines: WPMY-1, WPE1-NA22, BPH-1, LNCaP and VCaP Concentration: 1 nM-10 μM Incubation time: 48 hours and 72 hours for WPMY-1 cells, 72 hours for WPE1-NA22 cells , BPH-1 cells (48 hours and 72 hours), LNCaP cells (48 hours and 72 hours) Results: Cell viability was reduced in all prostate cell lines except PC-3 cells. Apoptosis analysis[2] Cell lines: WPE1-NA22, BPH-1, LNCaP and VCaP Concentration: 10 μM Incubation time: 24, 48 and 72 hours Results: Induced significant increase in caspase 3/7 activation.
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| ln Vivo |
Degarelix (0-10 μg/kg; subcutaneous injection; once) reduces plasma LH levels and plasma testosterone levels in castrated rats in a dose-dependent manner [3]. Degarelix is stable when incubated in microsomes and cryopreserved hepatocytes from animal liver tissue. In rats and dogs, the majority of the degarelix dose is eliminated via urine and feces in equal amounts (40-50% in each matrix) within 48 hours, whereas in monkeys the main route of excretion is feces (50 %) and kidney (22%)[4]. Animal model: Male Sprague-Dawley rat, castrated [3] Dosage: 0.3, 1, 3 and 10 μg/kg or 12.5, 50 and 200 μg/kg Administration: subcutaneous injection, once Result: Dose-dependent And the minimum reversible effective dose is 3 μg/kg to reduce plasma LH levels. For the 50 μg/kg and 200 μg/kg doses, absorption t1/2 values were 4 minutes and 30 minutes, Tmax values were 1 hour and 5 hours, and apparent plasma disappearance t1/2 values were 12 hours and 67 hours, respectively. The minimum effective dose is 1 μg/kg, and plasma testosterone levels decrease in a dose-dependent manner.
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| References |
[1]. Rick FG, et al. An update on the use of degarelix in the treatment of advanced hormone-dependent prostate cancer. Onco Targets Ther. 2013 Apr 16;6:391-402.
[2]. Sakai M, et al. In search of the molecular mechanisms mediating the inhibitory effect of the GnRH antagonistdegarelix on human prostate cell growth. PLoS One. 2015 Mar 26;10(3):e0120670. [3]. Broqua P, et al. Pharmacological profile of a new, potent, and long-acting gonadotropin-releasing hormoneantagonist: degarelix. J Pharmacol Exp Ther. 2002 Apr;301(1):95-102. [4]. Sonesson A, et al. Metabolite profiles of degarelix, a new gonadotropin-releasing hormone receptor antagonist, in rat, dog, and monkey. Drug Metab Dispos. 2011 Oct;39(10):1895-903. |
| Molecular Formula |
C84H107CLN18O18
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|---|---|
| Molecular Weight |
1692.31
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| Exact Mass |
1690.77
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| Elemental Analysis |
C, 60.34; H, 6.36; Cl, 2.17; N, 15.45; O, 15.68
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| CAS # |
934246-14-7
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| Related CAS # |
Degarelix; 214766-78-6
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| Appearance |
White to off-white solid powder
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| SMILES |
C[C@H](C(=O)N)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCNC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CC2=CC=C(C=C2)NC(=O)N)NC(=O)[C@H](CC3=CC=C(C=C3)NC(=O)[C@@H]4CC(=O)NC(=O)N4)NC(=O)[C@H](CO)NC(=O)[C@@H](CC5=CN=CC=C5)NC(=O)[C@@H](CC6=CC=C(C=C6)Cl)NC(=O)[C@@H](CC7=CC8=CC=CC=C8C=C7)NC(=O)C.CC(=O)O.O
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| InChi Key |
QMBXFMRFTMPFEY-YECCWIQASA-N
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| InChi Code |
InChI=1S/C82H103ClN18O16.C2H4O2.H2O/c1-45(2)35-60(72(107)92-59(16-9-10-33-87-46(3)4)80(115)101-34-12-17-68(101)79(114)88-47(5)70(84)105)93-74(109)63(38-51-23-30-58(31-24-51)91-81(85)116)95-76(111)64(39-50-21-28-57(29-22-50)90-71(106)66-42-69(104)100-82(117)99-66)97-78(113)67(44-102)98-77(112)65(41-53-13-11-32-86-43-53)96-75(110)62(37-49-19-26-56(83)27-20-49)94-73(108)61(89-48(6)103)40-52-18-25-54-14-7-8-15-55(54)36-52;1-2(3)4;/h7-8,11,13-15,18-32,36,43,45-47,59-68,87,102H,9-10,12,16-17,33-35,37-42,44H2,1-6H3,(H2,84,105)(H,88,114)(H,89,103)(H,90,106)(H,92,107)(H,93,109)(H,94,108)(H,95,111)(H,96,110)(H,97,113)(H,98,112)(H3,85,91,116)(H2,99,100,104,117);1H3,(H,3,4);1H2/t47-,59+,60+,61-,62-,63-,64+,65-,66+,67+,68+;;/m1../s1
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| Chemical Name |
(4S)-N-[4-[(2S)-2-[[(2S)-2-[[(2R)-2-[[(2R)-2-[[(2R)-2-acetamido-3-naphthalen-2-ylpropanoyl]amino]-3-(4-chlorophenyl)propanoyl]amino]-3-pyridin-3-ylpropanoyl]amino]-3-hydroxypropanoyl]amino]-3-[[(2R)-1-[[(2S)-1-[[(2S)-1-[(2S)-2-[[(2R)-1-amino-1-oxopropan-2-yl]carbamoyl]pyrrolidin-1-yl]-1-oxo-6-(propan-2-ylamino)hexan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-[4-(carbamoylamino)phenyl]-1-oxopropan-2-yl]amino]-3-oxopropyl]phenyl]-2,6-dioxo-1,3-diazinane-4-carboxamide;acetic acid;hydrate
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| Synonyms |
FE 200486; FE200486; FE-200486; ASP-3550; ASP 3550; ASP3550; Degarelix acetate; tradename Firmagon
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
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| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 0.5909 mL | 2.9545 mL | 5.9091 mL | |
| 5 mM | 0.1182 mL | 0.5909 mL | 1.1818 mL | |
| 10 mM | 0.0591 mL | 0.2955 mL | 0.5909 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT03689699 | Active Recruiting |
Drug: Nivolumab Drug: Degarelix Drug: BMS-986253 |
Prostate Cancer Adenocarcinoma of the Prostate |
Mark Stein | October 11, 2018 | Phase 1 Phase 2 |
| NCT03069937 | Active Recruiting |
Drug: Docetaxel Drug: Degarelix |
Metastatic Prostatic Adenocarcinoma |
Medical University of South Carolina |
March 1, 2017 | Phase 2 |
| NCT04301414 | Active Recruiting |
Drug: Degarelix Drug: BMS-986218 and Degarelix |
Prostate Cancer | Columbia University | February 25, 2020 | Early Phase 1 |
| NCT01994239 | Active Recruiting |
Drug: Degarelix Radiation: Pelvic Radiotherapy |
Adenocarcinoma of Prostate | UNICANCER | December 2012 | Phase 2 |
| NCT01542021 | Active Recruiting |
Drug: degarelix injection Drug: androgen deprivation therapy |
Prostate Cancer Prostatic Adenocarcinoma |
Memorial Sloan Kettering Cancer Center |
February 2012 | Not Applicable |
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