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Purity: ≥98%
Relugolix (formerly TAK-385; TAK385; trade names: Orgovyx and Relumina) is a non-peptidyl and orally bioactive antagonist of gonadotropin-releasing hormone (GnRH) approved in 2020 for use in the treatment of prostate cancer in men and uterine fibroids in women. It is also being developed as an endometriosis treatment. Relugolix inhibits GnRH in the presence of 40% fetal bovine serum with an IC50 of 0.33 nM. When compared to TAK-013, it has a stronger antagonistic activity and a higher affinity. While TAK-385 regulates the effects of LH and FSH on the ovary and lowers blood levels of estrogen, which are known to be linked to the development of endometriosis and uterine fibroids, Relugolix inhibits LH-RH from binding with the LH-RH receptor in the anterior pituitary gland and suppresses the secretion of luteinizing hormone (LH) and follicle stimulation hormone (FSH) from the anterior pituitary gland.
| Targets |
human GnRH ( IC50 = 0.33 nM ); monkey GnRH ( IC50 = 0.32 nM )
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|---|---|
| ln Vitro |
Relugolix shows a 30000-fold decrease for the rat receptor (IC50=9800 nM) but a strong binding affinity (IC50=0.32 nM) for the monkey receptor, which is comparable to that of the human receptor (IC50=0.33 nM). In the presence of 40% serum, TAK-385's antagonistic in vitro activity against the human receptor (IC90=18 nM) was 95 times greater than that against the monkey receptor (IC90=1700 nM)[1].
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| ln Vivo |
Relugolix (oral administration; 1-3 mg/kg; single dose for pharmacokinetic study) shows clear suppression of circulating LH levels in monkeys at a dose of 1 mg/kg and a good pharmacokinetic profile. Male cynomolgus monkeys show a pharmacokinetic profile with Cmax, Tmax, and AUCo values of 16.0 ng/mL, 2.7 h, and 90.1 ng, respectively[1].
Relugolix (oral administration; 3, 10, or 30 mg/kg; twice daily; 4 weeks) dramatically lowers the weight of the testicles, lowers the weight of the ventral prostate (3 mg/kg), and lowers the weight of the prostate to castrate levels (10 mg/kg) in male hGNRHR-knock-in mice[2]. Relugolix (oral administration; 30, 100, or 200 mg/kg; twice daily; 4 weeks) causes all mice to enter a constant diestrous phase during the first week at 100 mg/kg, and after 4 weeks in female hGNRHR-knock-in mice, this dose significantly reduces the weights of the uteri and ovaries[2]. |
| Animal Protocol |
Male hGNRHR-knock-in mice
3, 10 or 30 mg/kg Oral administration; 3, 10 or 30 mg/kg; twice daily; 4 weeks |
| References |
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| Molecular Formula |
C29H27F2N7O5S
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|---|---|
| Molecular Weight |
623.630391359329
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| Exact Mass |
623.18
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| Elemental Analysis |
C, 55.85; H, 4.36; F, 6.09; N, 15.72; O, 12.83; S, 5.14
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| CAS # |
737789-87-6
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| Related CAS # |
Relugolix-d6
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| Appearance |
Solid powder
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| SMILES |
CN(C)CC1=C(SC2=C1C(=O)N(C(=O)N2CC3=C(C=CC=C3F)F)C4=NN=C(C=C4)OC)C5=CC=C(C=C5)NC(=O)NOC
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| InChi Key |
AOMXMOCNKJTRQP-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C29H27F2N7O5S/c1-36(2)14-19-24-26(39)38(22-12-13-23(42-3)34-33-22)29(41)37(15-18-20(30)6-5-7-21(18)31)27(24)44-25(19)16-8-10-17(11-9-16)32-28(40)35-43-4/h5-13H,14-15H2,1-4H3,(H2,32,35,40)
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| Chemical Name |
1-[4-[1-[(2,6-difluorophenyl)methyl]-5-[(dimethylamino)methyl]-3-(6-methoxypyridazin-3-yl)-2,4-dioxothieno[2,3-d]pyrimidin-6-yl]phenyl]-3-methoxyurea
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| Synonyms |
TAK 385; TAK385; TAK-385; trade names: Orgovyx; Relumina
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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 Vitro) |
DMSO: 61~100 mg/mL (97.8~160.4 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 0.83 mg/mL (1.33 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 8.3 mg/mL clear DMSO stock solution to 400 μL of PEG300 and mix evenly; then add 50 μL of Tween-80 to the above solution and mix evenly; then add 450 μL of normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 0.83 mg/mL (1.33 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 8.3 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 0.83 mg/mL (1.33 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.6035 mL | 8.0176 mL | 16.0351 mL | |
| 5 mM | 0.3207 mL | 1.6035 mL | 3.2070 mL | |
| 10 mM | 0.1604 mL | 0.8018 mL | 1.6035 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 |
| NCT05765500 | Not yet recruiting | Drug: Relugolix Drug: Leuprolide |
Prostate Cancer Prostatic Neoplasms |
Dana-Farber Cancer Institute | January 2024 | Phase 2 |
| NCT05320406 | Recruiting | Radiation: Radiation therapy Drug: Leuprolide Drug: Relugolix |
Localized Prostate Carcinoma Stage I Prostate Cancer AJCC v8 |
Emory University | June 6, 2022 | Phase 4 |
| NCT05605964 | Recruiting | Drug: Relugolix Drug: Leuprolide Acetate |
Prostate Cancer | Myovant Sciences GmbH | January 25, 2023 | Phase 3 |
| NCT05679388 | Recruiting | Drug: Relugolix Pill Drug: Ritonavir |
Prostate Cancer Prostate Adenocarcinoma |
University of Chicago | February 13, 2023 | Phase 1 |
| NCT04666129 | Recruiting | Drug: Relugolix Drug: Abiraterone |
Metastatic Castration-Resistant Prostate Cancer Metastatic Castration-Sensitive Prostate Cancer |
Myovant Sciences GmbH | February 18, 2021 | Phase 1 |
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