Relugolix (TAK-385) possesses higher affinity and potent antagonistic activity for human (binding IC50=0.33 nM in the presence of serum) and monkey GnRH receptor (IC50=0.32 nM), but has low affinity for the rat GnRH receptor (IC50=9800 nM).
Relugolix (TAK-385) acts as an antagonist for human GnRH receptor in vivo and daily oral administration potently, continuously and reversibly suppresses the hypothalamic-pituitary-gonadal axis.
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Animal models | Six-week-old male hGNRHR-knock-in mice |
Formulation | 0.5% methylcellulose solution containing 6 mg/mL citric acid monohydrate |
Dosages | 3, 10 or 30 mg/kg |
Administration | oral |
Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
Animal A Km |
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
Molecular Weight | 623.63 |
Formula | C29H27F2N7O5S |
CAS Number | 737789-87-6 |
Purity | >98.5% |
Solubility | DMSO: ≥ 48 mg/mL |
Storage | at -20°C |
Medical Castration Using the Investigational Oral GnRH Antagonist TAK-385 (Relugolix): Phase 1 Study in Healthy Males.
MacLean DB, et al. J Clin Endocrinol Metab. 2015 Dec;100(12):4579-87. PMID: 26502357.
Suppression of the hypothalamic-pituitary-gonadal axis by TAK-385 (relugolix), a novel, investigational, orally active, small molecule gonadotropin-releasing hormone (GnRH) antagonist: studies in human GnRH receptor knock-in mice.
Nakata D, et al. Eur J Pharmacol. 2014 Jan 15;723:167-74. PMID: 24333551.
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