Sufugolix  (Synonyms: TAK-013)

Sufugolix (TAK-013) is a highly potent and orally available luteinizing hormone-releasing hormone (LHRH) receptor antagonist with an IC₅₀ of 0.1 nM.

IC50: 0.1 nM (human LHRH), 0.6 nM (monkey LHRH)^[1]

Sufugolix exhibits more than 3- and 2000-fold selectivity for the human receptor over the monkey and rat receptors, respectively. Sufugolix effectively antagonizes LHRH function on CHO cells expressing the human (IC₅₀=0.1 nM) and monkey (IC₅₀=0.6 nM) receptors. During the conformational analysis of sufugolix, using high-temperature molecular dynamics calculation, it is observed that the cis conformer of the methoxyurea is more populated than the trans conformer ^[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Oral administration of sufugolix causes almost complete suppression of the plasma LH levels in castrated male cynomolgus monkeys at a 30 mg/kg dose with sufficient duration of action (more than 24 h). The maximum plasma concentrations of sufugolix are 0.34 μM (reached 6 h after administration) and 0.18 μM (reached 4 h after administration) at 30 and 10 mg/kg doses, respectively^[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

667.72

C₃₆H₃₁F₂N₅O₄S

308831-61-0

固体

Light yellow to yellow

Room temperature in continental US; may vary elsewhere.

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• [1]. Sasaki S, et al. Discovery of a thieno[2,3-d]pyrimidine-2,4-dione bearing a p-methoxyureidophenyl moiety at the 6-position: a highly potent and orally bioavailable non-peptide antagonist for the human luteinizing hormone-releasing hormone receptor. J Med Chem. 2003 Jan 2;46(1):113-24.  [Content Brief]