First-in-Human, Double-Blind, Randomized Controlled Trial of an Oral Dose of GnRH Antagonist TU2670 in Healthy Women

Sungpil Han, Yong-Soon Cho, Yong‐Soon Cho, Seok-Kyu Yoon, Kyoung Soo Lim, Sang-Heon Cho, Sang‐Heon Cho, Jae Woo Kim, JaeWoo Kim, Sangmin Choe, Jin‐Ah Jung, Jinah Jung, Jong‐Lyul Ghim, Jong-Lyul Ghim, Sangkeun Choi, Min-Hee Lee, Minhee Lee, Seon Mi Kim, Hun-Taek Kim, Hyeong-Seok Lim, Jae Yoon Shim, Kyun‐Seop Bae, Kyun-Seop Bae
The Journal of clinical endocrinology and metabolism · 2020 · vol. 106(3) , pp. e1111–e1120 · doi:10.1210/clinem/dgaa939 · PMID:33347565 · W3117810442
article OA: bronze CC0 ⤵ 2 in-corpus citations
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⚙ AI-generated summary by claude@2026-06, 2026-06-09 ⓘ

This Phase 1 trial found the novel oral GnRH antagonist TU2670 to be safe and well-tolerated in healthy women, demonstrating dose-dependent suppression of LH, FSH, and estradiol.

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Abstract

OBJECTIVE: To evaluate the safety, tolerability, pharmacokinetics, and pharmacodynamics of TU2670, a novel orally active, nonpeptide gonadotropin-releasing hormone (GnRH) antagonist administered to healthy female participants. METHODS: This was a first-in-human, multicenter, phase 1, randomized, double-blind, placebo-controlled, single-dose ascending trial that took place in multiple medical centers. A total of 16 healthy premenopausal women (23 to 45 years of age) were randomized and received 20, 40, 80, and 160 mg TU2670 (GnRH antagonist) or placebo 7 days (±1 day) after the onset of menstrual bleeding. We performed a noncompartmental analysis for pharmacokinetic parameters and calculated relative minimum concentration values (Cmin, % Baseline) of serum pharmacodynamic (PD) markers (luteinizing hormone [LH], follicle-stimulating hormone [FSH], and estradiol). RESULTS: There were no significant differences among treatments with respect to vital signs, electrocardiography, adverse events, ovulation test results, and ultrasonography. The median Tmax of TU2670 occurred 0.75 to 1.00 hours after dosing, and concentrations then declined, with a mean apparent half-life (t1/2) of 3.0 to 5.9 hours. AUClast (17.7-417.9 ng·h/mL) and Cmax (8.1-95.4 ng/mL) increased in a dose-dependent manner. The PD analysis after a single administration of TU2670 revealed dose-dependent suppression of LH, FSH, and estradiol. Maximal suppression of the pre-dose baseline (%) was 58% to 82% at 6 to 8 hours for LH, 28% to 39% at 6 to 12 hours for FSH, and 34% to 82% at 12 to 24 hours for estradiol. CONCLUSION: The single administration of TU2670 in healthy premenopausal women was well tolerated and resulted in the dose-dependent suppression of LH, FSH, and estradiol, suggesting rapid and significant inhibition of pituitary and ovarian hormones.

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MeSH descriptors

Gonadotropin-Releasing Hormone Hormone Antagonists Organic Chemicals Administration, Oral Adolescent Adult Dose-Response Relationship, Drug Double-Blind Method Estradiol Estradiol Female Follicle Stimulating Hormone Follicle Stimulating Hormone Gonadotropin-Releasing Hormone Healthy Volunteers Hormone Antagonists Hormone Antagonists Hormone Antagonists Humans Luteinizing Hormone

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