ArticleACS medicinal chemistry letters2015
Optimization of Novel Antagonists to the Neurokinin-3 Receptor for the Treatment of Sex-Hormone Disorders (Part II).
Article in ACS medicinal chemistry letters, 2015. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 9 papers.
What it found
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The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.
Who cites it
9 citing papers in PubMed, 57 citations in OpenAlex.
- Randomized Controlled Trial of Neurokinin 3 Receptor Antagonist Fezolinetant for Treatment of Polycystic Ovary Syndrome.The Journal of clinical endocrinology and metabolism · 2021Trial
- Effect of the neurokinin 3 receptor antagonist fezolinetant on patient-reported outcomes in postmenopausal women with vasomotor symptoms: results of a randomized, placebo-controlled, double-blind, dose-ranging study (VESTA).Menopause (New York, N.Y.) · 2020Trial
- FDA approves Veozah (Fezolinetant) for menopausal symptoms: a new nonhormonal option.Annals of medicine and surgery (2012) · 2025Article
- Revolutionary treatment for menopausal symptoms: Veozah (Fezolinetant) receives FDA approval.Annals of medicine and surgery (2012) · 2024Article
- The significance of chirality in contemporary drug discovery-a mini review.RSC advances · 2024Review
- Structure-property Relationships Reported for the New Drugs Approved in 2023.Mini reviews in medicinal chemistry · 2024Review
- Synthetic Approaches to Piperazine-Containing Drugs Approved by FDA in the Period of 2011-2023.Molecules (Basel, Switzerland) · 2023Review
- Contemporary Non-hormonal Therapies for the Management of Vasomotor Symptoms Associated with Menopause: A Literature Review.TouchREVIEWS in endocrinology · 2021Review
- Qualitative study: burden of menopause-associated vasomotor symptoms (VMS) and validation of PROMIS Sleep Disturbance and Sleep-Related Impairment measures for assessment of VMS impact on sleep.Journal of patient-reported outcomes · 2021Article
Corrections and comments
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Authors and funding
8 authors at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Further lead optimization on N-acyl-triazolopiperazine antagonists to the neurokinin-3 receptor (NK3R) based on the concurrent improvement in bioactivity and ligand lipophilic efficiency (LLE) is reported. Overall, compound 3 (LLE > 6) emerged as the most efficacious in castrated rat and monkey to lower plasma LH, and it displayed the best off-target safety profile that led to its clinical candidate nomination for the treatment of sex-hormone disorders.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.