Oral investigational drugs currently in phase I or phase II for the amelioration of menopausal symptoms

Abstract

ABSTRACTIntroduction: Menopausal symptoms have a substantial effect on the quality of life of many women; hence, investigations for the amelioration of menopausal symptoms continue to be necessary. The two main approaches to the amelioration of symptoms are hormone therapy (HT) and non-hormonal therapy.Areas covered: This review provides a background for understanding the types of menopausal symptoms and their underlying physiology. The early clinical development of natural estrogen (estetrol, E4), neurokinin 3 receptor (NK3R) antagonists, and other non-hormonal therapies are covered. The status and outcome of these novel treatment modalities are also discussed.Expert opinion: The recent observation in the Women’s Health Initiative (WHI) trials that HT was not associated in the long-term with all-cause mortality, brings renewed interest in the development of new treatment modalities in postmenopausal women. Estetrol (E4), a native estrogen with selective action in tissues, is a potential next-generation HT with improved cardiovascular and breast safety. NK3R antagonists may become an interesting new modality for the amelioration of hot flushes in women with contraindications to estrogens.Trial registration: ClinicalTrials.gov identifier: NCT00163033.Trial registration: ClinicalTrials.gov identifier: NCT02834312.Trial registration: ClinicalTrials.gov identifier: NCT03192176.Trial registration: ClinicalTrials.gov identifier: NCT02865538.Trial registration: ClinicalTrials.gov identifier: NCT03596762.Trial registration: ClinicalTrials.gov identifier: NCT02668185.Trial registration: ClinicalTrials.gov identifier: NCT02803268.Trial registration: ClinicalTrials.gov identifier: NCT03291067.Trial registration: ClinicalTrials.gov identifier: NCT03541200.Trial registration: ClinicalTrials.gov identifier: NCT03285672.Trial registration: ClinicalTrials.gov identifier: NCT03518138.