Delving into the Latest Updates on Cyproterone Acetate/Estradiol Valerate with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

SH-461, Climen, 克龄蒙

Target

AR x ER

Action

antagonists, agonists

Mechanism

AR antagonists(Androgen Receptor antagonists), ERs agonists(Estrogen receptors agonists)

Therapeutic Areas

Nervous System DiseasesEndocrinology and Metabolic DiseaseSkin and Musculoskeletal Diseases+ [2]

Active Indication

DyspareuniaHot FlashesNeurasthenia+ [5]

Inactive Indication-

Originator Organization

Bayer AG

Active Organization

Bayer AG

Inactive Organization-

License Organization

Bayer Korea Ltd.

Daewon Pharmaceutical Co., Ltd.

Drug Highest PhaseApproved

First Approval Date

Czechia (01 Nov 1993),

DyspareuniaHot FlashesNeurasthenia+ [5]

Regulation-

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Structure/Sequence

Molecular FormulaC47H61ClO7

InChIKeyKQMFAQMCNGHNAD-QMPUQPNWSA-N

CAS Registry108116-22-9

Recent studies have showed that there were significant drug-drug interactions (DDI) from feminizing hormone therapy (FHT) towards emtricitabine/tenofovir disoproxil fumarate (F/TDF)-based pre-exposure prophylaxis (PrEP) among transgender women (TGW). New strategies for PrEP among TGW who use FHT are urgently needed. Because tenofovir alafenamide (TAF) can achieve higher intracellular TFV-DP levels with lower tenofovir plasma concentrations, it is promising that both plasma TFV and intracellular TFV-DP levels might not be significantly affected by FHT. The current study aims to determine the pharmacokinetics DDI between FHT and F/TAF-based PrEP among TGW.

Start Date24 Jan 2022

Sponsor / Collaborator

Thai Red Cross AIDS Research Centre

ChiCTR-TRC-14005030

/ RecruitingPhase 4IIT

The effect of dehydroepiandrosterone plus climen supplementation for patients with diminished ovarian reserve

Start Date05 Aug 2014

Sponsor / Collaborator

Anhui Medical University No. 1 Affiliated Hospital

ISRCTN45546616

/ CompletedNot Applicable

Ethynil-estradiol cyproterone acetate versus low-dose metformin-flutamide-pioglitazone in girls with hyperinsulinemic androgen excess: effects on parameters of chronic inflammation, and on risk factors for type 2 diabetes and cardiovascular disease

Start Date01 Feb 2010

Sponsor / Collaborator-

100 Clinical Results associated with Cyproterone Acetate/Estradiol Valerate

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100 Translational Medicine associated with Cyproterone Acetate/Estradiol Valerate

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100 Patents (Medical) associated with Cyproterone Acetate/Estradiol Valerate

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59

Literatures (Medical) associated with Cyproterone Acetate/Estradiol Valerate

01 Jun 2021·Zhongguo Zhong yao za zhi = Zhongguo zhongyao zazhi = China journal of Chinese materia medica

[Clinical efficacy of Bushen Huoxue Culuan Formula in treatment of infertility caused by diminished ovarian reserve due to kidney deficiency and blood stasis].

Article

Author: Wang, Kai-Li ; Wu, Jing-Xian ; Zhang, Hui-Xian ; Ma, Kun ; Peng, Bi-Hui

To study the clinical efficacy and safety of Bushen Huoxue Culuan Formula in treating infertility caused by diminished ovarian reserve(DOR) with kidney deficiency and blood stasis. A total of 100 DOR patients treated at Xiyuan Hospital, Acupuncture Hospital and Clinic of China Academy of Chinese Medical Sciences from 2017 to 2020 in line with the inclusion criteria were selected and randomly divided into experimental group and control group at the ratio of 1∶1. The experimental group was treated with Bushen Huoxue Culuan Formular, while the control group was treated with Climen and Clomiphene for 3 menstrual cycles. The ovulation rate, pregnancy rate, pregnancy success rate, serum hormone levels, and traditional Chinese medicine(TCM) symptom scores were observed in the 2 groups. The total effective rate was 92.00% in the experimental group and 72.00% in the control group, with a statistical difference between the two groups(P<0.01); the experimental group was superior to the control group in reducing FSH level, increasing AMH level, improving TCM symptoms, increasing pregnancy rate and pregnancy success rate, with a significant difference(P<0.05). There was no abnormal safety indicator and adverse reaction. Bushen Huoxue Culuan Formular is effective in treating infertility caused by DOR due to kidney deficiency and blood stasis, with a safety and reliability.

12 Mar 2021·Zhongguo zhen jiu = Chinese acupuncture & moxibustion

[Effect of regulating menstruation and promoting pregnancy acupuncture therapy on negative emotion in patients with premature ovarian insufficiency].

Article

Author: Yu, Xiao-Hua ; Fang, Yi-Gong ; Li, Hu ; Bai, Tian-Yu ; Xu, Cheng-Chao

OBJECTIVE:

To observe the influence of regulating menstruation and promoting pregnancy acupuncture therapy on negative emotions in patients with premature ovarian insufficiency (POI).

METHODS:

A total of 60 patients with POI were randomly divided into an acupuncture group and a western medication group, 30 cases in each group. The acupuncture group was treated with regulating menstruation and promoting pregnancy acupuncture therapy at Baihui (GV 20), Shenting (GV 24), Guanyuan (CV 4), Sanyinjiao (SP 6), Shenshu (BL 23), Ciliao (BL 32), etc. once a day, 5 times a week for 3 months. The western medication group was treated by oral administration of climen. The drug was given 1 tablet a day for 21 days and was stopped for 1 week as a course. The treatment was required 3 consecutive courses. The self-rating anxiety scale (SAS) score, modified Kupperman index (KI) score, agitated and depressive symptom scores in KI and serum level of follicle stimulating hormone (FSH) before and after treatment were compared between the two groups.

RESULTS:

After treatment, the SAS scores, KI scores and serum levels of FSH in the two groups and the scores of agitated and depressive symptom in the acupuncture group were lower than those before treatment (P<0.05), and the acupuncture group was lower than the western medication group (P<0.05).

CONCLUSION:

Regulating menstruation and promoting pregnancy acupuncture therapy can effectively improve the negative emotions of patients with POI and reduce serum level of FSH .

01 Feb 2020·Journal of traditional Chinese medicine = Chung i tsa chih ying wen pan

Effectiveness of nourishing Yin and tonifying Yang sequential therapy in combination with Climen on diminished ovarian reserve: a retrospective study.

Article

Author: Chen, Shuping ; Sun, Yuying ; Tan, Yong

OBJECTIVE:

To evaluate the clinical efficacy of nourishing Yin and tonifying Yang sequential therapy (NYTYST) in combination with the Western Medicine Climen in treating diminished ovarian reserve (DOR).

METHODS:

From September 2014 to September 2016, 46 patients with DOR who received NYTYST and Climen (treatment group) and 51 patients who received Climen only (control group) at the Jiangsu Provincial Traditional Chinese Medicine Hospital (Nanjing, China) were retrospectively reviewed. Before and at 3 months after treatment, serum levels of follicle-stimulating hormone (FSH), FSH/luteinizing hormone (LH), estradiol (E2), and anti-Mullerian hormone (AMH), the antral follicle count (AFC), stromal peak systolic velocity (PSV), symptom scores, and the clinical effectiveness rate were measured and compared between the two groups.

RESULTS:

After treatment, serum levels of FSH, FSH/LH and E2, and symptom scores were significantly decreased compared with before treatment (all P < 0.05) in the two groups. AMH levels, AFC, and PSV were significantly increased after treatment compared with before treatment in both groups (all P < 0.05). Serum levels of FSH, FSH/LH, and E2 after treatment were significantly lower in the treatment group than in the control group (all P < 0.05). However, AMH levels and the AFC were significantly higher after treatment in the treatment group than in the control group (both P < 0.05). The clinical effectiveness rate was significantly higher in the treatment group than in the control group (87% vs 68.6%, P < 0.05).

CONCLUSION:

NYTYST combined with Climen may be more effective in treating DOR than Climen alone.

100 Deals associated with Cyproterone Acetate/Estradiol Valerate

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External Link

KEGG	Wiki	ATC	Drug Bank
-	-	G03CA53	-

R&D Status

10 top approved records.

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Indication	Country/Location	Organization	Date
Dyspareunia	Czechia	Bayer AG	01 Nov 1993
Hot Flashes	Czechia	Bayer AG	01 Nov 1993
Neurasthenia	Czechia	Bayer AG	01 Nov 1993
Oestrogen deficiency	Czechia	Bayer AG	01 Nov 1993
Osteoporosis, Postmenopausal	Czechia	Bayer AG	01 Nov 1993
Sleep Wake Disorders	Czechia	Bayer AG	01 Nov 1993
Urinary Incontinence	Czechia	Bayer AG	01 Nov 1993
Vulvovaginal atrophy	Czechia	Bayer AG	01 Nov 1993