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chlormadinone acetate + ethinyl estradiol (Balianca / Belara / CG5025)

✓ Approved

Faes · AR · 小分子

什么是 chlormadinone acetate + ethinyl estradiol?

chlormadinone acetate + ethinyl estradiol 是一种小分子,由Faes研发。该药已获批,用于治疗相关适应症,给药途径:Oral (PO)。

药物档案

商品名Balianca, Belara, CG5025
公司Faes
药物类别小分子
分子靶点AR, ESR1
给药途径Oral (PO)
状态Approved

作用机制

分子靶点

chlormadinone acetate + ethinyl estradiol 作用于 2 个分子靶点:

ARandrogen receptor (TFM, NR3C4)
ESR1estrogen receptor 1 (ESR, ESTRR)
需要更深入的分析?Noah AI 可解释复杂机制并与同类药物比较。

治疗适应症

chlormadinone acetate + ethinyl estradiol 针对 2 个适应症,涉及 2 个治疗领域。

治疗领域疾病/病症分期
Reproductive system and breast disordersPolycystic ovaries✓ Approved
Endocrine disordersPolycystic ovarian syndrome✓ Approved

相关研究文献

PubMedChemistry & biodiversity2026-09-10

Antioxidant Activities of Pentacyclic Triterpenes From Melipona beecheii Propolis and Their Semisynthetic Derivatives.

Santana-Hernández Aarón A, Yam-Puc Alejandro A, Yah-Nahuat Pamela P, Vargas-Vargas María M et al.

Four principal fractions (I-IV) were obtained from the Melipona beecheii propolis. GC-MS analysis of these fractions allowed us to recognize 11 pentacyclic triterpenes (PTs), fraction I [β-amyrin acetate (1), germanicol acetate (2), moretenol acetate (3) and 24-methylencycloartan-3-ol acetate (4)]; fraction II [marsformosanone (5), β-amyrenone (6), germanicone (7) and lupenone (8)]; fraction III [β-amyrin (9) and, glutinol (10)]; and fraction IV [9 and α-amyrin (11)]. This is the first time that triterpenes 7 and 10 are reported in the propolis of M. beecheii. Three semisynthetic derivatives were prepared: the reduction of fraction II and the acetylation and oxidation of fraction IV. The ethanolic extract of propolis and fraction III presented the highest free DPPH radical scavenging capacity at 53.89 ± 8.39% and 47.77 ± 0.91%, respectively, using a concentration of 10 mg/mL. In contrast, the reducing power of Fe (III) analysis showed a strong reducing power of Fe(III) for all fractions and their derivatives with an EC50 = 0.8-1.0 mg/mL.

PMID 42720076
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PubMedInternational journal of women's health2026-09-10

Achieving Minimal-to-No Pain in Women with Endometriosis Treated with Relugolix Combination Therapy: SPIRIT Extension Trial.

Lukes Andrea S AS, Venturella Roberta R, Dynowski Krzysztof K, Wagman Rachel B RB et al.

Relugolix is an oral, non-peptide gonadotropin-releasing hormone receptor antagonist administered as once-daily combination therapy (relugolix-CT; 40 mg relugolix, 1 mg estradiol, 0.5 mg norethindrone acetate) to reduce endometriosis symptoms while potentially minimizing hypoestrogenic effects. In the 24-week SPIRIT1&2 studies, relugolix-CT significantly improved endometriosis-associated pain versus placebo, with improvements sustained over the 80-week open-label Long-Term Extension (LTE; all received relugolix-CT). This post hoc analysis of SPIRIT1, 2 and LTE data assessed temporal effects of relugolix-CT on minimal-to-no pain, amenorrhea, and analgesic-free status. This analysis included women who received relugolix-CT, delayed relugolix-CT, or placebo in SPIRIT 1 or 2 and entered the LTE. Cumulative probability and median time to minimal-to-no pain for dysmenorrhea and non-menstrual pelvic pain (NMPP), amenorrhea, and analgesic-free status were assessed. In SPIRIT1&2, 802/1261 women entered the LTE; 501/802 completed 104-week treatment. Median time to minimal-to-no pain for dysmenorrhea was 8 weeks for relugolix-CT and delayed relugolix-CT and was not reached with placebo within 24 weeks; cumulative probability of minimal-to-no dysmenorrhea at Week 24 was 82.5%, 86.4%, and 22.4%, respectively, increasing to 95.3%, 95.9%, and 94.9% at Week 104. Amenorrhea paralleled dysmenorrhea. Median time to minimal-to-no NMPP was 32, 28, and 40 weeks in the relugolix-CT, delayed relugolix-CT, and placebo groups, respectively; cumulative probability of minimal-to-no NMPP was 42.6%, 42.2%, and 28.9% at Week 24, increasing to 70.5%, 74.7%, and 74.3% at Week 104. In the relugolix-CT group, median time to analgesic-free status was 16 weeks; 68.8% and 94.9% were analgesic-free at Weeks 24 and 104. Delayed relugolix-CT results were similar. Analgesic-free status improved in the placebo group after relugolix-CT initiation. In this post hoc analysis, women receiving relugolix-CT for up to 104 weeks had rapid dysmenorrhea improvement with amenorrhea and reduced analgesic use, with longer treatment associated with further NMPP reduction.

PMID 42719373
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PubMedSmall (Weinheim an der Bergstrasse, Germany)2026-09-10

Manipulating the Buried Interfacial Dipole: The Role of Pyridine Acetate-Hydrochloride Isomers in Carbon-Based Perovskite Solar Cells Prepared in Air.

Shi Yifei Y, Gong Jianwen J, Wang Xu X, Hu Shuming S et al.

The buried interface between tin oxide and perovskite is the key factor for non-radiative recombination and energy level mismatch, which limits the performance and stability of perovskite solar cells. This work explores a simple interfacial dipole engineering strategy, where three pyridine acetate-hydrochloride (PAH) isomer molecules (2-PAH, 3-PAH, and 4-PAH) are used to modify the SnO2 electron transport layer. The 3-PAH-modified layer can control the work function of tin oxide, achieve the best energy level alignment, and improve the crystallization quality of the perovskite film, thereby effectively suppressing interface recombination and promoting electron extraction. All the devices are prepared in air, and the device optimized by 3-PAH achieved a champion energy conversion efficiency of 14.31% and demonstrated stability. Subsequent to an 800 h placement in an N2 glove box or a 340 h exposure to an air environment, the unencapsulated target devices that were modified by 3-PAH maintained 80.7% and 81.3% of their initial efficiency.

PMID 42717680
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PubMedAnnals of translational medicine2026-09-10

A comprehensive longitudinal study quantifying the systemic effects associated with ovariectomy and high-dose corticosteroids in a sheep model of osteoporosis.

Bisazza Katie T KT, Nelson Brad B BB, Anthony Russell V RV, Goodrich Laurie R LR et al.

The sheep is a common preclinical model for osteoporosis in humans and allows for robust longitudinal studies. Appropriate characterization of large animal models is necessary prior to selection for preclinical studies. We sought to comprehensively characterize the process of bone loss in a 12-month sheep model of osteoporosis, and report on the sheep clinical pathologies throughout osteoporosis model development. We induced osteoporotic bone loss in 10 sheep via ovariectomy and corticosteroid administration. Over a 12-month period, we performed serial bone density scanning, bone biopsy for microarchitecture and histomorphometry assessment, clinical assessments, and evaluated systemic levels of steroid hormones, as well as hematological and biochemical values. Statistical analysis was performed to compare the outcomes of osteoporotic sheep to healthy age-matched control sheep over time. We successfully induced osteoporotic-like bone loss in the experimental group by observing decreased bone density in the lumbar spine and tibia by 6 months, including changes to bone microarchitecture (i.e., trabecular thinning, decreasing bone volume) and histomorphometry (i.e., decreased trabecular bone ratio) indicative of bone remodeling disruption. We also reported comprehensive systemic changes in the same animals over time. Compared to control animals, we observed a significant disruption to clinical pathology parameters and steroid hormone production in osteoporotic sheep. Osteoporotic model development induced hematological and serological disruptions at 3 months, including neutrophilia, immune cell suppression, electrolyte and protein imbalances, hyperphosphatemia, and elevated liver enzymes. Additionally, administration of corticosteroids appeared to suppress cortisol production over the course of model development, followed by a surge of endogenous cortisol following cessation of corticosteroid treatment. Estradiol surprisingly did not drop to significantly lower levels than controls for the duration of the experiment, suggesting that there are extragonadal sources of estradiol production or dietary sources of phytoestrogens in the sheep differing from humans. Bone loss was induced in sheep within 3-6 months, and the most significant systemic disruptions appear to correlate with timing of high-dose corticosteroids. These findings offer a detailed characterization of the sheep model of osteoporosis, enabling investigators to distinguish the effects of treatment administration from those arising solely from model development.

PMID 42718873
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PubMedACS omega2026-09-10

Determination of Molecular Interactions between Copper Pigments and Soybean Oil Alkyd Resins in Paints: A Spectroscopic Study.

Costa Thiago Guimarães TG, Candeias António José Estêvão Grande AJEG, Gazotto Enzo Gimenes EG, Júnior Feik Amil de Campos FAC et al.

Alkyd paints are widely used in modern painting and can be obtained commercially or prepared from pure materials. Various formulations can be used to obtain these paints. Copper pigments can be found in various works of art and in industrial paints. The use of these pigments in modern resins can be a low-cost alternative for different applications. However, studies must be conducted to ensure safety when applying these paints. In this work, the interaction of Cu-(II) present in malachite, azurite, and copper acetate pigments with soybean oil-based alkyd resins when subjected to heat treatment above 50 °C was characterized. The results show that paintings containing malachite and azurite exhibited colorimetric ΔE values of 2.77 and 3.72, respectively, showing no significant chromatic change during the studied heat period. Fourier transform infrared (FTIR) spectroscopy revealed a decrease in the intensity of ester and phthalic groups in the resin over time, indicating that reactions occurred in these groups during the sample aging process. Raw copper acetate was initially present in the dimeric form; however, when mixed with a binder, monomeric species were formed, and the intensity of dimers decreased with the aging period, leading to the formation of only monomeric species with a color change. Scanning electron microscopy (SEM) analysis showed that the paint layers remained uniform even after the studied aging period. μ-Raman showed signals below 500 cm-1, which are attributed to Cu-O vibrational modes of new structures formed during the aging process of the paints. The chemical transformations do not lead to color changes in the pigments of malachite and azurite, so the results suggest that soybean oil-based alkyd resin could be a viable and cost-effective alternative to be used in the formulation with copper pigments. Furthermore, the data present can help understand the behavior of alkyd paints in the presence of copper pigments, assisting in the advancement of materials for use in painting materials.

PMID 42719401
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PubMedmBio2026-09-10

Sex and age differences in antibody responses to seasonal influenza vaccination are mediated by estrogenic upregulation of NF-κB and TNF signaling in B cells.

Park Han-Sol H-S, Yin Anna A, Zhou Weiqiang W, Wenstedt Eliane F E EFE et al.

Sex differences in the humoral immune responses to the seasonal quadrivalent influenza vaccine (QIV) in young adults (YA; 18-49 years old) or high-dose QIV in old adults (OA; 75+ years old) were analyzed to determine how age-related changes, including in steroids, impact sex differences in B cells. Among YAs, females had greater H3N2, but not H1N1, neutralizing antibody titers, and greater proportions of hemagglutinin (HA)+ CD19+ B cells and HA+ memory B cells than males through 28 days post-vaccination (DPV), that was not observed among OAs. Machine learning algorithms illustrated that baseline (0 DPV) steroids, including 17-hydroxyprogesterone, estrogens, and testosterone, as well as HA+ CD19+ B cells and HA+ antibody-secreting B cells (ASCs), were major predictors of seroconversion at 28 DPV, particularly in YA. Single-cell RNA sequencing demonstrated that CD19+ B cells from YA females had greater transcriptional activity at 7 DPV than YA males, with upregulation of genes with estrogen-response elements (EREs) along NF-κB-mediated TNF signaling pathways in B-cell subsets, which was mitigated in OA. Estradiol treatment of ASCs from YA females, but not males, increased the number and size of HA+ IgG+ cells and expression of ERE genes along the NF-κB-mediated TNF signaling pathway,that was inhibited by an estrogen receptor antagonist. Pharmacological inhibition of either NF-κB or TNF signaling blocked the ability of E2 to upregulate antibody secretion in cells from YA females. This study provides mechanistic insights into estrogen-mediated increases in influenza vaccine-induced antibody responses among reproductive-aged females and suggests a role for estrogen signaling in the reduction of sex differences in vaccine-induced immunity with old age. Sex differences in influenza vaccine-induced immune responses become less pronounced with old age, which we hypothesize could be related to changes in circulating gonadal steroids. Our study shows that after receipt of the seasonal influenza vaccine, young adult females, who have elevated estrogenic activity, have more B cells that recognize influenza hemagglutinin; their B cells have greater activity along estrogen signaling and inflammatory pathways, and mount stronger antibody responses than young adult males, with these sex differences being mitigated in old adults. We identify estrogen as a key driver of sex differences in influenza immunity by showing that ex vivo estradiol increases antibody production by B cells through the estrogen receptor and engagement with NF-κB. These findings help explain the biological basis for sex differences in vaccine immunity and suggest that the hormonal environment, not just chronological age, shapes how well a person responds to vaccination.

PMID 42720319
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