Faes · AR · Small Molecule
chlormadinone acetate + ethinyl estradiol is a small molecule developed by Faes. It is approved for therapeutic indications via oral (po).
| Brand Names | Balianca, Belara, CG5025 |
| Company | Faes |
| Drug Class | Small Molecule |
| Molecular Target | AR, ESR1 |
| Route | Oral (PO) |
| Status | Approved |
chlormadinone acetate + ethinyl estradiol acts on 2 molecular targets:
| AR | androgen receptor (TFM, NR3C4) |
| ESR1 | estrogen receptor 1 (ESR, ESTRR) |
chlormadinone acetate + ethinyl estradiol is developed for 2 unique indications across 2 therapeutic areas.
| Therapeutic Area | Condition | Phase |
|---|---|---|
| Reproductive system and breast disorders | Polycystic ovaries | ✓ Approved |
| Endocrine disorders | Polycystic ovarian syndrome | ✓ Approved |
Fatima Kaneez K, Khalid Shaukat S, Qadeer Kiran K, Shareef Huma H et al.
Malaria and dengue are among the most widespread vector-borne diseases globally. This study evaluated the larvicidal and repellent characteristics of Alstonia scholaris (Apocynaceae) flower extracts against the Anopheles stephensi and Aedes aegypti vectors. The crude methanolic extract was sequentially fractionated into ethyl acetate, n-butanol and aqueous fractions. Four different fractions were tested against Anopheles stephensi and Aedes aegypti at concentrations ranging from 78 to 1092 ppm and 625-6250 ppm, respectively. Larval mortality was observed after 24 h and analysed using probit analysis to estimate lethal concentrations (LC50). Repellency duration was assessed for adult Aedes aegypti using the various solvent extracts. The methanolic extract exhibited high efficacy against both Anopheles stephensi and Aedes aegypti larvae, with LC50 of 312 and 960 ppm, respectively. The ethyl acetate extract showed strong repellent activity, which is persistent up to 9 h (posttreatment) against adult Aedes aegypti. FTIR analysis of the methanolic extract identified functional groups such as aldehyde, amide, alkyl and carbonyl. GC-MS analysis revealed five major components: ursolic acid methyl ester (12.42%), lupeol (53.86%), lupeol acetate (10.95%), cycloeucalenol (2.62%) and hentriacontane (2.64%). These findings indicate that A. scholaris flower extracts in different solvents show potential larvicidal and mosquito repellent activity for the control of malaria and dengue.
Liu Qinxin Q, Han Rongshuang R, Wang Yi Y, Mao Tao T et al.
Sodium acetate (NaA), an acetate donor among short-chain fatty acid salts, is involved in intestinal epithelial homeostasis, mucosal inflammation, and host-microbiota interactions. However, its role in ulcerative colitis (UC), particularly in regulating epithelial apoptosis and gut microbiota remodeling, remains unclear. This study investigated the protective effects and potential mechanisms of NaA in experimental colitis. LPS-induced intestinal epithelial cell injury models using NCM460 and Caco-2 cells, together with a DSS-induced mouse colitis model, were established to evaluate the effects of NaA in vitro and in vivo. Cell viability was assessed using the CCK-8 assay. Colonic histopathology and mucus production were examined by H&E and AB/PAS staining. Immunohistochemistry, Western blotting, RT-qPCR, and ELISA were performed to detect barrier-related proteins, inflammatory cytokines, and apoptosis-associated molecules. Gut microbiota alterations were analyzed by 16S rRNA amplicon sequencing. NaA showed no obvious cytotoxicity within an appropriate concentration range and increased ZO-1 and Occludin expression in intestinal epithelial cells. Under LPS stimulation, NaA restored barrier protein expression and reduced the BAX/BCL-2 ratio and cleaved-caspase-3 expression in both NCM460 and Caco-2 cells. In DSS-induced colitis mice, NaA alleviated body weight loss, disease activity index elevation, colon shortening, and spleen index increase. NaA also attenuated colonic histological injury, increased AB/PAS-positive areas, restored ZO-1, Occludin, and MUC2 expression, and reduced IL-6, TNF-α, and IL-1β levels. Moreover, NaA inhibited excessive epithelial apoptosis. 16S rRNA amplicon sequencing and analysis showed that NaA partially reversed DSS-induced gut microbiota dysbiosis, as reflected by improved microbial diversity and community structure, increased Firmicutes/Bacteroidota ratio, reduced Bacteroides and Turicibacter abundance, and enrichment of potential beneficial genera, including Bifidobacterium, Lactobacillus, and Blautia. NaA alleviates experimental colitis by suppressing inflammation, inhibiting excessive epithelial apoptosis, preserving epithelial tight-junction and mucus barrier integrity, and partially restoring gut microbiota homeostasis. These findings suggest that acetate-based intervention may be a potential strategy for UC management through coordinated regulation of epithelial protection and microbial remodeling.
Latkal Hajar H, El Khabaze Soukayna S, Sadiki Moulay M, Msanda Fouad F et al.
Context/Aim: Tuberculosis remains one of the major current health challenges caused by a single infectious pathogen, Mycobacterium tuberculosis. The severity of this epidemic is mainly associated with the emergence of its multidrug-resistant and extensively drug-resistant strains against known anti-tuberculosis drugs. Hence, there is an urgent need to develop new antimycobacterial molecules to overcome this phenomenon. This study aimed to evaluate and compare the antimycobacterial activity of extracts from selected Moroccan medicinal plants. Nine plant species were selected for this study. Three different extracts were prepared from each species using distilled water, ethanol, and ethyl acetate. The obtained twenty-seven extracts were tested for their antimycobacterial activity using the disc diffusion method and the resazurin microtiter assay against two mycobacterial strains: Mycobacterium aurum and Mycobacterium smegmatis. Finally, extracts from the active plants were subjected to qualitative and quantitative phytochemical screening. The studied plant extracts exhibited variable antimycobacterial activity. The MIC values ranged from 0.3 to 50 mg/mL against Mycobacterium aurum and from 0.7 to 100 mg/mL against Mycobacterium smegmatis. Among the tested extracts, the ethyl acetate extract of Marrubium vulgare showed the highest activity, with bactericidal effects reflected by MBC values of 0.7 mg/mL and 1.5 mg/mL against M. aurum and M. smegmatis, respectively. Phytochemical screening indicated that the most active extracts were rich in flavonoids. The results demonstrate a promising antimycobacterial potential of the ethyl acetate extracts from Laurus nobilis, Marrubium vulgare, and Chamaerops humilis, as indicated by significant inhibition zone diameters and low MIC/MBC values. Qualitative and quantitative phytochemical screening suggests that this activity may be associated with the high content of flavonoids in these extracts. According to these results, the studied medicinal plants appear to be a promising source for isolating and purifying new effective antitubercular compounds.
Giersch Gabrielle E W GEW, Bradbury Karleigh E KE, Bozzini Brittany B, Guerriere Aaron Katelyn K et al.
Circulating sex hormones play important roles in reproductive and non-reproductive physiological homeostasis. We evaluated the relationships of sex hormones measured in urine and serum with ambient temperature (maximum and average daily temperatures) in male and female soldiers undergoing initial military training (n = 237, 125F; data are mean ± SD; age: 21 ± 4 years, BMI: 24 ± 3, body fat: 28 ± 7%). Participants provided intermittent blood samples for assessment of 17β-estradiol, total and free-testosterone, luteinizing hormone (LH), and sex hormone binding globulin. Females not using hormonal contraceptives (non-HC users) additionally provided daily first morning urine samples which were analyzed for metabolites of estrogen normalized to creatinine (estrone conjugates, E1C) and progesterone (pregnanediol glucuronide, PDG), LH, and follicle stimulating hormone (FSH). Linear mixed effects models were used to evaluate the relationship between maximum and average daily temperatures and circulating hormonal and gonadotropin concentrations. In urine collected from female non-HC users, maximum daily temperature was inversely associated with E1C and FSH (p = 0.0019, p < 0.001, respectively). Total testosterone was inversely related to maximum daily temperature in males (p < 0.001) and positively associated in both groups of females (non-HC users: p = 0.004, HC users: p = 0.018). Estradiol was inversely related to maximum daily temperature in female non-HC users only (p = 0.001). There was no relationship between temperature (maximum or average) and serum or urine LH, or urine PDG. These findings suggest that ambient temperature is associated with modest sex- and hormone-specific variation in circulating sex hormone concentrations during prolonged physical training.
Mane Shiom S, Udugade Babaso B, Patil Sachinkumar S, Sankpal Poournima P et al.
Breast cancer remains a major global health concern, creating an urgent need for safer and more effective treatments. This study aimed to identify novel progesterone receptor modulators as potential candidates for targeted breast cancer therapy using an integrated in silico approach. The X-ray-validated three-dimensional structure of the human progesterone receptor (PDB ID: 7AXK) was refined using PDB-REDO. Ulipristal acetate, aso-prisnil, and mifepristone were selected as reference ligands. Additional structurally similar compounds were identified through SwissSimilarity using the canonical SMILES of ulipristal acetate. A three-dimensional pharmacophore model describing the essential chemical features required for receptor binding was applied to screen compounds from the ChEMBL database. The selected molecules underwent molecular docking to determine their binding affinities and interactions with important receptor residues. ADME-Tox analysis was subsequently conducted to evaluate their drug-likeness, pharmacokinetic properties, and potential toxicity. PDB-REDO refinement improved the overall structural quality of the 7AXK protein, as assessed using Kleywegt's methodology. Docking and pharmacophore screening identified several compounds with strong predicted binding affinities and favourable interactions within the progesterone receptor's binding site. Selected compounds also demonstrated acceptable drug-like properties, promising pharmacokinetic behaviour, and comparatively favourable predicted safety profiles. The combined computational strategy effectively identified promising progesterone receptor modulators. These candidates show potential for developing targeted breast cancer treatments; however, molecular dynamics simulations and experimental validation are required. Several potential progesterone receptor modulators with favourable binding and ADME-Tox characteristics were identified. These findings demonstrate the value of computational methods in accelerating early-stage breast cancer drug discovery.
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