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synth conjugated estrogens (Enjuvia)

✓ Approved

Teva Pharmaceutical Industries Ltd. · ESR1

什么是 synth conjugated estrogens？

synth conjugated estrogens 是一种治疗药物，由Teva Pharmaceutical Industries Ltd.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Enjuvia
公司Teva Pharmaceutical Industries Ltd.
分子靶点ESR1
给药途径Oral (PO)
状态Approved
来源： ClinicalTrials.gov, Teva Pharmaceutical Industries Ltd.

作用机制

分子靶点

synth conjugated estrogens 作用于 1 个分子靶点：

ESR1estrogen receptor 1 (ER, ESR)
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

synth conjugated estrogens 针对 3 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 disordersAtrophic vulvovaginitis✓ Approved
Surgical and medical proceduresHormone replacement therapy✓ Approved
Reproductive system and breast disordersMenopausal symptoms✓ Approved

相关研究文献

PubMedJournal of the American Chemical Society2026-10-27

Double Boron-Deleting Annulation: Modular Access to Chiral Nonalternant B,N-Helicenes with Enhanced Chiroptical Properties.

Zhuang Weiwen W, Liu Junzhi J

Direct ring manipulation of planar polycyclic conjugated hydrocarbons into three-dimensional chiral frameworks remains largely underexplored. Herein, we report an unprecedented modular synthesis of nonalternant B,N-embedded helical molecular carbons (HMCs) (BN-HMCs, 12 examples) featuring diaza-pentagon-heptagon pairs via double boron-deleting annulation (dBDA). The quadruple-borylated precursors containing two B2N3-moieties were modularly constructed by C-N cross-coupling and subsequent borylation. The final dBDA process realized structural evolution of boron-centered cove edges into inner helical rims and elicited a dramatic elevation in racemization barriers as corroborated by theoretical calculations and chiral resolution. Double helicenes 2a-2c and 4b derived from twisted precursors with S-shaped orientation of B2N3-units, whereas monohelicenes 4a, 4c-4g, and 5 were generated from C-shaped planar precursors. The reorganized nonalternant skeletons exhibited pronounced red-shifted emission profiles as well as distinct circularly polarized luminescence (CPL) activity. Specifically, the deletion of boron atoms resulted in narrowed energy gaps for red-to-near-infrared emission (e.g., 730 nm for double [7]helicene 2c). Notably, dibenzofuran-based HMC 4d showed a high luminescence dissymmetry factor (|glum| = 0.011) and spirofluorene-based HMC 5 exhibited CPL brightness (BCPL) of 198 M-1 cm-1. These are among the highest values for 1,4-azaborine-embedded (1,4 B,N) HMCs. By escaping from flatland, this work establishes a facile late-stage modification strategy toward nonalternant HMCs with tunable helical architectures, enhanced π-conjugation, and distinct chiroptical properties.

PMID 42937951
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PubMedJournal of the American Chemical Society2026-10-27

Skeletal Distortion Manipulation in 2D-3D-Fused Boron Clusters Enables Solid-State Luminescence and Photothermal Conversion.

Sun Zhaofeng Z, Zong Jibo J, Xu Qingyang Q, Zhang Hongjian H et al.

Luminescent π-conjugated materials are central to modern optoelectronics, yet they are typically constructed from planar, rigid molecular frameworks. Herein, we introduce a conceptually distinct luminescent molecular platform based on three-dimensional (3D) boron cluster-fused conjugated heterocycles. Specifically, a phosphorus-containing heterocycle and a nitrogen-containing heterocycle were designed and synthesized. Both compounds exhibit typical aggregation-induced emission behavior through an skeletal distortion mechanism, which differs from the conventional restriction of intramolecular rotation. Comprehensive photophysical studies and theoretical calculations reveal that their weak emission in solution arises from efficient nonradiative decay driven by excited-state skeletal distortion, whereas this distortion is effectively suppressed in the aggregated state, resulting in bright luminescence. Exploiting this mechanism, we further developed an NIR-II luminogen incorporating a 2D-3D boron cluster-fused conjugated moiety that shows efficient photothermal conversion and enables multimodal imaging-guided photothermal therapy of tumors. Moreover, the boron-rich framework provides high boron content and favorable cellular boron uptake, highlighting its potential as a boron delivery agent for boron neutron capture therapy (BNCT). Overall, this work establishes 3D boron-cluster-fused conjugation as a versatile molecular strategy for regulating excited-state processes and constructing multifunctional phototheranostic materials.

PMID 42937871
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PubMedAntibiotics (Basel, Switzerland)2026-10-27

Cell-Penetration Peptide-Conjugated Octominin II Hybrid Inhibits the Multidrug-Resistant Shigella flexneri.

Jayasinghe Jayasinghage Nirmani Chathurnagika JNC, Nikapitiya Chamilani C, Dirisala Vijaya R VR, Kim Tae-Won TW et al.

Background/Objectives: The genus Shigella is one of the major pathological agents responsible for diarrhea and diarrhea-related mortality worldwide. It shows a decreasing sensitivity to most conventional antibiotics available today. Methods: Hence, an antimicrobial peptide, Octominin II, was conjugated to a cell-penetrating peptide (HIV-TAT) named TAT-Octominin II, and its antibacterial effect against Shigella flexneri was investigated. Results: TAT-Octominin II displayed minimum inhibitory and bactericidal concentrations of 10 and 25 µg/mL, respectively. It showed rapid membrane-permeabilizing activity, as observed in the ONPG assay. TAT-Octominin II treatment altered the cell membrane integrity and causing membrane damage in S. flexneri. Moreover, TAT-Octominin II increased oxidative stress, as evidenced by the upregulation of antioxidant genes, such as sodA, sodB, katG, oxyR, and soxR. Furthermore, TAT-Octominin II bound to genomic DNA and RNA, which likely inhibited the transcription and translation of bacterial proteins. In addition, TAT-Octominin II possessed lipopolysaccharide neutralization activity. In vitro toxicity analysis was performed using mammalian Raw 264.7 and HEK 293 cells, which showed no toxicity at lower concentrations (0-100 µg/mL). Conclusions: Overall, our results demonstrate that TAT-conjugated Octominin II exhibits enhanced antibacterial activity compared to Octominin II alone, suggesting that TAT-mediated delivery of AMPs could be a promising strategy to improve the therapeutic efficacy of AMPs.

PMID 42938774
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PubMedJournal of the American Chemical Society2026-10-27

Modulating the Electronic Properties of Conductive Conjugated Coordination Polymers with Atomic-Level Precision.

Noh Hyuk-Jun HJ, Pennington Doran L DL, Del Campo Mark M, Hendon Christopher H CH et al.

Conductive metal-organic frameworks and conjugated coordination polymers (CCPs) are promising platforms for low-power electronics and sustainable energy technologies, yet charge-transport design rules remain elusive. In diamine-based frameworks, Cu-coordinated motifs exhibit electrical conductivities several orders of magnitude lower than those of their Ni analogs, but the origin of this disparity has remained unclear, complicating rational selection of earth-abundant metal nodes for multifunctional materials. Here, we report the synthesis and atomic-resolution characterization of Cu-TABQ, a diamine-based CCP grown as single-crystals from tetraamino-p-benzoquinone and copper ions. Microcrystal electron diffraction reveals a distorted pseudosquare-planar Cu-coordination with asymmetric imine bonding, electron localization, and a structural model consistent with possible local protonation/hydrogen bonding. In contrast, Ni-TABQ adopts a planar, symmetric coordination environment that supports charge delocalization and near-metallic transport. Density functional theory suggests that protonation stabilizes the distorted Cu-TABQ structure and suppresses charge transport. Together, these results support an atomic-level explanation for metal-dependent transport in diamine-based frameworks and establish the metal-ligand coordination environment and protonation as tunable handles for designing conductive frameworks.

PMID 42937847
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PubMedNutrients2026-10-27

Changes in Bile Acid Metabolism and Nutrient-Stimulated Hormone Responses After Malabsorptive Metabolic Surgery: RYGB Versus SADI-S.

Jiménez-Varas Inés I, Ortega-Madueño Isabel I, Larrad-Sainz Angélica A, Barabash-Bustelo Ana A et al.

Background/Objectives: Bariatric-metabolic surgery (BMS) improves obesity through neuroendocrine mechanisms involving bile acids (BAs) and nutrient-stimulated gastrointestinal hormones. However, the underlying pathophysiology involved remains poorly understood. BAs are essential for the digestion and absorption of dietary fat and fat-soluble vitamins and act as nutrient-responsive signaling molecules, so their handling after malabsorptive procedures is relevant both to metabolic outcomes and to nutritional status. Methods: We prospectively compared Roux-en-Y gastric bypass (RYGB) and single-anastomosis duodeno-ileal bypass with sleeve gastrectomy (SADI-S) in a single-center case-control study including 37 RYGB and 31 SADI-S patients with severe obesity and 19 non-obese controls. Before and one year after surgery, participants underwent a standardized mixed-meal test (nutrient challenge) with measurement of 14 individual BA fractions, insulin, GLP-1, ghrelin, FGF19, leptin, and adiponectin; bile acid malabsorption was assessed one year after surgery with the 75Se-SeHCAT test, and weight was followed for up to 5 years. Results: Fasting total BAs increased after both techniques, with no significant between-technique difference in total BA exposure (primary outcome). The techniques were associated with distinct BA profiles: fasting concentrations of conjugated BAs (GCA, GCDCA, and TDCA) were higher after SADI-S than after RYGB (FDR-adjusted q < 0.05), with a similar but more variable pattern in postprandial AUCs, whereas RYGB was characterized by a greater postprandial rise in the unconjugated secondary BA DCA. After surgery, FGF19 increased progressively during the mixed-meal test, peaking at 90 min, and its increase correlated with the rise in conjugated BAs, particularly in SADI-S. The postprandial insulin peak shifted earlier in both techniques, with a lower insulin AUC in SADI-S; GLP-1 responses were supraphysiological, and ghrelin increased post RYGB but was suppressed after SADI-S. Leptin decreased markedly, and in an exploratory analysis, its decrease was associated with weight-loss success at 3 years. Weight loss was greater with SADI-S at 1 year, but not significantly different at 3 and 5 years; in an exploratory analysis, the increase in conjugated BAs correlated negatively with recurrence weight gain from nadir at 5 years. The SeHCAT test showed no bile acid malabsorption in SADI-S and normal retention in 90.6% of RYGB patients. Despite routine supplementation, total protein, zinc, copper, and the vitamin A/RBP and vitamin E/cholesterol ratios decreased after both techniques. Conclusions: In conclusion, RYGB and SADI-S are associated with differentiated BA and hormonal profiles. The predominance of conjugated BAs after SADI-S, which we hypothesize may be related to its longer biliopancreatic limb, emerges as a potential candidate mechanism for weight maintenance that requires confirmation and was not accompanied by clinically relevant bile acid malabsorption; however, the decreases observed in several micronutrients support careful nutritional follow-up after both techniques. Clinical trial registration: ISRCTN81954082.

PMID 42942969
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PubMedJournal of separation science2026-10-27

Hydrophilic Interaction Liquid Chromatography Enables Drug-to-Antibody Ratio Measurement of a Heterogeneous Lysine-Conjugated Antibody Fragment.

Makey Devin M DM, Favell Lauren B LB, Larson Eli J EJ, Barrientos Rodell C RC et al.

Accurate measurement of drug-to-antibody ratio (DAR) is essential for characterizing antibody-based conjugates, but heterogeneous lysine conjugation and hydrophilic payload structures can limit the selectivity of conventional hydrophobicity-based separations. Here, we describe an ion-pairing hydrophilic interaction liquid chromatography (HILIC) method for quantitative DAR measurement of a heterogeneous lysine-conjugated drug-Fc conjugate. Column chemistry, sample preparation, and mobile phase additives were systematically investigated. Reduced and deglycosylated samples analyzed on a bare silica column with methanesulfonic acid-containing mobile phases provided the highest selectivity and resolution. In silico retention modeling was used to rapidly optimize conditions that balanced resolution, robustness, and analysis time. Beyond enabling efficient method optimization, in silico retention modeling can support validation readiness by defining a robust method operating space early in development and strengthening the scientific rationale for assay-condition selection. The final method resolved DAR-related species from DAR0 to DAR7 and demonstrated linear detector response from drug-Fc solutions ranging from 1 to 15 mg/mL in concentration. Consistent average DAR values were observed across concentration levels, with recovery of 99.8%-101.3%. Replicate percent relative standard deviations for average DAR were <0.25%. Together, these results establish HILIC as a practical approach for quality control-friendly DAR measurement of highly heterogeneous, hydrophilic bioconjugates.

PMID 42934902
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