estrogens is a therapeutic agent developed by Teva Pharmaceutical Industries Ltd.. It is approved for therapeutic indications via intravaginal or oral (po).
| Brand Names | Cenestin, Bijuva, Barr |
| Company | Teva Pharmaceutical Industries Ltd. |
| Molecular Target | ESR1 |
| Route | Intravaginal, Oral (PO) |
| Status | Approved |
estrogens acts on 1 molecular target:
| ESR1 | estrogen receptor 1 (ER, ESR) |
estrogens is developed for 3 unique indications across 2 therapeutic areas.
| Therapeutic Area | Condition | Phase |
|---|---|---|
| Reproductive system and breast disorders | Atrophic vulvovaginitis | ✓ Approved |
| Surgical and medical procedures | Hormone replacement therapy | ✓ Approved |
| Reproductive system and breast disorders | Menopausal symptoms | ✓ Approved |
Wiesner Anna A, Jończyk-Potoczna Katarzyna K, Mikoś Marcin M, Krenke Katarzyna K et al.
Wang Ying Y, Liu Jian J, Fan Xiangyu X, Sun Xujing X et al.
Preheating polyacrylonitrile at 240 °C before sulfurization yields a highly intact ladder-like conjugated skeleton, enabling optimized SPAN with 52.07 wt% sulfur loading and reduced H2S release.
Todorović Aleksandra A, Ćujić Danica D, Knežević Jugović Zorica Z, Uskoković Petar P et al.
Although SARS-CoV-2 immunity has been widely investigated, the relationship between antibody levels and cellular immune responses following different routes of exposure to SARS-CoV-2 remains not fully revealed. In this study, cellular immunity was assessed using a newly developed whole-blood interferon-gamma release assay (nano-IGRA) based on gold nanoparticle (AuNP)-conjugated SARS-CoV-2 antigens. AuNP-conjugated and soluble antigens were compared regarding interferon gamma (IFN-γ) responses and intra- and interassay reproducibility in 112 individuals with immunity acquired through infection, vaccination, or both. Humoral immunity was evaluated by enzyme-linked immunosorbent assay (ELISA). Overall, 88% of participants were seropositive. AuNP-conjugated Spike (S) and Nucleocapsid (N) SARS-CoV-2 antigens induced significantly higher IFN-γ responses than soluble antigens in all exposure groups (p < 0.001). AuNP conjugation reduced intraassay variability by 62.4% and 61.4% for S and N, respectively, and interassay variability by 71.7% and 68.3%, respectively. Antibody levels correlated significantly with IFN-γ responses to S (ρ = 0.358, p < 0.001) and N (ρ = 0.309, p < 0.001). An interesting finding is that cellular responses were also detected in some seronegative individuals. Nano-IGRA, based on a novel AuNP-based approach, provides antigen-specific cellular immune assessment, combining enhanced IFN-γ responses with improved reproducibility. Further studies should establish diagnostic cut-offs, sensitivity, specificity, and clinical performance.
Nguyen Anh T L ATL, Ojong Cecile T CT, Dutilleul Pierre P, Aryee Alberta N A ANA
Njangsa seed oil (NSO) is rich in polyunsaturated fatty acids and represents an underexplored plant source for producing conjugated linoleic acid (CLA). This study explored the production of CLA from NSO via alkali isomerization, as well as and its stabilization by β-cyclodextrin (β-CD) inclusion complexation. A 3-factor factorial design was used to optimize reaction conditions, yielding a maximum purified CLA content of 46.42% from 2.5 g NSO at 180 °C for 3 h, with cis-9, trans-11 CLA as the predominant isomer. Inclusion complexation produced microparticles averaging 19.73 µm with 83.36% inclusion efficiency. Complexed CLA showed lower peroxide, para-anisidine, and thiobarbituric acid values than free CLA, indicating improved oxidative stability. Fourier transform infrared spectroscopy showed spectral changes consistent with interactions between the CLA-rich fraction and β-CD, while scanning electron microscopy and X-ray diffraction revealed changes in morphology and crystalline organization, respectively. These findings demonstrate the feasibility of producing NSO-enriched CLA and enhancing its oxidative stability through β-CD inclusion complexation.
Desai Devam A DA, Cristofoletti Rodrigo R
Unconjugated antisense oligonucleotides (ASOs) and GalNAc-conjugated small interfering RNAs (siRNAs) have emerged as transformative therapeutic modalities, but their translation remains hindered by complex pharmacokinetics characterized by rapid plasma clearance, heterogeneous tissue uptake, and prolonged intracellular retention. Physiologically based pharmacokinetic (PBPK) modeling offers a mechanistic framework to integrate these processes across species, yet applications to oligonucleotides remain limited, and existing efforts are typically restricted to specific chemistries or routes of administration. This study aimed to develop a cross-species PBPK platform to characterize the plasma and tissue disposition of unconjugated ASOs and GalNAc-siRNAs in preclinical species and humans, and to evaluate the consistency of estimated drug-specific parameters with pre-specified allometric scaling relationships within the domain of compounds and routes considered. Published datasets spanning mice, rats, non-human primates, and humans were integrated for representative unconjugated ASOs (Malat-1, GluR1, p-tau, tominersen) and GalNAc-siRNAs (ALN-AT3, givosiran, fitusiran). The PBPK model incorporated 11 tissue compartments, cerebrospinal fluid substructures, tissue substructures, endosomal trafficking, non-specific binding in kidney and liver, and ASGPR-mediated internalization for GalNAc-siRNAs. Parameters for endocytosis, exocytosis, and degradation were estimated, and estimated values were compared with pre-specified allometric exponents to assess physiological plausibility (i.e., as a consistency check rather than independent inference of scaling laws). The model captured plasma, liver, kidney, and CNS profiles across species, reproducing rapid systemic clearance with prolonged tissue half-lives. Estimated parameter values for endocytosis, exocytosis, and non-specific kidney binding were consistent with pre-specified allometric exponents (b = -0.25 and -0.2, respectively), supporting the physiological plausibility of the estimates. Sensitivity analyses identified endocytosis and rate of degradation as dominant determinants of systemic and tissue disposition. This work establishes a translational PBPK platform for unconjugated ASOs and GalNAc-conjugated siRNAs, enabling quantitative interspecies extrapolation within the domain of the compounds, routes, and species studied. The framework provides a mechanistic basis to support dose selection, safety assessment, and clinical translation for these subclasses; extrapolation to other oligonucleotide subclasses (e.g., GalNAc-ASOs, unconjugated siRNAs, LNP-formulated oligonucleotides) will require additional datasets and dedicated validation.
Yusupov F A FA, Abdykadyrov M Sh MS
To analyze modern data on the influence of biological sex and gender factors on mechanisms of neuroplasticity and functional recovery after neurosurgical interventions. We reviewed the databases (PubMed, Scopus, Russian Science Citation Index (RSCI) and Google Scholar) over the past 10 years. The review covers clinical trials, prospective and retrospective cohort studies and animal models of traumatic brain injury, surgery for brain cancer, vascular accidents and spinal cord injury. The main parameters were diffusion tensor imaging data, functional MRI, hormonal profile and standardized clinical scales including the modified Rankin scale, Barthel index, ASIA and FIM scales. Female brain has better interhemispheric connectivity that provides adaptive advantage in focal lesions of dominant hemisphere. Male brain is optimized for intrahemispheric signaling promoting faster motor coordination. Estrogens and progesterone have neuroprotective effect through modulation of inflammatory response and support of myelination, but this effect depends on age and phase of reproductive cycle. In clinical practice, women often demonstrate lower rates of functional independence at discharge after stroke due to comorbidity and social factors, despite equal or superior potential for neurological recovery compared to men. Biological sex is a critical determinant of neurosurgical outcomes. Discrepancy between biological recovery potential (higher in women) and actual functional outcomes (often better in men) highlights the need to develop personalized, gender-specific rehabilitation protocols taking into account specifics of connectome and hormonal backgrounds.
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