
Drug Discovery Today, Год журнала: 2024, Номер 30(1), С. 104255 - 104255
Опубликована: Ноя. 29, 2024
Язык: Английский
Drug Discovery Today, Год журнала: 2024, Номер 30(1), С. 104255 - 104255
Опубликована: Ноя. 29, 2024
Язык: Английский
Next research., Год журнала: 2025, Номер unknown, С. 100234 - 100234
Опубликована: Март 1, 2025
Язык: Английский
Процитировано
2Journal of Pharmacology and Experimental Therapeutics, Год журнала: 2025, Номер 392(3), С. 103391 - 103391
Опубликована: Янв. 20, 2025
Язык: Английский
Процитировано
1Brain Sciences, Год журнала: 2023, Номер 13(8), С. 1193 - 1193
Опубликована: Авг. 11, 2023
Schizophrenia is a chronic neuropsychiatric syndrome that significantly impacts daily function and quality of life. All the available guidelines suggest combined treatment approach with pharmacologic agents psychological interventions. However, one in three patients non-responder, effect on negative cognitive symptoms limited, many drug-related adverse effects complicate clinical management. As result, discovering novel drugs for schizophrenia presents significant challenge psychopharmacology. This selective review literature aims to outline current knowledge aetiopathogenesis present recently approved newly discovered pharmacological substances treating schizophrenia. We discuss ten drugs, which have been by FDA (Olanzapine/Samidorphan, Lumateperone, Pimavanserin). The rest are under trial investigation (Brilaroxazine, Xanomeline/Trospium, Emraclidine, Ulotaront, Sodium Benzoate, Luvadaxistat, Iclepertin). additional basic research required not only improve our understanding neurobiology potential targets schizophrenia, but also establish more effective therapeutical interventions syndrome, including attenuation avoiding dopamine blockade-related effects.
Язык: Английский
Процитировано
18ACS Omega, Год журнала: 2023, Номер 8(44), С. 41417 - 41426
Опубликована: Окт. 24, 2023
Schizophrenia is a chronic psychotic disorder characterized primarily by cognitive deficits. Drugs and therapies are helpful in managing the symptoms, mostly with long-term compliance. There pressing need to design more efficient drugs fewer adverse effects. Solubility, metabolic stability, toxicity, permeability, transporter effects important parameters efficacy of drug design, which turn depend upon different physical chemical characteristics drugs. In recent years, there has been growing interest developing computational tools for discovery development schizophrenia. Some these methods use machine learning algorithms predict side potential Other studies have used computer simulations understand molecular mechanisms underlying disease identify new targets development. Topological indices numeric quantities linked structure properties, reactivity, stability through quantitative structure–property relationship (QSPR). This work aimed at using statistical techniques link QSPR correlating properties connectivity linear regression. The model gives quite better estimation drugs, such as melting point, boiling enthalpy, flash molar refractivity, refractive index, complexity, weight, refractivity. Results validated comparing actual values estimated
Язык: Английский
Процитировано
18Medicinal Research Reviews, Год журнала: 2024, Номер unknown
Опубликована: Сен. 19, 2024
Abstract Since the first discovery of antipsychotics in 1950s, targeting dopaminergic drugs has manifested to well manage positive symptoms schizophrenia with limited efficacy for negative and cognitive symptoms. In past decades, extensive efforts have been undertaken towards development innovative agents that can effectively stabilize dopamine serotonin systems or target nondopaminergic pathways, leading various promising drug candidates entering into clinical trials. Notably, sigma‐2, 5‐HT 2A , α 1A receptor antagonist roluperidone, as a fixed‐dose combination M 1/4 agonist KarXT, submitted NDA applications. The dual ulotaront, which targets TAAR1 receptors, GlyT1 inhibitor iclepertin advanced phase 3 Nevertheless, satisfactory therapeutic strategies remain elusive. This review highlights current endeavors developing novel chemical small‐molecule entities combinations treatment since 2017, thus facilitating efficient next generation antipsychotics.
Язык: Английский
Процитировано
4Pharmacological Research, Год журнала: 2024, Номер 210, С. 107510 - 107510
Опубликована: Ноя. 19, 2024
Язык: Английский
Процитировано
4Journal of Psychopharmacology, Год журнала: 2024, Номер 38(6), С. 503 - 506
Опубликована: Апрель 23, 2024
A major effort of the pharmaceutical industry has been to identify and market drug treatments that are effective in ameliorating symptoms psychotic illness but without limitations current acting at dopamine D2 receptors. These include induction a range adverse effects, inadequate treatment response substantial proportion people with schizophrenia, generally poor negative cognitive features disease. Recently introduced have gone some way avoiding first these, reduced propensity for weight gain, cardiovascular risk extrapyramidal motor effects. Despite claims small improvements symptoms, these drugs not demonstrated increases efficacy. Of currently development as antipsychotic agents, several misleadingly described having novel ‘non-dopaminergic’ mechanisms may offer addressing effects It will be argued, using trace amine-associated receptor 1 agonist an example, new still act primarily through modulation dopaminergic neurotransmission and, primary pathology therefore unlikely much-needed efficacy required address unmet need associated resistance treatments.
Язык: Английский
Процитировано
3Acta Pharmaceutica Sinica B, Год журнала: 2025, Номер unknown
Опубликована: Май 1, 2025
Язык: Английский
Процитировано
0World Journal of Psychiatry, Год журнала: 2025, Номер 15(6)
Опубликована: Май 29, 2025
This minireview explores the role of acetylcholine and muscarinic receptors in pathophysiology schizophrenia summarizes latest data on xanomeline/trospium chloride, a novel antipsychotic approved by United States Food Drug Administration September 2024. Evidence suggests that cholinergic dysfunction, particularly an imbalance expression M1 M4 receptors, may contribute to symptoms schizophrenia. Xanomeline/trospium chloride combines xanomeline, receptor agonist, with trospium non-selective peripheral antagonist reduces side effects. Clinical trials have demonstrated significant reductions positive negative schizophrenia, improvements Positive Negative Syndrome Scale scores observed as early two weeks. A post-hoc analysis one trial revealed cognitive patients baseline impairment. medication was generally well-tolerated, mild-to-moderate gastrointestinal being most common adverse events. While these results are promising, further research is needed better understand its effectiveness safety real-world clinical practice, define optimal managing this complex psychiatric disorder.
Язык: Английский
Процитировано
0Schizophrenia Research, Год журнала: 2025, Номер 282, С. 1 - 18
Опубликована: Май 29, 2025
Язык: Английский
Процитировано
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