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hydroquinone (Melanasa Forte)

✓ Approved

Vinas · 小分子 · 小分子

什么是 hydroquinone？

hydroquinone 是一种小分子，由Vinas研发。该药已获批，用于治疗相关适应症，给药途径：Topical。

药物档案

商品名Melanasa Forte
公司Vinas
药物类别小分子
给药途径Topical
状态Approved
来源： ClinicalTrials.gov, Vinas

治疗适应症

hydroquinone 针对 2 个适应症，涉及 1 个治疗领域。

治疗领域疾病/病症分期
Skin and subcutaneous tissue disordersChloasma✓ Approved
Skin and subcutaneous tissue disordersSkin hyperpigmentation✓ Approved

相关研究文献

PubMedAAPS PharmSciTech2026-09-11

Bergapten-Loaded Dissolving Microneedles for Vitiligo Treatment: A Synergistic Strategy Combining Nanocrystal Technology and Physical Enhancement.

Lu Lingzhi L, Yang Huifen H, Liu Ruda R, Li Chunxue C et al.

Bergapten can effectively treat vitiligo by increasing the activity of melanocytes and tyrosinase, but its low solubility and poor transdermal effect limit its application. In this study, we used dissolvable microneedles (shells) loaded with bergapten nanocrystals (cores), a shell-nucleus-type formulation design, to treat vitiligo, organically integrating physical and pharmacological treatments, and to improve drug delivery efficiency. Firstly, bergapten was prepared into nanocrystals and screened for dissolvable microneedle matrix, and dissolvable microneedles were prepared by centrifugal spin-coating method; then, the quality studies of bergapten nanocrystals dissolvable microneedles (BP-NCs-DMNs) were carried out on the mechanical properties, in vitro solubility properties, skin puncture, and skin barrier restorative measurements and transdermal cumulative permeation experiments; finally, the pharmacological effects of bergapten dissolvable microneedles against vitiligo were verified by determining the tyrosinase (TYR), Interleukin-6 (IL-6), tumor necrosis factor-α (TNF-α), malondialdehyde (MDA), and superoxide dismutase (SOD) levels using a hydroquinone-induced mouse vitiligo model. As a result, the prepared bergapten microneedles could penetrate into the skin, and the skin did not show any redness, swelling, or excessive inflammation after removing the microneedles, and they could be dissolved in vitro in about 35 min. As a result of the in vitro transdermal experiment, the cumulative transmittance of bergapten in 24 h of bergapten microneedle was 257.9 μg/cm2, and the skin absorption rate of the drug was (57.15 ± 2.61) %. The hydroquinone-induced vitiligo model in mice further verified the effect of bergapten micropigmentation on skin pigmentation in mice. In this study, dissolvable bergapten microneedles were successfully established, which can significantly improve the transdermal drug delivery efficiency of bergapten and can effectively treat vitiligo disease.

PMID 42722792
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PubMedNature communications2026-09-11

Engineered polymerase-mediated efficient synthesis of site-specifically functionalized RNA and 2'-modified RNA oligonucleotides via genetic alphabet expansion.

Wu Jing J, Mei Junyan J, Chen Zhipeng Z, Shao Xinyu X et al.

2'-Modified RNA oligonucleotides have found broad use in biotechnology and biomedicine, requiring their efficient synthesis and controllable labelling. While engineered polymerases enable their synthesis, controllable labelling methods remain underdeveloped. Unnatural base pairs (UBPs) have been developed to expand the genetic alphabet, leading to not only the creation of semi-synthetic organisms, but also technologies for site-specific labelling of DNA and RNA. Herein we demonstrate that SFM4-6, an engineered polymerase optimized for 2'-modified RNA oligonucleotide synthesis, can efficiently synthesize unnatural base pair dNaM (2-methoxy-3-(2'-deoxy-β-D-erythro-pentofuranosyl)-naphthalene)-dTPT3 ((2'-deoxy-β-D-erythro-pentofuranosyl)-thieno[3,4]pyridine-2-thione) and its analogues, enabling site-specific incorporation of functionalized unnatural base-containing nucleotides into RNA and 2'-modified RNA oligonucleotides. By combining this with a strategy involving controlled pause and restart of primer extension, we establish methods for producing single or dual-labelled RNA and 2'-modified RNA oligonucleotides. These methods successfully produce various functional labelled RNA and 2'-modified RNA oligonucleotides, highlighting their broad applicability in nucleic acid research and biotechnology.

PMID 42722644
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PubMedMolecular therapy : the journal of the American Society of Gene Therapy2026-09-11

A phase 1/2 dose-escalation study of sepiapterin in patients with 6-pyruvoyl-tetrahydropterin synthase deficiency with hyperphenylalaninemia.

Longo Nicola N, Smith Neil N, McNutt Markey M, Whitley Chester B CB et al.

Oral sepiapterin (PTC923), a precursor of tetrahydrobiopterin (BH4), was evaluated in patients with 6-pyruvoyl-tetrahydropterin synthase (PTPS) deficiency in a phase 1/2, multicenter, open-label, randomized, intra-individual dose-escalation study. Patients stopped sapropterin (used to control hyperphenylalaninemia) for 2-4-days before being randomized 1:1 into 2 cohorts receiving sepiapterin at 2 doses (Cohort 1: 2.5 and 10 mg/kg/day; Cohort 2: 5 and 20 mg/kg/day) each for 7 days, separated by a 2-4-day washout period. Eight participants (5 male, 3 female, aged 2.2-20.0 years) completed the study (4 in each cohort). Overall, 7/8 participants (87.5%) experienced a total of 35 treatment-emergent adverse events; none were severe, serious, or led to discontinuation. Mean phenylalanine levels increased (up to 800-1200 μmol/L) after discontinuation of sepiapterin or sapropterin, and normalized (<130 μmol/L) with sepiapterin at all tested doses by Day 2. Blood BH4 concentrations increased with increasing single doses of sepiapterin, reaching a peak at approximately 3-4 hours, which was 2-3 hours after the sepiapterin peak. These results show that in patients with PTPS deficiency, sepiapterin is rapidly converted to BH4 and normalizes blood phenylalanine concentrations, with no dose-limiting toxicity or dose-related adverse events.

PMID 42723281
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PubMedF1000Research2026-09-11

Evaluation of the efficiency of the optimal combination of  hormonal, physical  and biological stimuli in the induction and growth of callus in Lavandula angustifolia Mill.

Mohammed Mohammed Abdulgafor MA, Dafer Alani Masara M, Mashaan Ahmed O AO, Almehemdi Ali F AF

Lavender is a crucial source of secondary metabolites with medicinal and industrial importance. Its exploitation faces challenges due to the limited availability of raw materials and their sensitivity to climate. Tissue culture techniques, particularly callus culture, represent the most sustainable method for the continuous production of these active compounds. This study focused on developing an effective protocol for inducing and stimulating callus cultures in lavender plants. Callus formation was stimulated from leaf tissue has cultured on MS medium supplemented with different concentrations of 2, 4-D (0, 1, 2 and 3) mg L -1. The cultures were incubated under light or dark conditions. In the multiplication: calli (Cultured in MS medium containing 1 mg, 2,4-D incubated in the dark) was transferred to MS medium containing different 2,4-D (0, 1, 2 and 3 mg.L -1) and BA (0,1 and 2 mg.L -1). The multiplied callus (Cultured in MS medium containing 1mg L -1 2, 4-D and 2 mg L -1 BA) was transferred into two nutrient media, MS and B5, each supplemented with different levels of chitosan (0, 50, 100, and 200 mg.L -1) along with combination of 1 mg.L -1 2, 4-D and 2 mg.L -1 BA. The results indicated that the optimal concentration for callus induction was 1 mg L -1 of 2,4-D, with the highest callus formation rate 95% recorded under dark conditions. Among all treatments, the combination of 2, 4-D 1 mg L -1 and BA 2 mg L -1 was the most effective for sustainable callus growth. Regarding the nutrient medium, B5 was more efficient than the MS medium. For the biostimulants, Chitosan at 100 mg L -1 recorded the highest efficiency in both fresh and dry callus weights. This study underscores the necessity of integrating hormonal, nutritional and environmental factors for optimal callus production.

PMID 42723645
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PubMedJournal of enzyme inhibition and medicinal chemistry2026-09-11

Exploring novel isatin derivatives as SARS-CoV-2 3CLpro inhibitors.

Song Jian J, Shi Cai C, Yang Boning B, Yang Jingxiang J et al.

A series of novel isatin derivatives were synthesised by incorporating phenyl, biphenyl, naphthyl and indolyl moieties into the N-1 position and screened in vitro against SARS-CoV-2 3CLpro, respectively. These isatin compounds with halogen substitution at the isatin ring and trifluoromethylbenzyl substitution at N-1 position were strong inhibitors of SARS-CoV-2 3CLpro. Furthermore, introduction of electron withdrawing groups at the C-5 and C-7 of isatin ring, such as bromo group, might be more favourable for the inhibition activity. The most potent compound 34 demonstrated an IC50 of 0.363 ± 0.045 µM against SARS-CoV-2 3CLpro. Additionally, a jump dilution assay, surface plasmon resonance (SPR) spectroscopy and in silico analysis were used to measure the binding of compound 34 to SARS-CoV-2 3CLpro respectively, supporting the obtained in vitro findings. Moreover, compound 34 inhibited viral cell proliferation with an IC50 of 0.404 ± 0.021 μM (selectivity index (SI) =170). Therefore, it is worth to further investigate compound 34 as a SARS-CoV-2 3CLpro inhibitor.

PMID 42723354
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PubMedEClinicalMedicine2026-09-11

The association of ADHD and ADHD medication with adherence to pharmacotherapy for type 2 diabetes: a population-based cohort study from seven countries.

Zhou Yiling Y, Yao Honghui H, Xie Tian T, Gillies Malcolm B MB et al.

Attention-deficit/hyperactivity disorder (ADHD) may compromise adherence to pharmacotherapy in adults with type 2 diabetes, but the relationship is unknown. We investigated the association of ADHD and ADHD medication with antidiabetic medication adherence in multinational cohort data. Using a common analytical protocol and population-based databases from seven countries, we identified adults initiating non-insulin antidiabetic medication between 2010 and 2020. ADHD was identified by diagnosis or ADHD medication use. We used the proportion of days covered (PDC) to measure antidiabetic medication adherence and defined the primary outcome, poor adherence, as PDC <80% over 1-, 2-, and 5-year follow-up periods. Time-to-first-discontinuation was the secondary outcome. Country-specific estimates were obtained using logistic and Cox regression and pooled using random-effects meta-analyses. Among 3,643,197 individuals included, 1,871,870 (51.4%) were female and 88,339 (2.4%) had ADHD (76,973 [87.1%] received ADHD medication). Overall, ADHD was not associated with poor adherence to antidiabetic medication (1-, 2-, and 5-year pooled odds ratios [OR]: 1.01 [95% CI 0.90-1.14], 1.03 [0.91-1.17], and 1.12 [0.95-1.31]); country-specific estimates ranged from 0.79 to 1.32, 0.80 to 1.35, and 0.80 to 1.47 at 1, 2, and 5 years, respectively. Among males, ADHD was associated with poorer adherence (1.09 [95% CI 1.00-1.20], 1.12 [1.00-1.24], and 1.23 [1.11-1.37] at 1, 2, and 5 years). Similar results were found for discontinuation. Among individuals with ADHD, ADHD medication use was consistently associated with better adherence over 1-, 2-, and 5-year follow-up periods (e.g., 5-year pooled OR 0.45 [0.30-0.67]); associations were directionally consistent across countries. Among adults with type 2 diabetes, ADHD may not necessarily compromise antidiabetic medication adherence when appropriately managed in routine care. ADHD pharmacological treatment may support adherence among adults with comorbid ADHD and type 2 diabetes, although its causal effect requires further evaluation. EU Horizon 2020 Research and Innovation Programme.

PMID 42724543
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