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更新于：2024-12-27

Lumefantrine

本芴醇

更新于：2024-12-27

概要

基本信息

药物类型

小分子化药

别名

(±)-2,7-Dichloro-9-((Z)-p-chlorobenzylidene)-α-((dibutylamino)methyl)fluorene-4-methanol、2-Dibutylamino-1-[2,7-dichloro-9-(4-chloro-benzylidene)-9H-fluoren-4-yl]-ethanol、2-Dibutylamino-1-{2,7-dichloro-9-[1-(4-chloro-phenyl)-meth-(Z)-ylidene]-9H-fluoren-4-yl}-ethanol

+ [5]

靶点

CYP2D6

作用机制

CYP2D6抑制剂(细胞色素P450家族成员2D6抑制剂)

治疗领域

感染

在研适应症

疟疾

非在研适应症-

原研机构

中国人民解放军军事医学科学院

在研机构

昆药集团股份有限公司

非在研机构-

最高研发阶段批准上市

首次获批日期

中国 (1987-01-01),

疟疾

最高研发阶段(中国)批准上市

特殊审评-

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结构/序列

分子式C30H32Cl3NO

InChIKeyDYLGFOYVTXJFJP-MYYYXRDXSA-N

CAS号82186-77-4

关联

项与本芴醇相关的临床试验

PACTR202311879488648

/ Recruiting临床4期IIT

Therapeutic efficacy of Artemether-Lumefantrine for the treatment of uncomplicated Plasmodium falciparum

开始日期2023-10-13

申办/合作机构

Centers for Disease Control & Prevention

ACTRN12623000241639

/ Recruiting临床4期IIT

Evaluation of the efficacy and safety of Artemether +Lumefantrine (Coartem®) with low-dose Primaquine for the treatment of uncomplicated Plasmodium falciparum and Plasmodium vivax malaria in three sites of Savanakhet, Salavanh, and Attopue province, Lao PDR 2022)

开始日期2022-10-01

申办/合作机构-

NCT05330273

/ Completed临床1期

A Phase I, Open-label, Fixed-sequence, Two-period, Crossover, Drug-drug Interaction Study to Investigate the Effect of Efavirenz on the Pharmacokinetics of Ganaplacide and Lumefantrine Combination in Healthy Participants

This study assessed the effect of multiple doses of a moderate inducer of cytochrome P450 (CYP) 3A4 (efavirenz) on the pharmacokinetics (PK) of ganaplacide and lumefantrine combination. Results from this study will provide guidance on prescribing ganaplacide and lumefantrine combination when co-administered with moderate inducers of CYP3A4.

开始日期2022-04-28

申办/合作机构

Novartis Pharmaceuticals Corp.

[+1]

100 项与本芴醇相关的临床结果

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100 项与本芴醇相关的转化医学

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100 项与本芴醇相关的专利（医药）

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1,367

项与本芴醇相关的文献（医药）

2025-01-01·JOURNAL OF PHARMACEUTICAL SCIENCES

Quantification of soluplus for dissolution tests: SEC method development and validation

Article

作者: Petersone, Liga ; Horváth, Zoltán Márk ; Mohylyuk, Valentyn

The quantification of both polymer and drug during the dissolution of an amorphous solid dispersion (ASD) in aqueous media arouses great interest and may aid in the formulation. However, the available quantification methods for polymer excipients are limited, expensive, and challenging compared to drugs. In this work, a size exclusion chromatography method (HPLC-SEC) was developed and validated to determine the concentration of a frequently used polymer excipient, Soluplus® (Sol). In order to develop a method for the quantification of dissolved Soluplus®, two methods (SEC-UV and SEC-RID) with two injection volumes were tested with standard solutions of three different batches of Soluplus. The developed HPLC-SEC-UV method showed acceptable linearity (R² > 0.9990) for all batches of Soluplus, good accuracies above a concentration of 0.1 mg/mL (coefficient of variation < 2 %), relatively good precision at a concentration of 0.1 mg/mL (coefficient of variation < 2.5 %), and high recoveries at a concentration of 0.75 mg/mL (coefficient of variation < 0.5 %). The presence of Felodipine (Fel) and Lumefantrine (Lum) in the liquid media did not interfere with Soluplus quantification. The use of various surfactants, such as Tween® 80, Tween® 20, Span® 80, Span® 20, Kolliphor® TPGS, and sodium lauryl sulphate at a low concentration (0.005 mg/mL) did not show any effect on Soluplus® and did not interfere with Soluplus® quantification with any of the Soluplus batches. The addition of lithium bromide (LiBr) to the mobile phase within a concentration range of 0.05-1.0 M did not improve Soluplus® quantification.

2025-01-01·INTERNATIONAL JOURNAL OF PHARMACEUTICS

Multi-method coamorphous systems of lumefantrine with alpha ketoglutaric acid: Comprehensive characterization, biological evaluation and stability analysis

Article

作者: Dhiman, Vivek ; Medtiya, Pravin ; Khemchandani, Rahul ; Tomar, Devendra Singh ; Golla, Vijaya Madhyanapu ; Khushwaha, Bhoopendra Singh ; Goud, Sridivya ; Pardhi, Ekta ; Mehra, Neelesh Kumar ; Godugu, Chandraiah ; Samanthula, Gananadhamu ; Shaikh, Nadeem

The coamorphous systems (CAM) of lumefantrine (LMF) and alpha-ketoglutaric acid (KGA) were developed using three different methods to address the solubility and bioavailability limitations of LMF. Powder X-ray diffraction spectroscopy (PXRD) and the differential scanning calorimetry (DSC) confirmed the complete amorphization of the three CAM by the halo pattern and glass transition temperature (Tg), respectively. Attenuated total reflectance-Fourier transform infrared spectroscopy (ATR-FTIR) and nuclear magnetic resonance spectroscopy (NMR) results indicated that intermolecular interactions existed in the three CAM. Solid-state molecular dynamics simulations revealed the different intermolecular disordered environments present in all three CAM. Solubility analysis showed 14.73×, 12.8× and 9.81× improvement in the liquid-assisted grinding-based coamorphous system (CAM LAG), solvent evaporation-based coamorphous system (CAM SE) and quench-cool-based coamorphous system (CAM QC), respectively, compared to LMF crystalline (LMF CRY). In the in-vitro dissolution experiment 2.63-, 2.16- and 2.17-times increments were observed in CAM LAG, CAM SE and CAM QC compared to LMF CRY, respectively. In-vivo pharmacokinetics study revealed 10.86-, 9.24- and 8.46- folds increments in C_max of CAM LAG, CAM SE and CAM QC, respectively, compared to LMF CRY. All three CAM illustrated anti-cancer activity in the A549 lung cancer cell line. Molecular dynamics simulation of LMF and KGA with Epidermal growth factor receptor (EGFR), a target for lung cancer treatment, revealed good binding affinity and stability. Stability studies performed under accelerated storage (40°C/75% RH) and extreme environmental conditions indicated that all three CAM have good stability. Different methods based prepared CAM have shown different physicochemical properties, bioavailability and stability profiles. These findings suggest that LMF-KGA CAM effectively addresses the solubility and bioavailability challenges of LMF, potentially leading to better therapeutic outcomes in lung cancer treatment.

2025-01-01·CURRENT PHARMACEUTICAL DESIGN

Recent Advancement in Drug Development for Treating Malaria using Herbal Medicine and Nanotechnological Approach

Article

作者: Deshmukh, Rohitas ; Dewangan, Hitesh Kumar ; Bhargava, Sarvesh

More than two hundred million people around the world are infected with malaria, a blood-borne disease that poses a significant risk to human life. Single medications, such as lumefantrine, primaquine, and chloroquine, as well as combinations of these medications with artemisinin or its derivatives, are currently being used as therapies. In addition, due to rising antimalarial drug resistance, other therapeutic options are needed immediately. Furthermore, due to anti-malarial medication failures, a new drug is required. Medication discovery and development are costly and time-consuming. Many malaria treatments have been developed however, most treatments have low water solubility and bioavailability. They may also cause drugresistant parasites, which would increase malaria cases and fatalities. Nanotechnology may offer a safer, more effective malaria therapy and control option. Nanoparticles' high loading capacity, concentrated drug delivery, biocompatibility, and low toxicity make them an attractive alternative to traditional therapy. Nanotechnologybased anti-malarial chemotherapeutic medications outperform conventional therapies in therapeutic benefits, safety, and cost. This improves patient treatment compliance. The limitations of malaria treatments and the importance of nanotechnological approaches to the treatment of malaria were also topics that were covered in this review. The most recent advancements in nanomaterials and the advantages they offer in terms of medication delivery are discussed in this article. The prospective therapy for malaria is also discussed. Additionally, the limitations of malaria therapies and the importance of nanotechnology-based approaches to the treatment of malaria were explored.

项与本芴醇相关的新闻（医药）

2024-11-21

·诺华集团

诺华荣登2024年药品可及性指数排名榜首

该指数彰显了诺华在药物研发与药品可及性方面的领导地位，诺华在这些方面均排名第一诺华积极推进抗疟疾药物可及，在中低收入国家/地区广泛注册产品，并通过包容性商业模式在多个国家/地区提升药品可及性，这些均被行业公认为最佳实践诺华在2024年药品可及性指数中表现出色，排名提升三位，荣登榜首近日，2024年药品可及性指数（ATMI）报告发布，诺华名列榜首，彰显了诺华在全球范围内提升药品可及性的领导地位。该指数是一份独立报告，每两年发布一次，旨在评估全球前20大研究型制药企业在改善药品、疫苗及诊断工具可及性方面的努力，覆盖了113个中低收入国家/地区（LMIC）的81种疾病。报告特别强调了诺华在非传染性疾病和重点高负担疾病（如疟疾、南美锥虫病和登革热）方面的领先产品组合和研发管线，以及针对后期研发管线产品制定的广泛可及性策略。报告中提到的最佳实践案例有一半与诺华相关。诺华荣登2024年药品可及性指数排行榜第一位，彰显了我们的基本承诺，即确保突破性创新药物能够惠及有需要的患者，无论他们身处何地。自诺华成立以来，我们始终将药品可及性作为优先事项，并在早期临床研发阶段就进行深度整合。作为一名从事公共卫生工作的医学科学家，我亲眼见证了像诺华这样的公司在为患者提供治疗方面产生的深远影响。行业各方在缩小药品可及性差距方面还有很多工作要做，但此次诺华获此殊荣离不开我们全球70,000多名员工与合作伙伴的不懈努力，大家共同致力于创想医药未来，改善人们生活质量，延长人类寿命。 2023年，诺华的药品惠及全球超过2.84亿患者，通过可及性计划惠及3,320万患者。报告特别强调了诺华的可及性计划如何助力公司实现这一目标，具体包括：将全面的药品可及性策略纳入公司整体战略之中，为所有重点后期研发管线产品制定可及性计划在中低收入国家/地区广泛注册创新产品，并实施包容性商业模式，提升多个低收入和最不发达国家/地区的产品可及性最佳实践“抗疟疾药物可及性计划”包括与Medicine for Malaria Venture（MMV）合作，推进新型ganaplacide/lumefantrine-SDF联合疗法治疗成人和儿童疟疾的III期临床试验此外，诺华还与被忽视疾病药物研发倡议组织（Drugs for Neglected Diseases Initiative，DNDi）合作，在埃塞俄比亚推进治疗内脏利什曼病的口服药物进入II期临床试验诺华全球健康部门总裁Lutz Hegemann 确保广泛和具有包容性的医疗创新可及性，是我们作为可持续发展企业最大化发挥积极影响力的关键。该指数表彰了我们已取得的成就，但我们的工作并未结束。我们将持续努力，与合作伙伴携手，确保我们所发现的每项创新成果能惠及每一个有需求的人。关于药品可及性指数药品可及性指数是由药品可及性基金会（Access to Medicine Foundation，ATMF）发布的双年度指数，旨在评估全球前20大研究型制药企业在提升中低收入国家/地区的药品及医疗服务可及性方面的表现。除药品可及性指数外，诺华还参与其他多项环境、社会和公司治理（ESG）评级，这些评级为投资者决策提供重要信息，包括CDP、Sustainalytics、ISS ESG和MSCI评级等。药品可及性基金会成立于2003年，致力于通过激励和动员制药企业，扩大其在中低收入国家/地区的基本医疗产品可及性，从而推动医疗生态系统改革。该基金会为独立非营利组织，资助方包括英国与荷兰政府、比尔及梅琳达·盖茨基金会（Bill & Melinda Gates Foundation）、利昂娜和哈里赫尔姆斯利慈善信托（Leona M. and Harry B. Helmsley Charitable Trust）、惠康基金会（Wellcome Trust）、安盛投资管理公司（AXA Investment Managers）以及斯图尔特投资者公司（Stewart Investors）。该基金会为荷兰注册慈善机构（具有ANBI地位）。

疫苗临床2期

2024-11-14

·drugs

Malaria Developing Resistance to Drug That Saves Children's Lives

THURSDAY, Nov. 14, 2024 -- Over 600,000 people worldwide die from mosquito-borne malaria each year, with the majority of these deaths happening among children under 5. Now, there's troubling news that the malaria parasite may be gaining resistance against artemisinin, the drug most often used to try and save these young lives. “This is the first study from Africa showing that children with malaria and clear signs of severe disease are experiencing at least partial resistance to artemisinin,” said study co-author Dr. Chandy John , who directs Indiana University's Ryan White Center for Infectious Diseases and Global Health, in Indianapolis. “It’s also the first study showing a high rate of African children with severe malaria experiencing a subsequent malaria episode with the same strain within 28 days of standard treatment with artesunate , a derivative of artemisinin, and an artemisinin combination therapy [ACT]," John added. Researchers presented their findings Thursday at the annual meeting of the American Society of Tropical Medicine and Hygiene in New Orleans. The findings were published simultaneously in the Journal of the American Medical Association. As the researchers explained in a meeting news release, the advent of artemisinin therapies two decades ago revolutionized malaria care. Plasmodium falciparum, the microscopic parasite that causes malaria, had grown resistant to standard medications, but artemisinin could swiftly cure the illness. But by 2008, there were already signs that P. falciparum was also developing resistance to the newer drug. Cases in Cambodia showed partial resistance to the drug and by 2013 there were instances where artemisinin completely failed to help infected patients. In the new study, partial resistance to artemisinin was found in 11 of 100 Ugandan children treated, John and colleagues reported. The treatment time needed to clear children of the parasite was also much longer in many cases. These children ranged in age from 6 months to 12 years and were all being treated for “complicated” malaria -- illness with signs of potentially life-threatening symptoms such as anemia or brain complications. As well, 10 children whose malaria was thought to have been cured saw a recurrence of the illness within a month, suggesting that artemisinin hadn't wiped the parasite out after all. All of the children did eventually recover. However, lab analysis determined that 10 carried forms of P. falciparum that harbored the same resistance mutations seen in resistant cases in Southeast Asia, the researchers said. That's the first time they've been spotted in African children with severe malaria, the team noted. Many of the children were also treated with a second (non-artemisinin) drug, lumefantrine . But a high number of kids who got the two-drug combination therapy also saw their illnesses come back, suggesting that the malaria parasite might be developing resistance to lumefantrine, too. “The fact that we started seeing evidence of drug resistance before we even started specifically looking for it is a troubling sign,” John noted. “We were further surprised that, after we turned our focus to resistance, we also ended up finding patients who had recurrence after we thought they had been cured.” Whatever your topic of interest, subscribe to our newsletters to get the best of Drugs.com in your inbox.

临床研究

2024-07-18

·Insight数据库

诺华 Q2 财报出炉：上半年净销售额增长 11% 至 243 亿美元！

7 月 18 日，诺华发布了 2024 年第二季度及上半年财务报告。报告显示：2024年第二季度该公司总净收入为 32 亿美元，净销售额为 125 亿美元（+9%，+11% cc[固定货币简称，下同] ）；2024 年上半年，该公司总净收入为 59 亿美元，净销售额为 243 亿美元（+9%，+11% cc）。截图来源：诺华官网第二季度财务表现净销售额为 125 亿美元（+9%，+11% cc[固定货币简称，下同] ）。营业收入为 40 亿美元（+43%，+47% cc）。净收入为 32 亿美元（+43%，+49% cc），主要得益于营业收入增加。核心营业收入为 50 亿美元（+17%，+19% cc）。核心营业收入利润率为净销售额的 39.6%，增加了 2.5 个百分点（+2.7 个百分点 cc）。核心净收入为 40 亿美元（+14%，+18% cc），主要由于核心营业收入增加。上半年财务表现净销售额为 243 亿美元（+9%，+11% cc）。营业收入为 74 亿美元（+36%，+43% cc）。净收入为 59 亿美元（+34%，+43% cc），主要得益于营业收入增加。核心营业收入为 95 亿美元（+16%，+21% cc），主要得益于净销售额增加，部分抵消了研发投资增加的影响。核心营业收入利润率为净销售额的 39.0%，增长 2.4 个百分点（+3.1 个百分点 cc）。核心净收入为 77 亿美元（+14%，+19% cc），主要由于核心营业收入增加。 2024年 Q2 诺华 TOP 20 销售额产品截图来源：诺华财报诺华在报告中表示，2023 年，该公司完成了向「纯」创新药物业务的转型。该公司明确专注于四个核心治疗领域：心血管-肾脏-代谢、免疫学、神经科学和肿瘤学，且每个领域都有多个重要的在售和管线资产，可解决高疾病负担并具有巨大的增长潜力。除了两个成熟的技术平台（化学和生物治疗）外，该公司的三个新兴平台（基因和细胞治疗、放射性配体治疗和 xRNA）也被列为优先研究领域。从地域上看，诺华主要专注于在美国、中国、德国和日本等重点地区发展。在报告中，诺华也介绍了该公司在第二季度的重要研发管线进展和亮点。获批进展 Fabhalta (Iptacopan)：在欧盟、日本和中国获批用于治疗成人罕见血液病阵发性睡眠性血红蛋白尿症（PNH）。 Lutathera (Lutetium Lu 177 dotatate) ：获 FDA 批准用于治疗患有生长抑素受体阳性胃肠胰神经内分泌肿瘤（GEP-NET）的儿科患者（≥12 岁）。监管更新 Scemblix (Asciminib)：FDA 授予 Scemblix 突破性疗法认定，用于治疗新诊断的费城染色体阳性慢性期慢性粒细胞白血病 (Ph+ CML-CP) 成年患者；已完成向 FDA 递交一线 CML 治疗的申请。 Atrasentan：FDA 已接受其用于治疗成人 IgA 肾病患者的申请。 Lutathera (Lutetium Lu 177 dotatate)：欧盟 EMA 已接受其用于治疗新诊断的、不可切除或转移性的、分化良好（G2 和 G3）、生长抑素受体阳性的成人 GEP-NET 的申请。正在进行的临床试验结果和其它亮点 Scemblix (Asciminib) 在 III 期 ASC4FIRST 研究中，针对新诊断的 Ph+ CML-CP 成人患者，Scemblix 在 48 周时表现出优于研究者选定的标准治疗酪氨酸激酶抑制剂 (TKI)（67.7% vs 49.0%）和单独使用伊马替尼（69.3% vs 40.2%）的响应率，并表现出良好的安全性和耐受性。这些结果已根据实时肿瘤学审评（RTOR, Real-Time Oncology Review）提交给 FDA。 Kisqali (Ribociclib) 在 HR+/HER2- 早期乳腺癌 III 期 NATALEE 研究中，对所有患者结束 Kisqali 治疗后的新分析表明，该药物具有持续的临床意义益处，且具有一致的安全性。结果将在即将召开的医学会议上公布。此外，在最终 iDFS 数据截止时，NATALEE 研究的亚组分析显示，在高风险淋巴结阴性 (N0) 疾病患者中，内分泌治疗中添加 Kisqali 可使 iDFS 风险降低 28%。在高风险 N0 亚组中观察到的疗效、安全性和耐受性特征与 NATALEE 研究总体人群一致。 Fabhalta (Iptacopan) III 期 APPEAR-C3G 数据显示，使用 Fabhalta 治疗并辅以支持性治疗的 C3 肾小球病患者在 6 个月时蛋白尿水平较安慰剂降低 35.1%。估计肾小球滤过率的次要终点数据显示，与安慰剂相比，6 个月内数值有所改善。研究还显示，Fabhalta 具有良好的安全性，没有新的安全信号。诺华计划于 2024 年下半年向 FDA 和 EMA 提交其治疗成人 C3 肾小球病适应症的申请。 III 期 APPLAUSE-IgAN 数据显示，与安慰剂相比，IgAN 患者在 9 个月内蛋白尿减少 38.3%。Fabhalta 耐受性良好，安全性良好，与之前报告的数据一致。 Atrasentan 预先指定的 III 期 ALIGN 数据中期分析结果显示，接受 Atrasentan 治疗的患者，加上肾素-血管紧张素系统抑制剂的支持性治疗，在 36 周时，与安慰剂相比，蛋白尿显著减少了 36.1%。。 Remibrutinib III 期 REMIX-1 和 REMIX-2 数据显示，口服 Remibrutinib 对慢性自发性荨麻疹患者具有持续疗效和长期安全性，最早在第 1 周观察到每周荨麻疹活动评分改善，并持续至第 52 周。在两项研究中，Remibrutinib 表现出良好且一致的安全性，长达一年，包括与安慰剂相比肝功能测试结果平衡。诺华计划于 2025 年向监管部门提交 Remibrutinib 的上市申请。 Coartem (Artemether-Lumefantrine) II/III 期 CALINA 研究数据表明，针对体重不到 5 公斤的疟疾婴儿开发的 Coartem 优化剂量具有所需的药代动力学特征以及良好的疗效和安全性。交易进展为符合对肿瘤学的战略重点，诺华收购了 MorphoSys AG 90% 以上的总股本，以丰富其产品管线，包括用于治疗骨髓纤维化的后期研究 BET 抑制剂 Pelabresib 和用于治疗实体瘤或淋巴瘤的早期研究 EZH2 和 EZH1 双重抑制剂 Tulmimetostat。诺华收购了 Mariana Oncology，这是一家专注于开发一系列实体瘤的新型放射性配体疗法 (RLT) 的生物技术公司。此次收购扩充了诺华的 RLT 项目组合，包括 MC-339，这是一种正在研究用于小细胞肺癌的锕基 RLT。诺华扩大了与 PeptiDream 的肽发现合作。根据多项目协议，PeptiDream 将针对诺华选定的靶点识别和优化新型大环肽，以用于 RLT 的潜在应用。诺华与 Arvinas 签署了独家战略许可协议，在全球范围内开发和商业化 ARV-766。ARV-766 是一种第二代 PROTAC® 雄激素受体 (AR) 降解剂，补充了诺华在前列腺癌领域的 RLT 平台。诺华首席执行官 Vas Narasimhan 在评论 2024 年第二季度业绩时表示：“诺华第二季度业绩表现强劲，净销售额增长 11%，核心营业利润率接近 40%。业绩反映了我们在美国和美国以外地区的主要增长动力持续强劲，这使我们能够上调 2024 财年指引。我们还在第二季度推进了我们的产品线，完成了向 FDA 提交一线 CML 药物 Scemblix 和 IgAN 药物 Atrasentan 的申请，在 NATALEE 研究中生成更新数据以支持 Kisqali 在早期乳腺癌中的强劲表现，并执行多项交易以扩大我们在 RLT 和前列腺癌领域的产品线。我们仍有望实现中期销售增长（2023-2028 年复合年增长率 +5%）和利润率（到 2027 年达到 40% 以上）指引。” 封面来源：企业 Logo 免责声明：本文仅作信息分享，不代表 Insight 立场和观点，也不作治疗方案推荐和介绍。如有需求，请咨询和联系正规医疗机构。 PR 稿对接：微信 insightxb 投稿：微信 insightxb；邮箱 insight@dxy.cn 多样化功能、可溯源数据…… Insight 数据库网页版等你体验点击阅读原文，立刻解锁！

财报突破性疗法

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