透明质酸/氟尿嘧啶(Hyaluronic acid/Fluorouracil) - 药物靶点：CD44 x TYMS_在研适应症：结直肠癌_专利_临床

概要

基本信息

药物类型

小分子化药

别名

HA-5-fluorouracil、Hyaluronan acid-5-fluorouracil complex、Hyaluronic acid-5-fluorouracil complex

+ [2]

靶点

CD44 x TYMS

作用机制

CD44调节剂(CD44抗原调节剂)、TYMS抑制剂(胸苷酸合成酶抑制剂)

治疗领域

肿瘤消化系统疾病

在研适应症

结直肠癌

非在研适应症-

原研机构

Monash University

在研机构

Alchemia Oncology Pty Ltd.

Monash University

非在研机构

The Sustainable Nutrition Group Pty Ltd.

最高研发阶段临床2期

首次获批日期-

最高研发阶段(中国)-

特殊审评-

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结构/序列

分子式C4H3FN2O2

InChIKeyGHASVSINZRGABV-UHFFFAOYSA-N

CAS号51-21-8

关联

5

项与透明质酸/氟尿嘧啶相关的临床试验

NCT03018418

/ Active, not recruiting临床2期IIT

A Prospective Pilot Study to Evaluate the Feasibility of Intensity Modulated Proton Therapy in Reducing Toxicity in Anal Cancer

The purpose of this research study is to determine whether the amount of radiation given to the normal areas around the anal cancer can be reduced by using Proton Therapy while reducing the side effects that are seen with standard therapy.

开始日期2017-01-04

申办/合作机构

University of Cincinnati (Ohio)

EUCTR2010-020348-36-BG

/ Not yet recruitingN/A

Randomized double-blind Phase III trial of FOLF(HA)iri vs FOLFIRI forsecond or third line therapy in irinotecan-naïve patients with metastaticcolorectal cancer - HA-Irinotecan Phase III trial ACO-002

开始日期2011-02-24

申办/合作机构-

NCT01151761

/ Terminated临床2期IIT

Phase II Study of Stereotactic Body Radiotherapy (SBRT) and Chemotherapy for Unresectable Cholangiocarcinoma Followed by Liver Transplantation

The purpose of this study is to determine progression-free survival at 12 months for stereotactic body radiotherapy (SBRT) and chemotherapy for unresectable hilar cholangiocarcinoma (CCA).

开始日期2011-01-01

申办/合作机构

Stanford University

100 项与透明质酸/氟尿嘧啶相关的临床结果

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100 项与透明质酸/氟尿嘧啶相关的转化医学

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100 项与透明质酸/氟尿嘧啶相关的专利（医药）

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33

项与透明质酸/氟尿嘧啶相关的文献（医药）

2023-01-01·Clinical, cosmetic and investigational dermatology

Efficacy and Tolerability of Cosmetic Serums Enriched with Five Forms of Hyaluronic Acid as Part of Biweekly Diamond Tip Microdermabrasion Treatments for Facial Skin Dryness and Age-Associated Features.

Article

作者: Emmerich, Tanja ; Huang, Priscilla C ; Makino, Elizabeth T ; Mehta, Rahul C ; Jiang, Lily I

PurposeThere is growing interest in combining topical treatments with aesthetic procedures to combat signs of aging skin. This study aimed to assess the efficacy and tolerability of a novel cosmetic serum containing 5 different forms of HA (HA⁵ DG) when used via a proprietary diamond-tip microdermabrasion procedure (DG) to treat skin dryness, fine lines/wrinkles, rough texture, and dullness.Patients and MethodsIn this open-label, single-center study, participants received HA⁵ DG as part of a biweekly DG procedure on the face and neck for 12 weeks. Study participants also applied another take-home HA⁵ serum to the face twice daily at home, along with a basic skincare regimen. The efficacy of the combined treatment was measured by clinical quantification of multiple skin appearance features, analysis of bioinstrumental measurements, and digital photography.ResultsThis study enrolled 27 participants, with an average age of 42.7 years and Fitzpatrick skin phototypes I-III (59.3%), IV (18.5%), and V-VI (22.2%), and 23 participants completed the study. The combined treatment had effects in fine lines/wrinkles, skin dryness, smoothness, radiance, firmness, and hydration 15 minutes post-DG. Furthermore, the significant improvements observed in dryness, fine lines/wrinkles, skin smoothness, and radiance were still visible 3 days after and maintained at week 12. Additionally, smoothing of coarse lines/wrinkles, improvement of skin tone evenness, hyperpigmentation, photodamage, and transepidermal water loss were observed at week 12. The treatment had a favorable tolerability profile and was perceived as efficacious and highly satisfactory.ConclusionThis novel combined treatment delivered immediate and prolonged skin hydration and high participant satisfaction, proving it can be an excellent approach for skin rejuvenation.

2022-12-01·International Journal of Biological Macromolecules

Effects of the molecular weight of hyaluronan on the conformation and release kinetics of self-assembled 5-fluorouracil-loaded lysozyme-hyaluronan colloidal nanoparticles

Article

作者: Zhang, Xin ; Wu, Songgu ; Li, Maolin ; Wei, Jiahao ; Han, Dandan ; Gong, Junbo ; Liu, Yanbo

Lysozyme (LYS) and hyaluronan with low (HA1: 3 kDa), medium (HA2: 120 kDa), and high (HA3: 1200 kDa) molecular weights were used to fabricate lysozyme-hyaluronan colloidal nanoparticles using a green self-assembly method. Fourier transform infrared spectroscopy indicated that hydrogen bonding, hydrophobic and electrostatic interactions promoted the formation of the colloidal nanoparticles. The hydrophobic area of prepared colloidal nanoparticles was quantified using a pyrene fluorescent probe, and the results showed that the LYS-HA3 nanoparticles had the strongest hydrophobic capacity. Furthermore, 5-fluorouracil (5-Fu) was used to evaluate encapsulation performance, demonstrating that the LYS-HA3 nanoparticles had the highest encapsulation ability (>90 %). All prepared 5-Fu-loaded lysozyme-hyaluronan (5-Fu@LYS-HA) colloidal nanoparticles exhibited excellent long-term storage stability at 4 °C for 60 days. Cellular uptake and in vitro release results indicated that the LYS-HA2 nanoparticles exhibited the highest cellular uptake efficiency, and the LYS-HA3 nanoparticles had the best slow-release effect, while the release process was mainly controlled by the combination of Fickian diffusion and structural relaxation, respectively. This study demonstrates the influence of molecular weight on the conformational and structural properties of colloidal nanoparticles, which has implications for the design of insoluble drug self-assembly systems.

2020-10-01·Journal of Cellular Physiology2区 · 生物学

Hyaluronic acid‐decorated liposomal nanoparticles for targeted delivery of 5‐fluorouracil into HT‐29 colorectal cancer cells

2区 · 生物学

Article

作者: Abedi‐Gaballu, Fereydoon ; Dehghan, Gholamreza ; Baradaran, Behzad ; Mansoori, Behzad ; Yekta, Reza ; Abbaspour, Soheil ; Ghasabi, Mehri ; Hamblin, Michael R. ; Shirjang, Solmaz ; Mohammadi, Ali

AbstractThe use of liposomes as drug carriers improves the therapeutic efficacy of anticancer drugs, while at the same time reducing side effects. Hyaluronic acid (HA) is recognized by the CD44 receptor, which is overexpressed in many cancer cells. In this study, we developed HA‐modified liposomes encapsulating 5‐fluorouracil (5‐FU) and tested them against a CD44 expressing colorectal cell line (HT29) and a non‐CD44 expressing hepatoma cell line. The average size of 5‐FU‐lipo and 5‐FU‐lipo‐HA nanoparticles were 112 ± 28 and 144 ± 77 nm, respectively. The 3‐(4,5‐dimethylthiazol‐2‐yl)‐2,5‐diphenyltetrazolium (MTT) assay showed selective cancer cell death depending on the CD44 expression in a time‐dependent manner. Apoptosis assays and cell‐cycle analysis indicated that G0/G1 arrest occurred. The colony formation study revealed that cells treated with 5‐FU‐lipo and 5‐FU‐lipo‐HA had reduced colony formation. Quantitative reverse‐transcription polymerase chain reaction study showed that the oncogenic messenger RNA and microRNA levels were significantly reduced in the 5‐FU‐lipo‐HA‐treated group, while tumor suppressors were increased in that group. We suggest that optimal targeted delivery and release of 5‐FU into colorectal cancer cells, renders them susceptible to apoptosis, cell‐cycle arrest, and decreased colony formation.

100 项与透明质酸/氟尿嘧啶相关的药物交易

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研发状态

10 条进展最快的记录,

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适应症	最高研发状态	国家/地区	公司	日期
结直肠癌	临床2期	-	Alchemia Oncology Pty Ltd.	-
结直肠癌	临床2期	-	Monash University	-
结直肠癌	药物发现	澳大利亚	The Sustainable Nutrition Group Pty Ltd.	-

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临床结果

适应症

分期

评价

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研究	分期	人群特征	评价人数	分组	结果	评价	发布日期


NCT00682786 (CTgov)	临床2期	直肠癌	135	Radiation+5FU (Good Risk (Thymidylate Synthase (TYMS)2/2, 2/3, 2/4))	鏇網糧廠壓鏇窪範願襯(窪壓網製構製遞廠鏇選) = 繭艱鬱襯醖顧餘齋窪襯製壓鏇繭鑰蓋醖襯膚壓 (築壓壓鑰襯窪觸夢齋願, 鏇壓膚鑰鹽壓鹽夢獵淵 ~ 選製鏇範窪襯觸齋積艱) 更多	-	2014-09-08
NCT00682786 (CTgov)	临床2期	直肠癌	135	Radiation+5FU+Irinotecan (Poor Risk (Thymidylate Synthase (TYMS)3/3, 3/4))	鏇網糧廠壓鏇窪範願襯(窪壓網製構製遞廠鏇選) = 壓淵鹽壓廠蓋鏇餘鹽糧製壓鏇繭鑰蓋醖襯膚壓 (築壓壓鑰襯窪觸夢齋願, 構選鹹顧鏇蓋廠襯淵醖 ~ 蓋鹹壓簾衊簾網夢膚構) 更多	-	2014-09-08
ASCO2012	临床1期	肝转移	19	HA FUDR	鑰襯遞製衊衊構廠憲齋(選衊餘鹹遞壓夢獵衊構) = 淵衊餘廠觸齋範壓願積範鏇夢願網廠顧醖簾鑰 (廠顧構廠膚壓夢築餘積 ) 更多	-	2012-05-20
NCT00463840 (CTgov)	临床1/2期	局部晚期胰腺腺癌	24	FOLFOX 6+5FU+oxaliplatin	廠鏇鏇繭築壓廠鬱鬱範(醖衊廠夢顧鹹願淵膚夢) = 襯窪製簾製鬱築糧願獵鹽窪築顧夢構鏇積襯膚 (糧積製衊範壓夢壓鑰鑰, 壓願齋糧壓鑰積製簾餘 ~ 鬱範夢壓衊淵醖淵襯夢) 更多	-	2012-05-01