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

Monash UniversityAlchemia Oncology Pty Ltd.

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-

结构

分子式C4H3FN2O2

InChIKeyGHASVSINZRGABV-UHFFFAOYSA-N

CAS号51-21-8

关联

8

项与透明质酸/氟尿嘧啶相关的临床试验

NCT03370406 / Recruiting临床1期IIT

Phase I, Dual Arm, Open-Label, Trial of Intralesional 5-Fluorouracil (5FU) and Intralesional 5FU Combined With Topical Imiquimod in Patients With Squamous Cell Carcinoma (SCC) of the Lower Extremities

This clinical trial proposes to evaluate a relatively unexplored approach to treatment of squamous cell carcinoma (SCC) on the lower extremities. The strategy is to directly and specifically deliver drug to the tumor. For the proposed phase I clinical trial, the investigators will perform intralesional injections of a well characterized, potent chemotherapeutic agent 5-fluorouracil (5FU) with and without a topical application of 5% imiquimod to kill topically accessible SCC cells. The goal of the study is to evaluate the safety profile and tolerability of intralesional-5FU with and without a concomitant topical imiquimod and measure the clinical objective response rate (ORR) in treated lesions compared to untreated lesions 3 weeks after treatment.

开始日期2018-08-03

申办/合作机构

National Cancer Institute

NCT01821729 / Unknown status临床2期

Phase II Feasibility Study of FOLFIRINOX-Losartan Followed by Accelerated Short Course Radiation Therapy With Capecitabine for Locally Advanced Pancreatic Cancer

This is a Phase II clinical trial, which tests the safety and effectiveness of an investigational combination of drugs to learn whether the combination of drugs works in treating a specific cancer. "Investigational" means that the combination of drugs is being studied. It also means that the FDA has not yet approved it for your type of cancer. Proton beam radiation therapy is an FDA approved radiation delivery system.
Conventional radiation therapy uses photons to treat cancer before patients undergo surgery to remove the tumor. In this study we are using radiation with protons, which spares surrounding tissue and organs from radiation. Proton radiation delivers radiation to the area requiring radiation with no dose beyond the treatment area. This may reduce side effects that patients would normally experience with conventional radiation therapy.
Researchers in the laboratory have discovered pathways inside cancer cells which contribute to the growth and survival of tumors. The FOLFIRINOX chemotherapy regimen is a combination of the drugs 5-fluorouracil, leucovorin and oxaliplatin. These chemotherapy drugs, along with the chemotherapy drug capecitabine, work by blocking these pathways and thereby preventing tumor growth. Capecitabine is FDA approved to be used alone or with other drugs to treat other types of advanced cancer, but not pancreatic cancer. In past research studies, FOLFIRINOX followed by radiation therapy with capecitabine has been identified as the most effective and active chemotherapy for patients with cancer that is spreading, and this is why we are using it to treat your type of cancer.
Losartan is classified as an angiotensin-receptor blocker (ARB), and is FDA approved for use in people with high blood pressure. Recent studies in people with different types of cancer, including pancreatic cancer, have shown that combining chemotherapy drugs with an ARB can help reduce/stop tumor growth more effectively than chemotherapy alone. Losartan has been used in previous research studies, and information from those research studies suggests that this drug in combination with FOLFIRINOX and capecitabine may be better at treating your type of cancer.
In this research study, we seek to determine whether combining FOLFIRINOX with Losartan before proton radiation therapy will be more efficient at controlling the growth of or shrinking your tumor than just FOLFIRINOX alone.

开始日期2013-07-01

申办/合作机构

The General Hospital Corp.

[+1]

EUCTR2010-020348-36-GB / 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2011-01-31

申办/合作机构-

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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34

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

Purpose:

There 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 Methods:

In 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.

Results:

This 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.

Conclusion:

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

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

Abstract:

The 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	澳大利亚	The Sustainable Nutrition Group Pty Ltd.	-
结直肠癌	临床2期	-	Alchemia Oncology Pty Ltd.	-
结直肠癌	临床2期	-	Monash University	-

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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


NCT01821729 (CTgov)	临床2期	局部晚期胰腺腺癌	50	Proton Beam Radiation+Leucovorin Calcium+irinotecan+Losartan+oxaliplatin+Irinotecan hydrochloride+FLUOROURACIL	膚獵廠觸廠膚積壓構積(廠製觸艱憲觸觸窪淵遞) = 窪艱獵鹹壓鏇鹽鹹鑰遞憲簾積鏇鹹觸窪積獵選 (鑰鑰壓艱鏇構膚齋選鏇, 襯糧簾網築鑰構膚糧觸 ~ 廠築鑰鏇齋襯製襯蓋製) 更多	-	2019-09-17
NCT00682786 (CTgov)	临床2期	直肠癌	135	Radiation+5FU (Good Risk (Thymidylate Synthase (TYMS)2/2, 2/3, 2/4))	廠糧願艱淵鏇廠選範網(築築遞衊糧鹹艱齋窪餘) = 築製鏇選選壓鑰艱鹹壓製繭網夢願鹹積鏇積淵 (網願構醖夢觸蓋觸積構, 顧顧製繭襯鹽願願遞選 ~ 鬱顧繭簾醖築顧鹹蓋鹹) 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))	廠糧願艱淵鏇廠選範網(築築遞衊糧鹹艱齋窪餘) = 願繭鹽網憲積簾網廠範製繭網夢願鹹積鏇積淵 (網願構醖夢觸蓋觸積構, 鏇鏇鬱觸積醖簾範觸顧 ~ 糧淵網鏇憲憲襯鏇觸艱) 更多	-	2014-09-08