TK-112690(TK-112690) - 药物靶点：Uridine phosphorylase_在研适应症：放射性口腔黏膜炎，头颈部鳞状细胞癌，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

METREXASSISTTM

靶点

Uridine phosphorylase

作用方式

抑制剂

作用机制

尿苷磷酸化酶抑制剂

治疗领域

肿瘤消化系统疾病口颌疾病

在研适应症

放射性口腔黏膜炎头颈部鳞状细胞癌结直肠癌+ [1]

非在研适应症-

原研机构

Tosk, Inc.

在研机构

Tosk, Inc.

非在研机构-

权益机构-

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C10H12N2O5

InChIKeyWLLOAUCNUMYOQI-JAGXHNFQSA-N

CAS号22423-26-3

关联

7

项与 TK-112690 相关的临床试验

CTRI/2023/11/060212

/ Recruiting临床2期

A Phase 2a, Multi-center, Open Label, Dose Optimization, Pilot Study to Assess the Safety and Tolerability at the Maximum Tolerated Dose of Parenteral TK-112690 in Non-Metastatic Squamous Cell Carcinoma of Head and Neck Patients Scheduled to Receive Chemoradiation. - NIL

开始日期2023-12-06

申办/合作机构

Tosk, Inc.

CTRI/2022/06/043202

/ Completed临床2期

A Phase 2a, multi-center, placebo-controlled, randomized, assessor blind study ofbolus 5-fluorouracil and infused leucovorin plus either infused TK 90 for parenteral use or infused TK 90 placebo administered weekly for 6 consecutive weeks to patients with colorectal cancer.

开始日期2022-07-26

申办/合作机构

Tosk, Inc.

CTRI/2022/06/043203

/ Completed临床2期

A Phase 2a, multi-center, placebo-controlled, randomized, assessor-blind study to assess the safety & efficacy of parenteral TK-90 or parenteral TK-90 placebo administered daily to Patients scheduled to receive radiotherapy for non-metastatic squamous cell carcinoma of the head and neck (SCCHN). - TOSK 0004

开始日期2022-06-24

申办/合作机构

Tosk, Inc.

100 项与 TK-112690 相关的临床结果

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100 项与 TK-112690 相关的转化医学

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100 项与 TK-112690 相关的专利（医药）

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53

项与 TK-112690 相关的文献（医药）

2015-05-01·Journal of Heterocyclic Chemistry

Cu(I)‐Catalyzed Efficient Synthesis of 2′‐Triazolo‐nucleoside Conjugates

作者: Parmar, V. S. ; Olsen, C. E. ; Rana, N. ; Prasad, A. K. ; Mathur, D.

A small library of thirty‐two 2′‐triazolyl uridine and 2′‐triazolyl‐5‐methyluridine has been synthesized by Cu(I)‐catalyzed condensation of 2′‐azido‐2′‐deoxyuridine and 2′‐azido‐2′‐deoxy‐5‐methyluridine with different alkynes and aryl propargyl ethers in almost quantitative yields. Triazolo‐nucleoside conjugates, which can be evaluated for different biological activity for suitable drug development, were unambiguously identified on the basis of 1H NMR, 13C NMR, IR, and HRMS data analysis. These compounds have been synthesized for the first time and have not been reported in the literature earlier.

2015-01-01·Journal of the Brazilian Chemical Society

A New Straightforward Synthesis of 2', 3'-Didehydro-2', 3'-dideoxy-2'-(2"-(trimethylsilyl)ethylthio)thymidine, Key Intermediate for the Synthesis of 2'-Substituted Thionucleosides

作者: Suely L. Galdino ; Maria C. A. Lima ; Ivan R. Pitta ; Lucas L. Franco ; Maralise P. Oliveira ; Cláudia M. O. Simões ; Jean-Luc Décout ; Ricardo J. Alves

We describe herein a straightforward and efficient preparation of 2',3'-dideoxy-2'-(2''-(trimethylsilyl)ethylthio)thymidine, which allows the preparation of diverse potentially antiviral and/or anticancer nucleosides (disulfides, thiols, sulfides, thiocyanates).

2014-09-01·ChemMedChem3区 · 医学

Synthesis and Antisense Properties of 2′‐O‐(2S‐Methoxypropyl)‐RNA‐Modified Gapmer Antisense Oligonucleotides

3区 · 医学

Article

作者: Thazha P. Prakash ; Punit P. Seth ; Jinghua Yu ; Sanjay K. Pandey ; Eric E. Swayze ; Hetal Khatri

AbstractTo ascertain whether increasing hydrophobicity can enhance the activity of second‐generation antisense oligonucleotides (ASOs) in muscle, we investigated the antisense properties of 2′‐O‐(2S‐methoxypropyl)‐RNA (2S‐MOP)‐modified ASOs. Synthesis of the 2S‐MOP 5‐methyl uridine phosphoramidite was accomplished on a multi‐gram scale by Lewis‐acid‐catalyzed ring opening of 5′‐O‐tert‐butyldiphenylsilyl ether‐protected 2,2′‐anhydro‐5‐methyl uridine with 2S‐methoxy‐1‐propanol. Synthesis of the 2S‐MOP 5‐methyl cytidine nucleoside from the corresponding 5‐methyl uridine nucleoside was accomplished by formation and displacement of a 4‐triazolide intermediate with aqueous ammonia. 2S‐MOP‐modified oligonucleotides were prepared on an automated DNA synthesizer and showed similar enhancements in duplex thermal stability as 2′‐O‐methoxyethyl RNA (MOE)‐modified oligonucleotides. 2S‐MOP‐containing antisense oligonucleotides were evaluated in Balb‐c mice and showed good activity for decreasing the expression levels of scavenger receptor B1 (Srb1) and phosphatase and tensin homologue (PTEN) mRNA in liver and muscle tissue.

100 项与 TK-112690 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
放射性口腔黏膜炎	临床2期	印度	Tosk, Inc.	2022-06-17
头颈部鳞状细胞癌	临床2期	印度	Tosk, Inc.	2022-06-17
结直肠癌	临床2期	印度	Tosk, Inc.	2022-06-15
粘膜炎	临床2期	印度	Tosk, Inc.	2019-05-15

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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


NCT04046250 (TK112690, CTgov)	临床2期	粘膜炎	22	TK-112690 (TK112690)	簾廠簾憲構蓋繭鏇衊艱(夢衊願獵構觸艱繭築醖) = 膚淵糧餘膚鑰遞鑰築網醖鏇繭糧繭艱憲繭範鑰 (鹹蓋遞醖鹽窪簾獵齋窪, 遞築窪蓋廠獵夢憲鹹鬱 ~ 願繭鹹構糧顧鑰衊鑰壓) 更多	-	2021-06-03
				Placebo TK-112690 (Placebo)	簾廠簾憲構蓋繭鏇衊艱(夢衊願獵構觸艱繭築醖) = 鹹願鹽淵夢鏇獵獵齋鹹醖鏇繭糧繭艱憲繭範鑰 (鹹蓋遞醖鹽窪簾獵齋窪, 窪糧鹹顧網壓夢網觸遞 ~ 構鑰鹽構願顧廠鏇糧遞) 更多