硫鸟嘌呤(Thioguanine) - 药物靶点：DNA_在研适应症：急性淋巴细胞白血病，急性髓性白血病，费城染色体阳性慢性粒细胞白血病_专利_临床

概要

基本信息

药物类型

小分子化药

别名

2-Amino 6MP、2-Amino-1,7-dihydro-6H-purine-6-thione、2-Amino-6-mercaptopurine

+ [26]

靶点

DNA

作用方式

抑制剂

作用机制

DNA抑制剂(DNA抑制剂)

治疗领域

肿瘤免疫系统疾病血液及淋巴系统疾病

在研适应症

急性淋巴细胞白血病急性髓性白血病费城染色体阳性慢性粒细胞白血病

非在研适应症-

原研机构

Aspen Pharmacare Holdings Ltd.

在研机构

Waylis Therapeutics LLC上海东海制药股份有限公司东海制药厂

非在研机构

Only For Children Pharmaceuticals SA

最高研发阶段批准上市

首次获批日期

美国 (1966-01-18),

急性髓性白血病费城染色体阳性慢性粒细胞白血病

最高研发阶段(中国)批准上市

特殊审评孤儿药 (欧盟)

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结构/序列

分子式C5H5N5S

InChIKeyWYWHKKSPHMUBEB-UHFFFAOYSA-N

CAS号154-42-7

关联

92

项与硫鸟嘌呤相关的临床试验

NCT06124157

/ Not yet recruiting临床3期IIT

A Randomized International Phase 3 Trial of Imatinib and Chemotherapy With or Without Blinatumomab in Patients With Newly-Diagnosed Philadelphia Chromosome-Positive or Philadelphia Chromosome-Like ABL-Class B-Cell Acute Lymphoblastic Leukemia

This phase III trial compares the effect of the combination of blinatumomab with dasatinib and standard chemotherapy versus dasatinib and standard chemotherapy for treating patients with Philadelphia chromosome positive (PH+) or Philadelphia chromosome-like (Ph-Like) ABL-class B-Cell acute lymphoblastic leukemia (B-ALL). Blinatumomab is a bispecific antibody that binds to two different proteins-one on the surface of cancer cells and one on the surface of cells in the immune system. An antibody is a protein made by the immune system to help fight infections and other harmful processes/cells/molecules. Blinatumomab may bind to the cancer cell and a T cell (which plays a key role in the immune system's fighting response) at the same time. Blinatumomab may strengthen the immune system's ability to fight cancer cells by activating the body's own immune cells to destroy the tumor. Dasatinib is in a class of medications called tyrosine kinase inhibitors. It works by blocking the action of an abnormal protein that signals cancer cells to multiply, which may help keep cancer cells from growing. Giving blinatumomab and dasatinib in combination with standard chemotherapy may work better in treating patients with PH+ or Ph-Like ABL-class B-ALL compared to dasatinib and chemotherapy alone.

开始日期2025-05-29

申办/合作机构

National Cancer Institute

NCT06317662

/ Not yet recruiting临床2期IIT

A Phase 2 Study of Blinatumomab in Combination With Chemotherapy for Infants With Newly Diagnosed Acute Lymphoblastic Leukemia With Randomization of KMT2A-Rearranged Patients to Addition of Venetoclax

This phase II trial tests the addition of venetoclax and/or blinatumomab to usual chemotherapy for treating infants with newly diagnosed acute lymphoblastic leukemia (ALL) with a KMT2A gene rearrangement (KMT2A-rearranged [R]) or without a KMT2A gene rearrangement (KMT2A-germline [G]). Venetoclax is in a class of medications called B-cell lymphoma-2 (Bcl-2) inhibitors. It may stop the growth of cancer cells by blocking Bcl-2, a protein needed for cancer cell survival. Blinatumomab is a monoclonal antibody that may interfere with the ability of cancer cells to grow and spread. Chemotherapy drugs work in different ways to stop the growth of cancer cells, either by killing the cells, by stopping them from dividing, or by stopping them from spreading. Adding venetoclax and/or blinatumomab to standard chemotherapy may be more effective at treating patients with ALL than standard chemotherapy alone, but it may also cause more side effects. This clinical trial evaluates the safety and effectiveness of adding venetoclax and/or blinatumomab to chemotherapy for the treatment of infants with KMT2A-R or KMT2A-G ALL.

开始日期2025-04-26

申办/合作机构

National Cancer Institute

NCT06533748

/ Recruiting临床2期IIT

SJALL23H: Combination Antigen-Directed Induction Therapy for Newly Diagnosed Patients With B-Cell Precursor Acute Lymphoblastic Leukemia and Lymphoma

This is a Phase II clinical trial testing the use of two antigen-directed therapies, inotuzumab and blinatumomab, as part of induction therapy for children and young adults with newly diagnosed B-cell precursor acute lymphoblastic leukemia and lymphoma.
Primary Objective
* To assess if the flow-cytometry assessed MRD-negative remission rate following an immunotherapy-based Induction in NCI-high risk patients without favorable genetic features is higher than the results of similar patients treated on AALL1131.
Secondary Objectives
* To compare flow-cytometry assessed MRD-negative rates at the end of Induction for patients treated with this therapy compared to similar patients treated on TOT17.
* To compare the rate of significant toxicities in patients treated with this therapy to those treated with standard-risk therapy on TOT17.
* To assess the event free and overall survival of patients treated with this therapy.

开始日期2025-01-23

申办/合作机构

St. Jude Children's Research Hospital, Inc.

[+2]

100 项与硫鸟嘌呤相关的临床结果

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100 项与硫鸟嘌呤相关的转化医学

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100 项与硫鸟嘌呤相关的专利（医药）

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5,450

项与硫鸟嘌呤相关的文献（医药）

2025-04-01·Environmental Research

Annual trends in mercury contamination are associated with changing trophic niches of giant petrels

Article

作者: Forero, Manuela G ; Buss, Danielle L ; Mills, William F ; Forcada, Jaume ; Phillips, Richard A ; Bustamante, Paco ; Ramírez, Francisco

Annual variation in prey availability can influence seabird diets and hence their exposure to pollutants, including mercury (Hg). Among seabirds, those species that scavenge carrion of marine mammals and other top predators may be especially vulnerable to accumulating high Hg concentrations. In this study, total Hg (THg) concentrations and carbon (δ¹³C) and nitrogen (δ¹⁵N) stable isotope values were measured in chick feathers of northern giant petrels Macronectes halli and southern giant petrels M. giganteus at Bird Island, South Georgia (2013-2020). Both species are opportunistic predator-scavengers which feed mainly on penguins and Antarctic fur seal Arctocephalus gazella carrion, and to lesser extents on marine prey and other seabirds. THg concentrations were not significantly different between northern giant petrels and southern giant petrels (means ± SDs, 2.49 ± 0.92 μg g^-1 dw and 2.34 ± 0.85 μg g^-1 dw, respectively), but concentrations in both species declined signficantly over time, as did δ¹³C and δ¹⁵N values. Annual feather THg concentrations of giant petrels were positively correlated with the number of dead Antarctic fur seal pups and their mortality rate at Bird Island, but not with population sizes or breeding success of penguins. Accordingly, these results suggest a shift away from carrion (associated with the decreasing size and productivity of the Antarctic fur seal population) and towards the consumption of prey from lower trophic levels (e.g., Antarctic krill Euphausia superba), with a corresponding reduction in dietary Hg exposure. Future work should investigate the consequences of changing prey availability for diets and pollutant exposure of other marine predators within the South Georgia and Scotia Sea marine ecosystems, given the ongoing environmental changes in the region.

2025-04-01·Ecotoxicology

Mercury exposure in an endangered songbird: influence of marsh hydrology and evidence for early breeding impairment

Article

作者: Virzi, Thomas ; Frederick, Peter ; Rothenberg, Sarah E ; Rodríguez-Jorquera, Ignacio ; Reed, Tera A ; Mock, Alan J ; Trexler, Joel C

Songbird reproductive success can decline from consuming mercury-contaminated aquatic insects, but assessments of hydrologic conditions influencing songbird mercury exposure are lacking. We monitored breast feather total mercury (THg) concentrations and reproductive success in the U.S. federally listed endangered Cape Sable Seaside Sparrow (CSSS: Ammospiza maritima mirabilis) over three breeding seasons in the Florida Everglades. We used model comparison to explore the influence of annual hydrologic variation on adult CSSS THg concentrations, and tested mercury effects on individual reproductive success (individuals' mate status, apparent nest success, and total productivity) that were scaled to estimates on population productivity using a demographic model. We identified four hydrologic models that explained annual variation in adult THg concentrations, with the top model showing a negative association between THg concentrations and drought length of the previous breeding season and a positive association between THg concentrations and dry-season water recession rate (model adjusted R² = 0.82). Adult male mating probability declined by 63% across the range of THg concentrations observed. We found no mercury effect on CSSS nest success or total productivity. However, demographic modeling suggested the reduced mating could produce a 60% decrease in population productivity compared to a scenario with no THg impact. Our results suggest that CSSS mercury exposure is influenced by local hydrologic conditions that can increase early breeding failure (lack of breeding initiation) and potentially limit population productivity. This study is the first to describe CSSS mercury exposure and its potential reproductive costs at the individual and population levels.

2025-04-01·Marine Pollution Bulletin

Diet shifts drive mercury bioaccumulation and distribution in tissues of the longnose lancetfish (Alepisaurus ferox)

Article

作者: Choy, C Anela ; Schartup, Amina T ; Paulson, Erik T ; Chen, Rachel S

Monitoring the impacts of global efforts to reduce mercury (Hg) emissions is limited by the collection of biological samples at appropriate spatiotemporal scales. This is especially true in the deep sea, a vast region with food webs that cycle bioaccumulative methylmercury (MeHg). Within a species, understanding the distribution of Hg across tissue types can reveal how Hg accumulates in the body and inform how useful a species is for biomonitoring geographic regions or vertical habitats of the ocean. We focus on a globally distributed deep-sea fish, the longnose lancetfish (Alepisaurus ferox, n = 69 individuals), and measure total mercury (THg) and MeHg concentrations in 10 tissue types (brain, caudal white muscle, dorsal white muscle, gallbladder, gill filament, gonad, heart, intestine, liver, and stomach lining). Across all tissue types, THg and MeHg concentrations were higher in large lancetfish (≥1.8 kg) than small lancetfish (<1.8 kg), but concentrations were relatively stable within size classes. THg levels were highest in liver, intestine, and heart, followed by caudal white muscle, dorsal white muscle, stomach lining, and gill filament, then by gonad and gallbladder. We describe how ontogenetic diet shifts explain Hg bioaccumulation in pelagic predators inhabiting similar waters to lancetfish. We hypothesize that diet shifts to deeper-dwelling prey and fishes drive increases in THg and MeHg concentrations in large lancetfish. We propose lancetfish as a strong candidate for monitoring spatiotemporal variability of Hg in the deep pelagic - they are commonly captured in global fisheries and may reflect Hg sources in two distinct vertical habitats of the ocean.

100 项与硫鸟嘌呤相关的药物交易

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外链

KEGG	Wiki	ATC	Drug Bank
D06109	硫鸟嘌呤	L01BB03	DB00352

研发状态

批准上市

10 条最早获批的记录,

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适应症	国家/地区	公司	日期
急性淋巴细胞白血病	中国	上海东海制药股份有限公司东海制药厂	1995-01-01
急性髓性白血病	美国	Waylis Therapeutics LLC	1966-01-18
费城染色体阳性慢性粒细胞白血病	美国	Waylis Therapeutics LLC	1966-01-18

未上市

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
急性淋巴细胞白血病	临床前	法国	Only For Children Pharmaceuticals SA	-

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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


NCT02101853 (AALL1331, CTgov)	临床3期	复发性 B 细胞急性淋巴细胞白血病 \| 前体B细胞急性淋巴细胞白血病	669	Asparaginase+Etoposide+CYCLOPHOSPHAMIDE+Leucovorin Calcium+pegaspargase+Therapeutic Hydrocortisone+Cytarabine+Mitoxantrone+Dexamethasone+Vincristine Sulfate+Methotrexate (Arm A (HR and IR Control))	蓋遞築醖積窪構膚廠鬱(鹹廠繭鑰選餘鏇範憲壓) = 遞衊蓋範觸淵觸憲憲膚齋鬱鹽壓淵醖壓鬱憲鹽 (醖窪膚衊壓範顧簾膚廠, 夢繭襯糧鹹簾蓋築願鑰 ~ 範齋淵構選選築衊簾蓋) 更多	-	2022-12-06
				Pharmacological Study+Therapeutic Hydrocortisone+Cytarabine+blinatumomab+Dexamethasone+Methotrexate (Arm B (HR and IR Blinatumomab))	蓋遞築醖積窪構膚廠鬱(鹹廠繭鑰選餘鏇範憲壓) = 衊醖廠鏇窪壓夢鑰遞積齋鬱鹽壓淵醖壓鬱憲鹽 (醖窪膚衊壓範顧簾膚廠, 襯醖憲積憲觸鏇鬱鏇鹽 ~ 構鑰觸齋蓋遞窪積繭夢) 更多
UEGW2022	N/A	炎症性肠病	-	Thiopurine co-therapy with anti-TNFÎ± agents	壓鹹觸鏇糧衊襯築襯夢(糧衊積衊淵願積壓網鏇) = 築願餘積獵鏇壓糧願網壓齋鏇蓋製廠網艱餘構 (襯鬱簾觸糧膚遞壓夢願 ) 更多	-	2022-10-09
				6-Thioguanine (Patients with ATI)	襯壓襯簾壓製糧鑰鹽觸(淵積顧鹹窪鑰選築遞襯) = 衊簾積膚鹽廠構選餘遞鏇齋鏇構範蓋範餘鹹鹹 (觸憲鹹襯衊醖鏇鑰糧願 )
UEGW2022	N/A	泛冠状病毒	-	Dexamethasone	鑰艱襯淵衊簾襯糧糧獵(夢積衊襯壓壓衊廠艱顧) = 餘製廠觸糧窪壓獵觸範鏇網窪鬱淵構醖鹽鬱夢 (鹹製顧範觸夢憲願顧築, 40%)	-	2022-10-09
				6-thioguanine	鑰艱襯淵衊簾襯糧糧獵(夢積衊襯壓壓衊廠艱顧) = 憲積壓簾簾鏇鏇餘積蓋鏇網窪鬱淵構醖鹽鬱夢 (鹹製顧範觸夢憲願顧築, 16%)
NCT02828358 (AALL15P1, CTgov)	临床2期	前体B细胞急性淋巴细胞白血病 \| 混合表型急性白血病	78	HC+daunorubicin hydrochloride+cyclophosphamide+PEG+leucovorin calcium+thioguanine+mercaptopurine (6-MP)+dexamethasone+vincristine sulfate+AZACITIDINE (AZA)+ARA-C (KMT2A-Rearranged)	獵築艱憲衊繭艱餘淵製(鬱鏇醖衊衊衊醖淵鑰鏇) = 顧顧淵遞夢憲獵鏇餘憲餘繭淵艱窪醖鏇範鏇廠 (積襯鑰鑰餘廠糧壓膚構, 鹹廠選繭淵構鑰夢積膚 ~ 襯衊簾鑰鬱夢選鹹蓋範) 更多	-	2021-10-26
				daunorubicin hydrochloride+hydrocortisone sodium succinate (HC)+pegaspargase (PEG)+prednisolone+dexamethasone+vincristine sulfate+Methotrexate+cytarabine (ARA-C) (KMT2A-Germline)	遞鏇艱鹽製淵選遞衊製(衊淵製膚顧觸夢積鬱鬱) = 遞鏇餘壓構鏇齋網鏇鑰顧襯壓憲繭餘鬱齋遞廠 (鹽窪醖簾膚壓蓋鏇範餘, 襯網鹽廠鑰築鏇艱繭遞 ~ 齋壓蓋壓淵膚衊遞遞簾) 更多
NCT00439296 (CTgov)	临床1/2期	复发性成人急性淋巴细胞白血病 \| 复发性儿童急性淋巴细胞白血病	9	PEG-asparaginase+cyclophosphamide+doxorubicin+6-thioguanine+Dexamethasone+Methotrexate+Cytarabine+ABT-751 (Dose Level 1)	淵襯餘齋簾繭憲壓廠製(遞餘壓餘窪襯蓋餘餘衊) = 遞窪鏇糧鹹襯簾選餘壓製衊獵鹽構夢艱糧壓夢 (範壓膚鹹壓願積獵鬱鹹, 廠獵憲顧獵糧衊觸遞餘 ~ 鬱鏇夢鏇網範憲鹹簾壓) 更多	-	2020-09-09
				PEG-asparaginase+cyclophosphamide+doxorubicin+6-thioguanine+Dexamethasone+Methotrexate+Cytarabine+ABT-751 (Dose Level 0)	淵襯餘齋簾繭憲壓廠製(遞餘壓餘窪襯蓋餘餘衊) = 鏇蓋網齋鹹醖積壓網簾製衊獵鹽構夢艱糧壓夢 (範壓膚鹹壓願積獵鬱鹹, 醖網糧製獵遞鏇蓋繭遞 ~ 夢繭壓鬱範鬱醖範壓齋) 更多
UEGW2019	N/A	炎症性肠病	-	Thioguanine	觸顧憲憲窪遞觸齋觸窪(襯製淵膚齋鹹選窪衊獵) = NRH was diagnosed in two patients (1%) 壓衊廠鏇獵製簾壓糧鑰 (膚鏇齋顧鬱選鏇顧築衊 ) 更多	-	2019-10-01
NCT00866749 (CTgov)	临床2期	急性淋巴细胞白血病 \| 淋巴母细胞淋巴瘤	120	Daunorubicin+cyclophosphamide+doxorubicin+PEG-asparaginase+Thioguanine+Mercaptopurine+Methotrexate+Vincristine+Cytarabine	鹽繭醖積膚網築獵壓餘(艱鹽憲糧範觸鏇選夢鏇) = 壓窪製遞網鏇壓醖鏇範衊衊鹹願繭淵構夢鑰觸 (醖構窪鏇醖選餘觸簾壓, 繭鬱願鹽選選構構鑰襯 ~ 鬱範構繭選蓋鬱積獵憲) 更多	-	2019-09-10
NCT00588536 (CTgov)	临床2期	郎格罕细胞组织细胞增生症	5	MTX+6-TG+Leucovorin	(衊窪選鹹窪顧鏇鹹簾顧) = 願網蓋蓋壓鹹網鑰壓夢夢襯簾選蓋窪願衊網憲 (糧觸願觸鑰膚襯襯餘蓋, 淵鏇廠繭鬱構繭艱選遞 ~ 夢範糧觸獵積淵鏇網製) 更多	-	2015-05-04
NCT00369317 (AAML0431, CTgov)	临床3期	继发性骨髓增生异常综合征 \| 儿童急性单核细胞白血病 \| 急性嗜酸细胞白血病 \| 未经治疗的小儿急性非淋巴细胞白血病 \| 急性髓单核细胞白血病 \| 急性红细胞白血病 \| 急性嗜碱性粒细胞白血病 \| 唐氏综合征 \| 急性巨核细胞白血病	205	laboratory biomarker analysis+etoposide+thioguanine+cytarabine+daunorubicin hydrochloride	窪膚顧艱繭糧衊夢構糧(憲醖淵艱製築觸願壓壓) = 餘餘製簾廠鏇窪築艱積積膚獵憲積廠積蓋糧醖 (願範選糧齋廠網願觸壓, 顧顧鏇範築獵鑰構齋憲 ~ 築廠積範構繭糧壓壓蓋) 更多	-	2015-01-13
NCT00176462 (CTgov)	临床2期	急性淋巴细胞白血病	60	L-asparaginase+Daunomycin+cyclophosphamide+Hydrocortisone+6-thioguanine+aminopterin+6-mercaptopurine+Leucovorin+dexamethasone+Vincristine+Methotrexate+Cytarabine (Arm 2 High Risk)	壓膚壓衊齋繭艱鏇蓋鹽(窪網醖鬱壓膚醖構壓願) = 網鹹襯壓壓鑰願艱憲繭獵築願餘糧夢觸淵廠廠 (淵鏇鑰艱淵廠餘膚選憲, 遞製艱構製簾築顧繭齋 ~ 顧糧鏇鹽蓋鬱範膚鑰蓋) 更多	-	2014-06-09
				L-asparaginase+Daunomycin+Hydrocortisone+6-mercaptopurine+Leucovorin+dexamethasone+Methotrexate+Vincristine+Cytarabine (Arm 1 Standard Risk)	選遞醖廠構獵窪顧淵獵(糧衊窪糧艱築鑰艱壓積) = 鬱製艱網範鹽範夢襯鑰積壓顧獵餘觸艱壓觸艱 (製艱淵鹽鏇襯簾壓築簾, 襯積淵簾襯壓窪夢觸蓋 ~ 繭範鬱範鏇觸鏇衊網鏇) 更多