Evidence map›Paper›PMID 26513662›Full record

ArticlePloS one2015

Prodrug AST-003 Improves the Therapeutic Index of the Multi-Targeted Tyrosine Kinase Inhibitor Sunitinib.

Qiang Huang, Changhua Zhou, Xiao Chen, Bing Dong, Siqi Chen, Ning Zhang, Yawei Liu, Anrong Li, Meicun Yao, Ji Miao and 2 more

Abstract read
In one paragraph

Article in PloS one, 2015. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 3 papers.

0numbers the graph read from it
0cells of the map it votes in
3citing papers in PubMed
–field-weighted citation impact
1 · What the graph read from it

What it found

Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.

The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.

2 · The registry

The trial behind it

Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.

Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.

3 · Its place in the literature

Who cites it

3 citing papers in PubMed.

  1. Article
  2. Article
  3. Article
4 · The record

Corrections and comments

PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.

5 · Who and what money

Authors and funding

12 authors.

Qiang HuangSchool of Pharmaceutical Sciences, Sun Yat-Sen University, Guangzhou, China; Centre for Cellular & Structural Biology, Sun Yat-Sen University, Guangzhou, China.
Changhua ZhouSchool of Pharmaceutical Sciences, Sun Yat-Sen University, Guangzhou, China; Centre for Cellular & Structural Biology, Sun Yat-Sen University, Guangzhou, China.
Xiao ChenSchool of Pharmaceutical Sciences, Sun Yat-Sen University, Guangzhou, China.
Bing DongSchool of Pharmaceutical Sciences, Sun Yat-Sen University, Guangzhou, China; Centre for Cellular & Structural Biology, Sun Yat-Sen University, Guangzhou, China.
Siqi ChenSchool of Pharmaceutical Sciences, Sun Yat-Sen University, Guangzhou, China; Centre for Cellular & Structural Biology, Sun Yat-Sen University, Guangzhou, China.
Ning ZhangPeking University Cancer Hospital, Beijing Institute for Cancer Research, Beijing, China.
Yawei LiuHealth Division of Guard Bureau, General Staff Department of PLA, Beijing, China.
Anrong LiAscenta Pharmaceuticals, Guangzhou, Guangdong, P. R. China.
Meicun YaoSchool of Pharmaceutical Sciences, Sun Yat-Sen University, Guangzhou, China.
Ji MiaoSchool of Pharmaceutical Sciences, Sun Yat-Sen University, Guangzhou, China.
Qing LiSchool of Pharmaceutical Sciences, Sun Yat-Sen University, Guangzhou, China; Centre for Cellular & Structural Biology, Sun Yat-Sen University, Guangzhou, China.
Zhong WangSchool of Pharmaceutical Sciences, Sun Yat-Sen University, Guangzhou, China; Centre for Cellular & Structural Biology, Sun Yat-Sen University, Guangzhou, China.

Funding

No grant is acknowledged in the PubMed record.

6 · The paper itself

Abstract

Patients have responded well to the multi-targeted tyrosine kinase inhibitor (TKI) Sunitinib in the clinic. But the severe toxic side effects associated with Sunitinib limit its therapeutic index. To improve the therapeutic index of Sunitinib, a prodrug strategy was employed to modify Sunitinib. The inactive prodrug AST-003 can be converted to Sunitinib in vitro and in vivo. Compared with Sunitinib, AST-003 has unique biochemical, cellular and pharmacokinetic properties with improved tolerability in mice and yield higher efficacy in tumor xenograft models. This prodrug strategy may constitute a novel paradigm to improve the therapeutic index of Sunitinib and other TKI or anti-angiogenesis drugs in general.

Indexed as

Angiogenesis InhibitorsAnimalsAntineoplastic AgentsBenzoatesCell Line, TumorCell ProliferationDisease Models, AnimalDrug SynergismDrug ToleranceEsterasesFemaleHumansHydrolysisIndolesMiceNeoplasmsAngiogenesis InhibitorsAntineoplastic AgentsAST-003BenzoatesEsterasesIndolesProdrugsProtein Kinase InhibitorsProto-Oncogene Proteins c-aktPyrrolesSTAT3 Transcription FactorSunitinib

Identifiers

PMID26513662
PMCPMC4626378

What OpenQuestion holds

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Registered trials

None linked

Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.