Evidence map›Paper›PMID 33506323›Full record

ArticleInvestigational new drugs2021

Effects of rifampicin on the pharmacokinetics of alflutinib, a selective third-generation EGFR kinase inhibitor, and its metabolite AST5902 in healthy volunteers.

Yun-Ting Zhu, Yi-Fan Zhang, Jin-Fang Jiang, Yong Yang, Li-Xia Guo, Jing-Jing Bao, Da-Fang Zhong

Abstract readClinical Trial, Phase I
PubMed Publisher
In one paragraph

Article in Investigational new drugs, 2021. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 6 papers.

0numbers the graph read from it
0cells of the map it votes in
6citing papers in PubMed
0.9field-weighted citation impact, top 26% of its field
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

6 citing papers in PubMed, 9 citations in OpenAlex.

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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

7 authors at 3 institutions in 1 country.

Yun-Ting ZhuState Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, 501 Haike Road, Shanghai, 201203, People's Republic of China.
Yi-Fan ZhangState Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, 501 Haike Road, Shanghai, 201203, People's Republic of China. yfzhang@simm.ac.cn.
Jin-Fang JiangHQ Bioscience Co., LTD, Suzhou, People's Republic of China.
Yong YangHQ Bioscience Co., LTD, Suzhou, People's Republic of China.
Li-Xia GuoState Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, 501 Haike Road, Shanghai, 201203, People's Republic of China.
Jing-Jing BaoShanghai Allist Pharmaceuticals Co., Ltd, Shanghai, People's Republic of China.
Da-Fang ZhongState Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, 501 Haike Road, Shanghai, 201203, People's Republic of China. dfzhong@simm.ac.cn.
Shanghai Institute of Materia Medica · CNBioscience (China) · CNChinese Academy of Sciences · CN

Funding

No grant is acknowledged in the PubMed record.

6 · The paper itself

Abstract

Background Alflutinib is a novel irreversible and highly selective third-generation EGFR inhibitor currently being developed for the treatment of non-small cell lung cancer patients with activating EGFR mutations and EGFR T790M drug-resistant mutation. Alflutinib is mainly metabolized via CYP3A4 to form its active metabolite AST5902. Both alflutinib and AST5902 contribute to the in vivo pharmacological activity. The aim of this study was to investigate the effects of rifampicin (a strong CYP3A4 inducer) on the pharmacokinetics of alflutinib and AST5902 in healthy volunteers, thus providing important information for drug-drug interaction evaluation and guiding clinical usage. Methods This study was designed as a single-center, open-label, and single-sequence trial over two periods. The volunteers received a single dose of 80 mg alflutinib on Day 1/22 and continuous doses of 0.6 g rifampicin on Day 15-30. Blood sampling was conducted on Day 1-10 and Day 22-31. The pharmacokinetics of alflutinib, AST5902, and the total active ingredients (alflutinib and AST5902) with or without rifampicin co-administration were respectively analyzed. Results Co-administration with rifampicin led to 86% and 60% decreases in alflutinib AUC

Indexed as

AdolescentAdultArea Under CurveCytochrome P-450 CYP3ACytochrome P-450 CYP3A InducersDrug InteractionsErbB ReceptorsFemaleHumansIndolesMaleMiddle AgedProtein Kinase InhibitorsPyridinesPyrimidinesRifampinaflutinibAST5902CYP3A4 protein, humanCytochrome P-450 CYP3ACytochrome P-450 CYP3A InducersEGFR protein, humanErbB ReceptorsIndolesProtein Kinase InhibitorsPyridinesPyrimidinesRifampinAlflutinibAST5902CYP3A4Drug-drug interactionRifampicin

Identifiers

PMID33506323
OpenAlexW3122926187

What Socratic holds

Textmetadata
Read underepoch 390

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 Socratic graph.