Evidence map›Paper›PMID 34145979›Full record

ArticleClinical pharmacology in drug development2021

Effects of Itraconazole and Rifampin on the Pharmacokinetics of Mobocertinib (TAK-788), an Oral Epidermal Growth Factor Receptor Inhibitor, in Healthy Volunteers.

Steven Zhang, Shu Jin, Celina Griffin, Zhongling Feng, Jianchang Lin, Karthik Venkatakrishnan, Neeraj Gupta

Registry-linked trialOpen access · hybridAbstract readClinical Trial, Phase I
In one paragraph

Article in Clinical pharmacology in drug development, 2021. The graph could read no effect estimate from its abstract, so it casts no vote on the map. It is linked to trial NCT03928327 (A Phase 1 Study of Oral TAK-788 to Evaluate the Drug-Drug Interaction With Itraconazole and Rifampin in Healthy Adult Subjects), which is not on this map. Cited by 9 papers.

0numbers the graph read from it
0cells of the map it votes in
9citing papers in PubMed
2.1field-weighted citation impact, top 12% 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.

NCT03928327 phase1completednot on this map

A Phase 1 Study of Oral TAK-788 to Evaluate the Drug-Drug Interaction With Itraconazole and Rifampin in Healthy Adult Subjects

TypeinterventionalSponsorMillennium Pharmaceuticals, Inc.Ran2019 to 2019Enrolled24ConditionsHealthy VolunteersArmsTAK-788, Itraconazole, Rifampin
3 · Its place in the literature

Who cites it

9 citing papers in PubMed, 22 citations in OpenAlex.

  1. Trial
  2. Trial
  3. Article
  4. Review
  5. Discovery of 3-Amino-1International journal of molecular sciences · 2022
    Article
  6. Review
  7. Discovery of mobocertinib, a new irreversible tyrosine kinase inhibitor indicated for the treatment of non-small-cell lung cancer harboring EGFR exon 20 insertion mutations.Medicinal chemistry research : an international journal for rapid communications on design and mechanisms of action of biologically active agents · 2022
    Review
  8. Review
  9. Review
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 2 institutions in 2 countries.

Steven ZhangMillennium Pharmaceuticals, Inc., Cambridge, Massachusetts, USA, a wholly owned subsidiary of Takeda Pharmaceutical Company Limited.
Shu JinMillennium Pharmaceuticals, Inc., Cambridge, Massachusetts, USA, a wholly owned subsidiary of Takeda Pharmaceutical Company Limited.
Celina GriffinMillennium Pharmaceuticals, Inc., Cambridge, Massachusetts, USA, a wholly owned subsidiary of Takeda Pharmaceutical Company Limited.
Zhongling FengMillennium Pharmaceuticals, Inc., Cambridge, Massachusetts, USA, a wholly owned subsidiary of Takeda Pharmaceutical Company Limited.
Jianchang LinMillennium Pharmaceuticals, Inc., Cambridge, Massachusetts, USA, a wholly owned subsidiary of Takeda Pharmaceutical Company Limited.
Karthik VenkatakrishnanMillennium Pharmaceuticals, Inc., Cambridge, Massachusetts, USA, a wholly owned subsidiary of Takeda Pharmaceutical Company Limited.
Neeraj GuptaMillennium Pharmaceuticals, Inc., Cambridge, Massachusetts, USA, a wholly owned subsidiary of Takeda Pharmaceutical Company Limited.
Millennium Engineering and Integration (United States) · USTakeda (United States) · US

Funding

No grant is acknowledged in the PubMed record.

6 · The paper itself

Abstract

Mobocertinib (TAK-788) is an investigational oral tyrosine kinase inhibitor targeting epidermal growth factor receptor and human epidermal growth factor 2. A phase 1 open-label, 2-period, fixed-sequence, 2-part study (NCT03928327) characterized effects of a strong CYP3A4 inhibitor (itraconazole) and inducer (rifampin) on the pharmacokinetics (PK) of mobocertinib and its active metabolites, AP32960 and AP32914. Healthy volunteers (n = 12 per part) received a single dose of mobocertinib alone (20 mg, part 1; 160 mg, part 2) and with multiple doses of itraconazole 200 mg once daily (part 1) or rifampin 600 mg once daily (part 2). Coadministration of itraconazole with mobocertinib increased the combined molar area under the plasma concentration-time curve from time 0 to infinity (AUC

Indexed as

Administration, OralAdultAniline CompoundsArea Under CurveCytochrome P-450 CYP3A InducersCytochrome P-450 CYP3A InhibitorsDrug InteractionsFemaleHumansIndolesItraconazoleMaleMiddle AgedProtein Kinase InhibitorsPyrimidinesRifampinAniline CompoundsCytochrome P-450 CYP3A InducersCytochrome P-450 CYP3A InhibitorsIndolesItraconazolemobocertinibProtein Kinase InhibitorsPyrimidinesRifampinCYP3A4drug-drug interactioninductioninhibitionmobocertinibnon-small cell lung cancer

Identifiers

PMID34145979
PMCPMC8453750
OpenAlexW3169194151

What OpenQuestion holds

Textmetadata
LicenceCC BY-NC-ND
Read underepoch 390

Registered trials

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.