Evidence map›Paper›PMID 35157234›Full record

ArticleEuropean journal of drug metabolism and pharmacokinetics2022

Clinical and Nonclinical Disposition and In Vitro Drug-Drug Interaction Potential of Felcisetrag, a Highly Selective and Potent 5-HT

Sandeepraj Pusalkar, Swapan K Chowdhury, Richard Czerniak, Xiaochun Zhu, Yuexian Li, Suresh K Balani, Diane Ramsden

Open access · hybridAbstract read
PubMed Full text at PMC Publisher
In one paragraph

Article in European journal of drug metabolism and pharmacokinetics, 2022. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 2 papers.

0numbers the graph read from it
0cells of the map it votes in
2citing papers in PubMed
0.4field-weighted citation impact, top 40% 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

2 citing papers in PubMed, 3 citations in OpenAlex.

  1. Felcisetrag stimulates 5-HTNaunyn-Schmiedeberg's archives of pharmacology · 2026
    Article
  2. Pharmacologic treatments for gastroparesis.Pharmacological reviews · 2025
    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 3 countries.

Sandeepraj PusalkarGlobal; Drug Metabolism and Pharmacokinetics, Takeda Development Center Americas, Inc., 35 Landsdowne Street, Cambridge, MA, 02139, USA.
Swapan K ChowdhuryGlobal; Drug Metabolism and Pharmacokinetics, Takeda Development Center Americas, Inc., 35 Landsdowne Street, Cambridge, MA, 02139, USA.
Richard CzerniakGlobal; Drug Metabolism and Pharmacokinetics, Takeda Development Center Americas, Inc., 35 Landsdowne Street, Cambridge, MA, 02139, USA.
Xiaochun ZhuGlobal; Drug Metabolism and Pharmacokinetics, Takeda Development Center Americas, Inc., 35 Landsdowne Street, Cambridge, MA, 02139, USA.
Yuexian LiGlobal; Drug Metabolism and Pharmacokinetics, Takeda Development Center Americas, Inc., 35 Landsdowne Street, Cambridge, MA, 02139, USA.
Suresh K BalaniGlobal; Drug Metabolism and Pharmacokinetics, Takeda Development Center Americas, Inc., 35 Landsdowne Street, Cambridge, MA, 02139, USA.
Diane RamsdenGlobal; Drug Metabolism and Pharmacokinetics, Takeda Development Center Americas, Inc., 35 Landsdowne Street, Cambridge, MA, 02139, USA. diane.ramsden@astrazeneca.com.ORCID http://orcid.org/0000-0003-2994-0728
Center for Global Development · USAstraZeneca (South Korea) · KR

Funding

No grant is acknowledged in the PubMed record.

6 · The paper itself

Abstract

BACKGROUND AND

objectiveFelcisetrag (previously TAK-954 or TD-8954) is a highly selective and potent 5-HT

methodsThe metabolism and victim and perpetrator drug interaction potentials towards cytochrome P450s (CYP) and transporters were determined using in vitro models. The excretion, metabolite profile, and pharmacokinetics were determined during unlabeled and radiolabeled ADME studies in rat and dog for comparison with human. Due to a low clinical dose (0.5 mg) and radioactivity (~ 1.5 μCi), a combination of liquid scintillation counting and accelerator mass spectrometry was used for analysis of samples in this study.

resultsThe ADME properties, including metabolite profile, for felcisetrag are generally conserved across species. Felcisetrag is primarily cleared through renal excretion (0.443) and metabolism in humans (0.420), with intact parent as the predominant species in circulation. There are multiple metabolites, each representing < 10% of the circulating radioactivity, confirming no metabolites in safety testing (MIST) liabilities. Metabolites were also detected in animals. The potential for major CYP- and transporter-based drug-drug interaction (DDI) of felcisetrag as a victim or perpetrator is considered to be low.

conclusionsFelcisetrag is primarily cleared in humans through renal excretion. Although the metabolism of felcisetrag is primarily through CYP3A, the potential for clinically relevant DDI as a victim is significantly reduced as metabolism plays a minor role in the overall clearance.

Indexed as

Cytochrome P-450 Enzyme SystemSerotoninAnimalsDogsDrug InteractionsHumansRatsCytochrome P-450 Enzyme SystemSerotonin

Identifiers

PMID35157234
PMCPMC9050781
OpenAlexW4213108641

What OpenQuestion holds

Textmetadata
LicenceCC BY-NC
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 OpenQuestion graph.