Clinical trial · Interventional
Effect of Tepotinib on the PK of the P-gp Substrate Dabigatran Etexilate
Phase I, Open-label, Single Sequence, Two-Period Study to Evaluate the Effect of Tepotinib on P-gp by Investigating the PK of the P-gp Probe Substrate Dabigatran Etexilate in Healthy Subjects
NCT03492437CI-TRIAL-00068628completedPhase 1Results postedClinicalTrials.gov clinicaltrialsProvenance
- Source
- ClinicalTrials.gov
- Retrieved
- Sep 8, 2026
- Layer
- normalized (units and labels harmonized; values unchanged)
- Run
- ING-CLINICALTRIALS-20260908-000001
Summary
Brief summary (as posted)
This study investigated the effect of Tepotinib on the pharmacokinetics (PK) of the p-glycoprotein (P-gp) probe substrate Dabigatran etexilate.
Conditions
Conditions (1)
Free-text conditions as registered, with the CancerIndex entity they were reconciled to and the match type.
| Condition (as posted) | Mapped entity | Match | Confidence |
|---|---|---|---|
| Healthy | — | UNRESOLVED | — |
Interventions
Interventions (2)
| Intervention | Type | Mapped drug | Match |
|---|---|---|---|
| Dabigatran Etexilate | Drug | — | UNRESOLVED |
| Tepotinib | Drug | Tepotinib | ALIAS |
Design
Arms and outcomes
Arms (2)
- type
- EXPERIMENTAL
- label
- Dabigatran Etexilate
- interventionNames
- Drug: Dabigatran Etexilate
- type
- EXPERIMENTAL
- label
- Tepotinib + Dabigatran
- interventionNames
- Drug: Dabigatran Etexilate
- Drug: Tepotinib
Primary outcomes (3)
- measure
- Area Under Plasma Concentration-time Curve From Time Zero to Last Sampling Time (Tlast) at Which the Concentration is at or Above the Lower Limit of Quantification (AUC0-t) of Total Dabigatran
- timeFrame
- Pre-dose, 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 6, 8, 12, 24, 48 and 72 hours Post-dose on Day 1 and Day 8
- description
- AUC0-t was calculated according to the mixed log linear trapezoidal rule.
Eligibility
Eligibility (as posted)
- Sex
- All
- Minimum age
- 18 Years
- Maximum age
- 44 Years
Show eligibility criteria text
Inclusion Criteria: * Healthy participants of non-child bearing potential * Body weight between 50 to 100 kilogram (kg) * Body mass index (BMI) between 18.5 and 29.9 kilogram per meter square (kg/m\^2) * A male participant must agree to use and to have his female partner of childbearing potential to use highly effective method of contraception * Participant must have given written informed consent before any study-related activities * All values for hematology, coagulation, and biochemistry tests of blood and urinalysis are within the normal range. Minor (solitary) non-clinically relevant deviation(s) are allowed as judged by the Investigator * Other protocol defined inclusion criteria could apply Exclusion Criteria: * Participation in a clinical study within 60 days prior to first drug administration * Whole blood donation or loss of \> 450 milliliter (mL) within 60 days prior to first drug administration * Any surgical or medical condition, or any other significant disease that could interfere with the study objectives, conduct, or evaluation * Supine systolic blood pressure (SBP) greater than (\>) 140 millimeter of mercury (mmHg) or less than (\<) 90 mmHg, diastolic blood pressure (DBP) \> 90 or \< 50 mmHg, and pulse rate \> 90 or \<50 beats per minute (bpm) at Screening and at admission on Day-1. * 12-Lead electrocardiograms (ECG) showing a corrected QT interval per Fridericia's formula (QTcF) \> 450 milliseconds (ms), PR \> 215 ms, or QRS \> 120 ms (at Screening) * Creatinine clearance estimated glomerular filtration rate (eGFR) \< 90 milliliter per minute (mL/min) (at Screening) * Participants with gall bladder removal or other relevant surgery of gastrointestinal tract * History of any malignancy * History of epilepsy * Ascertained or presumptive allergy/hypersensitivity to the active drug substance and/or excipients * Participants who in the Investigator's judgment were perceived as having an increased risk of bleeding * Positive screen for alcohol or drugs of abuse (at Screening and Day -1) * Positive screen for hepatitis B surface antigen (HBsAg), hepatitis C virus antibody (anti-HCV), and human immunodeficiency virus 1 and 2 antibodies (HIV1/HIV2 antibodies) (at Screening) * Excessive consumption of xanthine-containing food or beverages before study drug administration until collection of last pharmacokinetic (PK) sample in each period (at Screening and Day -1) * Receipt of any prescription or nonprescription medication within 14 days or 5 half-lives, before study drug administration * Smoker or former smoker who stopped smoking less than 6 months before the time of the Screening Visit * Intake of grapefruit, Seville orange, cranberry or juices of these 3 fruits, or St. John's Wort, from 14 days prior to Day -1 * Inability to communicate or cooperate with the Investigator * Other factors, which in the opinion of the Investigator may interfere with study conduct (at Screening and Day -1 of first Period only) * Legal incapacity or limited legal capacity * Participants kept in detention * Other protocol defined exclusion criteria could apply
References
Publications (1)
- DERIVEDYalkinoglu O, Becker A, Krebs-Brown A, Vetter C, Lupfert C, Perrin D, Heuer J, Biedert H, Hirt S, Bytyqi A, Bachmann A, Strotmann R. Assessment of the potential of the MET inhibitor tepotinib to affect the pharmacokinetics of CYP3A4 and P-gp substrates. Invest New Drugs. 2023 Aug;41(4):596-605. doi: 10.1007/s10637-023-01378-z. Epub 2023 Jul 6. PMID 37415001