Effect of a Known P-glycoprotein (P-gp) Inhibitor, Itraconazole, on the Pharmacokinetics (PK) of Engasertib

NCT07800429 | Not Yet Recruiting Phase 1 FDA Drug

• 2 other identifiers: ENG-1012026-526311-11-00
• Study Type: interventional
• Target: 27
• Locations: 0 countries
• Sites: N/A

Brief Summary

The primary objective of this trial is to assess the effect of a known P-gp inhibitor, itraconazole, on the PK of engasertib in healthy adult participants.

Conditions

Healthy Participants

Keywords

Engasertib; VAD044; P-gp Inhibitor; Itraconazole

Outcome Measures

Primary Outcomes (3)

• Area Under the Concentration-time Curve (AUC) from Zero to the Last Quantifiable Concentration (AUC0-tlast) of Engasertib

  Day 1 up to Day 26

• AUC from Zero to Infinity (AUC0-inf) of Engasertib

  Day 1 up to Day 26

• Maximum Plasma Concentration (Cmax) of Engasertib

  Day 1 up to Day 26

Study Arms (1)

Engasertib 40 mg + Itraconazole 200 mg

EXPERIMENTAL

All participants will take a single oral dose of engasertib 40 mg on Day 1. Participants will then take itraconazole 200 mg orally once daily (QD) from Day 12 to Day 24. On Day 15, a single oral dose of engasertib 40 mg will be administered 1 hour after the itraconazole dose.

Drug: Engasertib; Drug: Itraconazole

Interventions

Engasertib DRUG

Participants will take engasertib orally as capsules.

Also known as: VAD044

Engasertib 40 mg + Itraconazole 200 mg

Itraconazole DRUG

Participants will take itraconazole as 20 mL of 10 mg/mL oral solution.

Engasertib 40 mg + Itraconazole 200 mg

Eligibility Criteria

• Age: 18 Years - 55 Years
• Sex: all
• Healthy Volunteers: Yes
• Age Groups: Adult (18-64)

You may qualify if:

• Age of 18 to 55 years (both inclusive), at the time of signing the informed consent.
• Body weight ≥ 50 and \< 120 kg and a body mass index (BMI) within the range 18 to 30 kg/m\^2 (both inclusive) at screening.
• Male and female participants are eligible to participate if they are not fertile or if they agree to either be abstinent from intercourse where pregnancy can occur or use contraception/barrier as detailed in the protocol.
• Overtly healthy as determined by medical evaluation including medical history, physical examination, vital signs, electrocardiogram (ECG).
• Clinically acceptable clinical laboratory test results at screening.
• Non-smoker, former smoker or stable non-smoker (= 0 cigarettes, pipes, cigars, or others) for at least 3 months prior to screening. Participants must also have abstained from use of other nicotine containing products (e.g., nicotine patch, chewing gum or e-cigarettes) for at least 3 months before screening.
• Capable of giving signed informed consent.
• Re-admission: overtly healthy as determined by medical evaluation including check of changes in medical history compared to screening, clinical laboratory test results, abbreviated physical examination, vital signs, and ECG.

You may not qualify if:

• Any history or evidence of any clinically relevant cardiovascular, hepatic, renal, gastrointestinal, pancreatic, endocrinologic, hematologic, immunologic, metabolic, and/or other major disease or malignancy as determined by medical evaluation (including physical examination) capable of significantly altering the absorption, metabolism, or elimination of drugs; constituting a risk when taking the study intervention; or interfering with the interpretation of data.
• Any clinically important illness, medical/surgical procedure, or condition, which, in the opinion of the investigator, is likely to interfere with the study conduct.
• Known or suspected hypersensitivity to engasertib, or itraconazole, or any components of the formulation used.
• History of significant or uncontrolled skin disorders, per the Investigator's judgement.
• Any clinically significant history of allergic conditions (including allergies to more than 3 allergens, drug allergies, asthma, eczema, or anaphylactic reactions, but excluding untreated, asymptomatic, seasonal allergies at the time of dosing).
• History or presence of disorders of glucose metabolism.
• Known or suspected thyroid disorders as evidenced by assessment of thyroid-stimulating hormone (TSH) levels outside the normal reference range at screening.
• Known or suspected liver disorders (e.g., Morbus Gilbert / Meulengracht) and bile secretion/flow (cholestasis, also history of it).
• Difficulty in swallowing.
• History or evidence of malabsorption or any gastrointestinal surgery except appendectomy and herniotomy.
• History of any chronic disease which might interfere with the absorption, distribution, metabolism or excretion of the study drug.
• Lactose intolerance.
• Contraindications for the use of itraconazole.
• Tendency for vasovagal reactions (e.g., after venipuncture) or history of syncope.
• Febrile illness within 1 week before first dosing.

Sponsors & Collaborators

• Vaderis Therapeutics AG: lead

MeSH Terms

Interventions

Itraconazole

Intervention Hierarchy (Ancestors)

Triazoles; Azoles; Heterocyclic Compounds, 1-Ring; Heterocyclic Compounds; Piperazines

Central Study Contacts

Vaderis Therapeutics AG

CONTACT

44-823-3747; info@vaderis.com

Vaderis Therapeutics AG

CONTACT

844-823-3747; info@vaderis.com

Study Design

• Study Type: interventional
• Phase: phase 1
• Allocation: NA
• Masking: NONE
• Purpose: BASIC SCIENCE
• Intervention Model: SEQUENTIAL
• Sponsor Type: INDUSTRY
• Responsible Party: SPONSOR

Study Record Dates

• First Submitted: August 28, 2026
• First Posted: September 2, 2026
• Study Start: September 1, 2026
• Primary Completion: October 1, 2026
• Study Completion: October 1, 2026
• Last Updated: September 2, 2026

Record last verified: 2026-08

Data Sharing

• IPD Sharing: Will not share