Mass Balance and Absolute Oral Bioavailability of [14C]VH4524184

NCT07636928 | Not Yet Recruiting Phase 1 FDA Drug

• 2 other identifiers: 2238032026-525590-40
• Study Type: interventional
• Target: 9
• Locations: 0 countries
• Sites: N/A

Brief Summary

The purpose of the study is to assess the bioavailability, mass balance, pharmacokinetics, metabolism and excretion of radiolabeled (14C) VH4524184.

Conditions

HIV Infections

Keywords

VH4524184; Human immunodeficiency virus (HIV)

Outcome Measures

Primary Outcomes (48)

• Absolute bioavailability (F oral) of VH4524184 (Period 1)

  Day 1 up to Day 14

• Amount of total radioactivity (TRA) excreted in urine (Ae urine) (Period 1)

  Urine is collected until amount of radioactivity recovered in excreta (urine and feces) is at least 90% of administered radioactivity and \<1% has been recovered from excreta from 2 consecutive days (ie, the total for urine and feces is \<1% on 2 consecutive days).

  Day 1 up to Day 14

• Amount of TRA excreted in urine (Ae urine) (Period 2)

  Urine is collected until amount of radioactivity recovered in excreta (urine and feces) is at least 90% of administered radioactivity and \<1% has been recovered from excreta from 2 consecutive days (ie, the total for urine and feces is \<1% on 2 consecutive days).

  Day 15 up to Day 43

• Amount of TRA excreted in feces (Ae feces) (Period 1)

  Feces are collected until amount of radioactivity recovered in excreta (urine and feces) is at least 90% of administered radioactivity and \<1% has been recovered from excreta from 2 consecutive days (ie, the total for urine and feces is \<1% on 2 consecutive days).

  Day 1 up to Day 14

• Amount of TRA excreted in feces (Ae feces) (Period 2)

  Feces are collected until amount of radioactivity recovered in excreta (urine and feces) is at least 90% of administered radioactivity and \<1% has been recovered from excreta from 2 consecutive days (ie, the total for urine and feces is \<1% on 2 consecutive days).

  Day 15 up to Day 43

• Amount of TRA excreted in vomitus (Ae vomit) (Period 1)

  At Day 1

• Amount of TRA excreted in vomitus (Ae vomit) (Period 2)

  At Day 15

• Total amount of TRA excreted (Ae total) (Period 1)

  The Ae of TRA measured in urine, feces and vomitus (if applicable on Day 1 only). Urine and feces are collected until amount of radioactivity recovered in excreta (urine and feces) is at least 90% of administered radioactivity and \<1% has been recovered from excreta from 2 consecutive days (ie, the total for urine and feces is \<1% on 2 consecutive days).

  From Day 1 up to Day 14

• Total amount of TRA excreted (Ae total) (Period 2)

  The Ae of TRA measured in urine, feces and vomitus (if applicable on Day 15 only). Urine and feces are collected until amount of radioactivity recovered in excreta (urine and feces) is at least 90% of administered radioactivity and \<1% has been recovered from excreta from 2 consecutive days (ie, the total for urine and feces is \<1% on 2 consecutive days).

  Day 15 up to Day 43

• Fraction of TRA excreted in urine (fe urine) (Period 1)

  Urine is collected until the amount of radioactivity recovered in excreta (urine and feces) is at least 90% of administered radioactivity and \<1% has been recovered from excreta from 2 consecutive days (ie, the total for urine and feces is \<1% on 2 consecutive days).

  Day 1 up to Day 14

• Fraction of TRA excreted in urine (fe urine) (Period 2)

  Urine is collected until amount of radioactivity recovered in excreta (urine and feces) is at least 90% of administered radioactivity and \<1% has been recovered from excreta from 2 consecutive days (ie, the total for urine and feces is \<1% on 2 consecutive days).

  Day 15 up to Day 43

• Fraction of TRA excreted in feces (fe feces) (Period 1)

  Feces is collected until amount of radioactivity recovered in excreta (urine and feces) is at least 90% of administered radioactivity and \<1% has been recovered from excreta from 2 consecutive days (ie, the total for urine and feces is \<1% on 2 consecutive days).

  Day 1 up to Day 14

• Fraction of TRA excreted in feces (fe feces) (Period 2)

  Feces is collected until amount of radioactivity recovered in excreta (urine and feces) is at least 90% of administered radioactivity and \<1% has been recovered from excreta from 2 consecutive days (ie, the total for urine and feces is \<1% on 2 consecutive days).

  Day 15 up to Day 43

• Fraction of TRA excreted in vomitus (fe vomit) (Period 1)

  At Day 1

• Fraction of TRA excreted in vomitus (fe vomit) (Period 2)

  At Day 15

• Total fraction of TRA excreted (fe total) (Period 1)

  The fe of TRA measured in urine, feces and vomitus (if applicable on Day 1 only). Urine and feces are collected until amount of radioactivity recovered in excreta (urine and feces) is at least 90% of administered radioactivity and \<1% has been recovered from excreta from 2 consecutive days (ie, the total for urine and feces is \<1% on 2 consecutive days).

  Day 1 up to Day 14

• Total fraction of TRA excreted (fe total) (Period 2)

  The fe of TRA measured in urine, feces and vomitus (if applicable on Day 15 only). Urine and feces are collected until amount of radioactivity recovered in excreta (urine and feces) is at least 90% of administered radioactivity and \<1% has been recovered from excreta from 2 consecutive days (ie, the total for urine and feces is \<1% on 2 consecutive days).

  Day 15 up to Day 43

• Maximum concentration (Cmax) of VH4524184 in plasma (Period 1)

  Day 1 to Day 14

• Maximum concentration (Cmax) of VH4524184 in plasma (Period 2)

  Day 15 to Day 43

• Maximum concentration (Cmax) of [14C]VH4524184 in plasma (Period 1)

  Day 1 to Day 14

• Maximum concentration (Cmax) of TRA in plasma (Period 1)

  Day 1 to Day 14

• Maximum concentration (Cmax) of TRA in plasma (Period 2)

  Day 15 to Day 43

• Cmax of TRA in whole blood (Period 1)

  Day 1 to Day 14

• Cmax of TRA in whole blood (Period 2)

  Day 15 to Day 43

• Time to maximum concentration (tmax) of VH4524184 in plasma (Period 1)

  Day 1 to Day 14

• Time to maximum concentration (tmax) of VH4524184 in plasma (Period 2)

  Day 15 to Day 43

• Time to maximum concentration (tmax) of [14C]VH4524184 in plasma (Period 1)

  Day 1 to Day 14

• Time to maximum concentration (tmax) of TRA in plasma (Period 1)

  Day 1 to Day 14

• Time to maximum concentration (tmax) of TRA in plasma (Period 2)

  Day 15 to Day 43

• Time to maximum concentration (tmax) of TRA in whole blood (Period 1)

  Day 1 to Day 14

• Time to maximum concentration (tmax) of TRA in whole blood (Period 2)

  Day 15 to Day 43

• Area under the concentration-time curve from time zero to the last measured timepoint (AUC 0-t) of VH4524184 in plasma (Period 1)

  Day 1 to Day 14

• Area under the concentration-time curve from time zero to the last measured timepoint (AUC 0-t) of VH4524184 in plasma (Period 2)

  Day 15 to Day 43

• Area under the concentration-time curve from time zero to the last measured timepoint (AUC 0-t) of [14C]VH4524184 in plasma (Period 1)

  Day 1 to Day 14

• Area under the concentration-time curve from time zero to the last measured timepoint (AUC 0-t) of TRA in plasma (Period 1)

  Day 1 to Day 14

• Area under the concentration-time curve from time zero to the last measured timepoint (AUC 0-t) of TRA in plasma (Period 2)

  Day 15 to Day 43

• Area under the concentration-time curve from time zero to the last measured timepoint (AUC 0-t) of TRA in whole blood (Period 1)

  Day 1 to Day 14

• Area under the concentration-time curve from time zero to the last measured timepoint (AUC 0-t) of TRA in whole blood (Period 2)

  Day 15 to Day 43

• Area under the concentration-time curve from time zero to infinity (AUC 0-inf) of VH4524184 in plasma (Period 1)

  Day 1 to Day 14

• Area under the concentration-time curve from time zero to infinity (AUC 0-inf) of VH4524184 in plasma (Period 2)

  Day 15 up to Day 43

• Area under the concentration-time curve from time zero to infinity (AUC 0-inf) of [14C]VH4524184 in plasma (Period 1)

  Day 1 to Day 14

• Area under the concentration-time curve from time zero to infinity (AUC 0-inf) of TRA in plasma (Period 1)

  Day 1 to Day 14

• Area under the concentration-time curve from time zero to infinity (AUC 0-inf) of TRA in plasma (Period 2)

  Day 15 to 43

• Area under the concentration-time curve from time zero to infinity (AUC 0-inf) of TRA in whole blood (Period 1)

  Day 1 to Day 14

• Area under the concentration-time curve from time zero to infinity (AUC 0-inf) of TRA in whole blood (Period 2)

  Day 15 to Day 43

• Amount of VH4524184 excreted in urine (Ae urine) (Period 2)

  Day 15 to Day 43

• Fraction of VH4524184 excreted in urine (fe urine) (Period 2)

  Day 15 to Day 43

• Renal clearance of VH4524184 (CL R) (Period 2)

  Day 15 to Day 43

Secondary Outcomes (5)

• Number of participants with adverse events (AE), overall and by severity (Periods 1 and 2)

  Day 1 to Day 50

• Number of participants who discontinue treatment due to AEs (Periods 1 and 2)

  Day 1 to Day 50

• Change from baseline for aspartate aminotransferase (AST), alanine aminotransferase (ALT), total bilirubin, and alkaline phosphatase (Periods 1 and 2)

  On Days 2, 14, 16, 28 and 42

• Maximum toxicity grade increase from baseline for AST, ALT, total bilirubin, and alkaline phosphatase (Periods 1 and 2)

  On Days 2, 14, 16, 28 and 42

• Blood to plasma ratio of TRA (Periods 1 and 2)

  Day 1 to Day 14 (Period 1) and Day 15 to Day 28 (Period 2)

Study Arms (1)

VH4524184 Group

EXPERIMENTAL

Participants will receive a dose of VH4524184 under fasting conditions, followed by a microdose of radiolabelled \[14C\]VH4524184 administered 2.5 hours after first dose administration at time zero on Day 1 (Period1). After a 14 days wash-out period participants will receive a radiolabelled dose of \[14C\]VH4524184 on Day 15 under fasting conditions.

Drug: VH4524184; Drug: [14C]VH4524184 microdose; Drug: [14C]VH4524184

Interventions

VH4524184 DRUG

One dose of VH4524184 is administered to participants at time zero on Day 1 (Period 1).

VH4524184 Group

[14C]VH4524184 DRUG

One dose of radiolabelled \[14C\]VH4524184 is administered to participants at Day 15 (Period 2).

VH4524184 Group

[14C]VH4524184 microdose DRUG

A radiolabelled microdose of \[14C\]VH4524184 is administered 2.5 hours after VH4524184 dose administration on Day 1 (Period1).

VH4524184 Group

Eligibility Criteria

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

You may qualify if:

• Willing and able to sign the Informed Consent Form (ICF).
• Sex at birth: male or female; female participants must be of non-childbearing potential, or postmenopausal.
• Age: 18 to 55 years, inclusive, at screening.
• BMI: 18.0 to 32.0 kg/m\^2, inclusive, at screening.
• Female participants of non-childbearing potential must have unequivocal documentation that they are not of childbearing potential Postmenopausal female participants must have a serum follicle-stimulating hormone (FSH) concentration \>33.4 milli-international units per milliliter (mIU/mL) at screening to confirm menopause.
• Male participants, if not surgically sterilized and who have a female partner of childbearing potential, must agree to use a condom during any sexual intercourse until the completion of the follow-up visit.
• Male participants must agree not to donate sperm from admission on Day -1 until the completion of the follow-up visit.
• All prescribed medication must have been stopped at least 30 days and \>5 half-lives prior to admission to the clinical site on Day -1.
• All over-the-counter medication, vitamin preparations and other food supplements, or herbal medications must have been stopped at least 14 days prior to admission to the clinical site on Day -1. An exception is made for paracetamol that is allowed up to admission to the clinical site on Day -1.
• Ability and willingness to abstain from alcohol from 48 hours prior to screening and admission to the clinical site on Day -1 until the last PK sample.
• Ability and willingness to abstain from methylxanthine-containing beverages or food (coffee, black tea, green tea, white tea, cola, chocolate, energy drinks), and grapefruit (juice) from 48 hours prior to admission to the clinical site.
• Good physical and mental health based on medical history, physical examination, clinical laboratory, electrocardiogram (ECG), and vital signs, as judged by the Investigator.

You may not qualify if:

• Employee of ICON, the Sponsor, GSK or associated vendors.
• History of relevant drug and/or food allergies.
• History of drug hypersensitivity, delayed-type hypersensitivity, or severe hypersensitivity reactions, as well as history of sensitivity to the study drug.
• Using tobacco/nicotine products within 60 days prior to the first study drug administration.
• History of alcohol abuse or drug addiction within 5 years prior to screening.
• Positive drug and/or alcohol screen at screening or admission to the clinical site.
• Average intake of more than 24 units of alcohol per week.
• Positive screen for hepatitis B surface antigen (HBsAg), hepatitis C virus (HCV) antibodies, or human immunodeficiency virus (HIV) 1 and 2 antibodies at screening.
• Participation in a drug study with a small molecule drug within 30 days or 5 half-lives if known (whichever is longer) prior to the first study drug administration in the current study. Participation in a clinical study with a biological within 90 days or 5 half-lives if known (whichever is longer) prior to the first study drug administration in the current study. Participation in 4 or more other drug studies in the 12 months prior to the first study drug administration in the current study.
• Donation or loss of more than 450 mL of blood within 60 days prior to the first study drug administration. Donation or loss of more than 1.5 L of blood (for male participants)/more than 1.0 L of blood (for female participants) in the 10 months prior to the first study drug administration in the current study.
• Significant and/or acute illness within 14 days prior to the first study drug administration that may impact safety assessments, in the opinion of the Investigator.
• Any significant current/ongoing known or suspected pre-existing psychiatric condition, including depression, anxiety, and/or insomnia/sleep disturbances and/or suicidal ideation, in the opinion of the Investigator.
• Unsuitable veins for infusion or blood sampling.
• Participation in a study with a 14C dose of ≥0.1 megabecquerel (MBq) in the period of 1 year prior to screening.
• Irregular defecation pattern.

Sponsors & Collaborators

• ViiV Healthcare: lead

MeSH Terms

Conditions

HIV Infections; Acquired Immunodeficiency Syndrome

Condition Hierarchy (Ancestors)

Blood-Borne Infections; Communicable Diseases; Infections; Sexually Transmitted Diseases, Viral; Sexually Transmitted Diseases; Lentivirus Infections; Retroviridae Infections; RNA Virus Infections; Virus Diseases; Genital Diseases; Urogenital Diseases; Immunologic Deficiency Syndromes; Immune System Diseases; Slow Virus Diseases

Central Study Contacts

US GSK Clinical Trials Call Center

CONTACT

877-379-3718; GSKClinicalSupportHD@gsk.com

EU GSK Clinical Trials Call Center

CONTACT

+44 (0) 20 89904466; GSKClinicalSupportHD@gsk.com

Study Design

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

Study Record Dates

• First Submitted: May 29, 2026
• First Posted: June 9, 2026
• Study Start: June 15, 2026
• Primary Completion (Estimated): August 20, 2026
• Study Completion (Estimated): August 20, 2026
• Last Updated: June 9, 2026

Record last verified: 2026-06

Data Sharing

• IPD Sharing: Will share
• Shared Documents: STUDY PROTOCOL, SAP, ICF, CSR
• Time Frame: Anonymized IPD will be made available within 6 months of publication of primary, key secondary and safety results for studies in product with approved indication(s) or asset(s) with development terminated across all indications.
• Access Criteria: Anonymized IPD is shared with researchers whose proposals are approved by an Independent Review Panel and after a Data Sharing Agreement is in place. Access is provided for an initial period of 12 months, but an extension may be granted, when justified, for up to 6 months.