Mass Balance and Absolute Bioavailability of [14C]-VH4011499

A Phase 1, Open-label, Single-dose Study to Assess the Absolute Bioavailability, Mass Balance, Pharmacokinetics, Metabolism, and Excretion of [14C]-VH4011499 in Healthy Participants

The purpose of the trial is to characterize the absorption, metabolism, and excretion of [14C]-VH4011499, and to evaluate the absolute bioavailability of VH4011499.

Study Overview

• Status: Not yet recruiting
• Conditions: HIV Infections
• Intervention / Treatment: Drug: VH4011499; Drug: [14C]-VH4011499 (IV); Drug: [14C]-VH4011499 (oral)

• Study Type: Interventional
• Enrollment (Estimated): 18
• Phase: Phase 1

Contacts and Locations

• Study Contact: Name: US GSK Clinical Trials Call Center; Phone Number: 877-379-3718; Email: GSKClinicalSupportHD@gsk.com
• Study Contact Backup: Name: EU GSK Clinical Trials Call Center; Phone Number: +44 (0) 20 89904466; Email: GSKClinicalSupportHD@gsk.com

Participation Criteria

Eligibility Criteria

• Ages Eligible for Study: 18 years to 55 years (Adult)
• Accepts Healthy Volunteers: Yes
• Genders Eligible for Study: All

Description

Inclusion Criteria:

• Willing and able to sign the informed consent form.

• Sex at birth: male or female; female participants must be of non-childbearing potential, or postmenopausal.

• Age: 18 to 55 years, inclusive, at screening.

• Female participants are eligible to participate if they are of non-childbearing potential and are not breastfeeding or planning to breastfeed for at least 12 months following the last dose.

  • Female participants of non-childbearing potential must have unequivocal documentation (either by medical records and/or from the clinical interview) that they are not of childbearing potential (postmenopausal, medically sterile, or surgically sterile). 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, must agree to use a condom when having sexual intercourse with a female partner of childbearing potential from admission to the clinical site on Day -1 until the completion of the follow up visit.

• Male participants must agree not to donate sperm from admission to the clinical site on Day -1 until the completion of the follow-up visit.

• All prescribed medication must have been stopped at least 30 days or >5 half-lives (whichever is longer) prior to admission to the clinical site on Day -1 until completion of the follow-up visit.

• 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 until completion of the follow-up visit. An exception is made for paracetamol (≤ 2 g per day), which is allowed up to admission to the clinical site.

• Good physical and mental health based on medical history, physical examination, clinical laboratory test results, electrocardiogram (ECG), and vital signs, as judged by the Investigator.

Exclusion Criteria:

• 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 trial drug.
• Using tobacco/nicotine products within 30 days prior to the first trial drug administration. - Positive screen for hepatitis B surface antigen (HBsAg), hepatitis C virus (HCV) antibodies, or HIV 1 or 2 antibodies at screening.
• Unstable liver disease (as defined by any of the following: presence of ascites, encephalopathy, coagulopathy, hypoalbuminemia, esophageal or gastric varices, or persistent jaundice or cirrhosis), known biliary abnormalities (with the exception of Gilbert's syndrome or asymptomatic gallstones or otherwise stable chronic liver disease per investigator assessment).
• Known history of cirrhosis with or without viral hepatitis co-infection.
• History of clinically relevant hepatitis within the last 6 months.
• Any verified Grade 4 laboratory abnormality. - ALT >1.5x (upper limit of normal [ULN]).
• Total bilirubin >1.5x ULN.
• Estimated glomerular filtration rate (GFR) of <60 mL/min/1.73 m^2.
• QT interval corrected for heart rate according to Fridericia's formula (QTcF) >450 msec.
• Clinically significant cardiovascular disease, as defined by history/evidence of congestive heart failure, symptomatic arrhythmia, angina/ischemia, coronary artery bypass grafting surgery or percutaneous transluminal coronary angioplasty or any clinically significant cardiac disease.
• Unsuitable veins for infusion or blood sampling. - Participation in a trial with a [14C] dose of ≥0.1 MBq in the period of 1 year prior to screening.
• TRA in plasma must not exceed a [14C] / [12C] ratio of 1.31x10^-12. - Exposure to significant radiation (e.g., serial x-ray or CT scans, barium meal, etc.) in the 3 years prior to screening.
• Irregular defecation pattern (less than once per 2 days).

Study Plan

How is the study designed?

Design Details

• Primary Purpose: Basic Science
• Allocation: Non-Randomized
• Interventional Model: Parallel Assignment
• Masking: None (Open Label)

Number of Arms

2

Arms and Interventions

Participant Group / Arm	Intervention / Treatment
Experimental: VH4011499 Cohort 1; Participants will receive a single oral dose of VH4011499, followed by a single intravenous (iv) microtracer dose of [14C]-VH4011499.	Drug: VH4011499; VH4011499 will be administered orally.; Drug: [14C]-VH4011499 (IV); [14C]-VH4011499 will be administered as an iv infusion.
Experimental: VH4011499 Cohort 2; Participants will receive a single oral dose of [14C]-VH4011499.	Drug: [14C]-VH4011499 (oral); [14C]-VH4011499 will be administered orally.

What is the study measuring?

Primary Outcome Measures

Outcome Measure	Measure Description	Time Frame
Total Radioactivity (TRA) of the Cumulative Amount of Drug Excreted in Urine (Ae urine)	Urine is collected until the cumulative amount of radioactivity recovered in excreta (urine and feces) is at least 90% of the administered radioactivity and less than 1% of the administered radioactive dose is recovered during a 24-hour collection period on 2 consecutive collection days.	Up to 70 days
TRA of the Cumulative Amount of Drug Excreted in Feces (Ae feces)	Feces are collected until the cumulative amount of radioactivity recovered in excreta (urine and feces) is at least 90% of the administered radioactivity and less than 1% of the administered radioactive dose is recovered during a 24-hour collection period on 2 consecutive collection days.	Up to 70 days
Cohort 2 Only: TRA of the Cumulative Amount of Drug Excreted in Vomitus (Ae vomit)	Vomitus (if applicable) will be collected and included in the assessment until the cumulative amount of radioactivity recovered in excreta is at least 90% of the administered radioactivity and less than 1% of the administered radioactive dose is recovered.	Up to 70 days
TRA of the Total Amount of Drug Excreted (Ae total)	Total amount of TRA excreted in excreta, calculated as the sum of the cumulative amount of radioactivity recovered in urine, feces, and vomit (if collected). Urine, feces, and vomitus (if applicable) will be collected until the cumulative amount of radioactivity recovered in excreta is at least 90% of the administered radioactive dose and less than 1% of the administered radioactive dose is recovered during a 24-hour collection period on 2 consecutive collection days.	Up to 70 days
Fraction of the Administered Radiolabeled Dose Excreted in Urine (fe urine) as Total Drug Related Material	Fraction of the dose administered excreted (unchanged) in urine percentage. Urine is collected until the cumulative amount of radioactivity recovered in excreta (urine and feces) is at least 90% of the administered radioactivity and less than 1% of the administered radioactive dose is recovered during a 24-hour collection period on 2 consecutive collection days.	Up to 70 days
Cohort 2 Only: Fraction of the Administered Radiolabeled Dose Excreted in Feces (fe feces) as Total Drug Related Material	Fraction of the dose administered excreted in feces percentage. Feces are collected until the cumulative amount of radioactivity recovered in excreta (urine and feces) is at least 90% of the administered radioactivity and less than 1% of the administered radioactive dose is recovered during a 24-hour collection period on 2 consecutive collection days.	Up to 70 days
Cohort 2 Only: Fraction of the Administered Radiolabeled Dose Excreted in Vomitus (fe vomit) as Total Drug Related Material	Fraction of the dose administered excreted in vomitus percentage. Vomitus (if applicable) will be collected and included in the assessment until the cumulative amount of radioactivity recovered in excreta is at least 90% of the administered radioactivity and less than 1% of the administered radioactive dose is recovered.	Up to 70 days
Fraction of the Administered Radiolabeled Dose Excreted in Urine, Feces, and Vomitus (fe total) as Total Drug Related Material	Fraction of the dose administered excreted in urine, feces, and vomitus if applicable percentage. Urine, feces, and vomitus (if applicable) will be collected until the cumulative amount of radioactivity recovered in excreta is at least 90% of the administered radioactive dose and less than 1% of the administered radioactive dose is recovered during a 24-hour collection period on 2 consecutive collection days.	Up to 70 days
Maximum Observed Plasma Concentration (Cmax) of VH4011499		Up to 70 days
Time to Attain Cmax (tmax) of VH4011499		Up to 70 days
Area Under the Plasma Concentration-time Curve From Time Zero to the Last Quantifiable Concentration (AUC0-t) of VH4011499		Up to 70 days
Area Under the Plasma Concentration-time Curve From Time 0 to Infinity (AUC0-inf) of VH4011499		Up to 70 days
Cohort 1 Only: Cmax of [14C]-VH4011499		Up to 70 days
Cohort 1 Only: Tmax of [14C]-VH4011499		Up to 70 days
Cohort 1 Only: AUC0-t of [14C]-VH4011499		Up to 70 days
Cohort 1 Only: AUC0-inf of [14C]-VH4011499		Up to 70 days
Cmax of TRA in Plasma		Up to 70 days
Tmax of TRA in Plasma		Up to 70 days
AUC0-t of TRA in Plasma		Up to 70 days
AUC0-inf of TRA in Plasma		Up to 70 days
Cmax of TRA in Whole Blood		Up to 70 days
Tmax of TRA in Whole Blood		Up to 70 days
AUC0-t of TRA in Whole Blood		Up to 70 days
AUC0-inf of TRA in Whole Blood		Up to 70 days
Whole Blood-to-plasma Ratio of TRA	Cmax, AUC(0-t) and AUC(0-inf) TRA measured in whole blood compared to Cmax, AUC(0-t) and AUC(0-inf) TRA measured in plasma.	Up to 70 days
Cohort 2 Only: Ae urine of VH4011499		Up to 70 days
Cohort 2 Only: fe urine of VH4011499	Fraction of the dose administered excreted (unchanged) in urine percentage.	Up to 70 days
Cohort 2 Only: Renal clearance (CLR) of VH4011499		Up to 70 days

Secondary Outcome Measures

Outcome Measure	Time Frame
Number of Participants with Adverse Events (AEs) by Severity	Up to 77 days
Absolute Values of Total Bilirubin, Direct bilirubin, Alkaline Phosphatase (ALP), Aspartate Aminotransferase (AST), and Alanine Aminotransferase (ALT)	Up to 77 days
Change From Baseline in Total Bilirubin, Direct Bilirubin, ALP, AST, and ALT	Up to 77 days
Maximum Toxicity Grade Change From Baseline in Total Bilirubin, Direct Bilirubin, ALP, AST, and ALT	Up to 77 days
Cohort 1 Only: Absolute Oral Bioavailability (F oral) of VH4011499	Up to 70 days

Collaborators and Investigators

• Sponsor: ViiV Healthcare
• Investigators: Study Director: GSK Clinical Trials, GlaxoSmithKline

Study record dates

Study Major Dates

• Study Start (Estimated): November 9, 2026
• Primary Completion (Estimated): February 18, 2027
• Study Completion (Estimated): February 18, 2027

Study Registration Dates

• First Submitted: November 6, 2026
• First Submitted That Met QC Criteria: November 6, 2026
• First Posted (Actual): November 13, 2026

Study Record Updates

• Last Update Posted (Actual): November 13, 2026
• Last Update Submitted That Met QC Criteria: November 6, 2026
• Last Verified: November 1, 2026

More Information

Terms related to this study

• Keywords: VH4011499; Human immunodeficiency virus (HIV)
• Additional Relevant MeSH Terms: Blood-Borne Infections; Urogenital Diseases; Genital Diseases; Immune System Diseases; Infections; RNA Virus Infections; Virus Diseases; Communicable Diseases; Sexually Transmitted Diseases, Viral; Sexually Transmitted Diseases; Lentivirus Infections; Retroviridae Infections; Immunologic Deficiency Syndromes; Slow Virus Diseases; HIV Infections; Acquired Immunodeficiency Syndrome
• Other Study ID Numbers: 223808; 2026-527050-40 (Other Identifier: EU CT number)

Plan for Individual participant data (IPD)

• Plan to Share Individual Participant Data (IPD)?: YES

IPD Plan Description

Study Sponsor will assess requests from qualified researchers for anonymized individual patient-level data and related study documents. Data sharing is subject to certain criteria, conditions, and exceptions. For further information, refer to https://www.viiv-studyregister.com/documents/About_ViiV_Patient_Level_Data_Sharing_Final_28May2026.pdf

IPD Sharing 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.

IPD Sharing 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.

• IPD Sharing Supporting Information Type: STUDY_PROTOCOL; SAP; ICF; CSR

Drug and device information, study documents

• Studies a U.S. FDA-regulated drug product: Yes
• Studies a U.S. FDA-regulated device product: No
• product manufactured in and exported from the U.S.: Yes