A Study to Evaluate the Pharmacokinetic Effects of Different Storage Conditions for a Long-Acting Nanosuspension of Rilpivirine on Pharmacokinetics

Janssen Infectious Diseases BVBA61 enrolled

Overview

The purpose of this study is to compare the single-dose pharmacokinetics of rilpivirine (RPV) after intramuscular (IM) injection of rilpivirine long-acting parenteral formulation (RPV-LA) and 'aged' RPV-LA, in healthy adult participants.

This is a phase 1 randomized (study medication is assigned by chance), open-label (all people know the identity of the intervention), parallel-group, sequential study in healthy adult participants to investigate the effect of different storage conditions for RPV-LA on the single-dose pharmacokinetics of rilpivirine (RPV) after intramuscular injection. A total of 60 healthy adult participants will be enrolled in this study. The study will consist of 2 treatment sessions in a fixed sequential order : session 1 of up to day 8, all participants will receive a single oral dose of rilpivirine 25 milligram (mg) tablet on day 1, session 2 will consists of 2 treatment groups. The participants will be randomized in session 2 on Day 1 in a 1:1 ratio to Treatments A and B. Each treatment group will receive one IM injection of RPV LA on Day 1 of session 2. Session 1 and 2 will be separated by a washout period of at least 14 days. The total study duration for each participant will be approximately 6.5 months. Safety will be monitored throughout the study.

Study Type

INTERVENTIONAL

Allocation

RANDOMIZED

Purpose

TREATMENT

Masking

NONE

Enrollment

Conditions

Human Immunodeficiency Virus Type 1

Interventions

Rilpivirine (RPV)DRUG

Participants will receive one oral tablet of rilpivirine 25 milligram (mg) once on Day 1 of session 1.

Rilpivirine Long-Acting Parenteral Formulation (RPV-LA)DRUG

Participants will receive one intramuscular (IM) injection of rilpivirine long-acting parenteral formulation 600 mg once on day 1 of session 2.

Aged RPV-LADRUG

Participants will receive one intramuscular (IM) injection of aged rilpivirine long-acting parenteral formulation 600 mg once on day 1 of session 2.

Eligibility

Sex: ALLMin age: 18 YearsMax age: 55 YearsHealthy volunteers:

Medical Language ↔ Plain English

Inclusion Criteria: * Each participant must sign an Informed Consent Form (ICF) indicating that he or she understands the purpose of, and procedures required for, the study and are willing to participate in the study * Participant must be willing and able to adhere to the prohibitions and restrictions specified in this protocol * Participant must be healthy on the basis of a medical evaluation that reveals the absence of any clinically significant abnormality and includes a physical examination, medical history, vital signs, Electrocardiogram (ECG), and the results of blood biochemistry, hematology and coagulation tests and a urinalysis performed at Screening * A female participant of childbearing potential must have a negative serum (beta-human chorionic gonadotropin \[beta-hCG\]) at Screening and a negative urine pregnancy test on day 1 * Participant must be non-smoking for at least 3 months prior to selection Exclusion Criteria: * Female participant who is breastfeeding at Screening * Participants with a history of any illness that, in the opinion of the investigator, might confound the results of the study or pose an additional risk in administering study drug to the participant or that could prevent, limit or confound the protocol specified assessments. This may include, but is not limited to, renal dysfunction, significant cardiac, vascular, pulmonary, gastrointestinal, endocrine, neurologic, hematologic, rheumatologic, psychiatric, neoplastic, or metabolic disturbances * Has known allergies, hypersensitivity, or intolerance to rilpivirine (RPV) or its excipients * Has a history of drug allergy such as, but not limited to, sulfonamides and penicillins, or drug allergy witnessed in previous studies with experimental drugs * Having donated or lost more than 1 unit of blood (500 milliliter \[mL\]) within 60 days or more than 1 unit of plasma within 7 days before the first dose of study drug

Locations (1)

Unnamed facility

Antwerp, Belgium

Outcomes

Primary Outcomes

Maximum Observed Plasma Concentration (Cmax)

The Cmax is the maximum observed plasma concentration of rilpivirine.

Time frame: In session1: Pre-dose, 0.5, 1, 2, 3, 4, 5, 6, 9, 12, 16, 24, 48, 72, 120 and 168 hours post-dose; In session 2: Pre-dose, 1, 2, 4, 8, 12, 24, 48, 72, 96, 120, 168,216, 264, 336, 408, 528, 672, 1344, 2016, 2688, 3360 and 4032 hours post-dose

Area Under the Plasma Concentration-Time Curve From Time Zero (Day 1) to Day 28 (AUC[0-d28])

The AUC (0-d28) is the area under the plasma concentration-time curve for rilpivirine from time zero to day 28.

Time frame: In session1: Pre-dose, 0.5, 1, 2, 3, 4, 5, 6, 9, 12, 16, 24, 48, 72, 120 and 168 hours post-dose; In session 2: Pre-dose, 1, 2, 4, 8, 12, 24, 48, 72, 96, 120 and 168 hours post-dose

Area Under the Plasma Concentration-Time Curve From Time Zero to Last Quantifiable Time (AUC [0-last])

The AUC (0-last) is the area under the plasma concentration-time curve for rilpivirine from time zero to last quantifiable time.

Area Under the Plasma Concentration-Time Curve From Time Zero to Infinite Time (AUC[0-infinity])

The AUC (0-infinity) is the area under the plasma concentration-time curve from time zero to infinite time, calculated as the sum of AUC(last) and C(last)/lambda(z); wherein AUC(last) is area under the plasma concentrationtime curve from time zero to last quantifiable time, C(last) is the last observed quantifiable concentration, and lambda(z) is elimination rate constant.

Secondary Outcomes

Data from ClinicalTrials.gov

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Number of Participants With Adverse Events

An adverse event is any untoward medical event that occurs in a participant administered an investigational product, and it does not necessarily indicate only events with clear causal relationship with the relevant investigational product.

Time frame: Up to 180 Days

Time to reach the maximum observed plasma concentration (Tmax)

The Tmax is the actual sampling time to reach maximum observed plasma concentration of rilpivirine.

Elimination Rate Constant (Lambda [z]) of rilpivirine

The Lambda (z) determined by linear regression of the terminal points of the ln-linear plasma concentration-time curve.

Apparent Terminal Half-life (t[1/2]) of rilpivirine

Apparent terminal elimination half-life, calculated as 0.693/Lambda (z).