A Study of Bioavailability and Food Effect of SACT-1 and Edurant® Tablets in Healthy Adult Volunteers

NCT05358756 | Completed Phase 1 DMC FDA Drug

• 1 other identifier: 12190001
• Study Type: interventional
• Target: 16
• Locations: 1 country
• Sites: 1

Brief Summary

This was a Phase 1, open-label, randomized, single center, 3-period, 3-sequence, single-dose crossover bioavailability and food effect study between SACT-1 and Edurant® tablet.

Conditions

Healthy Subject

Outcome Measures

Primary Outcomes (1)

• Relative Bioavailability of SACT-1 and Edurant Tablet

  Compare the relative bioavailability of 150 mg SACT-1 (oral suspension) under fasted and fed conditions to 150 mg Edurant® (6 × 25 mg rilpivirine, oral tablets) under fed conditions.

  Up to 240 hours after dosing in each study period

Secondary Outcomes (2)

• Number of subjects with Adverse Events

  Up to 14 days after the final dose of the study drug.

• The effect of food (fasted or fed condition) on potential QT prolongation from administration of a single dose of 150 mg rilpivirine in healthy adult subjects.

  Up to 24 hours after dosing in each study period

Study Arms (3)

Treatment A :Fasted

EXPERIMENTAL

A single adminstration of SACT-1 (150 mg rilpivirine oral suspension) after a supervised overnight fast of at least 10 hours.

Drug: SACT-1

Treatment B: Fed

EXPERIMENTAL

A single adminstration of SACT-1 (150 mg rilpivirine oral suspension) after a supervised overnight fast of at least 10 hours followed by a high-fat, high calorie meal (fed).Subjects started the standardized high-fat, high-calorie breakfast 30 minutes prior to dosing and consumed this meal within the 30 minutes before dosing.

Drug: SACT-1

Treatment C: Fed

ACTIVE COMPARATOR

Adminstartion of Edurant, 150 mg (6 × 25 mg rilpivirine, oral tablets), after a supervised overnight fast of at least 10 hours followed by a high-fat, high calorie meal (fed).Subjects started the standardized high-fat, high-calorie breakfast 30 minutes prior to dosing and consumed this meal within the 30 minutes before dosing.

Drug: EDURANT 25Mg Tablet

Interventions

SACT-1 DRUG

Single administartion of 150mg SACT-1

Treatment A :Fasted; Treatment B: Fed

EDURANT 25Mg Tablet DRUG

Single administartion of six EDURANT 25mg tablets (Total 150mg)

Treatment C: Fed

Eligibility Criteria

• Age: 18 Years+
• Sex: all
• Healthy Volunteers: Yes
• Age Groups: Adult (18-64), Older Adult (65+)

You may qualify if:

• Healthy male or female volunteers ≥ 18 years of age.
• Males or non-pregnant, non-lactating females who are postmenopausal, naturally or surgically sterile (bilateral tubal ligation with surgery at least 6 weeks prior to study initiation or hysterectomy), or who agree to use effective contraceptive methods throughout the course of the study and for 30 days after the last dose of study drug. Postmenopausal is defined as at least 12 months natural spontaneous amenorrhea and a serum FSH concentration ≥ 40 IU/L), or at least 6 weeks following surgical menopause (bilateral oophorectomy).
• Females of childbearing potential and male subjects with female partners of childbearing potential must agree to use at least 1 of the following acceptable birth control methods during the study and for at least 30 days after the last dose:
• IUD in place for at least 3 months.
• Abstinence (not having heterosexual vaginal intercourse).
• Barrier method (condom or diaphragm) with spermicide for at least 14 days prior to screening and through study completion and for 30 days after the last dose of study drug.
• Stable hormonal contraceptive for at least 3 months prior to study and through study completion (an additional barrier method must be used during the study) and for 30 days after the last dose of study drug. Oral contraceptive use is not permitted in this study.
• Monogamous relationship with a vasectomized partner.
• Able to understand and provide signed informed consent.
• Normally active and otherwise judged to be in good health on the basis of medical history and physical examination.
• Females of childbearing potential must have a negative serum hCG pregnancy test at screening.
• BMI ≥ 19.0 and \< 32.0.
• Willing and able to consume the entire assigned meals, which include meat, dairy and carbohydrate components, within the designated time frames.
• Subjects must have normal hepatic function at the Screening Visit, defined as the following:
• Alanine aminotransferase \<1.5 × upper limit of normal (ULN); or

You may not qualify if:

• Known or suspected pregnancy, planned pregnancy, or lactation.
• History of allergic reaction to rilpivirine or other related drugs.
• Clinically significant illness or surgery within 4 weeks prior to dosing (including flu, flulike symptoms, diarrhea, vomiting).
• Positive test for hepatitis B, hepatitis C, or HIV at screening
• Clinically significant ECG abnormalities or vital sign abnormalities (systolic blood pressure lower than 90 or over 140 mmHg, diastolic blood pressure lower than 50 or over 90 mmHg, or heart rate less than 50 or over 100 bpm) at screening.
• Any clinically significant abnormal laboratory test results found during medical screening.
• A history of major mental illness that in the opinion of the Investigator may affect the ability of the subject to participate in the study.
• Clinically significant history or presence of any gastrointestinal pathology (eg, chronic diarrhea, inflammatory bowel diseases), unresolved gastrointestinal symptoms (eg, diarrhea vomiting), liver or kidney disease, gastric bypass, gastric stapling, use of Lapband, or other conditions known to interfere with the absorption, distribution, metabolism, or excretion of the drug.
• Any history of or active neurological, endocrine, cardiovascular, pulmonary, hematological, immunologic, psychiatric, or metabolic disease that is considered clinically significant by the Investigator.
• Use of prescription medication within 14 days prior to administration of study drug or OTC medicines (including natural food supplements and vitamins) within 14 days prior to administration of study drug.
• Use of any tobacco- or nicotine- containing product in the 3 months preceding the Period 1 dose administration.
• Any food allergy, intolerance, restriction, or special diet that, in the opinion of the Investigator, could contraindicate the subject's participation in this study.
• Recent history of (within the past 12 months), or strong potential for, alcoholic substance abuse. Alcohol abused will be defined as \> 14 drinks per week (1 drink = 12 oz beer, 5.0 oz wine, or 1.5 oz distilled spirits).
• Exposure to any investigational agent within 30 days prior to study entry.
• Subjects who donated (standard donation amount or more) blood or blood products (with the exception of plasma as noted below) within 56 days prior to the study.

Sponsors & Collaborators

• Aptorum International Limited: lead

Study Sites (1)

Novum Pharmaceutical Research Services

Fargo, North Dakota, 58104, United States

Location

MeSH Terms

Interventions

Rilpivirine; Tablets

Intervention Hierarchy (Ancestors)

Nitriles; Organic Chemicals; Pyrimidines; Heterocyclic Compounds, 1-Ring; Heterocyclic Compounds; Dosage Forms; Pharmaceutical Preparations

Study Officials

• Thomas Lee, PhD

  Aptorum International Limited

  PRINCIPAL INVESTIGATOR

Study Design

• Study Type: interventional
• Phase: phase 1
• Allocation: RANDOMIZED
• Masking: NONE
• Purpose: TREATMENT
• Intervention Model: CROSSOVER
• Sponsor Type: INDUSTRY
• Responsible Party: SPONSOR

Model Details: Each of the following treatments were given to subjects in a randomized sequence: Treatment A: SACT-1, 150 mg rilpivirine oral suspension (30.0 mg of rilpivirine \[equivalent to 33.0 mg of rilpivirine hydrochloride\] in each mL), fasted Treatment B: SACT-1, 150 mg rilpivirine oral suspension (30.0 mg of rilpivirine \[equivalent to 33.0 mg of rilpivirine hydrochloride\] in each mL), fed Treatment C: Edurant, 150 mg (6 × 25 mg rilpivirine, oral tablets), fed

Study Record Dates

• First Submitted: April 28, 2022
• First Posted: May 3, 2022
• Study Start: October 9, 2021
• Primary Completion: November 20, 2021
• Study Completion: December 14, 2021
• Last Updated: May 26, 2022

Record last verified: 2022-04

Locations

US (1)