A Study of the Pharmacokinetics of ASC09F in Healthy Subjects

A Study to Evaluate the Pharmacokinetics of ASC09F in Healthy Subjects After Multiple Doses

The objective of this study is to evaluate the pharmacokinetic parameters of ASC09F in healthy subjects after multiple oral dosing.

Study Overview

• Status: Completed
• Conditions: Healthy
• Intervention / Treatment: Drug: ASC09F

Detailed Description

This study will evaluate the safety and the pharmacokinetics of ASC09F tablets in healthy volunteers. Subjects will receive 7 days multiple oral doses of ASC09F tablets.

• Study Type: Interventional
• Enrollment (Actual): 12
• Phase: Phase 1

Contacts and Locations

Study Locations

• China
  • Beijing
    • Beijing, Beijing, China, 100069
      • Beijing Youan Hospital, Capital Medical University

Participation Criteria

Eligibility Criteria

• Ages Eligible for Study: 18 years to 45 years (ADULT)
• Accepts Healthy Volunteers: Yes
• Genders Eligible for Study: All

Description

Inclusion Criteria:

• 1. Age 18-45 (including boundary value), half men and half women. 2. Male weight ≥ 50kg, female weight ≥ 45kg;BMI ranges from 19 to 30kg/m2 (boundary value included).

  3. According to the medical history, physical examination, vital signs, laboratory examination and 12 lead electrocardiogram (ECG) examination, the general health condition is good, and there is no clinically significant abnormality in each index.

  4. Unplanned pregnancy within half a year and willing to take effective contraceptive measures within 30 days from the first administration of the study drug to the last administration.

  5. The pregnancy test of female subjects during the screening period is negative.

  6. Those who voluntarily sign the informed consent.

Exclusion Criteria:

• 1. Hepatitis B surface antigen (HBsAg), Hepatitis C virus antibody (HCV Ab), HIV antibody (HIV Ab) and syphilis antibody were tested positive.

  2. People who have taken special diet (including carambola, dragon fruit, mango, grapefruit, orange, etc.) or drunk alcohol, or had strenuous exercise, or other factors affecting drug absorption, distribution, metabolism, and excretion within 2 weeks before taking the study drug.

  3. Heavy smokers (14 units of alcohol per week: 1 unit = 285 mL beer, or 25 mL spirits, or 100 mL wine;Smoking daily ≥ 5 sticks) and no smoking or alcohol prohibition during the study period.

  4. Ingesting chocolate, any food or drink containing caffeine or xanthine in the 24 hours prior to taking the study drug.

  5. Patients who had donated blood or lost blood of more than 400ml within 3 months before taking the study drug.

  6. Those who have participated in other clinical trials and received study drug treatment within 3 months before taking study drug.

  7. Alcoholic or nonalcoholic fatty liver disease. 8. In addition to the above, the researchers judge that the participants are not suitable to participate in this clinical trial.

Study Plan

How is the study designed?

Design Details

• Primary Purpose: TREATMENT
• Allocation: NA
• Interventional Model: SINGLE_GROUP
• Masking: NONE

Number of Arms

1

Arms and Interventions

Participant Group / Arm	Intervention / Treatment
EXPERIMENTAL: ASC09F; ASC09F one tablet at a time, once per day, up to 7 days.	Drug: ASC09F; ASC09F (300 mg ASC09 and 100 mg Ritonavir) one tablet at a time, once per day, up to 7 days.

What is the study measuring?

Primary Outcome Measures

Outcome Measure	Measure Description	Time Frame
AUC of ASC09F	Evaluate the Area under the plasma concentration versus time curve after	On Day 1,2,3,4 after single doses and On Day 1,2,3,4 after multiple doses, respectively. The entire study will last up to 11 days.
Cmax of ASC09F	Evaluate the Peak Plasma Concentration after single and multiple oral doses of ASC09F administered to Chinese healthy volunteers.	On Day 1,2,3,4 after single doses and On Day 1,2,3,4 after multiple doses, respectively. The entire study will last up to 11 days.

Secondary Outcome Measures

Outcome Measure	Measure Description	Time Frame
t1/2 of ASC09F	Evaluate the Terminal-Phase Half-Life after single and multiple oral doses of ASC09F administered to Chinese healthy volunteers volunteers.	On Day 1,2,3,4 after single doses and On Day 1,2,3,4 after multiple doses, respectively. The entire study will last up to 11 days.
CL/F of ASC09F	Evaluate the Apparent Systemic Clearance after single and multiple oral dose of ASC09F administered to Chinese healthy volunteers.	On Day 1,2,3,4 after single doses and On Day 1,2,3,4 after multiple doses, respectively. The entire study will last up to 11 days.
Vd/F of ASC09F	Evaluate the Apparent Volume of Distribution after single and multiple oral dose of ASC09F administered to Chinese healthy volunteers.	On Day 1,2,3,4 after single doses and On Day 1,2,3,4 after multiple doses, respectively. The entire study will last up to 11 days.
Evaluation of the safety of ASC09F in healthy volunteers	Evaluate number of adverse events as a measure of safety of ASC09F.	Up to 11 days
Tmax of ASC09F	Evaluate the Time to reach the maximum plasma concentration after single single and multiple oral doses of ASC09F administered to Chinese healthy volunteers.	On Day 1,2,3,4 after single doses and On Day 1,2,3,4 after multiple doses, respectively. The entire study will last up to 11 days.

Collaborators and Investigators

• Sponsor: Ascletis Pharmaceuticals Co., Ltd.
• Collaborators: Beijing YouAn Hospital

Publications and helpful links

General Publications

• Dierynck I, Van Marck H, Van Ginderen M, Jonckers TH, Nalam MN, Schiffer CA, Raoof A, Kraus G, Picchio G. TMC310911, a novel human immunodeficiency virus type 1 protease inhibitor, shows in vitro an improved resistance profile and higher genetic barrier to resistance compared with current protease inhibitors. Antimicrob Agents Chemother. 2011 Dec;55(12):5723-31. doi: 10.1128/AAC.00748-11. Epub 2011 Sep 6.
• Hoetelmans RM, Dierynck I, Smyej I, Meyvisch P, Jacquemyn B, Marien K, Simmen K, Verloes R. Safety and pharmacokinetics of the HIV-1 protease inhibitor TMC310911 coadministered with ritonavir in healthy participants: results from 2 phase 1 studies. J Acquir Immune Defic Syndr. 2014 Mar 1;65(3):299-305. doi: 10.1097/QAI.0000000000000011.
• Stellbrink HJ, Arasteh K, Schurmann D, Stephan C, Dierynck I, Smyej I, Hoetelmans RM, Truyers C, Meyvisch P, Jacquemyn B, Marien K, Simmen K, Verloes R. Antiviral activity, pharmacokinetics, and safety of the HIV-1 protease inhibitor TMC310911, coadministered with ritonavir, in treatment-naive HIV-1-infected patients. J Acquir Immune Defic Syndr. 2014 Mar 1;65(3):283-9. doi: 10.1097/QAI.0000000000000003.

Study record dates

Study Major Dates

• Study Start (ACTUAL): November 9, 2020
• Primary Completion (ACTUAL): December 7, 2020
• Study Completion (ACTUAL): December 7, 2020

Study Registration Dates

• First Submitted: September 8, 2020
• First Submitted That Met QC Criteria: September 8, 2020
• First Posted (ACTUAL): September 14, 2020

Study Record Updates

• Last Update Posted (ACTUAL): January 11, 2021
• Last Update Submitted That Met QC Criteria: January 7, 2021
• Last Verified: September 1, 2020

More Information

Terms related to this study

• Additional Relevant MeSH Terms: Molecular Mechanisms of Pharmacological Action; Enzyme Inhibitors; Protease Inhibitors; TMC-310911
• Other Study ID Numbers: ASC-ASC09F-I-CTP-01

Plan for Individual participant data (IPD)

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

Drug and device information, study documents

• Studies a U.S. FDA-regulated drug product: No
• Studies a U.S. FDA-regulated device product: No