Pharmacokinetics and Safety Study of Apetrol ES (Apetrol)

A Randomized, Open Label, Single Dose, Cross-over, Phase I Trial to Investigate Safety and Pharmacokinetics of Apetrol ES and Megace® Under Fasting and Fed Conditions in Healthy Male Volunteers

A Randomized, Open Label, Single dose, Cross-over, Phase I Trial to Investigate Safety and Pharmacokinetics of Apetrol ES and Megace® in Healthy Male Volunteers.

Study Overview

• Status: Completed
• Conditions: Healthy
• Intervention / Treatment: Drug: Apetrol ES / Megace

Detailed Description

[Part 1] fasting [Part 2] fed

• Study Type: Interventional
• Enrollment (Actual): 79
• Phase: Phase 1

Participation Criteria

Eligibility Criteria

• Ages Eligible for Study: 20 years to 55 years (ADULT)
• Accepts Healthy Volunteers: Yes
• Genders Eligible for Study: Male

Description

Inclusion Criteria:

• Is a healty male between 20 and 55 years old.
• In a ± 20% than ideal body weight. [ideal body weight(kg) = height(cm)-100) x 0.9 (Broca's rule)
• Subjects who are considered to be suitable in conducting the clinical trial in serum test, hematology test, hemato-chemical test, urine test and 12-ECG result.
• Is willing and able to comply with scheduled visits, treatment plan, laboratory tests, and other study procedures.
• Agrees to use an adequate means of contraception during clinical trials
• Subject who has voluntarily decided to participate in this clinical trial and consented in writing.

Exclusion Criteria:

• Is allergic against Megestrol acetate or other drugs (Aspirin, NSAIDs, Antibiotics, etc.) or against foods, or has an clinically serious allergic history.
• Subjects who have present condition or past history of any disease involving liver, kidney, nervous system, immune system, respiratory system, or endocrine system; hematologic and oncologic disease; cardiovascular disease; or psychiatric disorder (mood disorder, obsessive-compulsive disorder, etc. that may affect ADME of investigational medicinal products.
• In the vital signs measured in sitting position at the screening visit, subjects who have hypertension desease(a systolic blood pressure of ≥ 150 mmHg or a diastolic blood pressure of ≥ 100 mmHg).
• Diabetic patients or the patients who are abnormal of impaired glucose tolerance.
• The patients who have a history of Arterial Embolism.
• The patients who have a history of adrenal insufficiency like hypotension or nausea or vertigo or asthenia or etc.
• Subjects who have a history of drug abuse or shown positive reaction to drugs that may be abused from a urine drug screening
• Subjects who took any specialized drug or an herbal medication within 2 weeks before the date of first administration or took any over the counter (OTC) drug within 1 week (however, they may be included as subjects if appropriate depending on the investigator's discretion)
• Subjects who had whole blood donation within 2 months or component blood donation within 1 month before the clinical trial.
• Subjects who have abnormal diets that may affect ADME of investigational medicinal products.
• Subjects who have been drinking extremely alcohol and caffeine (more than caffeine 5 cups/day, soju 3 cups/day, beer 3 cups/day, liquors 2 cups/day, 10 cigarettes/day) or can't refrain from drinking during the clinical trial period.
• Subjects who had administration a barbiturates within 1 month before the date of first drug administration
• Subjects who already participated in other clinical trials within 2 months before this clinical trial.
• Subjects who are considered to be unsuitable in conducting the clinical trial for other reason at the principal investigator's discretionary judgment

Study Plan

How is the study designed?

Design Details

• Primary Purpose: TREATMENT
• Allocation: RANDOMIZED
• Interventional Model: CROSSOVER
• Masking: NONE

Number of Arms

4

Arms and Interventions

Participant Group / Arm	Intervention / Treatment
Experimental: Megace : fed; Megace / Apetrol ES : comparator / test, fed	Drug: Apetrol ES / Megace; Sequences of administered drugs; Other Names: Apetrol ES(ES81) 625 mg / 5mL, Megace 800mg / 20mL
Experimental: Apetrol ES : fed; Apetrol ES / Megace : test / comparator, fed, cross-over	Drug: Apetrol ES / Megace; Sequences of administered drugs; Other Names: Apetrol ES(ES81) 625 mg / 5mL, Megace 800mg / 20mL
Experimental: Megace : fasting; Megace / Apetrol ES : comparator / test, fasting	Drug: Apetrol ES / Megace; Sequences of administered drugs; Other Names: Apetrol ES(ES81) 625 mg / 5mL, Megace 800mg / 20mL
Experimental: Apetrol ES : fasting; Apetrol ES / Megace : test / comparator, fasting, cross-over	Drug: Apetrol ES / Megace; Sequences of administered drugs; Other Names: Apetrol ES(ES81) 625 mg / 5mL, Megace 800mg / 20mL

What is the study measuring?

Primary Outcome Measures

Outcome Measure	Measure Description	Time Frame
Cmax	16 times(fasting), 15 times(fed)	Pre-dose(0h), 1, 2, 3, 4, 5, 6, (7), 8, 10, 12, 24, 48, 72, 96, 120 h
AUClast	16 times(fasting), 15 times(fed)	Pre-dose(0h), 1, 2, 3, 4, 5, 6, (7), 8, 10, 12, 24, 48, 72, 96, 120 h

Secondary Outcome Measures

Outcome Measure	Measure Description	Time Frame
AUCinf, %AUCextra	16 times(fasting), 15 times(fed)	Pre-dose(0h), 1, 2, 3, 4, 5, 6, (7), 8, 10, 12, 24, 48, 72, 96, 120 h
Tmax	16 times(fasting), 15 times(fed)	Pre-dose(0h), 1, 2, 3, 4, 5, 6, (7), 8, 10, 12, 24, 48, 72, 96, 120 h
t1/2	16 times(fasting), 15 times(fed)	Pre-dose(0h), 1, 2, 3, 4, 5, 6, (7), 8, 10, 12, 24, 48, 72, 96, 120 h

Collaborators and Investigators

• Sponsor: LG Life Sciences
• Collaborators: Severance Hospital
• Investigators: Principal Investigator: Kyungsoo Park, Ph D, MD, Yonsei University

Publications and helpful links

General Publications

• Chae DW, Son H, Guk J, Park C, Park K. Pharmacokinetics of a nanocrystal-containing megestrol acetate formulation: a single-dose, randomized, open-label, 2-part, 2-period crossover study in healthy Korean subjects. Int J Clin Pharmacol Ther. 2016 Sep;54(9):698-704. doi: 10.5414/CP202574.

Study record dates

Study Major Dates

• Study Start: April 1, 2010
• Primary Completion (Actual): June 1, 2010
• Study Completion (Actual): October 1, 2010

Study Registration Dates

• First Submitted: May 7, 2015
• First Submitted That Met QC Criteria: May 13, 2015
• First Posted (Estimate): May 18, 2015

Study Record Updates

• Last Update Posted (Estimate): May 18, 2015
• Last Update Submitted That Met QC Criteria: May 13, 2015
• Last Verified: May 1, 2015

More Information

Terms related to this study

• Keywords: Male Volunteers
• Additional Relevant MeSH Terms: Physiological Effects of Drugs; Antineoplastic Agents; Antineoplastic Agents, Hormonal; Contraceptive Agents, Hormonal; Contraceptive Agents; Reproductive Control Agents; Contraceptives, Oral; Contraceptive Agents, Female; Contraceptives, Oral, Synthetic; Contraceptives, Oral, Hormonal; Central Nervous System Stimulants; Appetite Stimulants; Megestrol; Megestrol Acetate
• Other Study ID Numbers: LG-ESCL001