A Phase 1 Study of Ertugliflozin in Healthy Male Participants (MK-8835-020)

Merck Sharp & Dohme (MSD)

Status and phase: Completed; Phase 1

Conditions: Type 2 Diabetes Mellitus

Treatments: Drug: 14^C-labeled ertugliflozin for IV use; Drug: Unlabeled ertugliflozin for oral use; Drug: 14^C-labeled ertugliflozin for oral use

Study type: Interventional

Funder types: Industry

Identifiers

NCT02411929

B1521043 (Other Identifier)

8835-020

Details and patient eligibility

About

This study will evaluate the absolute oral bioavailability (F) and fraction absorbed (Fa) of ertugliflozin following oral administration of unlabeled ertugliflozin (MK-8835) and intravenous (IV) and oral administration of 14^C-labeled ertugliflozin in healthy male participants.

Enrollment: 8 patients

Sex: Male

Ages: 18 to 65 years old

Volunteers: Accepts Healthy Volunteers

Inclusion criteria

• Healthy male subjects between the ages of 18 and 65 years.
• Body Mass Index (BMI) of 17.5 to 30.5 kg/m^2; and a total body weight >50 kg (110 lbs.)

Exclusion criteria

• Evidence or history of clinically significant hematological, renal, endocrine, pulmonary, gastrointestinal, cardiovascular, hepatic, psychiatric, neurologic, or allergic disease (including drug allergies, but excluding untreated, asymptomatic, seasonal allergies).
• Any clinically significant malabsorption condition (eg, gastrectomy, bowel resection).
• A positive urine drug screen for drugs of abuse or recreational drugs.
• Positive hepatitis B surface antigen (HBsAg), hepatitis C virus antibody (HCV Ab) or human immunodeficiency virus (HIV) results.
• History of abuse of alcohol or binge drinking and/or any other illicit drug use or dependence within 6 months of Screening.
• Current smokers and those who have smoked any substance within the last 12 months.
• Treatment with an investigational drug within 1 month preceding the first dose of study medication.
• Have participated in any clinical study with exposure to 14^C in the last 12 months.
• Any radiation exposure, including that which is projected to result from the present study, excluding background radiation but including diagnostic x-rays and other medical exposures. No occupationally exposed worker, as defined in the Ionising Radiation Regulation 1999, shall participate in the study.
• Use of prescription or nonprescription drugs (including vitamins and dietary supplements) within 7 days prior to the first dose of study medication.
• Use of herbal supplements within 28 days prior to the first dose of study medication.
• Blood donation (excluding plasma donations) of approximately 1 pint (500 mL) or more within 56 days prior to dosing.
• Participants who have previously participated in a clinical trial for ertugliflozin.
• Serious adverse reaction or serious hypersensitivity to any drug or the formulation excipients.

Trial design

Primary purpose: Treatment

Allocation: N/A

Interventional model: Single Group Assignment

Masking: None (Open label)

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8 participants in 1 patient group

Ertugliflozin

Experimental group

Description:

Period 1: Oral dose of 15 mg unlabeled ertugliflozin + intravenous (IV) dose of 100 µg 14\^C-labeled ertugliflozin containing approximately 400 nCi 14\^C. The 14\^C IV dose will be administered as an infusion over approximately 5 minutes starting at 55 minutes after the unlabeled oral dose. → Period 2: Oral dose 15 mg unlabeled ertugliflozin + oral dose of 100 µg 14\^C-labeled ertugliflozin containing approximately 400 nCi 14\^C. Both the unlabeled and 14\^C-ertugliflozin will be administered at the same time (no more than 5 minutes apart). Dosing in Periods 1 and 2 will be separated by a washout of at least 11 days.

Treatment:

Drug: 14^C-labeled ertugliflozin for oral use

Drug: 14^C-labeled ertugliflozin for IV use

Drug: Unlabeled ertugliflozin for oral use