To Evaluate The Relationship Between Plasma Drug Levels And Receptor Binding in Lung Using PET (Positron Emission Tomography) In Healthy Volunteers

Bristol-Myers Squibb (BMS)

Status and phase: Completed; Phase 1

Conditions: Immunology

Treatments: Drug: BMS-986020; Drug: [11C]BMT-136088

Study type: Interventional

Funder types: Industry

Identifiers

NCT02017730

IM136-106

Details and patient eligibility

About

The purpose of this study is to assess the safety and tolerability of a novel positron emission tomography (PET) tracer [11C]BMT-136088 in healthy adult subjects for measurement of availability of Lysophosphatidic Acid (LPA1) receptors in the human lung and to use this tracer to assess LPA1 receptor occupancy using [11C]BMT-136088 in the human lung following oral administration of Bristol Myers Squibb (BMS)-986020.

Full description

End point Classification: Pharmacokinetics/Pharmacodynamics

Enrollment: 20 patients

Sex: Male

Ages: 18 to 45 years old

Volunteers: Accepts Healthy Volunteers

Inclusion and exclusion criteria

For more information regarding BMS clinical trial participation, please visit www.BMSStudyConnect.com

Inclusion Criteria:

• Body weight at least 50kg (110lbs), Body Mass Index (BMI) within 19 to 32 kg/m2, inclusive
• Must be in good health as determined by medical history, physical examination, ECG, serum/urine biochemistry, hematology, and serology tests
• Negative hepatitis panel and negative human immunodeficiency virus (HIV)antibody screens

Exclusion Criteria:

• Any history or presence of clinically significant respiratory, Gastro Intestinal (GI), renal, hepatic, pancreatic, hematological, neurological (including history of seizure), cardiovascular, psychiatric (including known addictive disorders), musculoskeletal, genitourinary, immunological, or dermatological disorders, including all cancers
• Any acute or chronic condition that, in the opinion of the investigator in consultation with the BMS Medical Monitor, could jeopardize the subject's safety, tolerability, or pharmacokinetics of the BMS-986020
• Any major surgery within 4 weeks of study drug administration
• Existence of a cold, upper respiratory tract infection, or fever within 5 days prior to check-in
• Presence or history of any abnormality or illness that may affect absorption, distribution, metabolism or elimination of the study drug
• Donation of blood or plasma (exclude the screening visit) within 2 months prior to check in through end of synthesis (EOS), inclusive

Trial design

Primary purpose: Basic Science

Allocation: Non-Randomized

Interventional model: Parallel Assignment

Masking: None (Open label)

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20 participants in 4 patient groups

Part 1: [11C]BMT-136088 (Safety Study)

Experimental group

Description:

Single PET SCAN with single bolus injection of \[11C\]BMT-136088

Treatment:

Drug: [11C]BMT-136088

Part 2: [11C]BMT-136088 (Test/Retest study)

Experimental group

Description:

Single PET SCAN with Intravenous (IV) bolus plus infusion of \[11C\]BMT-136088 followed by a re-test PET scan (approximately 6 hours apart) with IV bolus plus infusion of \[11C\]BMT-136088

Treatment:

Drug: [11C]BMT-136088

Part 3: BMS-986020+[11C]BMT-136088 (Receptor Occupancy study)

Experimental group

Description:

BMS-986020 Tablets or Oral Solution of 4 dose levels from from the 6 dose levels of (50 mg, 150 mg, 300 mg, 600 mg, 1200 mg and 1500 mg) and 3 PET SCANS (Pre-Dose, Post-Dose1, Post-Dose2) with bolus plus infusion of \[11C\]BMT-136088

Treatment:

Drug: [11C]BMT-136088

Drug: BMS-986020

Part 4: [11C]BMT-136088 (Tissue Distribution study)

Experimental group

Description:

Single PET SCAN with \[11C\]BMT-136088 to evaluate additional tracer uptake sites in humans other than the lung, such as heart, kidney, liver, gallbladder, etc.

Treatment:

Drug: [11C]BMT-136088