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A Study to Evaluate the Safety and Pharmacokinetics of CNTX-6016 in Healthy Subjects

Phase 1
Completed
Conditions
Chronic Pain
Nociceptive Pain
Pain
Interventions
Registration Number
NCT04154501
Lead Sponsor
Centrexion Therapeutics
Brief Summary

A Phase 1 double-blind, placebo-controlled, randomized single ascending dose incorporating an open-label, 2-period crossover, food effect cohort.

Detailed Description

Not available

Recruitment & Eligibility

Status
COMPLETED
Sex
All
Target Recruitment
68
Inclusion Criteria
  • Is in good general health as determined by Investigator's review.
  • Has a body mass index (BMI) between 18 and 35 kg/m2.
  • Non- or ex-smoker (> 1 year) and has not used any nicotine containing products within 12 months prior to screening.
  • For females, is not currently pregnant and is either of non-childbearing potential or willing to use an adequate method of birth control.
  • For males, must agree to use barrier contraception and not to donate sperm.

Key

Exclusion Criteria
  • History of or active cardiac disease, including congestive heart failure, angina, or any arrhythmia.
  • Has any history or currently active type of cancer except excised or cured basal cell carcinoma.
  • Has a gastrointestinal disorder that could interfere with the absorption of orally administered drugs.
  • Has asthma or other severe respiratory disease (e.g., chronic obstructive pulmonary disease) requiring daily prescription medicine.
  • Currently has kidney, neurologic, metabolic, or liver disease, or other organ system disease.
  • Has a history, current evidence, or is being treated for depression, suicidal ideation, suicide attempt, or any other current psychiatric condition requiring active treatment.
  • Has an immunological disorder such as, but not limited to, human immunodeficiency virus (HIV), acquired, or congenital immune deficiency syndrome; autoimmune diseases, such as, but not limited to, rheumatoid arthritis, systemic lupus erythematosus, seronegative spondyloarthropathies or vasculitis, or any infection.
  • Has positive screening test for hepatitis B virus (HBV) or hepatitis C virus (HCV).
  • Is pregnant, lactating, or planning a pregnancy during the study.
  • Has used any prescribed medication within 30 days prior to the first admission or has plans to use any prescribed medication during the study (with the exception of hormonal contraceptives).
  • Positive urine screen for alcohol, cotinine, THC and/or drugs of abuse.
  • Ingestion of food or beverages containing grapefruit and/or grapefruit juice and/or pomelos during the 7 days prior to dosing and/or during the study period.

Study & Design

Study Type
INTERVENTIONAL
Study Design
CROSSOVER
Arm && Interventions
GroupInterventionDescription
Cohort 4 DrugCNTX-6016300 mg Oral Capsule
Cohort 1 DrugCNTX-601625 mg Oral Capsule
Cohort 2 DrugCNTX-601650 mg Oral Capsule
Cohort 6 DrugCNTX-6016600 mg Oral Capsule
Cohort 7 DrugCNTX-6016800 mg Oral Capsule
Cohort 9 DrugCNTX-60161000 mg Oral Capsule
Cohort 5 DrugCNTX-6016450 mg Oral Capsule
Cohort 3 DrugCNTX-6016100 mg Oral Capsule
Cohort 8 FastedCNTX-6016Participant will take 300 mg Oral Capsule in a fasting state, and then fed state.
Cohort 8 FedCNTX-6016Participant will take 300 mg Oral Capsule in a fed state, and then fasting state.
Primary Outcome Measures
NameTimeMethod
Safety of single doses of CNTX-6016 - TEAEsUp to 80 days

Information regarding treatment emergent adverse events was collected during each dose cohort.

Dose Proportionality of a single doses of CNTX-6016 in healthy subjects40 days

Dose Proportionality of a single doses of CNTX-6016 in healthy subjects.

CNTX-6016 Pharmacokinetics - TmaxUp to 40 days

Systemic exposure to CNTX-6016 measured by Tmax.

CNTX-6016 Pharmacokinetics - t1/2Up to 40 days

Systemic exposure to CNTX-6016 measured by t1/2.

CNTX-6016 Pharmacokinetics - AUC 0-infUp to 40 days

Systemic exposure to CNTX-6016 measured by AUC 0-inf.

CNTX-6016 Pharmacokinetics - AUC 0-t/infUp to 40 days

Systemic exposure to CNTX-6016 measured by AUC 0-t/inf.

CNTX-6016 Pharmacokinetics - CL/FUp to 40 days

Systemic exposure to CNTX-6016 measured by CL/F.

Effect of Gender on CNTX-6016 Pharmacokinetics - TmaxUp to 80 days

Effect of Gender on the systemic exposure to CNTX-6016 measured by tmax.

Effect of Gender on CNTX-6016 Pharmacokinetics - t1/2Up to 80 days

Effect of Gender on the systemic exposure to CNTX-6016 measured by t1/2

Effect of Gender on CNTX-6016 Pharmacokinetics - AUCUp to 80 days

Effect of Gender on the systemic exposure to CNTX-6016 measured by AUC.

Effect of Fasted or Fed State on CNTX-6016 Pharmacokinetics - CmaxUp to 40 days

Systemic exposure to CNTX-6016 in fasted or fed state as measured by Cmax

Effect of Fasted or Fed State on CNTX-6016 Pharmacokinetics - TmaxUp to 40 days

Systemic exposure to CNTX-6016 in fasted or fed state as measured by Tmax

Effect of Fasted or Fed State on CNTX-6016 Pharmacokinetics - t1/2Up to 40 days

Systemic exposure to CNTX-6016 in fasted or fed state as measured by t1/2

Effect of Fasted or Fed State on CNTX-6016 Pharmacokinetics - AUCUp to 40 days

Systemic exposure to CNTX-6016 in fasted or fed state as measured by AUC

Urinary ExcretionUp to 6 days

Urine was collected over a 3-day period (0-72 hrs) in Cohort 8 and analyzed for concentrations of CNTX-6016 in subjects in both the fasted and fed states using Liquid Chromatography Mass Spectrometry.

CNTX-6016 Pharmacokinetics - CmaxUp to 40 days

Systemic exposure to CNTX-6016 measured by Cmax.

CNTX-6016 Pharmacokinetics - AUC 0-tUp to 40 days

Systemic exposure to CNTX-6016 measured by AUC 0-t.

CNTX-6016 Pharmacokinetics - Vz/FUp to 40 days

Systemic exposure to CNTX-6016 measured by Vz/F.

Effect of Gender on CNTX-6016 Pharmacokinetics - CmaxUp to 80 days

Effect of Gender on the systemic exposure to CNTX-6016 measured by Cmax.

Secondary Outcome Measures
NameTimeMethod
Plasma and Urine Metabolite Mining5 days

Urine was collected over a 3-day period (0-72hrs) in Cohort 9 (1000mg) and analyzed for concentrations of parent and metabolites of CNTX-6016 using Liquid Chromatography Mass Spectrometry.

Trial Locations

Locations (1)

Altasciences Clinical Research

🇺🇸

Overland Park, Kansas, United States

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