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Single and Multiple-Ascending Dose Study of CRN00808 in Healthy Volunteers

Phase 1
Completed
Conditions
Healthy Volunteers
Interventions
Drug: CRN00808
Drug: Placebo Oral Solution
Drug: Placebo oral capsule
Drug: Midazolam oral solution
Registration Number
NCT03276858
Lead Sponsor
Crinetics Pharmaceuticals Inc.
Brief Summary

This single-center study will be conducted in 3 phases: a single-ascending dose phase (up to 8 cohorts, 8 subjects/cohort), a multiple-dose phase (up to 5 cohorts, 9 subjects/cohort), and a midazolam drug-drug interaction phase (one cohort of 8 subjects).

Detailed Description

The single-dose phase initiates with ascending doses of an oral solution followed by a 3-way crossover food effect and bioavailability (capsule formulation) cohort. Serum IGF-1 levels and GHRH-analog stimulated GH levels will be assessed as pharmacodynamics measures.

The first multiple-dose (7 days dosing) cohort will be initiated after the PK and safety data are available from the single-dose phase. Subsequent multiple-dose cohorts will have 10 days of dosing. Serum IGF-1 level and GH levels will be assessed as pharmacodynamics measures.

The last cohort in the study is midazolam drug-drug interaction study. The dose will be selected based on review of all pharmacokinetic and safety data for the single-dose and multiple-dose cohorts completed. On Day 1, 8 subjects will receive a single oral 2 mg dose of midazolam. Starting on Day 3 through Day 8, subjects will receive daily doses of CRN00808. On Day 9, subjects will be administered CRN00808 and 2 mg midazolam together.

Recruitment & Eligibility

Status
COMPLETED
Sex
All
Target Recruitment
99
Inclusion Criteria
  • BMI 18 to 30 kg/m2
  • Females postmenopausal or surgically sterile
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Exclusion Criteria
  • Any uncontrolled or active major systemic disease including, but not limited to: acromegaly (with or without pituitary surgery or radiation therapy), cardiac, pulmonary, gastrointestinal, metabolic, urogenital, neurological, immunological, psychiatric, or neoplastic disorder with metastatic potential
  • History or presence of malignancy within the past 5 years. Subjects who have been successfully treated (for 3 months or longer) with no recurrence of basal or squamous cell carcinoma of the skin or carcinoma in-situ of the cervix may be enrolled.
  • Use of any investigational drug within the past 60 days or 5 half-lives, whichever is longer
  • Have a medically significant abnormality observed during screening or the admission physical examination or in any other baseline measurements
  • Use of any prior medication without approval of the investigator within 14 days prior to admission
  • Tested positive at screening for HIV, hepatitis B surface antigen (HBsAg) or hepatitis C antibody (HCV-Ab) or has a history of a positive result
  • History of alcohol or substance abuse in the past 6 months
  • Any condition that in the opinion of the investigator would jeopardize the subject's appropriate participation in this Phase 1 study
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Study & Design

Study Type
INTERVENTIONAL
Study Design
PARALLEL
Arm && Interventions
GroupInterventionDescription
CRN00808 Oral SolutionCRN00808CRN00808 oral solution, single-dose
CRN00808 Oral CapsuleCRN00808CRN00808 oral capsule, single-dose and multiple-doses
Placebo Oral SolutionPlacebo Oral SolutionPlacebo oral solution, single-dose
Placebo Oral CapsulePlacebo oral capsulePlacebo oral capsule, single-dose and multiple doses
Midazolam Oral SolutionCRN00808Midazolam oral solution, two single-doses as part of the drug-drug interaction arm of the study
Midazolam Oral SolutionMidazolam oral solutionMidazolam oral solution, two single-doses as part of the drug-drug interaction arm of the study
Primary Outcome Measures
NameTimeMethod
Incidence of Treatment-Emergent Adverse Events [Safety and Tolerability] of CRN00808 single ascending doses using clinical assessments, telemetry, and Holter monitoring and subject self-reportingDay 1 through Day 10

ECG, clinical laboratory parameters, vital signs, physical examinations, telemetry, Holter monitoring

Incidence of Treatment-Emergent Adverse Events [Safety and Tolerability] of CRN00808 multiple ascending doses using clinical assessments and subject self-reportingDay 1 through Day 21

ECG, clinical laboratory parameters, vital signs, physical examinations

Secondary Outcome Measures
NameTimeMethod
AUC of CRN00808 single ascending dosesDay 1 through Day 7

plasma AUC

Cmax of CRN00808 multiple ascending dosesDay 1 through Day 20

plasma Cmax

Pharmacodynamics of CRN00808 in single ascending dose cohorts assessed by GHRH analog stimulated GH levelsDay -1 and Day 1

Suppression of serum GH induced by a GH secretagogue

Effect of CRN00808 on pharmacokinetics of midazolamDay 1 through Day 10

midazolam plasma AUC

Effect of CRN00808 on Cmax of midazolamDay 1 through Day 10

midazolam plasma Cmax

Tmax of CRN00808 multiple ascending dosesDay 1 through Day 20

plasma Tmax

Tmax of CRN00808 single ascending dosesDay 1 through Day 7

plasma Tmax

Relative bioavailability of capsule formulationDay 1 to Day 7

single-dose crossover arm only

Effect of food on Cmax of CRN00808Day 1 to Day 7

plasma Cmax compared with and without food in single dose arm

Pharmacodynamics of CRN00808 in multiple ascending dose cohorts assessed by serum IGF-1 and GHDay -1 to Day 21

serum IGF-1 and GH

AUC of CRN00808 multiple ascending dosesDay 1 through Day 20

plasma AUC

t1/2 of CRN00808 multiple ascending dosesDay 1 through Day 20

plasma t1/2

Cmax of CRN00808 single ascending dosesDay 1 through Day 7

plasma Cmax

t1/2 of CRN00808 single ascending dosesDay 1 through Day 7

plasma t1/2

Effect of CRN00808 on t1/2 of midazolamDay 1 through Day 10

midazolam plasma t 1/2

Effect of CRN00808 on Tmax of midazolamDay 1 through Day 10

midazolam plasma Tmax

Effect of food on AUC of CRN00808Day 1 to Day 7

Plasma AUC compared with and without food in single dose arm

Trial Locations

Locations (1)

Nucleus Network

🇦🇺

Melbourne, Victoria, Australia

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