None listed
Conditions
Brief summary
This is a Phase 1 study. This is a randomized, double-blind, placebo-controlled, dose-escalation study to evaluate the safety, tolerability, pharmacokinetics and pharmacodynamics of EQ121 following oral single (Part 1) and multiple (Part 2) ascending dose administration in healthy subjects. Approximately 104 adult healthy volunteers.
Interventions
EQ121 capsule is an oral solid dosage form manufactured at strengths of 1 mg and 12 mg.
Each EQ121 capsule contains EQ121 drug substance; mannitol, pregelatinized starch and microcrystalline cellulose as diluents; croscarmellose sodium as disintegrant; colloidal silicon dioxide as glidant; and magnesium stearate as lubricant.
Part 1: Participants in Australia will receive a single dose of orally administered EQ121 or matching placebo in each cohort as follows: Cohort 1: 3 mg; Cohort 2: 6 mg; Coh
EQ121 capsule is an oral solid dosage form manufactured at strengths of 1 mg and 12 mg. Each EQ121 capsule contains EQ121 drug substance; mannitol, pregelatinized starch and microcrystalline cellulose as diluents; croscarmellose sodium as disintegrant; colloidal silicon dioxide as glidant; and magnesium stearate as lubricant. Part 1: Participants in Australia will receive a single dose of orally administered EQ121 or matching placebo in each cohort as follows: Cohort 1: 3 mg; Cohort 2: 6 mg; Cohort 3: 12 mg; Cohort 4: 24 mg; Cohort 5: 36 mg; Cohort 6: 60 mg; Cohort 7: 96 mg; and Cohort 8: 120 mg. Part 2: Participants in Australia will receive orally administered EQ121 or matching placebo twice daily (twelve hours apart) for 14 days in each cohort as follows: Cohort 1: 12 mg; Cohort 2: 24 mg; Cohort 3: 36 mg; Cohort 4: 48 mg participants will be monitored via clinical site staff recording and reporting all number of pills taken while confined. Participants will ingest investigational drug or placebo on an empty stomach and will have a total of three overnight stays (admission on Day -1 until 48 hours post-dose on Day 3) in Part 1. Participants should be instructed to come to the clinic with an empty stomach after overnight fasting (minimum 8 hours) and to avoid eating for 4 hour after dosing. For participants in the Food Effect study, at their Day 8 visit: following an overnight fast of at least 8 hours, participants will complete a test meal in 30 minutes or less. Study drug will be administered with 240 mL of water. No food will be allowed for at least 4 hours post-dose. Water is allowed as desired except for 1 hour before and 2 hours after study drug administration. The test meal will be a high-fat (approximately 50 percent of total caloric content of the meal) and high-calorie (approximately 800 to 1000 calories) breakfast. There is no requirement for fasting at the second daily dose during BID [Twice-daily (12 hours apart] dosing. Dosing commences 30minutes after start of high fat breakfast. Adherence will be monitored via clinical site staff recording and reporting all number of pills taken while confined. Food effect dose was chosen based upon the highest strength of the capsule formulation. For participants in Cohort 3 (12 mg) of Part 1, after the completion of Cohort 3 and following a 7-day washout period, the same 8 participants will participate in the Food Effect study. At Day 8 visit. Food effect is only being conducted in the SAD cohort 3 and not in any other cohort.
Sponsors
EQRx, Inc
Study design
Allocation
Randomised controlled trial
Intervention model
Parallel
Primary purpose
Treatment
Masking
Blinded (masking used) (Subject, Caregiver)
Eligibility
Sex/Gender
All
Age
18 Years to 65 Years
Healthy volunteers
Yes
Inclusion criteria
1. Are capable of giving informed consent and complying with study procedures; 2. Healthy male or female participants, between the ages of 18 and 65 years, inclusive; 3. BMI of 18.0 to 32.0 kg per m2 inclusive and body weight not less than 50 kg; 4. Female participants must not be currently breast-feeding, and must meet one of the following criteria: a. Surgically sterile for at least 3 months prior to Screening by one of the following means: - Bilateral tubal ligation - Bilateral salpingectomy (with or without oophorectomy) - Surgical hysterectomy - Bilateral oophorectomy (with or without hysterectomy) b. Postmenopausal, defined as the following: - Last menstrual period greater than 12 months prior to Screening without an alternative medical cause, AND - Postmenopausal status confirmed by serum FSH concentration at Screening greater than 40 mIU per mL c. Female subjects of childbearing potential: • must not have a positive serum pregnancy test at Screening and must have a negative urine pregnancy test on admission • must use at least one of the following protocol-specified highly effective methods of birth control, AND must agree to use barrier contraception (male condom) during heterosexual intercourse, from the time of Screening until at least 30 days after the last dose of study drug. - Partner vasectomy (at least 6 months prior to Screening; vasectomized partner should be the sole partner of the female subject) - Combined (estrogen and progestogen containing) hormonal contraception (oral, intravaginal, transdermal, injectable) - Progestogen-only hormonal contraception (oral, injectable, implantable) - Implantable device (implantable rod or intrauterine device) 5. Male participants must agree to utilize a highly effective method of contraception (condom) during heterosexual intercourse from clinic admission until 90 days following the last dose of study drug and must refrain from donating sperm for this same period. Vasectomized males do not need to use additional forms of contraception providing that the procedure was performed at least 12 weeks prior to Screening and an absence of sperm in the ejaculate has been documented. Total sexual abstinence may be considered acceptable at the discretion of the Investigator; 6. Considered healthy by the Investigator, based on participant’s reported medical history, full physical examination, clinical laboratory tests, 12-lead ECG, and vital signs
Exclusion criteria
1. Inability to attend all the study visits or comply with study procedures; 2. Evidence or clinically significant history of gastrointestinal, cardiovascular, musculoskeletal, endocrine, hematologic, psychiatric, renal, hepatic, bronchopulmonary, neurologic, immunologic, lipid metabolism disorders, or drug hypersensitivity as determined by the Investigator; 3. Hospital admission or major surgery within 3 months prior to Screening; 4. A history of drug abuse, or a positive test at Screening or at Admission for drugs of abuse; 5. A history of alcohol abuse according to medical history within 6 months prior to Screening (drinking 14 units of alcohol per week: 1 unit equals to 360 mL of beer, or 37 mL of spirits, or 120 mL of wine) at Screening or upon admission to the clinical site; 6. Positive screen for drugs of abuse or alcohol at Screening or at Admission; 7. Taken any prescription medications within 14 days or 5 half-lives (whichever is longer), or any injectable prescription medications within 30 days or 10 half-lives (whichever is longer), of the first dose of study drug; 8. Taken an investigational drug within 3 months or 5 half-live, whichever is longer from the Screening date; 9. Any liver function panel analyte (LFT) value greater than 1.5 X upper limits of normal reference range (ULN) which includes AST, ALT, Bilirubin, Alkaline Phosphatase, and GGT at Screening or at Admission; 10. Any White Blood Cell (WBC), ANC, hemoglobin, or platelet count less than the lower limit of normal at Screening or at Admission that is clinically significant in the opinion of the Investigator; 11. Serum creatinine greater than upper limit of normal at Screening or Admission; 12. Any condition or finding that in the opinion of the Principal Investigator or designee would put the participant or study conduct at risk if the participant were to participate in the study.
Outcome results
None listed