A Randomized, Double Blind, Single-Ascending Dose Study to Investigate the Safety, Tolerability, and Pharmacokinetic Profile of EIK1005 in Healthy Participants.
Healthy Participant Study to Assess Safety, Tolerability and Pharmacokinetic Profile of EIK1005, a Werner helicase inhibitor.
EIKON Therapeutics, Inc.
48 participants
Apr 22, 2025
Interventional
Conditions
Summary
This study is to investigate the safety, tolerability, and PK of EIK1005 in healthy participants. EIK1005 is a potent and selective inhibitor of WRN, which has been identified as a synthetic lethal target in MSI-H cells. MSI-H is a marker of cancer cells with defective mismatch repair. WRN inhibition (WRNi) acts on MSI-H cells, and thus WRNi is not expected to have an effect on healthy tissue. EIK1005 is noncytotoxic and is been considered has as potential targeted therapy in patients with MSI-H or dMMR solid tumors.
Eligibility
Inclusion Criteria6
- Woman of non-childbearing potential (WONCBP) or a man who is at least 18 years at the time of signing the ICF.
- Healthy as determined by the Principal Investigator with no clinically significant abnormalities and no active clinically significant condition or disease.
- Total body mass index (BMI) between 18 kg/m2 and 32 kg/m2 (inclusive).
- Adequate organ and marrow function.
- Male participants who are sexually active with women of childbearing potential (WOCBP) must agree to use an approved and highly effective contraceptive method throughout the study Visit 1 to 90 days after the last dose of study drug. Male participants cannot donate sperm for 90 days after the last dose of study drug.
- Willing and able to provide written, informed consent for the study.
Exclusion Criteria12
- Participant has a history or presence of clinically relevant medical condition(s) or disease(s).
- Participant has a history or presence of any malignancy in the last 5 years except surgically cured skin cancers.
- Participant is known to have Lynch syndrome, Werner Syndrome (progeria), or has a first degree relative with Werner Syndrome (progeria).
- Participant has a history of relevant drug hypersensitivity, to the active drug substance and/or formulation ingredients.
- Participant uses any prescribed medication or over-the-counter drug within 7 Days or 5 times the half-life of the respective drug, whichever is longer prior to the first administration of EIK1005. The Principal Investigator may determine exceptions in consultation with the Sponsor.
- There is a mean resting QTcF > 450 ms in men and QTcF > 460 ms in women obtained from triplicate ECGs.
- Participant who has been diagnosed with hepatitis B virus (HBV) infection or has an active hepatitis C virus (HCV) infection.
- Participant with positive human immunodeficiency virus (HIV) serology or known HIV diagnosis.
- Participant has received a live-virus vaccination within 90 days of the start of study drug.
- Participant had major surgery (< 3 months prior to receiving EIK1005 or placebo).
- Participant has donated or lost >= to 450 mL of blood within 90 days prior to Screening.
- Participant is unable or unwilling to swallow pills.
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Interventions
EIK1005 is a potent and selective inhibitor of the Werner helicase (WRN), which has been identified as a synthetic lethal target in microsatellite instability high (MSI-H) cells. MSI-H is a marker of cancer cells with defective mismatch repair .WRN inhibition (WRNi) acts on MSI-H cells, and thus WRNi is not expected to have an effect on healthy tissue. EIK1005 is noncytotoxic and is being considered as a potential targeted therapy in patients with MSI-H or dMMR solid tumors. EIK1005 or placebo will be administered orally. For participants who are enrolled in Period 1 (fasted conditions) or Period 2 (fed conditions), they will receive one dose of EIK1005 or placebo; for participants who are enrolled in both Period 1 and Period 2, they will receive two doses of EIK1005 or placebo. EIK1005 will be administered via oral tablet. Six dose levels will be assessed in Period 1 of the study: 50 mg, 100 mg, 200 mg, 400 mg, 800 mg and 1000 mg. Dose for Period 2 will be determine after evaluation of Period 1 data. The study drug administration will be performed in-house under the supervision of the study team to ensure 100% adherence to the intervention. For the fasted condition, participants will fast at least 10 hours prior to receiving a single dose of EIK1005. For the fed condition, participants will receive a meal in which greater than or equal to 50% of calories are from fat with total calories ranging from 800 to 1000. The meal will accommodate dietary needs including but not limited to vegan, vegetarian, Halal, or Kosher. Participants will then remain in the clinic for 3 days and will return on Day 8 for a follow-up visit. Medical assessments including blood draws will be performed during this time. If a Period 1 participant from the selected dose cohort is not eligible or is unwilling to participant Period 2 (the food effect cohort), a new participant will be enrolled as a replacement and receive the same treatment assignment as the replacing participant. Therefore, there might be a participant or some participants who will be enrolled only into Period 2.
Locations(1)
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ACTRN12625000334404