A Dose Calibration Study Comparing IkT-001Pro to Imatinib Mesylate 400mg

NCT05623774 | Completed Phase 1 DMC FDA Drug

• 1 other identifier: IkT-001Pro-501
• Study Type: interventional
• Target: 64
• Locations: 1 country
• Sites: 1

Brief Summary

This study investigates the safety, tolerability and dose equivalence of drug IkT-001Pro in healthy volunteers (18 to 55 years old) in comparison to imatinib mesylate. This study is designed in 3 parts. Part A consists of 3 cohorts. In cohort 1 healthy participants will take a single, oral dose of 400mg IkT-001Pro then will be followed by a single dose of 400mg Imatinib mesylate after a 7-day washout. Cohort 2 and 3 will follow the same structure as cohort 1 with a different Ikt-001Pro dose. Part B will be chosen using Part A data by statistical procedures. Part B will enroll 32 subjects to demonstrate the bioequivalence of IkT-001Pro (the 'Test') to 400 mg imatinib delivered as imatinib mesylase (the 'Reference'). Part C (Dose Equivalence at 600 mg): Part C will enroll up to eight (8) subjects to demonstrate bioequivalence of imatinib delivered as 800 mg IkT-001Pro (the 'Test') to 600 mg imatinib delivered as imatinib mesylate ('the Reference')

Conditions

CML

Outcome Measures

Primary Outcomes (5)

• Exposure of imatinib after administration of IkT-001Pro and imatinib mesylate, as measured by area under the concentration-time curve for imatinib from time zero to last measurable concentration (AUC(0-last))

  Area under the concentration-time curve for imatinib from time zero to last measurable concentration (AUC0-last)

  Day 1 through day 12

• Exposure of imatinib after administration of IkT-001Pro and imatinib mesylate, as measured by area under the concentration-time curve for imatinib from time zero to infinity (AUC0-inf)

  Area under the concentration-time curve for imatinib from time zero to infinity (AUC(0-inf))

  Day 1 through day 12

• Exposure of imatinib after administration of IkT-001Pro and imatinib mesylate, as measured by the maximum plasma concentration (Cmax) of imatinib

  The maximum plasma concentration (Cmax) of imatinib

  Day 1 through day 12

• Safety: Incidence and temporal profile of treatment-emergent adverse events (TEAEs) evaluated by type/nature, severity/intensity, seriousness, and relationship to study intervention

  Incidence and temporal profile of treatment-emergent adverse events (TEAEs)

  Day 1 through day 12

• Safety: Proportion of those in each dosing cohort who discontinued the assigned regimen

  Proportion of those in each dosing cohort who discontinued the assigned regimen

  Day 1 through day 12

Secondary Outcomes (6)

• Exposure of imatinib after administration of IkT-001Pro and imatinib mesylate, as measured by imatinib pharmacokinetic parameters for terminal rate constant

  Day 1 through day 12

• Exposure of imatinib after administration of IkT-001Pro and imatinib mesylate, as measured by imatinib pharmacokinetic parameters for terminal half-life

  Day 1 through day 12

• Exposure of imatinib after administration of IkT-001Pro and imatinib mesylate, as measured by imatinib pharmacokinetic parameters for time to maximum concentration

  Day 1 through day 12

• Exposure of imatinib after administration of IkT-001Pro and imatinib mesylate, as measured by imatinib pharmacokinetic parameters for dose normalized maximum concentration

  Day 1 through day 12

• Exposure of imatinib after administration of IkT-001Pro and imatinib mesylate, as measured by imatinib pharmacokinetic parameters for dose normalized area under the time concentration curve to last time point

  Day 1 through day 12

Study Arms (3)

Dose Calibration

ACTIVE COMPARATOR

In Part A, cohorts will consist of 8 subjects who will receive a single dose of Ikt-001Pro and then cross over to a single does of imatinib following a 7 day washout.

Drug: Imatinib Mesylate; Drug: IkT-001Pro

Dose Equivalance

ACTIVE COMPARATOR

In Part B, up to 16 subjects will receive IkT001-Pro and up to 16 subjects will receive 400mg of imatinib mesylate. After a 7 day washout period the subjects will switch to receive the drug they did not previously receive.

Drug: Imatinib Mesylate; Drug: IkT-001Pro

Dose Equivalence at 600 mg):

ACTIVE COMPARATOR

In Part C, up to eight (8) subjects will be administered a single dose of 800 mg IkT-001Pro. After a 7-day washout period, the subjects will switch to 600 mg imatinib.

Drug: Imatinib Mesylate; Drug: IkT-001Pro

Interventions

Imatinib Mesylate DRUG

400mg tablet

Dose Calibration; Dose Equivalance; Dose Equivalence at 600 mg):

IkT-001Pro DRUG

100mg or 400mg tablet

Dose Calibration; Dose Equivalance; Dose Equivalence at 600 mg):

Eligibility Criteria

• Age: 18 Years - 55 Years
• Sex: all
• Healthy Volunteers: Yes
• Age Groups: Adult (18-64)

You may qualify if:

• Subject must have all questions about the study answered and must have signed the informed consent document before any study-specific procedures are performed.
• Healthy ambulatory male and female subjects \> 18 to \< 55 years of age at the Screening visit, with no history or evidence of clinically relevant medical disorders as determined by the Investigator in consultation with the Sponsor.
• Bodyweight \> 50 kg and body mass index (BMI) \> 18.0 and \< 32.0 kg/m2 at the screening visit.
• Physical examination, clinical laboratory values, vital signs, and electrocardiogram (ECG) data. Vital signs and clinical laboratory values must be within the normal range and or deemed not clinically significant by the PI and ECG tracings must be normal at baseline and/or deemed not clinically significant by the PI.
• Female subjects must be postmenopausal, permanently sterile (bilateral tubal occlusion), or of childbearing potential with a negative pregnancy test, non-breastfeeding, and using two highly effective methods of birth control prior to screening and through completion of the last follow-up visit. If a subject discontinues early after receiving a dose of study drug, she must continue this method of birth control for at least 7 days following the last dose of the study drug. Highly effective methods of birth control are defined as follows: hormonal (ie, established use of oral, implantable, injectable, or transdermal hormonal methods of contraception); placement of an intrauterine device; placement of an intrauterine system; and mechanical /barrier method of contraception (ie, condom or occlusive cap \[diaphragm or cervical/vault cap\] in conjunction with spermicide \[foam, gel, film, cream or suppository\]).
• Male subjects must agree to practice an acceptable method of highly effective birth control from the Screening visit, while on study and for 7 days after receiving the last dose of study drug. Highly effective methods of birth control include sexual abstinence; vasectomy; or a condom with spermicide (men) in combination with their partner's highly effective method.
• Males must be willing to abstain from sperm donation from the screening visit, while on study and through 30 days after receiving the last dose of study drug.

You may not qualify if:

• Any subject with previous exposure to imatinib or known hypersensitivity to imatinib.
• Clinically significant abnormal values for hematology, clinical chemistry or urinalysis at the screening and admission visits. Abnormalities considered to be non-clinically significant by the Investigator are acceptable.
• Clinically significant abnormal renal function defined as a creatinine clearance rate \< 90 mL/min
• Significant history (within six months prior to receiving the study drug) and/or presence of hepatic, renal, cardiovascular, pulmonary, gastrointestinal, endocrinological, hematological, dermatological, psychiatric, neurological, immunologic, ophthalmologic, metabolic, fluid retention and edema, bleeding disorders including hemorrhage or oncological disease.
• Any subject with a history, presence and/or current evidence of serologic positive result for hepatitis B surface antigen, hepatitis C antibodies, or HIV antibodies 1 or 2.
• Recent history (within previous six months prior to screening) of alcohol or drug abuse (as judged by the investigator), or has consumed \> 2 alcohol drinks/day during the last three months prior to screening (one glass is approximately equivalent to: beer \[284 mL\], wine \[125 mL/4 ounces\], or distilled spirits \[25 mL/1 ounce\]). Subjects that consume three glasses of alcoholic beverages per day but less than 14 glasses per week may be enrolled at the discretion of the Investigator. Positive screens for alcohol or controlled substances at the screening or admission visits will disqualify a subject from study participation.
• Any subject who currently uses or has regularly used tobacco or tobacco-containing products (cigarettes, pipes, etc.) for at least 30 days prior to screening or positive urine cotinine screen (\>300 ng/mL) at the screening or admission visits.
• Any subject who has received treatment with an investigational drug during the 30 days prior to screening. Exposure to an investigational medical device within 30 days of screening.
• Use of agents known to affect drug metabolism: use of any known CYP3A4 inducers and/or inhibitors or consumed grapefruit juice, grapefruit, Seville oranges or St John's Wort or products containing these within 14 days prior to first administration of study drug. Strong inducers of CYP3A4 include dexamethasone, phenytoin, carbamazepine, rifampin, rifabutin, rifampicin and phenobarbital. Strong inhibitors of CYP3A4 include ketoconazole, itroconazole, clarythromycin, atazanavir, indinavir, nefazodone, nelfinavir, ritonavir, saquinavir, telithromycin and voriconazole.
• Investigative site personnel or their immediate families (spouse, parent, child or sibling whether biological or legally adopted).
• Any subject unwilling or unable to comply with study procedures.
• Pregnant or nursing women.

Sponsors & Collaborators

• Inhibikase Therapeutics: lead

Study Sites (1)

Celerion

Tempe, Arizona, 85283, United States

Location

MeSH Terms

Interventions

Imatinib Mesylate

Intervention Hierarchy (Ancestors)

Benzamides; Amides; Organic Chemicals; Benzoates; Acids, Carbocyclic; Carboxylic Acids; Benzene Derivatives; Hydrocarbons, Aromatic; Hydrocarbons, Cyclic; Hydrocarbons; Piperazines; Heterocyclic Compounds, 1-Ring; Heterocyclic Compounds; Pyrimidines

Study Officials

• Michelle Valentine, DO

  Celerion

  PRINCIPAL INVESTIGATOR

Study Design

• Study Type: interventional
• Phase: phase 1
• Allocation: NON RANDOMIZED
• Masking: NONE
• Purpose: TREATMENT
• Intervention Model: CROSSOVER
• Sponsor Type: INDUSTRY
• Responsible Party: SPONSOR

Model Details: This is a crossover design dose calibration study in healthy volunteers to identify a dose of IkT-001Pro film-coated tablets that would be equivalent to imatinib free base 400 mg film-coated tablets containing imatinib mesylate

Study Record Dates

• First Submitted: November 9, 2022
• First Posted: November 21, 2022
• Study Start: December 16, 2022
• Primary Completion: June 30, 2024
• Study Completion: December 30, 2024
• Last Updated: November 6, 2025

Record last verified: 2025-11

Data Sharing

• IPD Sharing: Will not share

Locations

US (1)