On March 15, 2023 Inhibikase Therapeutics, Inc. (Nasdaq: IKT) ("Inhibikase" or "Company"), a clinical-stage pharmaceutical company developing protein kinase inhibitor therapeutics to modify the course of Parkinson’s disease, Parkinson’s-related disorders and other diseases of the Abelson Tyrosine Kinases, reported an interim update from the dose escalation portion of its ‘501’ bioequivalence study of IkT-001Pro, the Company’s prodrug formulation of imatinib mesylate designed to enhance the safety and efficacy of imatinib (marketed as Gleevec) in patients with Chronic Myelogenous Leukemia (CML) (Press release, Inhibikase Therapeutics, MAR 15, 2023, View Source [SID1234628825]).
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The 501 trial is evaluating IkT-001Pro at four single ascending doses in the dose escalation portion of the study to select the bioequivalent dose, followed by a dose confirmation portion to confirm the bioequivalent dose. The study will enroll a total of 59 male and female healthy volunteers, aged 25 to 55. The study is designed to evaluate the safety profile of IkT-001Pro as well as compare the pharmacokinetic exposure of IkT-001Pro to the standard of care dose of 400 mg imatinib mesylate in order to identify a bioequivalent dose.
As of March 15, 2023, the Company has enrolled 19 of 27 healthy volunteers in the dose calibration portion of the study, completing 3 of 4 planned escalating doses at 300, 400 and 500 mg IkT-001Pro. To date, IkT-001Pro has shown a favorable safety profile, with only 4 mild adverse events observed, none of clinical significance. IkT-001Pro has high oral bioavailability and a pharmacokinetic profile of delivered imatinib that closely matches the exposure of imatinib delivered as 400 mg imatinib mesylate. Upon completion of the dose escalation phase, the Company will conduct a confirmatory analysis of the bioequivalent dose of IkT-001Pro in 32 additional healthy volunteers using a two-period crossover design. The Company remains on track to complete the 501 trial in the second quarter of 2023.
"We have made great progress in our 501 trial, since dosing the first patients in December," stated Dr. Milton Werner, President and Chief Executive Officer. "To date, our observations in the trial have followed expectations and are in line with our previously reported preclinical data, where we demonstrated that delivery of imatinib as IkT-001Pro was well tolerated. With the rapid completion of the first three dose cohorts, we are on track to complete the 501 trial in the second quarter of 2023."
Following the completion of the 501 trial, Inhibikase plans to initiate a discussion with the FDA on the parameters for approval of IkT-001pro under the 505(b)(2) statute.
About IkT-001Pro
IkT-001Pro is a prodrug formulation of imatinib mesylate and has been developed to improve the safety of the first FDA-approved Abelson (Abl) kinase inhibitor, imatinib (marketed as Gleevec). Imatinib is commonly taken for hematological and gastrointestinal cancers that arise from Abl kinase mutations found in the bone marrow or for gastrointestinal cancers that arise from c-Kit and/or PDGFRa/b mutations in the stomach; c-Kit, PDGFRa/b and Abl are all members of the Abelson Tyrosine Kinase protein family. IkT-001Pro has the potential to be a safer alternative for patients and may improve the number of patients that reach and sustain major and/or complete cytogenetic responses in stable-phase CML and/or reduce the relapse rate for these patients. In preclinical studies, IkT-001Pro was shown to be as much as 3.4 times safer than imatinib in non-human primates, reducing burdensome gastrointestinal side effects that occur following oral administration. Imatinib delivered as IkT-001Pro was granted Orphan Drug Designation for stable-phase CML in September 2018.
About Chronic Myelogenous Leukemia
Chronic myeloid leukemia1 is a slowly progressing cancer that affects the blood and bone marrow. In CML, a genetic change takes place in immature myeloid cells — the cells that make most types of white blood cells. This change creates an abnormal gene product called BCR-ABL which transforms the cell into a CML cell. Leukemia cells increasingly grow and divide in an unregulated manner, eventually spilling out of the bone marrow and circulating in the body via the bloodstream. Because they proliferate in an uncontrolled manner, the excessive production of myeloid cells acts like a liquid tumor. In time, the cells can also settle in other parts of the body, including the spleen. CML is a form of slow-growing leukemia that can change into a fast-growing form of acute leukemia that is difficult to treat.