On June 22, 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 that it has selected the bioequivalent dose 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) and provided an update on its ‘501’ bioequivalence study (Press release, Inhibikase Therapeutics, JUN 22, 2023, View Source [SID1234632849]).

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The ‘501’ bioequivalence study has evaluated IkT-001Pro at four single ascending doses of 300, 400, 500 and 600 mg, leading to the selection of 600 mg IkT-001Pro as the bioequivalent dose to 400 mg imatinib mesylate. The pivotal phase of the study was dosed with bioequivalent IkT-001Pro in 31 healthy volunteers; one subject was excluded pre-dose due to aberrant clinical laboratory values. The Company expects to complete the pivotal clinical phase of the study by the end of the second quarter.

"Based on the safety signals we have seen at the 600 mg dose of IkT-001Pro relative to 400 mg imatinib mesylate, we believe that we have identified the appropriate go-forward dose for standard-of-care treatment with IkT-001Pro," stated Dr. Milton Werner, President and Chief Executive Officer of Inhibikase Therapeutics. "We plan to add an additional cohort to the ‘501’ trial in the third quarter to evaluate bioequivalence of IkT-001Pro relative to 600 mg imatinib mesylate with repeat dosing. 600 mg imatinib mesylate is commonly used to treat CML, but is poorly tolerated by up to 50% of patients. We believe IkT-001Pro may overcome the poor tolerability of high dose imatinib experienced by many patients, further differentiating the advantage of IkT-001Pro over current standard-of-care."

Following the completion of the ‘501’ trial, Inhibikase will 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 leukemia[1] 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.