Data: ALPHA-1062 a Bioequivalent to Approved Therapy Razadyne

Alpha Cognition’s candidate oral tablet ALPHA-1062, for mild to moderate Alzheimer’s disease, showed efficacy as a bioequivalent substitute for the approved therapy Razadyne (galantamine), according to top-line data from a trial with healthy volunteers.

Per this new data, as a delayed-release tablet, ALPHA-1062 showed an equivalent pharmacokinetic profile — meaning it metabolizes in and is excreted from the body in a similar way — to galantamine hydrobromide extended-release tablets.

The findings support pivotal evidence from an earlier trial in which ALPHA-1062 was deemed a possible bioequivalent to galantamine hydrobromide in an immediate release formulation.

“We have successfully demonstrated that ALPHA-1062 is bioequivalent to two different release formulations of galantamine hydrobromide, the immediate release and the extended release,” Cedric O’Gorman, MD, Alpha Cognition‘s chief medical officer, said in a company press release.

Alpha now expects to use both trials’ data in filing a new drug application (NDA) with the U.S. Food and Drug Administration, seeking the approval of ALPHA-1062. That application is expected by the second quarter of next year, the company said.

“We are delighted with these additional positive registrational bioequivalence results from our second study of our lead asset, ALPHA-1062, which further strengthens our NDA filing,” expected by June 2023, said O’Gorman.

ALPHA-1062 in trials

ALPHA-1062, designed as a delayed-release tablet, is a pro-drug of galantamine hydrobromide that is metabolized once inside the body into its active form. This allows ALPHA-1062 to remain inert while it passes by the stomach, and to be absorbed in the small intestine as an inactive compound, becoming metabolized only when it reaches the liver. There, its active compound — galantamine — is released into circulation.

This delay in activation allows the medication to reach the brain with greater bioavailability.

Razadyne, by Janssen, is sold both as immediate-release (IR) and extended-release (ER) tablets. It works to slow the progression of symptoms in mild to moderate Alzheimer’s. The therapy, however, is linked with gastrointestinal side effects and can also cause insomnia.

The findings from both Alpha trials support the therapeutic effects of ALPHA-1062 to slow the progression and symptoms of Alzheimer’s disease. The medication has been shown to have fewer side effects, which have included nausea, vomiting, and diarrhea.

“ALPHA-1062, a prodrug of galantamine, was designed to limit gastrointestinal side effects and, if approved, could provide a meaningful advancement for patients with Alzheimer’s,” O’Gorman said.

In the most recent study, 40 healthy individuals were randomly assigned to receive ALPHS-1062, given as a 5 mg dose twice daily, or 8 mg of galantamine hydrobromide ER, administered once daily for seven days.

After a seven-day washout period — which allows the medication to fully clear the body — the participants “crossed over” to the other arm of the study. They then received the other therapy for another seven days.

Top-line results showed that ALPHA-1062 was bioequivalent to galantamine hydrobromide ER. Specifically, exposure to ALPHA-1062 was 107% of that of galantamine hydrobromide ER, with a peak exposure of 127%.

The maximum concentration of ALPHA-1062 was lower than that of galantamine hydrobromide IR and higher than its ER formulation.

According to the company’s press release, these results support the bioequivalence of ALPHA-1062 to both galantamine hydrobromide IR and ER formulation.

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