PHARMACEUTICALS

 

Wafermine contains the non-opioid drug Ketamine

Ketamine has been shown to be effective for the management of moderate to severe pain and provides a useful alternative to opioid analgesia. Ketamine, has also been shown to reduce hyperalgesia (the heightened sensitivity to pain) that occurs in many pain states and also through long-term usage of opioids. When used with opioids, ketamine has also been shown to have a dose-sparing effect on the amount of opioid analgesia required.

The rapidly dissolving wafer once placed under the tongue, causes ketamine to be absorbed through the mucous membrane into the bloodstream, without having to pass through the hostile acidic and enzymatic environment in the gastrointestinal tract or be subjected to the loss of active ketamine by hepatic metabolism (hepatic first pass effect).

With Wafermine, ketamine can now be delivered sublingually in a rapid and predictable manner to the bloodstream without the potential harmful initial spike in ketamine concentrations seen following intravenous administration.

Phase 1 Clinical Study

Study Design & Objective: An open label, two-way crossover Phase 1 study to evaluate the absolute bioavailability and clinical tolerability of a novel sublingual wafer formulation of ketamine in 8 healthy male volunteers (KET-001).

All subjects were administered with Wafermine 25mg sublingually (SL) and ketamine solution 10mg intravenously (IV) on two separate occasions.

Results for SL administration

(The absolute bioavailability of racemic ketamine from a novel sublingual formulation, British Journal of Clinical Pharmacology, 2013)

Phase 2 Single-Dose Clinical Studies

Study Design & Objective: A randomised, double-blind, parallel, placebo-controlled dose-ranging study to assess the analgesic efficacy, tolerability, safety and pharmacokinetics profile of Wafermine in 120 adults following a third molar extraction, examining a dosing range of 25 mg to 50 mg (KET-003), and a Phase 2 clinical study on Wafermine in 80 adults with higher doses of 70 mg and 100 mg (KET-005).

Results for SL administration of Ketamine

Results: In both studies, Wafermine produced rapid onset of pain relief, usually by 10 minutes post dose, with maximum effects generally at around 20-30 minutes, before subsiding over 1-2 hours.

Phase 2 Multi-Dose Efficacy Study

Study Design & Objective: a randomised, double-blind, placebo-controlled trial in a total of 125 female and male participants who underwent either abdominoplasty or bunionectomy surgery.

All Subjects (n=125)

4 treatment arms:
Placebo (n=39), 25mg (n=10), 50mg (n=38), 75mg (n=38)

Results for SL administration of Ketamine

 

Dexmedetomidine is formulated with iX Biopharma’s patented WaferiX technology and has the potential to be used for the treatment of multiple indications including dementia-related agitation.

Dementia is one of the leading causes of disability for elderly adults globally, and spending on managing the condition exceeds USD 1 trillion annually. In 2020, more than 5.8 million people in the United States were living with Alzheimer’s disease (the most common type of dementia2), and these persons collectively experience an aggregate of over 100 million agitation episodes annually.

There are currently no FDA-approved therapies for the treatment of this condition. Current approaches to address agitation are suboptimal. These include over-sedating therapies such as antipsychotics and benzodiazepines which produce adverse effects that are particularly severe for elderly patients, and physical restraints to ensure the safety of patients.

iX Biopharma’s sublingual dexmedetomidine wafer is administered by placing the wafer under the tongue, for rapid disintegration, greater absorption and improved bioavailability. Patients may benefit from faster and more predictable therapeutic action. Moreover, the drug is non-invasive, non-traumatic, convenient and easy to use during out-patient care.