Our portfolio of sublingual pharmaceutical products is built on the WaferiX platform technology, and includes pipeline products in the late stage of development
Non-opioid with opioid sparing effects
Positive in Phase 2b clinical studies:
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.
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.
(The absolute bioavailability of racemic ketamine from a novel sublingual formulation, British Journal of Clinical Pharmacology, 2013)
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.
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
Completed Phase 1 Sublingual Dexmedetomidine Clinical Study
The Phase 1 pharmacokinetic clinical study achieved several positive results:
1. High bioavailability: The sublingual wafer showed an impressive 70-80% absolute bioavailability across all dosages tested.
2. Fast onset of action: The sublingual wafer achieved a peak drug concentration in 1.5 hours (Tmax), with drug detectable in plasma as early as 5 minutes post dosing.
3. Dose proportional: The drug exposure was proportional across the dosing range.
4. Safety profile: Sublingual wafers were safe and well tolerated; there were no serious adverse events.
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.
By utilising iX Biopharma’s proprietary sublingual technology WaferiX, we have demonstrated in a phase 1 pharmacokinetic study (BUP001) that BnoX facilitates the rapid absorption of buprenorphine (median Tmax 1.0 hour) with greater absolute bioavailability of 45%. These results suggest superior pharmacokinetics to currently marketed sublingual buprenorphine formulations.LEARN MORE
BnoX , is a sublingual buprenorphine oral wafer.
With the spotlight currently on the global opioid epidemic, there is now an increasing recognition that buprenorphine can be a critical and emerging compound and which has been shown to be useful for pain management.
Buprenorphine has also been shown to provide longer lasting pain relief with fewer side effects compared to other opioids. It also exhibits a ceiling effect – higher doses do not result in unwanted additional opioid effects, including euphoria and respiratory depression. Patients are therefore less likely to develop an addiction and/or tolerance, while the risk of death is also greatly reduced.
Buprenorphine is known for its poor bioavailability (reported to be 10% or less) when ingested orally. However, by utilising iX Biopharma’s proprietary sublingual technology WaferiX , we have demonstrated in a phase 1 pharmacokinetic study (BUP001) that BnoX facilitates the rapid absorption of buprenorphine (median Tmax 1.0 hour) with greater absolute bioavailability of 45%. These results suggest superior pharmacokinetics to currently marketed sublingual buprenorphine formulations.
Sildenafil citrate has been shown to be a hallmark drug for the treatment of erectile dysfunction in males. Utilising WaferiX, Wafesil is a sildenafil wafer that is administered sublingually. Wafesil comes in a new dosage form and route of administration for patients who cannot or prefer not to swallow. Wafesil is approved for marketing in Australia, outlicensed for China market.
Silcap is a novel small sildenafil capsule that is easy to swallow. Silcap is approved for marketing in Australia and Singapore.