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Lumosa Therapeutics is dedicated to the development of innovative new drugs for the treatment of unmet medical needs in the fields of CNS and inflammatory diseases.


LT - 1001

A Novel Long-Acting Analgesic Injection

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Medical Needs

Pain is one of the most commonly seen symptoms in patients. Pain can be classified on the basis of the duration and pattern of occurrence along with the affected body part. Pain is deemed as the fifth observation symptom ranked after breathing, body temperature, pulse and blood pressure. Acute pain resulted from trauma, surgeries, or disease being either repetitive or persisting brings intolerable torment to people who suffer from it. Therefore, giving adequate pain relief (analgesic) is the most exigent task for the healthcare personnel. Painkillers that exert effect on the CNS can relieve pain but do not affect consciousness are divided into two groups: the opioid analgesics and the non-opioid analgesic (NSAIDs, such as aspirin etc.).

The opioid analgesics can inhibit the release of transmitters from neuron synapses through binding to theμ-opioid receptors and deliver great analgesic effect for moderate to severe pain. To handle pain induced by diseases, trauma, surgery and cancer, traditional opioid drugs such as morphine are widely used for treatment in patients but it has serious side effect including nausea, constipation, drug addiction and drug tolerance, physiological dependence and respiratory depression. Without having the ceiling effect, the side effects of morphine can increase with dosing escalation, which results in high risks of drug overdose and death resulted from respiratory depression. WHO 2014 reported 69,000 fatalities every year due to morphine overdoses. Unfortunately, the drugs currently on market used in pain management are either short-acting or lasting for maximally three days. In addition to the rising healthcare burden and expenditure for pain management, the quality of life and recovery progress in patients suffering from acute or chronic pain disorders are heavily impacted/encumbered because of the psychological pressure from repetitive dosing and inadequate pain control over a long period of time.

Prevent the prolonged pain and to optimize the operational results.
• Promote the combination of pain treatment to bring up the outcome in post-
• operative pain management
• Reduce opioid use while managing pain
• Decrease frequent attention and readmission in order to reduce the burden of healthcare personnel.
• Improve patients’ qualify of life / rehabilitate patients’ productivity

Market Opportunities

In the clinical setting, pain is grouped under acute or chronic pain categories. Acute pain management focuses on controlling incidental conditions; such as cancer breakthrough pain and post-operative pain; using mostly opioid analgesics. Chronic pain management often involves controlling arthritis and neuropathic pain with NSAIDs.

According to the IMS Health database, pain (with the sales of US $65 billion annual sales for analgesics) ranked number two globally in therapeutic area in 2012, surpassed only by antineoplastics (anticancer drugs). Within the analgesics category, 42% and 20% of the market size falls under the category of acute pain management and post-operative pain, respectively.

Competitive Advantage

High Success Rate in Development
The active ingredient in LT-1001 (NALDEBAIN®) is quickly metabolized to nalbuphine, after released into systemic circulation from the injection site. No other significant metabolites identified. LT-1001 is expected to have similar pharmacological effects and safety profile as that of nalbuphine, but overcome nalbuphine's short duration of action using a sustained release formulation.

Not a Controlled Substance
Nalbuphine (the active drug of LT-1001) is a mixed agonist-antagonist opioid analgesics, thus possess less abuse potential than morphine which are pure μ-agonists. Nalbuphine is NOT listed as a controlled substance in Europe, United States or Taiwan; therefore, it is more convenient for the physicians to prescribe than the traditional opioid analgesics which are mostly controlled substances.

High Safety Profile
Unlike morphine, nalbuphine exhibits a ceiling effect on respiratory depression such that an increase in dose greater than 30 mg does not produce further respiratory depression. In addition, LT-1001 is designed to provide sustained-release of nalbuphine over an extended time with a reduced plasma Cmax, thus avoids the side effects associated with extremely high levels of nalbuphine. LT-1001 does not cause gestrointestinal bleeding and other severe side effects commonly seen with NSAIDs.

Longer Analgesic Effect
Nalbuphine drug concentration in the blood after a single IM injection of LT-1001 maintains in the effective range up to 5 to 7 days. This greatly reduces the need for frequent administration of analgesics to patients post-operatively. Consequently, the workload of healthcare professionals and the risk of dispensing errors can be greatly reduced.

Patent Portfolio
LT-1001 was patented in Taiwan, USA, Europe, Japan, Korea, China and several other major markets. Additional product-related patents were for long-term market protection.

Product Positioning

LT-1001 is the only one-week long-acting analgesic injection with an analgesic effect comparable to that of morphine. A single IM injection of LT-1001 provides up to 7 days of pain relief for patients after surgery. It would effectively reduce the workload of healthcare professionals with significantly less need to care for patients in pain. Unlike morphine, nalbuphine (the active drug of LT-1001) exhibits a ceiling effect on respiratory depression such that increases in dose greater than 30 mg do not produce further respiratory depression. This greatly reduces the risk of respiratory depression and possible overdose death that is often associated with morphine. LT-1001 can be widely applied to treat the same moderate to severe acute pain (as preoperative and postoperative analgesia, and obstetrical analgesia during labor and delivery) as that indicated for short-acting nalbuphine.

LT-1001 (Naldebain®) Drug Profile

Name: NALDEBAIN® (marketed in Taiwan by InteRx)
Dosage: 75 mg per 1ml.
Dosage Form/Route: Injectable/Injection.
Strength and package: 150mg/2ml in a vial.
Administration: IM injection.
Indication: For moderate to severe pain relief after surgery.
Status: Approved by Taiwan FDA (TFDA) in 2017Q1; approval process for other regions of the world still pending.

 

Package insert approved by Taiwan FDA (in Chinese)

Licensing

LT1001 is currently undergoing licensing discussion and negotiation with potential partners worldwide. The collaboration model is In-licensing and/or R&D collaborations on manufacturing, IP and marketing. Upfront payments, milestone payments and royalty may be considered. The business terms can vary based on the model of collaboration and the regions licensed.

R&D Pipeline
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