New Anti-Attention Deficit Hyperactivity Disorder (ADHD) Medication (BLI-1008)
Target Indication
BLI-1008 is extracted from an herb that is used traditionally as sedative in Chinese Medicine. BLI-1008 inhibits the reuptake of norepinephrine through the suppression of the norepinephrine transporter. Therefore, BLI-1008 is developed as a treatment for Attention Deficit Hyperactivity Disorder (ADHD).
Drug Type
New drug category: Botanical new drug
Formulation: Oral capsule
Foresight and Global Development
Attention deficit hyperactivity disorder (ADHD) is a common psychiatric disorder affecting children and adolescents. According to the research by National Institute of Mental Health (NIMH), approximately 3-5% children are affected by ADHD. Up to 30-50% patients with ADHD continued with their symptoms into adulthood.
ADHD patients usually show inattentive, hyperactive or impulsive symptoms. These symptoms often lesd to poor school performance and lack of self-control which might further affect personality, interpersonal skills, or even lead to anti-social behavior.
Although current medications such as stimulants are effective in controlling symptoms, however, concerns about abuse and addiction limit their use. Other non-stimulating ADHD drugs also have side effects such as gastrointestinal discomfort, reduced appetite, or fatigue. The BLI-1008 may be developed as a valuable treatment for ADHD medications. ADHD therapeutics market was valued at about $3.9 billion in 2010, and is forecasted to grow at a compound annual growth rate (CAGR) of 8.0% over the next eight years, reaching $7 billion by 2018.
Result
1. In-vitro radioligand-binding assay
Summary: BLI-1008 possesses the activity of inhibiting norepinephrine transporter, a mechanism for treating ADHD.
Assay name
Concentration of BLI-1008
% of Inhibition
IC50
Norepinephrine Transporter
0.3 μg/mL
20
2.102 μg/mL
1 μg/mL
34
3 μg/mL
60
10 μg/mL
76
30 μg/mL
84
2. Safety
Repeated dose 28-day subacute oral toxicity studies have demonstrated that NOAEL (no-observed adverse effect level) of BLI-1008 is 3000 mg/kg/day for both dogs and rats.
A phase I study of BLI-1008 on another indication has indicated that there is no safety concern for single dose oral administration up to 3800 mg in healthy volunteers. Furthermore, side effects common to other ADHD treatments, such as reduction of appetite, were not observed.
Product Advantage
BLI-1008 is extracted from Traditional Chinese Medicine widely used in Asia and Europe.
In animal studies, it was revealed that BLI-1008 reduced total activity in an ADHD mouse model.
BLI-1008 has been proven safe with limited in side effects in a phase I human clinical trial on another indication. BLI-1008 does not reduce appetite, as supported by the same clinicaltrial.
BLI-1008 is covered by 11 patents in 8 countries as the US, United Kingdom, Japan, Germany, France, Italy, Switzerland and Taiwan.
Research and Development Stage
Subvention granted by the "R&D Research Enhancement Project" Hsinchu Science Park Bureau, Ministry of Science and Technology.
