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Clinical Data

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Two Phase I clinical studies were conducted in Malaysia (ART001) and South Africa (ART002) respectively. In total, 32 healthy male subjects were enrolled and completed the study.

  • ART001 was an open labelled randomised trial to determine the pharmacokinetics, bioequivalence and relative bioavailability of artemether when administered as 3mg/actuation sublingual spray, 6mg/actuation sublingual spray and oral tablets in 16 healthy male subjects.
  • ART002 was an open labelled randomised trial to determine the multiple dose pharmacokinetics of artemether and dihydroartemesinin when administered as artemether sublingual spray 3mg/actuation and artemether sublingual spray 6mg/actuation in 16 healthy male subjects.

The results showed that artemether sublingual spray had a higher bioavailability when compared to the artemether oral solid dosage. No evidence to suggest the occurrence of auto-induction following multiple administrations of artemether sublingual spray. Overall, ArTiMist™ showed to be safe and well tolerated.

T3 - single sublingual administration of 30mg Artemether Sublingual Spray 6mg/actuation; T4 - single oral administration of 30mg Artemether tablets (3x10mg tab)

T3 – single sublingual administration of 30mg Artemether Sublingual Spray 6mg/actuation; T4 – single oral administration of 30mg Artemether tablets (3x10mg tab)

Day1vsDay5_time_hour

Phase II clinical study (ART003) was conducted in Rwanda. The study was an open label randomised comparative trial to establish the efficacy of 3mg/kg ArTiMist™ when compared to intravenous (IV) quinine in children with severe or complicated P. falciparum malaria, or uncomplicated P. falciparum malaria with gastrointestinal complication

ArTiMist™ was rapidly absorbed and easily administered. 93.3% (14 patients) of the children in the ArTiMist™ arm had a ≥90% reduction in parasite count within 24 hours after the first dose vs. 66.7% (10 patients) in the IV Quinine. Complete parasite clearance was reached in about 37 hours by ArTiMist™ vs. about 51 hours by IV Quinine.

Additional information can be found on www.clinicaltrials.gov, clinical study identifier NCT01047436.

Phase III clinical study was conducted in three African countries (Rwanda, Ghana and Burkina Faso). The study was an open label, randomised, active controlled, multi-centre study, conducted to demonstrate ArTiMist™ superiority in reducing parasite count by ≥90% within 24 hours from first dosing when compared to IV Quinine in children with P. falciparum severe malaria and uncomplicated malaria with gastrointestinal complications.

ArTiMist™ primary point was achieved with 94.3% (66 out of 70 patients) of the children in the ArTiMist™ arm showing a ≥90% reduction in parasite count within 24 hours after the first dose vs. 39.4% (28 out of 71 patients) in the IV Quinine arm.

The secondary efficacy parameters demonstrated a statistically significant difference between the treatments. The parasite count fell by 50% and 90% in just about 9 and 15 hours respectively with ArTiMist™; whereas for the IV Quinine it took c.19 and c.29 hours for the parasite count to fall by 50% and 90% respectively.

Additional information can be found on www.clinicaltrials.gov, clinical study identifier NCT01258049.

ArTiMist™ is contained in a 10mL, Type 1 glass bottle fitted with a valve pump and a 100µL actuator constructed from pharmaceutical grade materials and are commercially available off-the-shelf.

ArTiMist™ contains 7.9mL of 60mg per mL artemether in mygliol base with a menthol flavour.

Each container contains sufficient solution for 50 actuations; each actuation contains 6mg of artemether.

Artemether is stable for 48 months at 30C 75%RH (ICH 4)

The following papers have been published on peer-reviewed journal(s):

Pharmacokinetics of a novel sublingual spray formulation of the antimalarial drug artemether in African children with malaria

http://aac.asm.org/content/59/6/3208.abstract

Pharmacokinetics of a novel sublingual spray formulation of the antimalarial drug artemether in health adults

http://aac.asm.org/content/early/2015/03/17/AAC.05013-14.abstract

Efficacy of a novel sublingual spray formulation of artemether in African children with falciparum malaria

http://aac.asm.org/content/early/2015/08/18/AAC.00243-15.abstract