Rescue Therapy for End-Dose Wearing “Off”

Due to the low concentration of levodopa between dosing intervals, the patient will have “Off” episodes, which are characterized by return of symptoms, such as bradykinesia or even sudden and transient freezing of gait (FOG). FOG is terrifying and dangerous, which tremendously compromise the quality of life and may lead to life-threatening incident/accident.

About 50% of Parkinson's patients with a disease for more than 10 years experience FOG. As the disease progresses, the FOG incidence increases.

WD-2010 is a drug-device combination product, comprising a proprietary device called AcuSiS® and a fast-dissolving levodopa/carbidopa granular formulation. The Acusis® device is designed to alleviate the difficulty in swallowing of tablets and capsules for the patients with dysphagia, especially for the PD patients suffering disabling “Off” episodes. WD-2010 is enabling a quick onset rescue for acute, intermittent treatment of “Off” episodes.

The fast-dissolving granules inside the device can form in-situ a homogeneous suspension at sipping.

WD Pharma has announced the positive results of a Phase I pharmacokinetic study. This was a randomized, open-label, two-treatment, two-sequence, two-period crossover study in 12 healthy adult volunteers. After randomization, subjects in Group A were administered with a single dose of WD-2010 (CD/LD: 25/100 mg) in the fasting state, while in Group B, a single dose of Sinemet generic equivalent-Mylan’s tablets (CD/LD: 25/100 mg) was administered in the same condition.

Figure 8 shows the pharmacokinetic profiles of plasma LD after administration of WD-2010 or Mylan’s tablets. The results show that tmax and Cmax for LD are, respectively, 0.667±0.3536 hr and 1376.9±422.6 ng/ml for WD-2010 and 0.961±0.5567 hr, and 1146.3±468.3 ng/ml for Mylan’s tablets. The difference in LD tmax between these two groups is 22.5 mins for the median, indicating potential faster onset of action with WD-2010.

Figure 8. Plasma LD Profiles in healthy volunteers after administration of WD-2010 or Mylan’s tablets in fasting conditions. Error bars represent SEs of the mean (n=12).