Table 1 Plasma and Cerebral Spinal Fluid Levels in rats treated with Exendin-4 in the form of s.c. PT302 and immediate release Exendin-4

From: Post-treatment with PT302, a long-acting Exendin-4 sustained release formulation, reduces dopaminergic neurodegeneration in a 6-Hydroxydopamine rat model of Parkinson’s disease

Formulation

Dose

Plasma (pg/ml)

CSF (pg/ml)

CSF/Plasma ratio

PT302(low)

0.46 mg/kg/14days

1853.3

18.3

0.01

PT302(high)

2.0 mg/kg/14days

2316.8

30.0

0.011

Exendin-4 low

2.3 µg/kg/day (1.15 BID)

93.5

Under LLOQ

N/A

Exendin-4 Medium

4.6 µg/kg/day (2.3 BID)

576.9

Under LLOQ

N/A

Exendin-4 High

10 µg/kg/day (5 BID)

5819.3

Under LLOQ

N/A

  1. LLOQ: lower limit of quantification (6.9 pg/ml).
  2. PT302 was administered as a one-time s.c. dose, and plasma and CSF were sampled exactly 14 days later.
  3. Immediate release Exendin-4 was administered s.c. twice daily × 14 days, and plasma and CSF were sampled 90 min following the final dosing.
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