K-252a is a potent inhibitor of nerve growth factor (NGF) and therefore has the ability to inhibit keratinocyte proliferation. K-252a is strongly lipophilic and therefore passes freely into the cell membranes of keratinocytes and accumulates at a systemic level. In order to reduce the dermal absorption and reduce the possible long-term systemic toxicity this study will assess a PEGylated derivative of K-252a named CT327. This approach should improve the safety profile of the K-252a molecule while maintaining its activity. The primary objective is to assess the safety and tolerability of single and repeat doses of CT327 when applied topically to the skin of healthy male volunteers. The secondary objective is to evaluate the eventual systemic absorption (pharmacokinetics; PK) of CT327 following single and repeat doses in healthy male subjects.
Study Type
INTERVENTIONAL
Allocation
RANDOMIZED
Purpose
TREATMENT
Masking
QUADRUPLE
Enrollment
16
Cream (10 g) was applied at an even thickness over a test area on the back of 10 x 10 cm to give an exposure of 1000 μg/dm2.
Cream (10 g) was applied at an even thickness over a test area on the back of 10 x 10 cm to give an exposure of 100 μg/dm2.
Safety as defined by local tolerability, subject incidence of TEAEs, and clinically significant changes in lab safety tests, ECGs, vital signs and PE findings.
Each subject received a single topical dose of CT327 (or placebo) followed by a single topical dose of CT327 (or placebo) on five consecutive days with a washout period of 7 days between the two dosing periods.
Time frame: 2 weeks
Pharmacokinetic
The secondary endpoint is determination of eventual CT327 plasma levels. PK blood sampling day 1: 0 h, 2 h, 4 h, 6 h, 12 h, 24 h, and 2 h post dose on days 9, 10, 11, 12 and 13.
Time frame: 2 weeks
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