Nektar Therapeutics‘ investigational drug candidate for neuropathic pain, NKTR-171, has demonstrated dose-dependent analgesia with notably reduced central nervous system (CNS)-related side effects in preclinical studies.
NKTR-171 is a novel sodium channel blocker intended to treat neuropathic pain while avoiding the severe CNS side effects associated with existing therapies.
Nektar Therapeutics senior vice president and chief scientific officer Dr Stephen Doberstein said sodium channels are known to play a significant role in the changes in neuronal excitability that lead to neuropathic pain.
"We are extremely pleased that NKTR-171 exhibits effective analgesia in multiple neuropathic pain models without generating the CNS side effects observed with current therapies used to treat neuropathic pain," Doberstein said.
"We look forward to continuing to prepare NKTR-171 for our first human studies, which are planned for 2013."
In vitro and in vivo preclinical studies evaluating the pharmacokinetics and efficacy of NKTR-171 demonstrated that the investigational drug effectively obstructs the inactivated state of sodium channel cells, while reducing brain to plasma ratio.
NKTR-171 demonstrated comparable efficacy to gabapentin in well-validated animal models of persistent neuropathic pain.
The investigational candidate did not notably impair motor coordination at analgesic doses in an established preclinical model of sedative potential in animals.
Study data suggests that the ability to provide analgesia at doses that do not cause significant side effects (therapeutic index) could potentially be greater for NKTR-171 than for presently available therapies.