Xenon Pharmaceuticals acquired a potassium channel modulator XEN1101 (formerly 1OP2198) for the potential treatment of epilepsy from 1st Order Pharmaceuticals to expand its neurology pipeline. The small-molecule, next-generation, voltage-gated Kv7 potassium channel opener will initially be developed for treatment-resistant focal or partial-onset seizures in adults. Xenon said it projects filing an IND or IND-equivalent for clearance to start first-in-man trials, during the fourth quarter of 2017.

1st Order acquired 1OP2198 from an undisclosed third party, and Xenon will have to honor financial responsibilities under that deal. The firm expects to make up-front and milestone payments of $1.1 million in 2017. Moving forward, payments due to 1st Order and the third party could include $1 million in clinical development milestones, up to $13 million in regulatory milestones, and up to about $33.6 million in sales-based and other milestones, plus sales royalties.

Xenon says preclinical studies indicate that XEN1101 may exhibit a better pharmacokinetic, selectivity, and pharmacology profile when compared with first-generation potassium channel modulators such as ezogabine. “Based on its mechanism of action, XEN1101 potentially represents a therapeutically differentiated alternative to the antiepileptic medications currently available and could provide a better safety and tolerability profile when compared with earlier generation potassium channel modulators,” stated Simon Pimstone, MBChB, Ph.D., FRCPC, Xenon president and CEO. “Early clinical development is expected to include a pharmacodynamic readout in the first quarter of 2018 and Phase II development beginning by mid-2018.”

1st Order’s co-founder, president, and CSO, Christopher Crean, added, “Having been involved in the final development and approval of ezogabine, I am pleased to see Xenon move ahead with XEN1101, a promising next-generation therapeutic based on a proven mechanism. … I am hopeful that the advancement of XEN1101 will ultimately lead to a new treatment option for patients with epilepsy.”

Within the last month, Xenon said it projected filing for approval to start clinical development with another epilepsy drug candidate, this one a proprietary Nav1.6 inhibitor, XEN901, by the end of 2017.

Xenon’s acquisition of XEN1101 comes just over a month after the firm confirmed dropping further development of its acne candidate XEN801 after the topical stearoyl Co-A desaturase-1 inhibitor failed in a Phase II trial.


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