LOXL2 Inhibitors

LOXL2 inhibitors for multiple indications

Pharmaxis has developed two first-in-class, mechanism-based small molecules that inhibit Lysyl Oxidase Like 2 (LOXL-2) for the treatment of fibrotic diseases including NASH, liver, IPF, heart and kidney fibrosis.

The two lead compounds, each with differentiated PK / PD profile have demonstrated efficacy in pre clinical models of fibrosis and have completed preclinical tox studies. The first compound successfully completed phase 1 in October 2018.

In addition to studying the safety and pharmacokinetic profile, the clinical trial also investigated the degree to which the drug can inhibit the target enzyme LOXL2 which is implicated in several different fibrotic diseases. Importantly, Pharmaxis has been able to demonstrate a large and highly significant inhibition of this enzyme in blood serum for a full 24 hours from a single dose and that daily dosing over a 14-day period now meets our targeted  effect of greater than 80% inhibition at the 400mg dose.

The second compound clinical trial will report in the December quarter of 2018.

The LOXL2 program has been conducted in collaboration with UK biotechnology company Synairgen plc (LSE: SNG).

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Phase I
Description Phase 1 clinical trial - first molecule
Sites Two phase 1 units in Australia
Subjects Single Ascending Dose stage: 48; Multiple Ascending Dose stage: 24
Status Complete
More Information

The Phase 1 trial for a second Pharmaxis LOXL2 compound being studied has recently completed dosing and will report in the December 2018 quarter.

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