Servier, an independent international pharmaceutical company, and the company Galapagos NV announce the start of a global Phase 2 trial with S201086/GLPG1972 in knee osteoarthritis patients: ROCCELLA.

Servier and Galapagos have submitted and will further submit clinical trial applications in a number of countries in North and South America, Europe and Asia. The study will now be initiated in the US and Hungary with other countries expected to follow, pending the respective regulatory approvals.

ROCCELLA will be a multiregional, randomized, double-blind, placebo-controlled, dose ranging trial evaluating the efficacy and safety of three different once-daily doses of S201086/GLPG1972 in patients with knee osteoarthritis (OA). ROCCELLA is planned to recruit approximately 850 patients in up to 15 countries. Galapagos will be responsible for ROCCELLA in the United States, where 300 patients are targeted to be recruited. Servier will run the trial in all other countries.

The primary objective of ROCCELLA is to demonstrate the efficacy of at least one dose of S201086/GLPG1972 compared to placebo in reducing cartilage loss after 52 weeks of treatment. Cartilage thickness will be measured using quantitative magnetic resonance imaging of the central medial tibiofemoral compartment of the target knee. Secondary objectives include safety and tolerability, several additional measures of structural progression, changes in bone area, pain, function, stiffness, and patient global assessment.

S201086/GLPG1972 is a disease-modifying osteoarthritis drug (DMOAD) candidate targeting efficiently a cartilage degrading enzyme called ADAMTS-5, as confirmed in two animal models. A Phase 1 trial in healthy volunteers met all its safety and pharmacokinetic targets and also demonstrated that S201086/GLPG1972 reduced by approximately 50% within two weeks the blood level of ARGS neoepitope, a biomarker for cartilage breakdown. In a more recent Phase 1b trial in OA patients in the United States, similar findings were seen over a four-week period. Specifically, S201086/GLPG1972 was well tolerated and it reduced, in a dose-dependent manner, the ARGS neoepitope blood levels by up to 50%.

“People living with osteoarthritis of the knee experience a major loss of quality of life, mainly because of the ever-present pain and increasing loss of mobility. Any therapeutic innovation that can prevent or slow down the underlying cartilage loss will thus address a huge unmet patient need for the many people affected by osteoarthritis in our aging populations”, said Lode Dewulf, Chief Patient Officer at Servier.

“The robust design of ROCCELLA should provide deep insights into the disease-modifying potential and the safety and tolerability of this novel therapeutic candidate in patients with knee OA. We have seen clear target engagement in OA patients; now we should be able to answer how this translates to protection against cartilage breakdown,” said Dr. Walid Abi-Saab, Chief Medical Officer of Galapagos. “We look forward to working with our collaboration partner Servier to execute ROCCELLA as rapidly as possible, with the goal of providing OA patients with a first disease-modifying drug.”

”Due to its unique mechanism of action based on the inhibition of cartilage degradation, S201086/GLPG1972 has the potential to help patients with osteoarthritis by altering the course of their disease. We look forward to launch the ROCCELLA phase 2 trial as a global effort conducted jointly by Servier and Galapagos to fulfill the needs of patients suffering from osteoarthritis”, said
Philippe Moingeon Head of Center for Therapeutic Innovation at Servier.

OA is a highly prevalent and disabling pathology. So far, no treatment is available to counteract disease progression, and patients are left with only symptomatic treatments. As a result, OA represents an important unmet medical need. Galapagos developed investigational molecule S201086/GLPG1972 with the potential of becoming a first-in-class DMOAD as part of a collaboration with Servier signed in 2010. Galapagos has full U.S. commercial rights to S201086/GLPG1972. Under the terms of the agreement, Galapagos is also eligible to receive development, regulatory and other milestone payments plus royalties upon commercialization outside the United States.