Certa’s SSc treatment candidate FT011 now known as asengeprast

Phase 2b clinical trial planned after earlier results showed lung function gains
by Lindsey Shapiro, PhD | September 24, 2024

FT011, Certa Therapeutics’ oral treatment candidate for systemic sclerosis (SSc), will now be known under the generic name asengeprast.

That decision was made by the World Health Organization (WHO), which is responsible for assigning International Non-Proprietary Names, or INNs, to pharmaceutical substances or active ingredients. INNs are globally recognized, unique identifiers for such substances, and may be understood as the generic name for an active ingredient in a medication. INNs are public property and aren’t owned by any particular company.

“The granting of an INN for our lead drug candidate asengeprast is another important step in [the] development of this important therapy,” Darren Kelly, PhD, CEO, founder, and managing director of Certa, said in a company press release. “​​We are continuing to drive the clinical development of asengeprast and believe it has the potential to address a critical need for people living with SSc, a debilitating condition with the highest mortality amongst rheumatic diseases.” Kelly is also a professor at the University of Melbourne in Australia.

The company plans to launch a confirmatory Phase 2b clinical trial with SSc patients after positive data from a Phase 2a clinical trial (NCT04647890) showed the treatment eased disease severity and improved lung function. It’s also working to develop biomarkers and gene signatures for identifying patients most likely to respond to the treatment.
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In SSc, the immune system launches harmful self-reactive attacks that cause fibrosis, or excessive scarring of the skin and internal organs.

​How does asengeprast work in SSc?
Asengeprast is a first-in-class therapy designed to block activity at the G protein-coupled receptor 68 (GPR68), a driver of fibrosis. GPR68 is normally silent, but gets activated in response to injury, causing inflammation and scarring.

The experimental oral therapy was granted orphan drug status in the U.S. and Europe, along with fast track status in the U.S. These designations offer financial and regulatory incentives to help accelerate a therapy’s clinical development.

Certa indicates an extensive body of preclinical research shows the therapy’s promising efficacy for inflammatory and fibrotic diseases, and that it’s been found safe and with good pharmacological properties in Phase 1 studies.

The Phase 2a trial enrolled 30 people with diffuse cutaneous SSc who were randomly assigned to either of two daily oral doses of asengeprast (200 or 400 mg), or a placebo, on top of standard care for about three months. Results showed 60% of patients treated with asengeprast’s higher dose and 20% given the lower dose exhibited meaningful improvements in their clinical status, as assessed by a composite measure of disease severity and organ damage, compared with 10% of those on the placebo.

The therapy was also associated with improved lung function and was generally favored over the placebo in patient- and physician-reported measures of health status.
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Certa is developing a portfolio of other GPR68 inhibitors for treating fibrotic kidney diseases including focal segmental glomerulosclerosis, diabetic nephropathy, and chronic kidney disease.