Rhizen Pharmaceuticals AG Announces First Patient Dosed in a Phase 2 Study of RP7214 in Covid-19 Patients

• First study of RP7214, a DHODH inhibitor, in Covid-19 patients with mild, symptomatic disease on the background of promising preclinical efficacy & Phase 1 healthy volunteer safety

• Randomized, placebo-controlled Phase 2 study is designed to evaluate the effect of RP7214 on viral load & clearance, disease biomarkers and clinical improvement in patients’ status along with the tolerability and immunomodulatory activity of RP7214.

• RP7214 is expected to function by inhibiting the DHODH enzyme on host cells and limit their ability to support viral replication. This unique mechanism of action, if successful in the clinic, is expected to be complementary to other antiviral drugs that directly inhibit the virus.

• Future plans may include testing RP7214 in partially/fully vaccinated patients with breakthrough covid-19 infections as part of a broader clinical development program. As infections continue to persist and spread despite increasing vaccinations, there is growing need for a convenient oral anti-viral treatment option that patients can potentially self-administer at home while will in turn reduce burden on the healthcare infrastructure and allow resumption of economic activity.

(BUSINESS WIRE) -- Rhizen Pharmaceuticals AG, a clinical-stage oncology & inflammation-focussed biopharmaceutical company, today announced that the first patient has been dosed in a Phase 2 clinical trial of RP7214, a small molecule oral dihydroorotate dehydrogenase (DHODH) Inhibitor. The randomized, double-blind, placebo-controlled, Phase 2 study will evaluate the efficacy & safety of oral RP7214, in covid-19 patients with mild, symptomatic disease with an underlying risk factor on the background of promising preclinical efficacy & phase 1 healthy volunteer safety. The study is being conducted in India across 12 centres in coordination with Rhizen’s India affiliate, Incozen Therapeutics Pvt ltd., and is designed to enrol up to 204 patients across both study arms.

Viral replication involves a huge demand for building blocks and relies on nucleotides derived from host cells. DHODH is a rate-limiting enzyme in the pyrimidine biosynthesis pathway, inhibition of which leads to depletion of host nucleotide pools required for viral replication. RP7214 is a small molecule potent inhibitor of human DHODH with low nanomolar potency with demonstrated selective activity on SARS-COV-2 replication in a preclinical setting without any effect on the host cells. The known anti-inflammatory potential of DHODH inhibitors along with RP7214’s high oral bioavailability and wide safety window as demonstrated in a healthy volunteer Phase-1 study provides compelling rationale for testing RP7214 in mild COVID patients. With a profile that fundamentally addresses replication of the viral genome, RP7214 is expected to be agnostic to the mutational status of SARS-COV-2 in patients thereby offering a potential means to avoid disease progression and hospitalizations.

“DHODH inhibition is an interesting therapeutic approach that has broad application across oncology, inflammation & anti-infectives. In addition to our development efforts with RP7214 in AML, we are pleased that Rhizen has been able to respond to this pandemic by progressing the development of this program in Covid-19. In this study, we expect to get a read on the ability of RP7214 to inhibit the viral replication & clearance and induce an anti-inflammatory response” said Swaroop Vakkalanka, Ph.D., Founder & CEO of Rhizen Pharma. Swaroop also added that “Given the orthogonal nature of this host-directed mechanism of RP7214, we expect that RP7214 will eventually also combine well with direct acting antiviral agents, across a broad range of RNA-viral indications. If therapeutically active, we expect RP7214 will play a major role in mitigating & reducing the severity of de novo and breakthrough infections in both unvaccinated and vaccinated individuals, thereby becoming an important public health tool that can help reduce the burden on healthcare systems and allow economic activity to resume.”

RP7214 was earlier studied in a Phase I first-in-human healthy volunteer study in the US under an IND across both single-dose, multiple-dose and fed-fasted conditions and was found to be very well-tolerated across all doses tested, with high bioavailability and dose-proportional plasma concentrations.

About Rhizen Pharmaceuticals AG.:

Rhizen Pharmaceuticals is an innovative, clinical-stage biopharmaceutical company focused on the discovery and development of novel oncology & inflammation therapeutics. Since its establishment in 2008, Rhizen has created a diverse pipeline of proprietary drug candidates targeting several cancers and immune associated cellular pathways.

Rhizen has proven expertise in the PI3K modulator space with the discovery of our first PI3Kδ & CK1ε asset Umbralisib that has been successfully developed & commercialized in MZL & FL by our licensing partner TG Therapeutics (TGTX) in USA. Beyond this, Rhizen has a deep oncology & inflammation pipeline spanning discovery to Phase 2 clinical development stages.

Rhizen is headquartered in Basel, Switzerland. For additional information, please visit https://www.rhizen.com/

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