Rhizen doses first patients with advanced solid tumours

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11.11.2021

Rhizen Pharmaceutics has commenced a multi-center, phase I/Ib trial to evaluate its novel polymerase inhibitor (RP12146) in patients with advanced solid tumours. Conducted in Europe, the two-phase study aims, among other things, to determine safety, tolerability, maximum tolerated dose.

Based in Basel, Rhizen is an innovative, clinical-stage biopharmaceutical company focused on discovering and developing novel oncology and 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.

The company’s poly (ADP-ribose) polymerase (PARP) inhibitor (RP12146) has shown preclinical activity and efficacy comparable to the approved PARP inhibitor Olaparib. It also demonstrated improved preclinical safety as seen in the preclinical IND-enabling toxicology studies, an advantage that Rhizen will translate in the clinical studies.

The company is now dosing the first patients in a multi-centre, phase I/Ib trial to evaluate RP12146 in patients with advanced solid tumours. The two-part study, conducted in Europe, has been designed to initially determine safety, tolerability, maximum tolerated dose (MTD). It also aims to find a recommended phase II dose (RP2D) of RP12146 and subsequently assess its anti-tumour activity in expansion cohorts with HRR mutation-enriched ES-SCLC, ovarian and breast cancer patients.

The PARP program RP12146 is part of a larger DNA Damage Response (DDR) platform at Rhizen that includes a preclinical-stage polymerase theta (Polθ) inhibitor program, including a preclinical-stage Polθ inhibitor program. The DDR platform enables novel, proprietary, in-house combinations. Rhizen expects the platform to allow novel proprietary combinations of its PARP and Polθ assets, given the mechanistic synergy and opportunity across PARP resistant/refractory settings.

“PARP inhibitors are a great success story in the DNA damage response area, but they are not without safety concerns that have limited realization of their full potential. Although our novel PARP inhibitor competes in a crowded space, we expect its superior preclinical safety to translate into the clinic. This will differentiate our program and allow us to extend its application beyond the current landscape of approved indications and combinations”, said Swaroop Vakkalanka, Founder & CEO of Rhizen Pharma. “Our PARP program is foundational for our DDR platform efforts and will be the backbone for several novel proprietary combinations that we hope to bring into development in the future”, he added.

(Press release / RAN)

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