Rhizen Pharmaceuticals AG Announces Promising Interim Data Presentation From an Ongoing Phase II Study of Tenalisib (RP6530) in Locally Advanced or Metastatic Breast Cancer Patients At ESMO Breast Cancer Meeting 2022

• Rhizen Pharma reports encouraging initial results from an ongoing phase II trial to evaluate Tenalisib (RP6530; isoform selective dual PI3K δ/γ inhibitor with additional SIK3 inhibitory activity) in patients with locally advanced or metastatic breast cancer (mBC)

• Tenalisib was well tolerated and showed encouraging preliminary efficacy as a single agent in both primary and secondary resistant mBC; Data supports further development of Tenalisib in patients with HR+ and HER2- MBC

(BUSINESS WIRE) -- Rhizen Pharmaceuticals AG (Rhizen), a Switzerland-based privately held, clinical-stage biopharmaceutical company announced today that it is presenting promising interim data from an ongoing Ph2 trial of Tenalisib in locally advanced or metastatic breast cancer patients, at the ESMO Breast Cancer Meeting, in Berlin, Germany from May 3-5, 2022.

This multi-center, randomized phase II study is being conducted in eastern Europe and is designed to assess Tenalisib’s anti-tumor activity (clinical benefit rate at the end of 6 months, disease control rate and overall response rates) and safety across two dose levels. The study also includes translational assessments intended to delineate the effect of Tenalisib’s multivalent mechanism on relevant cytokines/chemokine levels and gene expression changes within the tumor microenvironment.

The study included 40 enrolled patients (39 HR+/Her2- and 1 TNBC) presenting with stage IV A or IV B advanced or metastatic disease with majority of the patients having significant distal metastases to the bone, lymph nodes, lung and liver. The study population included patients with both primary resistance (~40%) and secondary resistance (~60%) to endocrine therapy and with ~50% of the patients undergoing prior chemotherapy treatment in a metastatic setting.

As of April 18^th 2022, the initial results from the study showed that Tenalisib was well tolerated across dose levels with majority of reported adverse events being mild-to-moderate in severity. Discontinuations and dose reductions due to related AEs were minimal (5-7.5%). The median duration of treatment thus far was ~4 months (0.93 to 6.23+ months) with ~60% of patients continuing on the study. The median time to response was 1.8 months and preliminary efficacy results indicate an encouraging 67.5% DCR which is maintained across patients with primary endocrine resistance as well. Correlation of responses observed with gene expression profiles by RNA sequencing from tumor biopsy samples post treatment with Tenalisib and analysis of cytokine/chemokine levels post Tenalisib treatment are underway.

“We are encouraged by the early activity seen with Tenalisib in the advanced/metastatic disease setting where patients have limited treatment options once they have failed CDK inhibitors and endocrine therapies. As these results continue to translate into durable responses, we will be engaging with key opinion leaders and regulatory agencies to discuss the monotherapy and combination development plans and registration-enabling study designs.” said Swaroop Vakkalanka, Founder & CEO of Rhizen Pharma. Swaroop also added that “Given the relevance of Tenalisib’s multi-valent mechanism across solid tumors, we expect these results will pave the way Tenalisib’s development to be expanded into other solid tumors. We are designing Tenalisib’s clinical programme carefully to arrive at an optimized dose and also deploy randomized study designs to fully elucidate its efficacy and safety.”

Rhizen indicated that Tenalisib, in addition to its selective dual PI3K δ/γ inhibitory activity, also has Salt-Inducible Kinase 3 (SIK3) activity via its principal metabolite, that could potentially contribute to its chemo-sensitization effect, especially in breast cancer. Rhizen hopes to establish the single agent activity of Tenalisib in this current study after which it plans to expand the assessment across additional solid tumor indications and combinations both with chemotherapeutic agents and with immune-checkpoint inhibitors.

About Tenalisib (RP6530):

Tenalisib (RP6530) is a highly selective, next-generation, orally active, dual PI3K δ/γ inhibitor with additional SIK3 activity, that is currently in phase II clinical development for solid tumors & haematological malignancies. Tenalisib has been granted US FDA Fast Track & Orphan-Drug Designations for treatment of r/r PTCL and CTCL and had recently published data from its phase II study evaluating Tenalisib both as monotherapy and in combination with Romidepsin in r/r PTCL & CTCL which showed robust responses of ~75% ORR in r/r PTCL and ~54% in r/r CTCL. The combination was well tolerated with no additional toxicities noted over & above those of the individual agents, confirming Tenalisib’s superior safety profile in its class. Overall, Tenalisib has been studied in ~200 patients across studies till now and has shown potentially better safety outcomes vis-à-vis other agents in the PI3K class.

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

Forward-looking statements

This press release may contain certain forward-looking statements relating to the company and its business. Although the company believes its expectations are based on reasonable assumptions, all statements other than statements of historical fact included in this press release about future events are subject to (i) change without notice and (ii) factors beyond the company’s control. These statements may include, without limitation, any statements preceded by, followed by, or including words such as “target,” “believe,” “expect,” “aim,” “intend,” “may,” “anticipate,” “estimate,” “plan,” “project,” “will,” “can have,” “likely,” “should,” “would,” “could”, and other words and terms of similar meaning or the negative thereof. Forward-looking statements involve certain risks, uncertainties and other factors which could cause the actual results, financial condition, performance or achievements of the company to be materially different from those expressed or implied by such statements. Readers should therefore not place undue reliance on these statements, particularly not in connection with any contract or investment decision. Except as required by law, the company assumes no obligation to update any such forward-looking statements, or to update the reasons actual results could differ materially from those anticipated in the forward-looking statements, even if new information becomes available in the future.

View source version on businesswire.com: https://www.businesswire.com/news/home/20220504005543/en/