On June 1, 2023 GenEros Biopharma Ltd. ("GenEros" or "the Company"), a biopharmaceutical company dedicated to discovering, developing, and commercializing novel medicines for diseases with unmet medical needs, reported that it will unveil the preliminary data from the phase I clinical trial of GEC255, a unique KRAS G12C inhibitor, at the 2023 American Society of Clinical Oncology (ASCO) (Free ASCO Whitepaper) Annual Meeting (Press release, GenEros Biopharma, JUN 1, 2023, View Source [SID1234632366]).

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As of the data cutoff date of February 3, 2023, preliminary data from the study (NCT05768321) sponsored by GenEros Biopharma demonstrated encouraging results. Sixteen NSCLC patients with the KRAS G12C mutation were enrolled in the Phase I dose escalation, followed by dose expansion in selected doses. All patients were at clinical stage IIIC-IV and had undergone a median of 1 (range 0-6) prior systemic treatments, including platinum-based chemotherapy (75%) and immune checkpoint inhibitors (44%).

Tumor response was evaluated in 13 subjects at least once. Among them, 10 subjects (76.9%) achieved objective responses (complete or partial response), while 12 subjects (92.3%) demonstrated disease control (objective response or stable disease). In the 600mg dose group, the objective response rate (ORR) was 83.3%, and the disease control rate (DCR) was 100% (n=6). Notably, significant efficacy was observed at low doses of 200mg and 400mg QD, with some patients achieving partial response for over a year and continuing to benefit.

Fifteen patients experienced treatment-related adverse events, primarily Grade 1 or Grade 2. The most common adverse events (AEs) included diarrhea, ALT increase, rashes, and anemia. No dose-limiting toxicity was observed, and the maximum tolerated dose (MTD) has not been reached.

The KRAS G12C mutation occurs in approximately 12-14% of non-small cell lung cancer (NSCLC) patients. This mutation leads to uncontrolled cell growth and proliferation, contributing to cancer development.

GEC255, a novel and innovative small molecule with high selectivity, excellent target engagement ability, and a favorable pharmacological profile, has demonstrated promising anti-tumor activity in advanced non-small cell lung cancer (NSCLC) patients with the KRAS G12C mutation. It stands as a potential best-in-class KRAS G12C inhibitor.

"The trial results are highly encouraging," stated Dr. You Lu, the lead investigator of the trial. "GEC255 has shown significant anti-tumor activity in advanced NSCLC patients who have not responded to other treatments. These results justify further investigation of GEC255 in larger clinical trials."

2023 ASCO (Free ASCO Whitepaper) Annual Meeting Presentation Details:
Title: Phase I study evaluating the safety, tolerability, pharmacokinetics (PK), and efficacy of GEC255, a novel KRASG12C inhibitor, in advanced solid tumors
Abstract #: 9112 | Poster Bd #:100
Session: Lung Cancer—Non-Small Cell Metastatic
Date and Time: June 4, 2023, at 8:00 – GMT-5 11:00