On April 8, 2022 Biomea Fusion, Inc. (Nasdaq: BMEA), a clinical-stage biopharmaceutical company dedicated to discovering and developing novel covalent small molecules to treat and improve the lives of patients with genetically defined cancers and metabolic diseases, reported new data at the American Association of Cancer Research (AACR) (Free AACR Whitepaper) Annual Meeting demonstrating BMF-219’s potent and highly effective activity in multiple preclinical models of DLBCL, MM, and KRAS human ex vivo tumor models and cell lines in poster presentations (Press release, Biomea Fusion, APR 8, 2022, View Source [SID1234611679]). In addition, the company presented a Trial In Progress (TIP) poster presentation detailing the design of Biomea’s ongoing Phase I clinical trial (COVALENT-101).

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The preclinical and TIP presentations can be viewed on Biomea’s website at View Source

"Today, we unveiled a dataset in which single agent BMF-219 demonstrated pronounced cytotoxic activity across multiple liquid and solid tumor types that we will be pursuing in the clinic. These data clearly show BMF-219’s powerful cell-killing activity in a broad spectrum of tumor types, including a very robust pan-KRAS effect," said Steve Morris, MD, Biomea’s Chief Medical Officer. "In liquid and solid tumor preclinical studies, BMF-219 has demonstrated a highly differentiated profile from both non-covalent menin inhibitors as well as clinical-stage and FDA-approved covalent KRAS G12C inhibitors. We are very excited to see how this differentiated profile translates in the clinical setting across multiple liquid and solid tumors."

In comparison to two highly specific KRAS G12C inhibitors, BMF-219 exhibited broader potency across KRAS-mutated cell lines (G12C, G12D, G13D, and G12V) and ex vivo PDX tumor models indicating pan-KRAS activity with over 90% growth inhibition in most of these models. Additionally, BMF-219 showed the potential to increase the depth of response across G12C cell lines, notably achieving a higher percentage of cell killing in G12C colorectal cancer cells compared to the commercially available KRAS inhibitor sotorasib and another clinical-stage KRAS inhibitor. Additionally, BMF-219 exhibited robust growth inhibition as a single agent against high-grade B-cell lymphoma cell lines that are known to have low response to standard of care, as well as in multiple MM cells with TP53 and RAS mutations at similar drug concentrations.

A targeted pan-KRAS inhibitor has the potential to treat the 25-35% of NSCLC, 40-45% of CRC, and ~90% of pancreatic cancer patients who have KRAS-mutant tumors. If approved, BMF-219 could be an effective treatment for relapsed/refractory DLBCL and MM, where patients have a significant unmet need despite a large armamentarium of therapeutic options. Additionally, we believe BMF-219 has the potential to be an effective therapeutic option for menin-dependent acute leukemias, including the >45% of AML patients that are believed to have menin-dependent disease.

Poster Presentation Details

Details for the upcoming presentations are as follows:

Anti-tumor activity of irreversible menin inhibitor, BMF-219, in high-grade B-cell lymphoma and multiple myeloma preclinical models (Abstract #1205)

Session Category: Experimental and Molecular Therapeutics
Session Title: Novel Targets and Pathways
Session Date and Time: Tuesday, April 12, 2022 9:00 AM – 12:30 PM
Location: New Orleans Convention Center, Exhibit Halls D-H, Poster Section 24
Poster Board Number: 23
Permanent Abstract Number: 2654

Irreversible menin inhibitor, BMF-219, inhibits the growth of KRAS-mutated solid tumors (Abstract #1202)

Session Category: Experimental and Molecular Therapeutics
Session Title: Signaling Pathway Inhibitors
Session Date and Time: Tuesday, April 12, 2022 9:00 AM – 12:30 PM
Location: New Orleans Convention Center, Exhibit Halls D-H, Poster Section 25
Poster Board Number: 8
Permanent Abstract Number: 2665

COVALENT-101: ​A Phase 1 study of BMF-219, a novel oral irreversible menin inhibitor, as a single agent in patients with relapsed/refractory (R/R) acute lymphocytic/acute myeloid leukemia (ALL/AML), diffuse large B-cell lymphoma (DLBCL), and multiple myeloma (MM) (NCT05153330)​ (Abstract #7613)

Session Category: Clinical Trials
Session Title: Phase I Trials in Progress 1
Session Date and Time: Tuesday, April 12, 2022 9:00 AM – 12:30 PM
Location: New Orleans Convention Center, Exhibit Halls D-H, Poster Section 34
Poster Board Number: 10
Permanent Abstract Number: CT210