Biomea Fusion, Inc. announced dosing of the first patient with type 2 diabetes in the Phase II portion of COVALENT-111 in the U.S. This trial is a randomized, double-blinded, placebo-controlled study evaluating the safety, tolerability, pharmacokinetics (PK), and pharmacodynamics (PD) of six dose levels of BMF-219 administered orally daily in 28-day cycles followed by a 26-week evaluation period. Beta cells in the pancreas are responsible for producing, storing, and releasing insulin. Adequate insulin production helps ensure glucose homeostasis.

Menin is thought to function as the brake and a key regulator for beta cell growth in the pancreas, acting as a checkpoint, to prevent excessive beta cell proliferation in healthy individuals. Low beta cell mass is a root cause of type 2 diabetes; without enough healthy, functional beta cells, people with type 2 diabetes are unable to produce sufficient amounts of insulin. BMF-219 was designed to specifically inhibit menin's capacity to interact with transcriptional partners that drive the expression of cell cycle protein regulators, including those that prevent the replication and expansion of beta-cells.

Preclinical studies have shown the potential of BMF-219 to restore and balance beta cells mass. COVALENT-111 is a multi-site, randomized, double-blinded, placebo-controlled Phase I/II study. In the completed Phase I portion of the trial, healthy subjects were enrolled in single ascending dose cohorts.

As previously reported, the Phase I portion of COVALENT-111 has been completed, and BMF-219 was generally well tolerated with an encouraging PK and PD profile in healthy volunteers. The Phase II portion, ongoing in Canada and the U.S., consists of multiple ascending dose cohorts enrolling adult patients with type 2 diabetes uncontrolled by current therapies. COVALENT-111 is designed to examine the capacity of BMF-219 to potentially provide long-term glycemic control to patients by restoring their pool of beta cells.

Loss of functional beta cell mass is a core component of the natural history in both types of diabetes type 1 diabetes (mediated by autoimmune dysfunction) and type 2 diabetes (mediated by metabolic dysfunction). Beta cells are found in the pancreas and are responsible for the synthesis and secretion of insulin. Insulin is a hormone that helps the body use glucose for energy and helps control blood glucose levels.

In patients with diabetes, beta cell mass and function are diminished, leading to insufficient insulin secretion and hyperglycemia. Menin is thought to act as a brake on beta-cell turnover and growth, supporting the notion that inhibition of menin could lead to the regeneration of normal, healthy beta cells. Based on these and other scientific findings, Biomea is exploring the potential for BMF-219-mediated menin inhibition as a viable therapeutic approach to permanently halt or reverse progression of type 2 diabetes.

Diabetes is considered a chronic health condition that affects how the body turns food into energy and results in too much sugar in the bloodstream. Over time, this can cause serious health problems and damage vital organs. Most people with diabetes have a shorter life expectancy than people without this disease.

The CDC estimates 1 in 3 Americans will develop diabetes at some point in their life. More than 37 million people of all ages (about 11% of the US population) have diabetes today. 96 million adults (more than 1 in 3) have pre-diabetes, blood sugars that are higher than normal but not high enough to be classified as diabetes.

Diabetes is also one of the largest economic burdens on the United States' health care system with $1 out of every $4 in US health care costs being spent on caring for people with diabetes. Despite the availability of current medication, there is a significant need in the treatment and care of patients with diabetes.