Gan & Lee Pharmaceuticals Presented Two Positive Clinical Results of Once-weekly Insulin GZR4 at the 60th Annual Meeting of the European Association for the Study of Diabetes (EASD 2024)

• In Phase Ia clinical study, GZR4 demonstrated favorable safety and tolerability profiles in healthy subjects, maintaining a stable glucose-lowering effect for up to one week with a single administration.
• In Phase Ib clinical study, patients with Type 2 diabetes mellitus (T2DM) receiving six weeks of GZR4 treatment were safe and well tolerated. GZR4 also exhibited improvements in fasting blood glucose (FBG), glycated hemoglobin (HbA1c), and time in range (TIR) across all dosage groups, outperforming the insulin degludec (IDeg) group.

BEIJING, Sept. 14, 2024 /PRNewswire/ -- Gan & Lee Pharmaceuticals (Gan & Lee, Shanghai Stock Exchange: 603087) announced the clinical results from two Phase I trials of the Company's independently developed novel once-weekly insulin analog, GZR4, in healthy Chinese subjects and patients with T2DM in oral presentation and short oral discussion at the 60th Annual Meeting of the European Association for the Study of Diabetes (EASD 2024).

Statement:
1.    GZR18 injection is an investigational drug and has not yet been approved in China.
2.    Gan & Lee Pharmaceuticals does not recommend the use of any unapproved drugs/indications.

Phase Ia Study Results

This placebo-controlled and active-comparator-controlled, single-center, single-dose,  randomized, dose-escalation study aimed to evaluate the safety, tolerability, pharmacokinetics (PK), and pharmacodynamics (PD) of GZR4 in healthy adult male participants. The study was conducted following a dose-escalation design, starting from lower doses and progressively increasing to higher doses. Participants in cohorts 1-4 randomly receiving a subcutaneous injection of GZR4 (1, 3, 6, or 12 nmol/kg) or placebo, while cohort 5 received a single dose of 0.4 U/kg (2.4 nmol/kg) insulin degludec (IDeg) as an active comparator. A 24-hour glucose clamp procedure was conducted on days 2 and 7 respectively post-GZR4 administration in cohorts 2-4, and on day 1 post-IDeg administration in cohort 5.

GZR4 exhibited favorable safety and tolerability in healthy subjects, with no serious adverse events (SAEs) reported, and no discontinuations due to the investigational product-related adverse events. PD results indicated that the glucose infusion rate (GIR) on day 7 was approximately 80% of that on day 2 in subjects receiving 12 nmol/kg GZR4, indicating that the glucose-lowering effect of GZR4 persists for approximately one week. Meanwhile, the area under the GIR-time curve on day 2 (AUC_GIR,24-48h) and day 7 (AUC_GIR,144-168h) for the 6 nmol/kg dose of GZR4 was similar to the 24-hour GIR (AUC_GIR,0-24h) for the 0.4 U/kg (2.4 nmol/kg) of IDeg (37.84 ± 9.86 versus 40.60 ± 14.39 h*mg/kg/min, respectively)^*, implying that the average daily glucose-lowering effect of GZR4 is comparable to that of IDeg. Convert accordingly, it is estimated that the potency of GZR4 is approximately 2.5-fold greater than that of IDeg when evaluating based on a similar molar concentration.