Approval Probability
TA Base Rate
Adjusted LOA
ML Risk
Acarbose · 6 trials · 3 indications
RatioCmax=Cmax,day1/ Cmax,day-1 Cmax,day-1: Maximum serum glucose after 75g sucrose loading on Day -1 Cmax,day1: Maximum serum glucose after 75g sucrose loading and single dose administration of study drug on Day 1
RatioAUC(0-4)=AUC(0-4),day1/AUC(0-4),day-1 AUC (0-4),day1: AUC of serum glucose from time 0 to 4 hours on Day 1 AUC(0-4),day-1: AUC of serum glucose from time 0 to 4 hours on Day -1
Cmax: Maximum observed drug concentration in measured matrix after single dose administration / maximum drug concentration in plasma after single dose administration
AUC (0-tlast): AUC from time 0 to the last data point \> LLOQ (lower limit of quantification)
AUC: Area under the concentration vs. time curve from zero to infinity after single (first) dose
| Arm | Type | Description |
|---|---|---|
| Acarbose plus metformin arm | EXPERIMENTAL | Participants received loose combination of acarbose and metformin 3 times daily. |
| Metformin plus placebo arm | ACTIVE_COMPARATOR | Participants received loose combination of placebo and metformin 3 times daily. |
| Arm 1 | EXPERIMENTAL | - |
| Arm 2 | PLACEBO_COMPARATOR | - |
| Treatment A-washout-treatment B | EXPERIMENTAL | Subject will receive a single oral dose of acarbose/metformin FDC (Treatment A, 50 mg acarbose/500 mg metformin) in period 1, followed by a single oral dose of 50mg acarbose and 500mg metformin as loose combination (Treatment B) in period 2. Washout interval between 2 treatment periods was at least 7 days. |
| Treatment B-washout-treatment A | EXPERIMENTAL | Subject will receive a single oral dose of 50 mg acarbose and 500 mg metformin as loose combination (Treatment B) in period 1, followed by a single oral dose of acarbose/metformin FDC (Treatment A, 50mg acarbose/500 mg metformin) in period 2. Washout interval between 2 treatment periods was at least 7 days. |
| Acarbose/Metformin FDC | EXPERIMENTAL | Day 0: oral sucrose load (75 g sucrose dissolved in 225 mL water) without Acarbose/Metformin FDC; Day 1: oral sucrose load plus single dose of 1 tablet Acarbose/Metformin FDC (containing 50 mg Acarbose and 500 mg Metformin) |
| Acarbose+Metformin | ACTIVE_COMPARATOR | Day 0: oral sucrose load (75 g sucrose dissolved in 225 mL water) without loose combination of Acarbose and Metformin; Day 1: oral sucrose load plus single dose of 1 tablet each of a loose combination of Acarbose 50 mg and Metformin 500 mg |
| Acarbose | ACTIVE_COMPARATOR | Day 0: oral sucrose load (75 g sucrose dissolved in 225 mL water) without comedication; Day 1: oral sucrose load plus single dose of 1 tablet Acarbose 50 mg |
| Metformin | ACTIVE_COMPARATOR | Day 0: oral sucrose load (75 g sucrose dissolved in 225 mL water) without comedication; Day 1: oral sucrose load plus single dose of 1 tablet Metformin 500 mg |
| Arm 3 | ACTIVE_COMPARATOR | Day 0: oral sucrose load (75 g sucrose dissolved in 225 mL water) without Glucobay standard tablet 100 mg; Day 1: oral sucrose load plus Glucobay standard tablet 100 mg taken with water |
| Name | Type | Description |
|---|---|---|
| Acarbose | DRUG | Uptitrated in the treatment phase from 50 mg per day for 1 week, followed by 100 mg per day for another week, and 150 mg per day for the rest 14 weeks, oral, with the first mouthful of main meal |
| Metformin | DRUG | 500 mg 3 times daily, oral, with the first mouthful of main meal |
| Placebo | DRUG | Acarbose matching placebo, oral |
| Acarbose (Glucobay, BAYG5421) | DRUG | 50 mg TID |
| Acarbose/Metformin FDC(BAY81-9783) | DRUG | Single dose: 50 mg acarbose/500 mg metformin tablet, oral |
| Glucobay | DRUG | Single dose: 50 mg tablet, oral |
| Glucophage | DRUG | Single dose: 500 mg tablet, oral |
| Acarbose/Metformin FDC (BAY81-9783) | DRUG | Acarbose/Metformin FDC (BAY81-9783)50mg/500mg, oral, single dose |
| Acarbose (Glucobay ODT, BAYG5421) | DRUG | - |
Inclusion Criteria: * Males and females, aged 18 to less than 80 years * Diabetes mellitus type 2, that is insufficently controlled with metformin defined by HbA1c between 7.0 % and 10.0%, inclusive * Body mass index between 22 and 45 kg/m\^2, inclusive * Women and men of reproductive potential mus...
Acarbose is used to treat type 2 diabetes mellitus (also called Diabetes Mellitus, Type II). It is being developed by Bayer AG as a small molecule therapy for metabolic disease. The clinical program includes both Acarbose alone and fixed-dose combinations with metformin for patients with type 2 diabetes.
Acarbose targets MGAM (maltase-glucoamylase) and AMY2A (pancreatic alpha-amylase). It acts as an inhibitor of these enzymes. By inhibiting these carbohydrate-digesting enzymes, Acarbose reduces the breakdown of complex carbohydrates into glucose, which lowers postprandial blood glucose levels in patients with type 2 diabetes.
Acarbose is developed by Bayer AG, which trades on the OTC market under the ticker BAYRY. Bayer is the sponsor of the clinical development program for Acarbose and its fixed-dose combination with metformin.
Acarbose is in Phase 3 clinical development for type 2 diabetes. The program includes a completed Phase 3 trial of a loose-dose combination of Acarbose and metformin in metformin-failure patients, along with Phase 1 bioequivalence studies. It is investigational and has not been approved by the FDA for these uses.
Acarbose has been studied in four completed trials. These include NCT03349684, a Phase 3 trial of Acarbose and metformin in metformin-failure type 2 diabetes patients in China, and three Phase 1 bioequivalence studies: NCT04065581 in China, NCT01728740 in South Korea, and NCT01554631 in Germany.
Yes, Acarbose is also known by the brand name Glucobay and the development code BAYG5421. Related names include Glucobay ODT (orally disintegrating tablet) and fixed-dose combination products such as Acarbose/Metformin FDC (BAY81-9783). These refer to the same active ingredient, Acarbose, developed by Bayer.