Details
| Stereochemistry | ABSOLUTE |
| Molecular Formula | C20H18N6O3S2 |
| Molecular Weight | 454.525 |
| Optical Activity | UNSPECIFIED |
| Defined Stereocenters | 1 / 1 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
CC1=NC=CC=C1OC2=CC(SC3=NC=CC=C3)=CN=C2NC4=NC(=NS4)[C@H](O)CO
InChI
InChIKey=PCOMIRCNMMNOAP-CQSZACIVSA-N
InChI=1S/C20H18N6O3S2/c1-12-15(5-4-8-21-12)29-16-9-13(30-17-6-2-3-7-22-17)10-23-19(16)25-20-24-18(26-31-20)14(28)11-27/h2-10,14,27-28H,11H2,1H3,(H,23,24,25,26)/t14-/m1/s1
| Molecular Formula | C20H18N6O3S2 |
| Molecular Weight | 454.525 |
| Charge | 0 |
| Count |
|
| Stereochemistry | ABSOLUTE |
| Additional Stereochemistry | No |
| Defined Stereocenters | 1 / 1 |
| E/Z Centers | 0 |
| Optical Activity | UNSPECIFIED |
AMG-151 [AMG 151, ARRY-403] was under development with Amgen for the treatment of type 2 diabetes mellitus (T2DM). AMG 151 binds to glucose-bound glucokinase distinctly from glucose- or adenosine triphosphate–binding sites
to activate glucokinase selectively. AMG 151 was in a phase I trial for the treatment of Type 2 diabetes. AMG 151 in a twice-daily dosing regimen decreased fasting
and postprandial glucose in patients with type 2 diabetes inadequately controlled with metformin. In all AMG 151 once-daily
dose groups and in the AMG 151 200-mg twice-daily dose
group, significant reductions were observed in glucose
AUC0–240 in after a MTT from baseline to day 28 compared with placebo. However, Amgen disconinued the development of AMG-151.
Approval Year
PubMed
| Title | Date | PubMed |
|---|---|---|
| Utilizing physiologically based pharmacokinetic modeling to inform formulation and clinical development for a compound with pH-dependent solubility. | 2015 Apr |
|
| AMG 151 (ARRY-403), a novel glucokinase activator, decreases fasting and postprandial glycaemia in patients with type 2 diabetes. | 2016 Feb |
Sample Use Guides
Type 2 diabetes: Patients received oral AMG 151 at 50, 100 or 200 mg twice daily, AMG 151 at 100, 200 or 400 mg once daily or matching placebo for 28 days. AMG 151 significantly reduced FPG when administered twice daily but not when administered once daily in patients with type 2 diabetes treated with metformin.
Route of Administration:
Oral
| Substance Class |
Chemical
Created
by
admin
on
Edited
Sat Dec 16 09:06:02 UTC 2023
by
admin
on
Sat Dec 16 09:06:02 UTC 2023
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| Record UNII |
P8B61X2X2D
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| Record Status |
Validated (UNII)
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| Record Version |
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P8B61X2X2D
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25235269
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AMG-151 FREE BASE
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admin on Sat Dec 16 09:06:02 UTC 2023 , Edited by admin on Sat Dec 16 09:06:02 UTC 2023
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PRIMARY | Official Title: A Phase 1, Double-blind, Randomized, 2-Way Crossover, Placebo-controlled Study to Investigate the Effect of AMG 151 on 24-hour Ambulatory Blood Pressure and Glucose Levels in Subjects With Type 2 Diabetes Mellitus.Purpose: This is a phase 1, randomized, double-blind, placebo-controlled, 2-way crossover study to evaluate the effect of AMG 151 on 24-hour ambulatory blood pressure and glucose levels in subjects with type 2 diabetes mellitus who are on a stable regimen of metformin alone, metformin and a dipeptidyl peptidase-4 inhibitor (DPP4), metformin and a thiazolidinedione (TZD), or metformin, a DPP4, and a TZD for a minimum of 3 months prior to randomization. | ||
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1304015-76-6
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300000042394
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TARGET -> ACTIVATOR |
ALLOSTERIC INHIBITOR
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| Related Record | Type | Details | ||
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ACTIVE MOIETY |
Originator: Array BioPharma; Class: Antihyperglycaemic, Small molecule; Mechanism of Action: Glucokinase stimulant; Highest Development Phase: Discontinued for Type 2 diabetes mellitus; Most Recent Events: 07 Aug 2013 ARRY 403 is no longer licensed to Amgen worldwide, 19 Apr 2013 Amgen terminates phase I trial in Type-2 diabetes mellitus in USA (NCT01755442), 01 Nov 2012 Amgen initiates enrolment in a phase I trial for Type-2 diabetes mellitus in USA (NCT01755442)
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ACTIVE MOIETY |
Patients received oral AMG 151 at 50, 100 or 200mg twice daily, AMG 151 at 100, 200 or 400mg once daily or matching placebo for 28 days. A significant linear dose-effect trend was observed with the twice-daily regimen (p=0.004) for change in FPG to day 28. No trend was observed with the once-daily regimen. A higher incidence of hypoglycaemia and hypertriglyceridaemia was observed with AMG 151 administration. AMG 151 significantly reduced FPG when administered twice daily but not when administered once daily in patients with type 2 diabetes treated with metformin.
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